Solid oral dosage forms comprising tavapadon
Pharmaceutical tablets with tavapadon and fillers address the limitations of existing Parkinson's disease treatments by optimizing D1 receptor activation, providing sustained symptom relief with minimized side effects.
Patent Information
- Authority / Receiving Office
- WO · WO
- Patent Type
- Applications
- Current Assignee / Owner
- Filing Date
- 2025-10-06
- Publication Date
- 2026-04-09
AI Technical Summary
Existing treatments for Parkinson's disease, such as levodopa and D2-selective agonists, suffer from motor complications and adverse effects, while D1-selective agonists like tavapadon face tolerability issues and poor pharmacokinetics, necessitating a need for formulations that provide sustained motor symptom relief with reduced adverse events.
Pharmaceutical tablets comprising 0.25% to 15% tavapadon free base and at least 80% to 90% fillers, including various sugars, starches, and celluloses, designed to optimize tavapadon delivery and minimize side effects.
The tablets offer improved control of Parkinson's disease motor symptoms with reduced adverse events by targeting D1 dopamine receptors, enhancing tavapadon's therapeutic efficacy and pharmacokinetic properties.
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Figure US2025049565_09042026_PF_FP_ABST
Abstract
Description
SOLID ORAL DOSAGE FORMS COMPRISING TAVAPADONCROSS REFERENCE TO RELATED APPLICATION
[0001] This application claims the priority benefit of U.S. Provisional Application No. 63 / 703,836, filed on October 4, 2024, which is hereby incorporated by reference herein in its entirety.FIELD
[0002] The present disclosure pertains to pharmaceutical tablets comprising tavapadon and processes for preparing such dosage forms.BACKGROUND
[0003] Parkinson’s disease (PD) is a progressive neurodegenerative disease characterized by deficits in motor control arising from the loss of dopaminergic neurons in the substantia nigra pars compacta and subsequent depletion of dopamine in motor regions of the striatum. Poewe et al., Nat Rev Dis Primers 2017; 3(1): 17013. Standard treatment remains the restoration of dopaminergic function through administration of the synthetic dopamine precursor levodopa (1- dopa) and subsequent activation of DI -like and D2-like dopamine receptors. Rizek et al., CMAJ 2016; 188: 1157-1165; Charvin et aL, Nat Rev Drug Discov 2018; 17: 804-822; and Ossig C et al„ Neurol Clin 2015; 33: 19-37. However, while use of levodopa provides efficacy and is generally well tolerated, long-term treatment can lead to fluctuating motor responses and dyskinesias in many individuals. Bastide et al., Prog Neurobiol 2015; 132: 96-168.
[0004] There has long been interest in the potential of DI - or D2-selective receptor agonists as an alternative to levodopa in subjects with Parkinson’s disease. Clinical trials of limited duration with prototype full DI agonists demonstrated that, while these agents exhibited robust antiparkinsonian effects on motor symptoms challenges with pharmacokinetics, cardiovascular parameters, and side effects including dyskinesias made them ill-suited for further clinical advancement. Rascol et al., Ann Neurol 1999; 45:736-741. In contrast, efforts to develop D2- selective agonists with suitable clinical properties were more successful, with several receiving approval for the treatment of Parkinson’s disease, including pramipexole, ropinirole, and rotigotine. In general, these agents exhibit less-frequent motor complications than levodopa but are not as effective for controlling motor symptoms. Dietrichs et al., Acta Neurol Scand 2017; 136: 378-385. D2-selective agonists are also associated with an increased incidence of specificadverse effects (AEs), including nausea, somnolence, hypotension, compulsive behaviors, and hallucinations, particularly in the elderly. Stowe et al., Cochrane Database Syst Rev 2008: 2: CD006564. Thus, there remains a need for agents that provide effective and predictable control of motor symptoms while avoiding side effects associated with activation of D2-like receptors.
[0005] Existing clinical and preclinical data provide theoretical support for the long-standing hypothesis that selective activation of DI -like receptors may be an important therapeutic option for Parkinson’s disease. Kim et al., Front Biol (Beijing) 2015; 10: 230-238. To date, however, attempts to develop DI -selective agonists have been hampered by tolerability issues (notably, acute hypotension) and poor pharmacokinetics (e.g. short half-life and low oral availability).
