47 results about "Controlled-Release Formulations" patented technology

The invention provides an oral solid formulation comprising (a) one or more controlled release components comprising a core comprising levodopa, esters or salts thereof and wherein the one or more controlled release components; and (b) one or more immediate release components comprising levodopa, esters or salts thereof. The oral solid formulation also contains a decarboxylase inhibitor and about 80% to 100% of the decarboxylase inhibitor present in the oral solid formulation is present in the one or more immediate release components.

The invention belongs to the technical field of pesticide preparations, and particularly relates to kresoxim-methyl drug-loaded microspheres as well as a preparation method and application thereof. The 9% pyraclostrobin drug-loaded microspheres (Pyr (at) COzein) are prepared by modifying a Zein-pesticide emulsifier 500 # complex with n-caprylic alcohol, and the n-caprylic alcohol has a synergistic effect on pyraclostrobin, so that not only can the defect of a sustained and controlled release preparation in the aspect of fast-acting sterilization be made up, but also the use dosage of pyraclostrobin can be reduced, the risk of pesticide residue can be reduced, and the drug-loaded microspheres have a good application prospect. The ecological safety is improved.

The invention provides an oral solid formulation comprising (a) one or more controlled release components comprising a core comprising levodopa; and (b) one or more immediate release components comprising levodopa. The oral solid formulation also contains a decarboxylase inhibitor wherein the one or more controlled release components are substantially free of the decarboxylase inhibitor.

The invention provides an oral solid formulation comprising (a) a plurality of controlled release components comprising (i) a core comprising a mixture of levodopa and at least one pharmaceutically acceptable excipient, (ii) a controlled release coating surrounding the core, (iii) a muco-adhesive coating surrounding the controlled release coating and (iv) an enteric coating surrounding the muco-adhesive coating; and (b) one or more immediate release components comprising levodopa. The oral solid formulation also contains carbidopa and about 80% to 100% of the carbidopa in the oral solid formulation is present in the one or more immediate release components.

The invention provides an oral solid formulation comprising (a) one or more controlled release components comprising a core comprising levodopa, esters or salts thereof and wherein the one or more controlled release components; and (b) one or more immediate release components comprising levodopa, esters or salts thereof. The oral solid formulation also contains a decarboxylase inhibitor and about 80% to 100% of the decarboxylase inhibitor present in the oral solid formulation is present in the one or more immediate release components.

A PLG copolymer material, called a PLG(p) polymer material adapted for use in a controlled release formulation for a bioactive material is provided, wherein the formulation exhibits a reduced initial burst effect when introduced into the tissue of a patient in need thereof. A method of preparing the PLG copolymer material is also provided, as are methods of use.

Provided herein are methods of treating COVID-19 in a subject in need thereof, comprising administering to the subject a 25-hydroxyvitamin D compound. Also provided herein are hard capsule dosage forms of 25-hydroxyvitamin. In aspects, the 25-hydroxyvitamin D is administered as a controlled release formulation, optionally an extended release oral formulation, such as Rayaldee® extended release calcifediol capsules. Methods of treating SARS-CoV-2 infection including reducing SARS-CoV-2 viral load are provided. Methods of treating SARS-CoV-2 infection including increasing an immune response are provided.

The present disclosure provides a method for delivering a neuroprotective polypeptide to at least a portion of a central nervous system (CNS) of a subject. The method includes administering to the systemic blood circulation of the subject a therapeutically effective amount of a neuroprotective polypeptide by a controlled-release formulation or a device providing a sustained release of the neuroprotective polypeptide including at least one neuroprotective polypeptide selected from the group consisting of GLP-1, exendin-4, or a therapeutically effective GLP-1 or exendin-4 analogue; the neuroprotective polypeptide binds to and activates a receptor that binds at least one of GLP-1, exendin-4, or a combination thereof; and the controlled-release neuroprotective formulation or the sustained release of the neuroprotective polypeptide enhances the delivery of the neuroprotective polypeptide across a blood-brain barrier (BBB) of the subject to at least a portion of the CNS relative to a rapid release formulation of the neuroprotective polypeptide. Also disclosed is a method of treating a subject with a CNS-related disease or reducing at least one symptom of a CNS-related disease in a subject in need thereof.

