29 results about "Controlled-Release Formulations" patented technology

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.

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.

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.

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.

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 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.

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.

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.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to an aripiprazole-4-chlorobenzoic acid-hydrate crystal form and a preparation method thereof. A basic unit of the aripiprazole crystal form is composed of one molecule of aripiprazole, one molecule of 4-chlorobenzoic acid and one molecule of water. The aripiprazole crystal form obtained by the invention has relatively high stability, and the dissolving property of the aripiprazole crystal form can meet the requirements of a sustained and controlled release preparation on the drug release characteristic, so that the stable and sustained release of the drug is realized, and the curative effect and the safety of the preparation are improved. The preparation process of the crystal form is simple, conditions are mild, process control and large-scale production are easy to realize, and the crystal form has a wide industrialization prospect.

The invention discloses a polypeptide for promoting bone formation and application thereof. The amino acid sequence of the polypeptide is as shown in SEQ ID NO. 1. The polypeptide provided by the invention contains 8 amino acid oligopeptides, has the characteristics of small molecule, easiness in absorption and capability of being made into a sustained and controlled release preparation, and is suitable for clinical medication characteristics and requirements of osteoporosis patients. The polypeptide is convenient to synthesize, can be industrially produced, and has a good application prospect in the fields of foods, medicines, health-care products and the like.

The present disclosure relates generally to treatment of central nervous system disorders associated with phosphodiesterase 10A (PDE10A) such as schizophrenia, bipolar disease, and Alzheimer's disease, as therapeutics for neurological and psychiatric disorders. This 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 improves the tolerability profile.

To provide a solid preparation for a highly lipophilic physiologically active substance such as cannabinoid which releases the physiologically active substance and can be prepared by a simple method.SOLUTION: The present invention relates to a product for the release of a highly lipophilic bioactive substance comprising a core and a coating on the core, wherein the coating comprises one or more highly lipophilic bioactive substances, one or more water-soluble film-forming agents and up to 20% by weight, based on the weight of all components, of other excipients.SELECTED DRAWING: Figure 1

The invention provides compositions and methods for the treatment of depression and other psychiatric disorders. In particular, the invention provides sustained- or controlled-release formulations, particularly extended or slow release formulations, which include at least one monoamine oxidase inhibitor (MAOI), as well as combination therapies that include at least one MAOI and at least one norepinephrine-reuptake-inhibitor (NRI), for use in such compositions and methods. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

To provide a novel drug carrier and a drug release controlled preparation using the drug carrier.SOLUTION: A drug carrier according to an embodiment includes an aggregate of cello-oligosaccharides each having, at the anomeric position of a reducing end, a substituent containing an alkyl group. A drug release controlled preparation according to an embodiment includes the drug carrier and a hydrophobic drug.SELECTED DRAWING: Figure 2

Providing a controlled-release formulation containing dorotaberine or its salts, or an active substance with a similar tendency to degrade through oxidation / hydrolysis. [Solution] The present invention provides a controlled-release formulation containing dorotaberine or a salt thereof, or an active substance with a similar tendency to degrade through oxidation / hydrolysis. The present invention provides a once- or twice-daily controlled-release formulation of dorotaberine or a salt thereof that avoids fluctuations in plasma levels, reduces pill burden and side effects through a simplified dosing schedule, and consequently improves patient compliance. The present invention also provides a method for preparing a controlled-release formulation of dorotaberine or a salt thereof. The present invention further provides a controlled-release formulation of dorotaberine or a salt thereof for the treatment of at least one symptom of gastrointestinal, biliary, urinary, and gynecological disorders characterized by a spastic state of smooth muscle in a subject.

The present invention relates to a biphasic controlled-release preparation and preparation thereof. The biphasic controlled-release preparation can take effect quickly in vivo, quickly reach a peak value of blood drug concentration, then keep stable release, maintain stable blood drug concentration and reduce the fluctuation between wave peaks and wave valleys. The controlled-release preparation consists of three parts, namely an immediate-release layer, a tablet core layer and a blocking layer. The immediate-release layer is rapidly dissolved in vitro, and the combination of the remaining tablet core layer and the blocking layer can maintain the zero-order release in vitro.

The present invention relates to a product for the release of highly lipophilic bioactive substances, comprising a core and a coating on the core, wherein the coating comprises one or more highly lipophilic bioactive substances, one or more water-soluble film-forming agents, and up to 20% by weight of other excipients based on the weight of all ingredients.

The present application relates to the field of drug sustained-release controlled-release preparation, and particularly relates to a potassium chloride pellet and a preparation method and a mother method thereof, the mother method of the potassium chloride pellet comprising the following steps: (a) crushing potassium chloride crystals and mixing the potassium chloride crystals with a diluent having hydrogen bond forming capacity to form a potassium chloride mixed powder; (b) in a granulator, spraying the potassium chloride mixed powder with an aqueous binder to make the mixed powder wet and the surface of the potassium chloride partially dissolve, and at the same time, the diluent forms a network structure by hydrogen bond adsorption of moisture, and then initial mother core particles are formed under the action of mechanical force; (c) drying and screening the initial mother core particles to obtain potassium chloride pellet mother particles. The present application adopts direct mixing of potassium chloride and a diluent having hydrogen bond forming capacity to form a mother, discards the sucrose carrier in the traditional sugar pellet process, expands the scope of the applicable population and simplifies the process route, and the roundness, particle size uniformity and mechanical strength of the mother core particles are significantly improved.

It is proposed that dissipation of relative benefit during long-term treatment is due to long-term tolerance to stimulant medications. To improve adherence and persistence of medication use, it is advantageous to develop medications that are not undermined by long-term tolerance. Disclosed herein in certain implementations are methods for the prevention of accumulated tolerance to stimulant medication for the treatment of ADHD based on two principles: (a) retaining the initial immediate-release component of controlled-release formulations, and (b) replacing the subsequent sustained-release component (i.e., an ascending delivery of stimulant medication to counteract acute tolerance) with a controlled-release component designed to prevent carry-over effects on background tonic dopamine.