[0006] Tavapadon is a D1 / D5 dopamine receptor agonist being investigated for the treatment of Parkinson’s disease. By targeting the DI dopamine receptor, tavapadon aims to improve motor control symptoms while minimizing adverse events (AEs) that may be mechanistically linked to D2 / D3 dopamine receptor agonists, such as L-Dopa. There is continuing need to develop formulations for tavapadon for more effective treatment of Parkinson’s disease to provide sustained relief of motor symptoms with a reduced likelihood of adverse events.
[0007] Accordingly, there remains a need in the art for pharmaceutical tablets suitable for administering tavapadon to patients with Parkinson’s disease.Summary
[0008] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler.
[0009] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler.
[0010] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose,dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof.
[0011] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof.
[0012] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calciumcarbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is cellulose.
[0013] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is cellulose.
[0014] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixturesthereof; wherein at least one filler is dibasic calcium phosphate.
[0015] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is dibasic calcium phosphate.
[0016] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is cellulose; wherein the cellulose is microcry stal line cellulose.
[0017] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% byweight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is cellulose; wherein the cellulose is microcrystalline cellulose.
[0018] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is lactose.
[0019] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar,confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is lactose.
[0020] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is lactose; wherein the lactose is lactose monohydrate.
[0021] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powderedcellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler is lactose; wherein the lactose is lactose monohydrate.
[0022] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose.
[0023] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microciystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate,monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose.
[0024] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate.
[0025] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixturesthereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate.
[0026] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate.
[0027] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate,magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate.
[0028] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate; wherein a coating is added to the pharmaceutical tablet.
[0029] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources ofa- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate; wherein a coating is added to the pharmaceutical tablet.
[0030] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microciystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0031] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar,confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0032] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol,polyethylene glycol, titanium dioxide, and talc.
[0033] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; wherein at least one filler comprises cellulose and lactose; wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate; wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0034] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one disintegrant.
[0035] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one disintegrant.
[0036] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powderedcellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof.
[0037] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof.
[0038] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight.
[0039] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin,tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight.
[0040] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starch glycolate.
[0041] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starch glycolate.
[0042] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone,crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starch glycolate; wherein a coating is added to the pharmaceutical tablet.
[0043] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starch glycolate; wherein a coating is added to the pharmaceutical tablet.
[0044] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starch glycolate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0045] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodiumstarch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starch glycolate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0046] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starch glycolate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0047] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one disintegrant; wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight; wherein at least one disintegrant is sodium starchglycolate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0048] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one lubricant.
[0049] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one lubricant.
[0050] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof.
[0051] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof.
[0052] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearylfumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight.
[0053] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight.
[0054] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesium stearate.
[0055] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesiumstearate.
[0056] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0057] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0058] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises apolymer coating.
[0059] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0060] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0061] Another aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising at least one lubricant; wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodiumlauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one lubricant is present in an amount of about 1% by weight; wherein at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0062] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant.
[0063] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant.
[0064] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant isselected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof.
[0065] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium steaiyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof.
[0066] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25%by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmeliose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight.
[0067] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate,fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight.
[0068] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose,microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof.
[0069] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calciumsulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof.
[0070] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodiumstarch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1 % by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate.
[0071] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising; at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powderedcellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate.
[0072] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose,carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0073] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose,carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0074] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose,carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0075] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose,carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0076] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose,carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0077] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powderedcellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0078] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodiumstarch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate.
[0079] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate,magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate.
[0080] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate,tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon.
[0081] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose,microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon.
[0082] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, ricestarch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate.|0083] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein:at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodiumstarch glycolate; and about 1 mg magnesium stearate.
[0084] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microciystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0085] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrantis present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0086] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant isselected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0087] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodiumstarch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0088] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- andamorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0089] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactosemonohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 0.25% by weight of tavapadon; about 64% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon; about 63.83 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to thepharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0090] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrantis sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate.
[0091] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least onedisintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate.
[0092] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrantis present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1 % by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
[0093] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearylfumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
[0094] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof,magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate.
[0095] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose,carmeliose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate.
[0096] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate,magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0097] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified orprocessed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0098] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein:at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starchglycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0099] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrantis sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0100] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodiumlauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about I mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0101] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone,crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate; comprising: about 1% by weight of tavapadon; about 63% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon; about 63.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0102] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calciumsulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate.
[0103] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- andamorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate.
[0104] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified orprocessed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
[0105] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugarspheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
[0106] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactosemonohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
[0107] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of atleast one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
[0108] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microciystalline cellulose; about 32% byweight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate.
