58 results about "Sustained Release Formulations" patented technology

The present invention provides, in part, compositions comprising a peptide that is larazotide or larazotide derivative, or salt thereof, contained within a matrix that provides for controlled release and sustained release formulations. The present invention contemplates that these compositions, formulations and methods can be useful for treating diseases and disorders of the small bowel.

The present application provides approximately spherical lactic acid-glycolic acid copolymer (PLGA) microparticles comprising a biologically active substance, wherein an average volume-based particle diameter of the PLGA microparticles is 1 µm or more and 150 µm or less, and a Reactive Span Factor (R.S.F.) of the PLGA microparticles is satisfied with formula (1): 0.1 < (R.S.F.) ≤ 1.7 formula (1), wherein an R.S.F. means (D90 - D10) / D50; D90 is a particle diameter (µm) corresponding to the cumulative 90% by volume of the cumulative particle diameter distribution from the small particle side; D50 is a particle diameter (µm) corresponding to the cumulative 50% by volume of the cumulative particle diameter distribution from the small particle side; and D10 is a particle diameter (µm) corresponding to the cumulative 10% by volume of the cumulative particle diameter distribution from the small particle side; and an efficient production method thereof. The present invention provides the approximately spherical PLGA microparticles having an average volume-based particle diameter of 1 µm or more and 150 µm or less wherein there are few coarse particles or ultrafine particles without a classification step, and the particle diameter distribution is sharp around the target particle diameter.

Provided herein are pharmaceutical formulations comprising glucokinase activator, or a prodrug, or a pharmaceutically acceptable salt, an isotope labeled analogue, a crystalline form, a hydrate, a solvate, or a diastereomeric or enantiomeric form thereof and the use thereof for treating diseases; the pharmaceutical formulations are in the form of immediate-release formulations, extended-release formulations, or combination of immediate-release formulation and extended-release formulations. The pharmaceutical formulations achieved once-a-day therapy for some diseases, in particular, type II Diabetes Mellitus with obesity. The pharmaceutical formulations exhibit sustained 24 hours of glucose-lowering effects. The pharmaceutical formulations also achieved lower Cmax, extended T1 / 2 as well as maintained similar bioavailability and increased MRT compared with commercial Dorzagliatin tablet, enhanced the pharmacology effect of restoring the glucose stimulated GLP-1 secretion in diabetes with obesity.

The invention provides a long-acting microsphere sustained release preparation and a preparation method thereof, and belongs to the technical field of sustained release preparations, the long-acting microsphere sustained release preparation is prepared from the following raw materials of effective components: 9.5 to 10.5 parts of antipsychotic drug, 48 to 50 parts of hydroxypropyl-beta-cyclodextrin, 50 to 52 parts of polylactic acid-glycolic acid copolymer, 1.25 to 1.3 parts of glycerol triacetate and 10 to 11 parts of polyvinyl alcohol. The preparation method comprises the following steps: firstly, the hydroxypropyl-beta-cyclodextrin is used for clathration of the antipsychotic drug, the obtained clathrate compound is further clathrated by the polylactic acid-glycolic acid copolymer, and the long-acting microsphere sustained release preparation is obtained. According to the invention, the double-valve design of beta-CD and PLGA synergistic inclusion is utilized, so that the preparation can realize two-stage release; the macroscopic slow release characteristic of the PLGA is combined with the microcosmic express characteristic of the hydroxypropyl-beta-cyclodextrin, so that the technical limitation of a single carrier is broken through.

The present disclosure relates to a method of preparing a sustained release formulation, the method comprises, mixing of a carrier composition with a volatile organic substance to form a blend; the carrier composition comprises: (i) a hydrophobic organic carrier; and (ii) a quaternary amine, as well as to methods of preparing the sustained release formulation. Also forming part of the present disclosure is a sustained release formulation comprising a blend of: (i) a hydrophobic organic carrier; (ii) a quaternary amine and (iii) a volatile organic substance; wherein the sustained release formulation is essentially water free; and wherein the quaternary amine is of a source different from the source of the hydrophobic organic carrier, as well as to the uses of the sustained release formulation for controlling a target organism. Finally, there is a disclosed carrier composition comprising a blend of: (i) a hydrophobic organic carrier; and (ii) a quaternary amine.