Formula I Provided is 4-(6-oxo-2-(trifluoromethyl)-3,6-dihydrochromeno[7,8-d]imidazol-8-yl)benzonitrile of Formula I, also known as CF3CN, for use in the treatment of positive symptoms of schizophreni

The invention discloses a CaCO3-based validamycin controlled release preparation and a preparation method thereof, and the preparation method comprises the following steps: taking glucose, amino acid and water as raw materials, reacting under a microwave heating condition, and standing to obtain carbon dots; wherein the amino acid is one or a mixture of more of lysine, histidine and arginine; the preparation method comprises the following steps: mixing validamycin, water and calcium acetate, stirring, adding carbon dots, and stirring to obtain a validamycin / carbon dot mixed solution; and adding a sodium carbonate aqueous solution into the validamycin / carbon dot mixed solution, stirring, standing, and drying the obtained precipitate to obtain the CaCO3-based validamycin controlled release preparation. The controlled release preparation has the characteristics of high drug loading rate, controllable drug release, simple preparation process and the like, and provides a new strategy for developing CaCO3-based nano pesticides.

Provided are compositions comprising nicorandil compound(s) in a controlled release formulation that releases at least about 30% of the nicorandil compound(s) into the intestine of human subjects. Such compositions can include a gastric acid dissolution susceptible component (GADSC) and a gastric acid dissolution resistant component (GADRC), wherein upon maintaining the composition in contact with a pH 1.2 dissolution media for a period of about 2 hours (1) the GADRC releases a statistically significantly smaller proportion of the one or more nicorandil compounds in the GADRC than the proportion of one or more nicorandil compounds release from the GADSC and (2) the composition releases no more than 50% of the one or more nicorandil compounds contained in the composition. The invention further provides methods of product such compositions and therapeutic uses of compositions, e.g., comprising once-daily administration of the composition to treat one or more diseases or conditions, including angina.

The present invention discloses a nano-intelligent pesticide slow-release material and a preparation method of its aqueous dispersion controlled-release preparation, comprising the following steps: S1. Prepare nano-hollow silica by the hard template method; S2. Modify to prepare an environment-responsive nano-hollow silica; S3. Load pesticide active substances by the solvent evaporation method to obtain an environment-responsive pesticide slow-release agent; S4. Prepare a nano-intelligent pesticide aqueous dispersion controlled-release preparation. The prepared nano-hollow silica is spherical in shape, with a particle diameter of 80-100 nm; the nano-hollow silica prepared by this method can be used to directly embed pesticide active substances; it has the characteristic of environmental responsiveness. The preparation method of the present invention has low cost, mild reaction conditions, and no three wastes; the product has a high loading rate, good water dispersibility, a long effective period, and reduces the number of pesticide applications; it has the characteristic of environmental responsiveness. When the temperature rises and the pH decreases, the polymer shell swells and collapses, and the pesticide is rapidly released, which can improve the utilization efficiency of the pesticide.

The present invention relates to tablet composition for oral administration of Ruxolitinib phosphate, with a combination of low viscosity HPMC and high viscosity HPMC.

The application belongs to the field of drug design, and discloses a preparation method of oral solid controlled-release preparation based on micro-droplet spraying, comprising the following steps: S1, separating and designing the distribution of active pharmaceutical ingredients and pharmaceutical excipients in the preparation; S2, recombining the ingredient information after the separation and design; S3, converting the ingredient distribution information after the combination into a slice recognizable by a 3D printing device; S4, printing by using a double-channel micro-droplet spraying 3D printer; and S5, using a powder material to receive the ingredients sprayed by the printer, so as to bond and form a solid preparation. The concentration gradient function defined by the application defines the concentration distribution method of the active pharmaceutical ingredients in the preparation, and solves the problem that the controlled-release preparation cannot achieve ideal controlled-release effect in principle; the 3D printing of the oral solid controlled-release preparation by using the double-channel micro-droplet spraying principle can change the existing preparation process mode, and can prepare the oral solid controlled-release preparation meeting the functional design requirements.

The invention provides an oral solid formulation comprising (a) a plurality of controlled release components comprising (i) a core comprising a mixture of levodopa and at least one pharmaceutically acceptable excipient, (ii) a controlled release coating surrounding the core, (iii) a muco-adhesive coating surrounding the controlled release coating and (iv) an enteric coating surrounding the muco-adhesive coating; and (b) one or more immediate release components comprising levodopa.