[0109] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microciystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least onedisintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate.
[0110] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearylfumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.10111] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone,crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0112] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate,magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0113] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, ricestarch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0114] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25%by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesiumstearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0115] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrantis present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon; wherein the pharmaceutical tablet comprises about 59.08 mg of microcrystalline cellulose; about 31.92 mg of lactose monohydrate; about 3 mg sodium starch glycolate; and about 1 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0116] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone,crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177.24 mg of microcrystalline cellulose; about 95.76 mg of lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate.
[0117] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate,magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177.24 mg of microcrystalline cellulose; about 95.76 mg of lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate.
[0118] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified orprocessed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microciystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177.24 mg of microcrystalline cellulose; about 95.76 mg of lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0119] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein:at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177.24 mg of microcrystalline cellulose; about 95.76 mgof lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0120] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrantis sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177.24 mg of microcrystalline cellulose; about 95.76 mg of lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0121] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearylfumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177.24 mg of microcrystalline cellulose; about 95.76 mg of lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0122] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose,carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177.24 mg of microcrystalline cellulose; about 95.76 mg of lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0123] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- andamorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon; wherein the pharmaceutical tablet comprises about 177,24 mg of microcrystalline cellulose; about 95.76 mg of lactose monohydrate; about 9 mg sodium starch glycolate; and about 3 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0124] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein:at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1 % by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
[0125] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25%by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesiumstearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
[0126] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesium stearate.
[0127] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrantis present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesium stearate.
[0128] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant isselected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0129] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodiumstarch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet.
[0130] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- andamorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0131] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactosemonohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesiumstearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating.
[0132] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 15% by weight of tavapadon free base; and at least about 80% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrantis sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0133] One aspect of the invention pertains to a pharmaceutical tablet comprising: about 0.25% by weight to about 5% by weight of tavapadon free base; and at least about 90% by weight of at least one filler; further comprising: at least one disintegrant; and at least one lubricant; wherein: at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof; at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glycerylpalmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof; wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight; wherein: at least one filler comprises lactose and cellulose; at least one disintegrant is a starch; and at least one lubricant is stearic acid or salts thereof; wherein: at least one filler comprises lactose monohydrate and microcrystalline cellulose; at least one disintegrant is sodium starch glycolate; and at least one lubricant is magnesium stearate comprising: about 5% by weight of tavapadon; about 59% by weight of microcrystalline cellulose; about 32% by weight of lactose monohydrate; about 3% sodium starch glycolate; and about 1% magnesium stearate; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon; wherein the pharmaceutical tablet comprises about 118.16 mg of microcrystalline cellulose; about 63.84 mg of lactose monohydrate; about 6 mg sodium starch glycolate; and about 2 mg magnesium stearate; wherein a coating is added to the pharmaceutical tablet; wherein the coating comprises a polymer coating; wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
[0134] Another aspect of the invention pertains to any of the preceding embodiments wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon unless otherwise stated.
[0135] Another aspect of the invention pertains to any of the preceding embodiments wherein the pharmaceutical tablet comprises about 1 mg of tavapadon unless otherwise stated.
[0136] Another aspect of the invention pertains to any of the preceding embodiments wherein the pharmaceutical tablet comprises about 5 mg of tavapadon unless otherwise stated.
[0137] Another aspect of the invention pertains to any of the preceding embodiments wherein the pharmaceutical tablet comprises about 10 mg of tavapadon unless otherwise stated.
[0138] Another aspect of the invention pertains to any of the preceding embodiments wherein the pharmaceutical tablet comprises about 15 mg of tavapadon unless otherwise stated.
[0139] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about 12 pm.
[0140] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3]of about 12 gm; wherein the pharmaceutical tablet comprises about .25 mg of tavapadon.
[0141] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about 12 |im; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
[0142] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about 12 pm; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
[0143] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about 12 pm; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
[0144] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about 12 pm; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
[0145] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, wherein about 75% or more of the tavapadon is released in 20 minutes in 0.01N HC1 with 0.15% or 0.2 % SDS.
[0146] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, wherein about 75% or more of the tavapadon is released in 20 minutes in 0.01N HC1 with 0.15% or 0.2 % SDS; wherein the pharmaceutical tablet comprises about .25 mg of tavapadon.