The sustained-release formulation of this invention, with its increased initial release, exhibits a rapid release effect within 24 hours after administration, followed by a sustained-release effect, thus simultaneously achieving both prolonged efficacy and rapid initial release. The sustained-release formulation of this invention, containing microspheres of leuprorelin, possesses excellent bioavailability and has been proven safe in humans; therefore, it can be effectively and safely used to treat various luteinizing hormone-releasing hormone-related diseases such as endometriosis, uterine fibroids, prostate cancer, premenopausal breast cancer, and central precocious puberty.

The present invention relates to a pharmaceutical composition comprising a pharmaceutically acceptable vehicle and non-pungent derivatives of capsaicin, in their tautomeric forms and pharmaceutically acceptable salts, as the sole active ingredient, for use in the stimulation of the sphenopalatine ganglion and the enhancement of cerebral blood flow, to prevent or reduce brain injury resulting from decreased cerebral blood flow. The composition is administered via the oral transmucosal route, preferably in the form of a mucoadhesive tablet, and may be formulated for immediate or prolonged release, ensuring effective and tolerable absorption while avoiding the irritant effects associated with pungent capsaicin.

The present application relates to microspheres in which a physiologically active substance is uniformly dispersed and a sustained release preparation containing the same. In the present application, provided are microspheres having a lactic acid / glycolic acid copolymer (PLGA) as a main component in which a physiologically active substance is uniformly dispersed, the microspheres being characterized in that the average volume-based particle diameter of the microspheres is 1 [mu] m to 150 [mu] m, and blocks or pores of the physiologically active substance are not present in the microspheres in an amount of 1.5 [mu] m or more. The microspheres according to the present invention can appropriately control the initial release amount of a physiologically active substance and the release rate during the subsequent release period, and can continuously release the physiologically active substance in a living body for a certain period of time.

The application discloses a kind of self-assembly hydrogel, preparation method and application, belong to material field.The application claims to protect a kind of self-assembly hydrogel, it is formed by glycyrrhizic acid, five gallate glucose and paeonol by molecular self-assembly;Wherein, the mass ratio of glycyrrhizic acid and five gallate glucose, paeonol is (10~60) :(1~8) :(2~8).The self-assembly hydrogel provided by the application is suitable for skin, raw material is natural, biocompatibility is good, mechanical and storage stability is excellent, can release paeonol and the transdermal effect is good, three components synergistically improve atopic dermatitis and other skin inflammation, and clinical value is high.In addition, the preparation process of the self-assembly hydrogel of the application is simple, can be prepared using conventional one-pot method, easy to produce.Therefore, the self-assembly hydrogel of the application has the prospect of developing into paeonol sustained-release delivery system, paeonol transdermal sustained-release preparation or skin inflammation treatment drug.

This invention relates to the field of pharmaceutical formulation technology, specifically to a sustained-release formulation of rifabutin, and more specifically, to a sustained-release rifabutin formulation composition for treating Helicobacter pylori infection. The key technical point of this invention is that it uses a novel antibiotic for treating Helicobacter pylori infection as the active ingredient, supplemented with specific inactive ingredients, including a hydrophilic gel-type matrix sustained-release material, a swelling agent, a buoyancy aid, and a lubricant. Through the synergistic effect of the hydrophilic gel-type matrix sustained-release material, the swelling agent, and the buoyancy aid, the composition can rapidly swell in gastric juice and maintain a floating state, thereby significantly prolonging the residence time of the formulation in the stomach and upper small intestine. This invention solves the technical problem of conventional formulations having a short residence time in the stomach and requiring frequent administration to maintain an effective antibacterial concentration, achieving the goal of effectively eradicating Helicobacter pylori by reducing the number of doses while maintaining an effective concentration at the site of infection for a longer period.