The absence of regulatory T cells (Treg) may underlie disorders including but not limited to autoimmunity, dermatitis, periodontitis and even transplant rejection. Enhancing local numbers of Treg through in situ Treg expansion or induction is contemplated herein as a treatment option for these disorders. Current methods for in vivo Treg expansion are not Treg specific and are associated with many adverse side-effects. The data presented herein provides in vitro testing of a Treg-inducing microparticle providing a predictable controlled release for combinations of cytokines and drugs (e.g., IL-2, TGF-β, and / or rapamycin) resulting in targeted Treg migration. These controlled release microparticles are also capable of inducing FoxP3+ Treg in human cells in vitro suggesting that these compositions be developed into an in vivo Treg induction and expansion therapy.

The present disclosure relates generally to the treatment of central nervous system disorders associated with phosphodiesterase 10A (PDE10A), such as schizophrenia, bipolar affective disorder, and Alzheimer's disease, as therapies for neurological and psychiatric disorders. The present disclosure provides controlled release formulations of 2-methyl-N-((5-methyl-1, 3, 4-thiadiazol-2-yl) methyl)-6-(((1S, 2S)-2-(5-methylpyridin-2-yl) cyclopropyl) methoxy) pyrimidin-4-amine (Compound A) and their use in the treatment of schizophrenia and other psychiatric disorders that improve tolerance characteristics.

The invention relates to the technical field of medicinal preparations, and provides a diclofenac sodium medicinal preparation as well as a preparation method and application thereof. The diclofenac sodium pharmaceutical preparation is prepared from the following components in parts by weight: 1 to 10 parts of diclofenac sodium, 5 to 10 parts of cationic lipid, 1 to 5 parts of PEGylated lipid and 0.1 to 5 parts of a surfactant. The active component diclofenac sodium in the pharmaceutical preparation is delivered through liposome, so that the preparation is endowed with a better transdermal absorption effect; meanwhile, an excellent controlled release effect is achieved, so that the blood concentration is more stable, and the liposome microcapsule is encapsulated, so that the stimulation to the stomach and intestine is effectively reduced, and the compliance of a patient can be effectively improved; the pharmaceutical preparation not only can be prepared into an external transdermal patch, but also can be prepared into an oral controlled-release preparation, and is wide in application.

The invention relates to the field of drug sustained-release and controlled-release preparations, in particular to potassium chloride pellets and a mother method and a preparation method thereof, and the mother method of the potassium chloride pellets comprises the following steps: (a) crushing potassium chloride crystals, and mixing the crushed potassium chloride crystals with a diluent with hydrogen bond forming ability to form potassium chloride mixed powder; (b) in a granulator, spraying a water-based adhesive into the potassium chloride mixed powder, so that the mixed powder is wet, the surface of potassium chloride is partially dissolved, meanwhile, the diluent adsorbs moisture through a hydrogen bond to form a network structure, and then initial mother nucleus particles are formed under the action of mechanical force; and (c) drying and screening the initial mother nucleus particles to obtain the potassium chloride pellet master batch. According to the invention, potassium chloride and the diluent with hydrogen bond forming ability are directly mixed for starting, a sucrose carrier in a traditional sugar pill process is abandoned, the range of applicable people is expanded, the process route is simplified, and meanwhile, the roundness, the particle size uniformity and the mechanical strength of mother nucleus particles are remarkably improved.

The present invention relates generally to the field of ocular therapeutics and the development thereof for use in humans or animals. More particularly, it relates to DHODH inhibitor compounds and their use for the treatment of ophthalmic diseases and disorders. The invention also relates to the local administration of such ophthalmic compositions, and in particular to their intravitreal administration. The invention relates also to controlled release formulations of therapeutically active agents, in particular of DHODH inhibitor compounds administered intraocularly, in particular in the posterior segment of the eye.

A production process for controlling the active ingredients of Cistanche deserticola Ma is provided, including: (1) crushing and screening the raw material of Cistanche deserticola Ma, mixing the powder of Cistanche deserticola Ma with a solvent, and then performing ultrasonic extraction; (2) performing centrifugation on the extraction solution, then performing membrane separation on the supernatant; (3) concentrating the solution containing the active ingredients of Cistanche deserticola Ma under vacuum, then mixing the concentrated solution with excipients and stirring evenly to prepare a controlled release formulation; (4) drying the prepared controlled release formulation of the active ingredients of Cistanche deserticola Ma to obtain a dried controlled release product of the active ingredients of Cistanche deserticola Ma. By adopting ultrasonic extraction, centrifugal impurity removal, membrane separation, vacuum concentration, and drying, the efficient extraction and purification of active ingredients in Cistanche deserticola Ma have been achieved, improving product quality and stability.