[0147] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, wherein about 75% or more of the tavapadon is released in 20 minutes in 0.01N HC1 with 0.15% or 0.2 % SDS; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
[0148] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, wherein about 75% or more of the tavapadon is released in 20 minutes in 0.01N HC1 with 0.15% or 0.2 % SDS; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
[0149] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, wherein about 75% or more of the tavapadon is released in 20 minutes in 0.01N HC1 with 0.15% or 0.2 % SDS; wherein the pharmaceutical tablet comprises about 10 mgof tavapadon.
[0150] Another aspect of the invention pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, wherein about 75% or more of the tavapadon is released in 20 minutes in 0.01N HC1 with 0.15% or 0.2 % SDS; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
[0151] Another embodiment pertains to a method of manufacturing a pharmaceutical tablet comprising tavapadon and at least one filler; the steps comprising:(a) blending tavapadon with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
[0152] Another embodiment pertains to a method of manufacturing a pharmaceutical tablet comprising tavapadon and at least one filler; the steps comprising:(a) blending tavapadon with filler and disintegrant to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
[0153] Another embodiment pertains to a method of manufacturing a pharmaceutical tablet comprising tavapadon and at least one filler; the steps comprising:(a) blending tavapadon with filler, disintegrant and intragranular portion lubricant to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
[0154] Another embodiment pertains to a method of manufacturing a pharmaceutical tablet, the steps comprising(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend;and(e) compressing the final blend into tablets.[01551 Another embodiment pertains to a method of manufacturing a pharmaceutical tablet, the steps comprising(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets, wherein the disintegrant is sodium starch glycolate.
[0156] Another embodiment pertains to a method of manufacturing a pharmaceutical tablet, the steps comprising(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets, wherein the disintegrant is sodium starch glycolate and the lubricant is magnesium stearate.
[0157] Another embodiment pertains to a method of manufacturing a pharmaceutical tablet, the steps comprising(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets, wherein the disintegrant is sodium starchglycolate, the lubricant is magnesium stearate, and the filler is microcrystalline cellulose and lactose monohydrate.
[0158] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler wherein disintegration of the tablet is achieved within 15 minutes under guidelines and requirements of United States Pharmacopeia (USP) general chapter <701>.
[0159] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, manufactured by:(a) blending tavapadon with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
[0160] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, manufactured by:(a) blending tavapadon with filler and disintegrant to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
[0161] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler, manufactured by:(a) blending tavapadon with filler, disintegrant, and intragranular portion lubricant to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
[0162] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; manufactured by(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend;and(e) compressing the final blend into tablets.
[0163] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; manufactured by(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets; wherein the disintegrant is sodium starch glycolate.
[0164] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; manufactured by(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets; wherein the disintegrant is sodium starch glycolate and the lubricant is magnesium stearate.
[0165] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; manufactured by(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets; wherein the disintegrant is sodium starchglycolate, the lubricant is magnesium stearate, and the filler is microcrystalline cellulose and lactose monohydrate.
[0166] Another embodiment pertains to pharmaceutical tablet comprising tavapadon and at least one filler, wherein 90% or more dissolution of the tablet is achieved under guidelines and requirements of United States Pharmacopeia (USP) general chapter <711>.
[0167] Another embodiment pertains to a method for treating Parkinson's Disease (PD) in a patient, comprising administering to the patient a pharmaceutical formulation comprising:(a) about 0.25% by weight to about 15% by weight of tavapadon free base; and(b) at least about 80% by weight of at least one filler; wherein the Parkinson's Disease is effectively treated.
[0168] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about < 25 m.
[0169] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about < 25 pm; wherein the pharmaceutical tablet comprises about .25 mg of tavapadon.