The invention belongs to the technical field of medical drugs, and discloses a nifedipine biphase sustained release preparation and a preparation method thereof. The nifedipine biphase sustained-release preparation consists of a double-layer tablet core and a film coating, wherein the double-layer tablet core consists of a drug-containing quick-release layer and a drug-containing sustained-release layer; nifedipine is respectively dispersed in the sustained-release layer and the quick-release layer according to a certain proportion. The biphasic sustained release preparation provided by the invention can take effect quickly, has stable and lasting drug effect, is safe and reliable, and is simple and efficient in preparation process.

Drug-loaded microspheres containing both a steroidal anti-inflammatory drug and a non-steroidal anti-inflammatory drug and injectable formulations containing the microspheres for sustained release of both drugs are disclosed. Methods of making such drug-loaded microspheres, formulations, and use of them for treating pains and inflammations, especially those caused by rheumatoid arthritis or osteoarthritis using such microspheres and formulations are also described.

A malleable sustained release formulation is created utilizing a local anesthetic wherein the composition is made sustained release by incorporating it into a bovine or porcine hemostatic agent. The composition is malleable enough to fit into a cavity such as a dental cavity and form the shape of the cavity. In addition to providing sustained release of the anesthetic, the composition also provides quicker reduction in bleeding.

The present invention provides pharmaceutical compositions and methods for treating fatigue or excessive daytime sleepiness associated with narcolepsy. [Solution] A pharmaceutical composition comprising an immediate-release component containing 4-((L-valyl)oxy)butanoic acid and a controlled-release component containing 4-((L-valyl)oxy)butanoic acid, as well as the pharmacokinetics of 4-((L-valyl)oxy)butanoic acid and γ-hydroxybutyrate after oral administration of the pharmaceutical composition are disclosed.

Pharmaceutical compositions of colchicine for once-a-day oral administration are provided. The formulations comprise a sustained-release component and an optional immediate-release component, the compositions of which can be selectively adjusted, respectively, to release the active ingredient along a pre-determined or desired release profile. Methods of treating or preventing cardiovascular disease and / or inflammatory disease in mammalian subjects comprising the administration of the novel formulations disclosed herein are also provided.

Disclosed is a sustained-release formulation of semaglutide. The sustained-release formulation of semaglutide comprises semaglutide or a pharmaceutically acceptable salt thereof, triacylglycerol, phosphatidylcholine, absolute ethanol, a solubilizer, and a pH regulator.

The invention relates to a preparation method of a multilayer sustained-release drug-loaded microsphere for articular cavity injection, and belongs to the field of biomedical materials and sustained-release preparations. The microsphere aims at solving the problems that traditional articular cavity lubricating gel is short in acting time and uncontrollable in drug release, and common drug-loaded microspheres are remarkable in burst release and insufficient in lubricity. The microsphere is constructed by adopting a natural material with good biocompatibility, collagen is taken as a core to load a drug, and a chitosan controlled release layer and a sodium hyaluronate lubricating layer are sequentially coated through electrostatic adsorption and covalent crosslinking to form the composite microsphere with a'core-shell-lubrication 'multilayer structure. The preparation method is based on a technical path technology of combining'crosslinking agent premixing emulsification-in-situ reaction curing 'and'layer-by-layer self-assembly-covalent crosslinking', and effective entrapment of drugs, stable construction of a controlled release structure and regulation and control of a degradation period are realized by optimizing process conditions. The microsphere can realize long-acting release of a medicine in a simulated environment, and the sodium hyaluronate on the outer layer of the microsphere material can improve the injection and pushing smoothness and is beneficial to the instant lubricity of the microsphere and retention of the microsphere in an articular cavity; all layers of materials are biodegradable, and degradation products have a potential nutrition support effect on joint tissues. The invention provides a microsphere delivery system with comprehensive performance for local treatment of joint diseases such as osteoarthritis.