The application relates to the technical field of biological medicine manufacturing, and discloses a controlled-release type preparation composition for realizing ovary function recovery, which comprises a core active unit, a moisturizing slow-release unit and a plant extract component. The core active unit is an anisotropic core-shell structure microcapsule with asymmetric charge distribution, which is composed of chitosan, polyglutamic acid and an internal compound, and a layer of outwardly radiating carboxyl brush-shaped molecular chain is distributed on the surface of the core active unit. The moisturizing slow-release unit comprises a polymer skeleton formed by rosmarinic acid and hyaluronic acid, and the polymer skeleton internally occludes elemene. The application utilizes a kinetic restriction mechanism to construct an anisotropic surface layer topology, avoids mucus protein adsorption, induces anti-inflammatory immune regulation by physically adapting mucosal receptors, the moisturizing slow-release unit firstly constructs a physical barrier to repair damage, and the core active unit is used to realize component graded controlled release.

The invention discloses a controlled release preparation and a preparation method thereof. Specifically, the controlled release preparation comprises a drug crystal and a polymer coating wrapping the drug crystal, the preparation method of the controlled release preparation comprises the following steps: carrying out polymerization reaction on a monomer on the surface of a drug crystal to form a polymer coating, or carrying out cross-linking reaction on a polymer on the surface of the drug crystal to form the polymer coating. The controlled release preparation is high in drug loading capacity, long in drug release time, capable of achieving long-acting zero-order release of drugs, simple in preparation method and high in encapsulation efficiency.

A formulation of octreotide or pharmaceutically acceptable salts thereof, which provides controlled release of a therapeutically effective amount of octreotide for a period of at least about two months. Methods of treating acromegaly, decreasing growth hormone, decreasing IGP-1, and treating conditions associated with carcinoid tumors and VIPomas by administering a controlled release formulation of octreotide are provided herein.

To provide modified release formulations of 2-methyl-2-(3-methyl- 4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts thereof, and methods of treatment with the modified release formulations.SOLUTION: An embodiment of the present disclosure includes a modified release formulation comprising a therapeutically effective amount of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile and at least one release modifier.SELECTED DRAWING: None

Provided are a novel drug carrier and a drug release-controlling formulation using the same. A drug carrier according to an embodiment comprises an aggregate of cellooligosaccharides having, at an anomeric position of a reducing terminal, a substituent including an alkyl group. A drug release-controlling formulation according to an embodiment comprises said drug carrier and a hydrophobic drug.

The invention provides an oral solid formulation comprising (a) a plurality of controlled release components comprising (i) a core comprising a mixture of levodopa and at least one pharmaceutically acceptable excipient, (ii) a controlled release coating surrounding the core, (iii) a muco-adhesive coating surrounding the controlled release coating and (iv) an enteric coating surrounding the muco-adhesive coating; and (b) one or more immediate release components comprising levodopa. The oral solid formulation also contains carbidopa and about 80% to 100% of the carbidopa in the oral solid formulation is present in the one or more immediate release components.

The invention relates to the technical field of pharmaceutical preparations, and particularly discloses a cilostazol controlled-release preparation and a preparation method thereof. The preparation is based on a composite carrier composed of mesoporous silica and low-substituted hydroxy propyl cellulose, the cilostazol is highly dispersed in the composite carrier in an amorphous state through combination of ball milling pretreatment and a high-temperature fluidized bed melt dispersion process, and a final tablet is obtained through tabletting by adopting a step-by-step design of internally and externally adding a disintegrating agent. The dissolution rate of the cilostazol preparation prepared by the invention is greater than or equal to 80% within 15 minutes and greater than or equal to 95% within 30 minutes, so that rapid and stable drug release is realized, and the risk of burst release of the drug and adverse reaction caused by fluctuation of blood concentration are effectively reduced; and the preparation shows excellent stability, and an acceleration test (6 months) result shows that the increase of related substances of the preparation is less than or equal to 0.5%, the change rate of the dissolution rate is less than or equal to 3%, and the consistency and reliability of the curative effect in the clinical medication process can be effectively guaranteed.