[0170] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about < 25 pm; wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
[0171] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about < 25 pm; wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
[0172] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about < 25 pm; wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
[0173] Another embodiment pertains to a pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about < 25 pm; wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.Brief Description of the Drawings
[0174] Figure 1: Process Flow for the Manufacturing of Tavapadon 0.25 mg Tablets Used inPhase 3 Clinical Studies
[0175] Figure 2: Process Flow for the Manufacturing of Tavapadon 1 and 5 mg Tablets Used inPhase 3 Clinical Studies
[0176] Figure 3: Dissolution Profile for Varying API Particle Size (0.25 mg)
[0177] Figure 4: Dissolution Profile for Varying API Particle Size (1 mg)
[0178] Figure 5: Dissolution Profile for Varying API Particle Size (5 mg)
[0179] Figure 6: Dissolution Profile for Varying API Particle Size (15 mg)
[0180] Figure 7: Varying Levels of Disintegrant, Sodium Starch Glycolate, 0.25 mg
[0181] Figure 8: Varying Levels of Disintegrant, Sodium Starch Glycolate, 1 mg
[0182] Figure 9: Varying Levels of Disintegrant, Sodium Starch Glycolate, 15 mg
[0183] Figure 10: 0.25 mg Core vs. Coated
[0184] Figure 11: 1 mg Core vs. Coated
[0185] Figure 12: 5 mg Core vs. Coated
[0186] Figure 13: 10 mg Core vs. Coated
[0187] Figure 14: 15 mg Core vs. Coated
[0188] Figure 15. Aqueous Dissolution for 0.25 mg
[0189] Figure 16. Aqueous Dissolution for 1 mg
[0190] Figure 17. 1 mg Apparatus and RPM Evaluation in 900 mL of 0.01N HC1 with 0.15%SDS
[0191] Figure 18. 15 mg Apparatus and RPM Evaluation in 900 mL of 0.01N HC1 with 0.2%SDS
[0192] Figure 19. Media Evaluation for 0.25 mg Tablets in 900 mL at 75 RPM
[0193] Figure 20. Media Evaluation for 1 mg Tablets in 900 mL at 75 RPM
[0194] Figure 21. Media Evaluation for 15 mg Tablets in 900mL at 75 RPM
[0195] Figure 22. Media Evaluation for 5 mg, 10 mg, and 15 mg Tablets in 900 mL at 75 RPM
[0196] Figure 23. Biorelevant 0.25 mg
[0197] Figure 24. Biorelevant 1 mg
[0198] Figure 25. Biorelevant 15 mg
[0199] Figure 26. 0.25 mg Coated vs. Uncoated
[0200] Figure 27. 1 mg Coated vs. Uncoated
[0201] Figure 28. 5 mg Coated vs. Uncoated
[0202] Figure 29. 10 mg Coated vs. Uncoated
[0203] Figure 30. 15 mg Coated vs. Uncoated
[0204] Figure 31. 0.25 mg Particle Size
[0205] Figure 32. 1 mg Particle Size
[0206] Figure 33. 5 mg Particle Size
[0207] Figure 34. 15 mg Particle Size
[0208] Figure 35. Formulations Evaluation, Sodium Starch Glycolate, 0.25 mg
[0209] Figure 36. Formulation Evaluation, Sodium Starch Glycolate, 1 mg
[0210] Figure 37. Formulation Evaluation, Sodium Starch Glycolate, 15 mg
[0211] Figure 38. Manufacturing Process Flow for Tavapadon 0.25 mg Tablets
[0212] Figure 15. Manufacturing Process Flow for Tavapadon 1.0 mg and 5.0 mg Tablets
[0213] Figure 40. Manufacturing Process Flow for 15 mg Tavapadon Tablets
[0214] Figure 41. Dissolution of 15 mg Tavapadon TabletsDetailed Description
[0215] The ...
Claims
WE CLAIM:
1. A pharmaceutical tablet comprising:(a) about 0.25% by weight to about 15% by weight of tavapadon free base; and(b) at least about 80% by weight of at least one filler.
2. The pharmaceutical tablet of claim 1 comprising:(a) about 0.25% by weight to about 5% by weight of tavapadon free base; and(b) at least about 90% by weight of at least one filler.
3. The pharmaceutical tablet of claim 2, wherein at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose- based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof.
4. The pharmaceutical tablet of claim 3, wherein at least one filler is cellulose.
5. The pharmaceutical tablet of claim 3, wherein at least one filler is dibasic calcium phosphate.
6. The pharmaceutical tablet of claim 4, wherein the cellulose is microcrystalline cellulose.
7. The pharmaceutical tablet of claim 3, wherein at least one filler is lactose.
8. The pharmaceutical tablet of claim 7, wherein the lactose is lactose monohydrate.
9. The pharmaceutical tablet of claim 3, wherein the filler comprises cellulose and lactose.
10. The pharmaceutical tablet of claim 9, wherein the cellulose is microcrystalline cellulose and the lactose is lactose monohydrate.
11. The pharmaceutical tablet of claim 10, wherein the filler comprises about 59% to about 64% by weight of microcrystalline cellulose and about 31% to about 33% by weight of lactose monohydrate.
12. The pharmaceutical tablet of claim 11, wherein a coating is added to the pharmaceutical tablet.
13. The pharmaceutical tablet of claim 12, wherein the coating comprises a polymer coating.
14. The pharmaceutical tablet of claim 13, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
15. The pharmaceutical tablet of claim 3, further comprising at least one disintegrant.
16. The pharmaceutical tablet of claim 15, wherein at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesium aluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof.