The invention relates to the technical field of sustained-release preparations, and discloses a hydrogel dressing based on a sugar response sustained-release drug as well as a preparation method and application of the hydrogel dressing. HA-PBA is used as a first network to provide sugar responsiveness and biological activity, PVA is used as a second network to enhance mechanical strength and moisture retention, HA-PBA and PVA form boric acid ester bonds under the alkaline condition of 7.2-9.0, a double-network structure is formed through interaction of the boric acid ester bonds and hydrogen bonds, and the hydrogel is obtained. The hydrogel formed by the invention can be endowed with self-healing and shear thinning characteristics, and the shear thinning characteristic enables the hydrogel to have injectability, so that the hydrogel is suitable for minimally invasive implantation; and the self-healing capability ensures that the dressing recovers integrity after the wound surface deforms. When the hydrogel is used for treating chronic diabetic wounds, borate bonds are dissociated under high glucose concentration, so that the degradation of the hydrogel network is accelerated, the functional protein medicine is released to realize treatment, and the treatment accuracy is improved.

Provided are a sustained-release preparation and a preparation method therefor. The sustained-release preparation comprises a pharmaceutically active ingredient, triacylglycerol, phosphatidylcholine, a solvent, a solubilizer, and a pH regulator. The preparation method comprises: thoroughly mixing the pharmaceutically active ingredient, triacylglycerol, phosphatidylcholine, the solvent, the solubilizer, and the pH regulator.

The present invention relates to a solid oral pharmaceutical for Tetrahydrocannabinol (API) or any other Cannabinoid (API) with a novel, well defined method to enhance solubility of active pharmaceutical ingredients (API) with low solubility in aqueous media and use those enhanced API in a new approach of preparing modified and / or sustained release pharmaceutical formulation for API which are regularly not suitable for sustained release formulations because of their low solubility. This invention is applicable for small molecule API (molecular weight < 1000) for which the solubility can be enhanced by formation of a e.g., Cyclodextrin Complex regardless which Cyclodextrin or derivate thereof is employed according to the method described in this invention. Tetrahydrocannabinol and other Cannabinoids can be found in a wide range of indications like pain relief, insomnia, anti- depression and others.

The present application relates to the construction method of the ophthalmic protein drug sustained-release preparation, the ophthalmic protein drug is contacted with the weakly interacting excipient of pharmaceutically acceptable, and the protein pre-holding complex is formed;The first hydration excipient and the second hydration excipient are sequentially added to the protein pre-holding complex, and the layered hydrated protein complex is formed;The layered hydrated protein complex is dispersed in the first continuous phase of the ionizable group-containing pharmaceutically high polymer, and the ion pairing release blocking layer is formed in the periphery by adjusting the ion environment, and the intermediate is obtained;The intermediate is dispersed in the second continuous phase of the ophthalmic pharmaceutically acceptable, and the ophthalmic protein drug sustained-release preparation is prepared.The ophthalmic protein drug is pre-held with the weakly interacting excipient, the differentiated occupation area and the layered hydration structure are constructed, the protein stability is improved;Through the stage ion regulation, the pharmaceutically high polymer forms the non-closed ion pairing release blocking layer, the protein release fine control is realized, the drug efficacy is prolonged and the curative effect is improved.

The present application relates to a kind of amoxicillin gastric retention sustained-release preparation, which contains amoxicillin, sustained-release material, swelling agent and other pharmaceutical adjuvant, preferably also contains stabilizer or ion regulator.The combination of the above-mentioned adjuvant can be retained in the stomach for up to 24 hours, the complete release time is 10-24h, which can significantly prolong the retention time of amoxicillin in the stomach, has the advantages of fast floating, high effective concentration of drug in the stomach, long stable concentration time, and is beneficial to reduce the frequency of drug administration of patients;Further preferably, it is made into a double-layer tablet containing immediate-release layer, which can quickly reach effective concentration and also can be released slowly and continuously, maintaining effective concentration for a long time;When combined with proton pump inhibitors such as vonolabian, etc., combination kit or compound, only 1-2 times per day is needed, which can further improve the therapeutic effect and patient compliance.

The invention relates to a sustained release preparation for treating benign prostatic hyperplasia. The sustained release preparation contains silodosin and a sustained release material, the sustained-release material is a hydrophilic gel skeleton sustained-release material with the viscosity of 1000 mPa.s or above. The sustained-release preparation disclosed by the invention can realize an expected sustained-release effect in vivo.