17. The pharmaceutical tablet of claim 16, wherein at least one disintegrant is present in an amount of about 3% by weight.
18. The pharmaceutical tablet of claim 17, wherein at least one disintegrant is sodium starch glycolate.
19. The pharmaceutical tablet of claim 18, wherein a coating is added to the pharmaceutical tablet.
20. The pharmaceutical tablet of claim 19, wherein the coating comprises a polymer coating.
21. The pharmaceutical tablet of claim 20, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
22. The pharmaceutical tablet of claim 3, further comprising at least one lubricant.
23. The sold oral dosage form of claim 22, wherein at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodiumlauryl sulfate, magnesium lauryl sulfate, and mixtures thereof.
24. The pharmaceutical tablet of claim 23, wherein at least one lubricant is present in an amount of about 1% by weight.
25. The pharmaceutical tablet of claim 24, wherein at least one lubricant is magnesium stearate.
26. The pharmaceutical tablet of claim 25, wherein a coating is added to the pharmaceutical tablet.
27. The pharmaceutical tablet of claim 26, wherein the coating comprises a polymer coating.
28. The pharmaceutical tablet of claim 27, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
29. The pharmaceutical tablet of claim 3, further comprising:(c) at least one disintegrant; and(d) at least one lubricant.
30. The pharmaceutical tablet of claim 29, wherein:(b) at least one filler is selected from the group consisting of lactose, anhydrous lactose, lactose monohydrate, lactitol, maltitol, mannitol, sorbitol, xylitol, dextrose, dextrose monohydrate, fructose, sucrose, sucrose-based diluents, compressible sugar, confectioner’s sugar, sugar spheres, maltose, inositol, hydrolyzed cereal solids, starches, com starch, wheat starch, rice starch, potato starch, tapioca starch, starch components, amylose, dextrates, modified or processed starches, pregelatinized starch, dextrins, cellulose, powdered cellulose, microcrystalline cellulose, silicified microcrystalline cellulose, food grade sources of a- and amorphous cellulose and powdered cellulose, cellulose acetate, calcium salts, calcium carbonate, tribasic calcium phosphate, dicalcium phosphate, dibasic calcium phosphate, monobasic calcium sulfate monohydrate, calcium sulfate, granular calcium lactate trihydrate, magnesium carbonate, magnesium oxide, bentonite, kaolin, sodium chloride, and mixtures thereof;(c) at least one disintegrant is selected from the group consisting of starches, pregelatinized starch, sodium starch glycolate, clays, magnesiumaluminum silicate, cellulose-based disintegrants, powdered cellulose, microcrystalline cellulose, methylcellulose, low-substituted hydroxypropylcellulose, carmellose, carmellose calcium, carmellose sodium, croscarmellose sodium, alginates, povidone, crospovidone, polacrilin potassium, gums, agar, guar gum, locust bean gum, gum karaya, pectin, tragacanth gum, colloidal silicon dioxide, and mixtures thereof; and(d) at least one lubricant is selected from the group consisting of glyceryl behenate, stearic acid and salts thereof, magnesium stearate, calcium stearate, sodium stearate, hydrogenated vegetable oils, glyceryl palmitostearate, talc, waxes, sodium benzoate, sodium acetate, sodium fumarate, sodium stearyl fumarate, PEGs, PEG 4000, PEG 6000, poloxamers, polyvinyl alcohol, sodium oleate, sodium lauryl sulfate, magnesium lauryl sulfate, and mixtures thereof.
31. The pharmaceutical tablet of claim 30, wherein at least one disintegrant is present in an amount of about 3% by weight and at least one lubricant is present in an amount of about 1% by weight.
32. The pharmaceutical tablet of claim 31, wherein:(b) at least one filler comprises lactose and cellulose;(c) at least one disintegrant is a starch; and(d) at least one lubricant is stearic acid or salts thereof.
33. The pharmaceutical tablet of claim 31, wherein:(b) at least one filler comprises lactose monohydrate and microcrystalline cellulose;(c) at least one disintegrant is sodium starch glycolate; and(d) at least one lubricant is magnesium stearate.
34. The pharmaceutical tablet of claim 33, wherein a coating is added to the pharmaceutical tablet.
35. The pharmaceutical tablet of claim 34, wherein the coating comprises a polymer coating.
36. The pharmaceutical tablet of claim 35, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
37. The pharmaceutical tablet of claim 33, comprising:(a) about 0.25% by weight of tavapadon;(b) about 64% by weight of microcrystalline cellulose;(c) about 32% by weight of lactose monohydrate;(d) about 3% sodium starch glycolate; and(e) about 1% magnesium stearate.
38. The pharmaceutical tablet of claim 37, wherein the pharmaceutical tablet comprises about 0.25 mg of tavapadon.
39. The pharmaceutical tablet of claim 38, wherein the pharmaceutical tablet comprises:(b) about 63.83 mg of microcrystalline cellulose;(c) about 31.92 mg of lactose monohydrate;(d) about 3 mg sodium starch glycolate; and(e) about 1 mg magnesium stearate.
40. The pharmaceutical tablet of claim 39, wherein a coating is added to the pharmaceutical tablet.
41. The pharmaceutical tablet of claim 40, wherein the coating comprises a polymer coating.
42. The pharmaceutical tablet of claim 41, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
43. The pharmaceutical tablet of claim 33, comprising:(a) about 1% by weight of tavapadon;(b) about 63% by weight of microcrystalline cellulose;(c) about 32% by weight of lactose monohydrate;(d) about 3% sodium starch glycolate; and(e) about 1% magnesium stearate.
44. The pharmaceutical tablet of claim 43, wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
45. The pharmaceutical tablet of claim 44, wherein the pharmaceutical tablet comprises:(b) about 63.08 mg of microcrystalline cellulose;(c) about 31.92 mg of lactose monohydrate;(d) 3 about mg sodium starch glycolate; and(e) about 1 mg magnesium stearate.
46. The pharmaceutical tablet of claim 45, wherein a coating is added to the pharmaceutical tablet.
47. The pharmaceutical tablet of claim 46, wherein the coating comprises a polymer coating.
48. The pharmaceutical tablet of claim 47, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
49. The pharmaceutical tablet of claim 33, comprising:(a) about 5% by weight of tavapadon;(b) about 59% by weight of microcrystalline cellulose;(c) about 32% by weight of lactose monohydrate;(d) about 3% sodium starch glycolate; and(e) about 1% magnesium stearate.
50. The pharmaceutical tablet of claim 49, wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
51. The pharmaceutical tablet of claim 49, wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
52. The pharmaceutical tablet of claim 50, wherein the pharmaceutical tablet comprises:(b) about 59.08 mg of microcrystalline cellulose;(c) about 31.92 mg of lactose monohydrate;(d) about 3 mg sodium starch glycolate; and(e) about 1 mg magnesium stearate.
53. The pharmaceutical tablet of claim 52, wherein a coating is added to the pharmaceutical tablet.
54. The pharmaceutical tablet of claim 53, wherein the coating comprises a polymer coating.
55. The pharmaceutical tablet of claim 54, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
56. The pharmaceutical tablet of claim 51, wherein the pharmaceutical tablet comprises:(b) about 177.24 mg of microcrystalline cellulose;(c) about 95.76 mg of lactose monohydrate;(d) about 9 mg sodium starch glycolate; and(e) about 3 mg magnesium stearate.
57. The pharmaceutical tablet of claim 56, wherein a coating is added to the pharmaceuticaltablet.
58. The pharmaceutical tablet of claim 57, wherein the coating comprises a polymer coating.
59. The pharmaceutical tablet of claim 58, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
60. The pharmaceutical tablet of claim 49, wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
61. The pharmaceutical tablet of claim 60, wherein the pharmaceutical tablet comprises:(b) about 118.16 mg of microcrystalline cellulose;(c) about 63.84 mg of lactose monohydrate;(d) about 6 mg sodium starch glycolate; and(e) about 2 mg magnesium stearate.
62. The pharmaceutical tablet of claim 61, wherein a coating is added to the pharmaceutical tablet.
63. The pharmaceutical tablet of claim 62, wherein the coating comprises a polymer coating.
64. The pharmaceutical tablet of claim 63, wherein the coating comprises polyvinyl alcohol, polyethylene glycol, titanium dioxide, and talc.
65. The pharmaceutical tablet of any one of claims 1-36, wherein the pharmaceutical tablet comprises about .25 mg of tavapadon.