Disclosed is a sustained-release formulation of semaglutide, which comprises semaglutide or a pharmaceutically acceptable salt thereof, triacylglycerol, phosphatidylcholine, absolute ethyl alcohol, a solubilizing agent, and a pH adjusting agent.

To provide a sustained release formulation that exhibits sufficient dissolution after 24 hours and comprises stable guanfacine or a pharmaceutically acceptable salt thereof.SOLUTION: A sustained release formulation comprises: guanfacine or a pharmaceutically acceptable salt thereof as an active ingredient; a binder; and a pH adjusting agent. Here, the pH adjusting agent is L-aspartic acid.SELECTED DRAWING: None

The present invention relates to sustained release formulations of Potassium chloride crystals having a mesh size ranging from about 60 to 100 mesh, combined with one or more pharmaceutically acceptable excipients, wherein the potassium chloride crystals are coated with a coating solution comprising cellulosic polymer in an amount up to 9% w / w based on the total weight of the granules and to processes for their preparation.

Approximately spherical lactic acid-glycolic acid copolymer (PLGA) microparticles include a biologically active substance. An average volume-based particle diameter of the PLGA microparticles is 1 μm or more and 150 μm or less. A Reactive Span Factor (R.S.F.) of the PLGA microparticles is satisfied with formula (1): 0.1<(R.S.F.)≤1.7 formula (1), wherein an R.S.F. means (D90−D10) / D50; D90 is a particle diameter (μm) corresponding to the cumulative 90% by volume of the cumulative particle diameter distribution from the small particle side; D50 is a particle diameter (μm) corresponding to the cumulative 50% by volume of the cumulative particle diameter distribution from the small particle side; and D10 is a particle diameter (μm) corresponding to the cumulative 10% by volume of the cumulative particle diameter distribution from the small particle side.

The present application relates to a new medical use of Astragaloside IV, and particularly relates to the use of Astragaloside IV in the preparation of a medicine for promoting the osteogenic differentiation of BMSCs of a patient with congenital scoliosis. The present application discloses that Astragaloside IV can specifically up-regulate the expression of WISP2, and then activate the Wnt / β-catenin pathway, significantly improve the alkaline phosphatase activity, mineralization capacity and osteogenic related gene expression of CS-BMSCs. Through cell induction, animal implantation and targeted sustained-release preparation and other experimental means, the present application confirms the safety and effectiveness of Astragaloside IV in repairing CS-related osteoporosis, and has a good application prospect.

Disclosed is a sustained-release formulation of semaglutide. The sustained-release formulation of semaglutide comprises semaglutide or a pharmaceutically acceptable salt thereof, triacylglycerol, phosphatidylcholine, absolute ethanol, a solubilizer, and a pH regulator.

The invention provides sustained-release cellulose, a preparation method thereof and an oral sustained-release preparation, and relates to the field of sustained-release preparation carriers. The preparation method of the slow-release cellulose comprises the following steps: mixing a hydrogen bond acceptor, a hydrogen bond donor and water, and forming a uniform and transparent eutectic solvent under heating and stirring conditions; wherein the hydrogen bond donor is carboxyl-containing organic acid, and the number of carboxyl groups in the carboxyl-containing organic acid is greater than or equal to 2; and adding a cellulose raw material into the eutectic solvent, reacting, carrying out solid-liquid separation on the reaction product, washing the solid obtained by solid-liquid separation with water until the solid is neutral, and drying to obtain the slow-release cellulose. The prepared slow-release cellulose has the pH response characteristic, the structure of the slow-release cellulose changes along with different environmental pH values, and when the slow-release cellulose serves as a carrier of a slow-release preparation, carboxyl of the slow-release cellulose is protonized in an acid environment, the structure is compact, and the slow-release cellulose has a slow-release effect; in a neutral / alkaline environment, carboxyl deprotonation and network swelling are realized, and targeted release of drugs is promoted.