66. The pharmaceutical tablet of any one of claims 1-36, wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
67. The pharmaceutical tablet of any one of claims 1-36, wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
68. The pharmaceutical tablet of any one of claims 1-36, wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
69. The pharmaceutical tablet of any one of claims 1-36, wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
70. A pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about 12 pm.
71. The pharmaceutical tablet of claim 70, wherein the pharmaceutical tablet comprises about .25 mg of tavapadon.
72. The pharmaceutical tablet of claim 70, wherein the pharmaceutical tablet comprisesabout 1 mg of tavapadon.
73. The pharmaceutical tablet of claim 70, wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
74. The pharmaceutical tablet of claim 70, wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
75. The pharmaceutical tablet of claim 70, wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
76. A pharmaceutical tablet comprising tavapadon and at least one filler, wherein about 75% or more of the tavapadon is released in 20 minutes in 0.01N HC1 with 0.15% or 0.2 % SDS.
77. The pharmaceutical tablet of claim 76, wherein the pharmaceutical tablet comprises about .25 mg of tavapadon.
78. The pharmaceutical tablet of claim 76, wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
79. The pharmaceutical tablet of claim 76, wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
80. The pharmaceutical tablet of claim 76, wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
81. The pharmaceutical tablet of claim 76, wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
82. A method of manufacturing a pharmaceutical tablet comprising tavapadon and at least one filler; the steps comprising:(a) blending tavapadon with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
83. The method of claim 82, further comprising(a) blending tavapadon with filler and disintegrant to obtain the precompaction blend.
84. The method of claim 82, further comprising(a) blending tavapadon with filler, disintegrant, and intragranular portionlubricant to obtain the pre-compaction blend.
85. A method of manufacturing a pharmaceutical tablet, the steps comprising(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets.
86. The method of manufacturing of claim 85, wherein the disintegrant is sodium starch glycolate.
87. The method of manufacturing of claim 86, wherein the lubricant is magnesium stearate.
88. The method of manufacturing of claim 87, wherein the filler is microcrystalline cellulose and lactose monohydrate.
89. A pharmaceutical tablet comprising tavapadon and at least one filler wherein disintegration of the tablet is achieved within 15 minutes under guidelines and requirements of United States Pharmacopeia (USP) general chapter <701>.
90. A pharmaceutical tablet comprising tavapadon and at least one filler, manufactured by:(a) blending tavapadon with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules; and(d) compressing into tablets.
91. The pharmaceutical tablet of claim 90, manufactured by:(a) blending tavapadon with filler and disintegrant to obtain the precompaction blend.
92. The pharmaceutical tablet of claim 90, manufactured by:(a) blending tavapadon with filler, disintegrant, and intragranular portion lubricant to obtain the pre-compaction blend.
93. A pharmaceutical tablet comprising tavapadon and at least one filler; manufactured by(a) blending tavapadon, disintegrant, and intragranular portion lubricant with filler to obtain a pre-compaction blend;(b) compacting the pre-compaction blend to form ribbons;(c) milling the ribbons into granules;(d) blending the granules with extra granular portion lubricant to form a final blend; and(e) compressing the final blend into tablets.
94. The pharmaceutical tablet of claim 93, wherein the disintegrant is sodium starch glycolate.
95. The pharmaceutical tablet of claim 93, wherein the lubricant is magnesium stearate.
96. The pharmaceutical tablet of claim 93, wherein the filler is microcrystalline cellulose and lactose monohydrate.
97. A pharmaceutical tablet comprising tavapadon and at least one filler, wherein 90% or more dissolution of the tablet is achieved under guidelines and requirements of United States Pharmacopeia (USP) general chapter <711>.
98. A method for treating Parkinson's Disease (PD) in a patient, comprising administering to the patient a pharmaceutical formulation comprising:(a) about 0.25% by weight to about 15% by weight of tavapadon free base; and(b) at least about 80% by weight of at least one filler; wherein the Parkinson's Disease is effectively treated.
99. A pharmaceutical tablet comprising tavapadon and at least one filler; wherein the tavapadon is comprised of particles having an average D[4,3] of about < 25 pm.
100. The pharmaceutical tablet of claim 99, wherein the pharmaceutical tablet comprises about .25 mg of tavapadon.
101. The pharmaceutical tablet of claim 99, wherein the pharmaceutical tablet comprises about 1 mg of tavapadon.
102. The pharmaceutical tablet of claim 99, wherein the pharmaceutical tablet comprises about 5 mg of tavapadon.
103. The pharmaceutical tablet of claim 99, wherein the pharmaceutical tablet comprises about 10 mg of tavapadon.
104. The pharmaceutical tablet of claim 99, wherein the pharmaceutical tablet comprises about 15 mg of tavapadon.
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