Abstract

Provided are a celecoxib nanocrystal injection, a preparation method therefor, and use thereof, belonging to the field of pharmaceutical formulations. The provided celecoxib nanocrystal injection comprises celecoxib nanocrystals, a wetting agent, a stabilizer, and an osmotic pressure regulator. Moreover, the average particle diameter of the celecoxib nanocrystals is 100-500 nm. Optionally, the celecoxib nanocrystal injection further comprises a pH regulator and/or a lyoprotectant. After intravenous injection, the provided celecoxib nanocrystal injection can be rapidly dissolved in plasma, so that the application expectation of rapid onset of action in clinical acute pain management can be met. The celecoxib nanocrystal injection is prepared by adopting a combined technique of ball milling method and high-pressure homogenization. The ball milling method can process the micron-sized raw materials to the nanoscale, which can be further processed to a target particle diameter by high-pressure homogenization.

IPC Classes  ?

• A61K 9/10 - DispersionsEmulsions
• A61K 9/14 - Particulate form, e.g. powders
• A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
• A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
• A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]

Abstract

A gemcitabine liposome pharmaceutical composition, a preparation method therefor and use thereof. According to the preparation method for the liposome, by means of optimization and control of the proportion of phospholipid to cholesterol, the proportion of the total lipid to an optional long circulating functional material, the proportion of the total lipid to a drug, and the type and the concentration of a salt solution in an aqueous interior, a liposome, which has high encapsulation efficiency, good storage stability, and high filtering performance, is not easy to leak, is stable and controllable to release, prolongs the half-life remarkably, improves the therapeutic effect, and reduces toxic and side effects, is prepared. In addition, the provided liposome prescription and preparation process are simple, and scaled-up production and clinical popularization and application are facilitated.

IPC Classes  ?

• A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• A61K 9/1278 - Post-loading, e.g. by ion or pH gradient
• A61P 35/00 - Antineoplastic agents

Abstract

A continuous delivery preparation capable of being stably released and a preparation method therefor, wherein the preparation includes an active pharmaceutical ingredient and a gel carrier, and the gel carrier includes a biodegradable polymer, an organic solvent, a hydrophobic additive, and an optional hydrophilic gel matrix material. Compared with an in-situ gel prepared using a conventional Atrigel technology, the delivery preparation has the effect of slowing down in vitro and vivo burst release of the drug after a small amount of the hydrophobic additive and the optional hydrophilic gel matrix material are added, and the in-vivo blood drug concentration can be maintained for more than one week in a safe and effective range. The preparation method of the preparation is simple.

IPC Classes  ?

• A61K 9/06 - OintmentsBases therefor
• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/4985 - Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
• A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
• A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
• A61K 47/22 - Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers

Abstract

Disclosed in the present application is a long-acting and sustained-release preparation composition of lumateperone, the composition comprising lumateperone or a salt thereof and a polymer material, wherein the mass ratio of lumateperone to the polymer material is 0.5 : 9.5 to 5 : 5; the polymer material comprises a main material, i.e. polylactide, and an optional release regulator; the mass of the release regulator is 0% to 95% of that of the main material, i.e. polylactide; and the release regulator is selected from one of or a mixture of more than one of polylactide or polylactide-glycolide. The long-acting and sustained-release preparation of the present invention can achieve a sustained-release effect ranging from one week to three months, can improve the compliance of a patient, and has no obvious burst release in the early stage and no release lag phase, has stable release of the preparation, and ensures the safety and effectiveness of drug release.

IPC Classes  ?

• A61K 9/16 - AgglomeratesGranulatesMicrobeadlets
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61P 25/18 - Antipsychotics, i.e. neurolepticsDrugs for mania or schizophrenia

Abstract

A method for preparing a sterile in-situ gel on the basis of a solvent removal technique and a product thereof. Provided is a method for preparing an in-situ gel. Compared with traditional sterile production methods for in-situ gel preparations, the viscosity of a preparation solution is reduced by means of adding a volatile solvent in the production process, so that filtering and sterilization can be performed, and subsequently, the volatile solvent in the preparation can be removed by means of various methods, which does not have any adverse effect on the finally prepared in-situ gel preparation. Research data shows that for the in-situ gel preparation prepared by means of using the preparation method, volatile solvent residues therein meet safety standards, and compared with preparations prepared by the traditional preparation method of radiation sterilization, the types and amounts of degradation impurities of the polymer and pharmaceutically active ingredients therein are reduced, so that the safety of the preparation is improved.

IPC Classes  ?

• A61K 9/06 - OintmentsBases therefor
• A61K 47/36 - PolysaccharidesDerivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
• A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
• A61L 2/02 - Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lensesAccessories therefor using physical phenomena

Abstract

A gemcitabine liposome pharmaceutical composition, a preparation method therefor and use thereof. According to the preparation method for the liposome, by means of optimization and control of the proportion of phospholipid to cholesterol, the proportion of the total lipid to an optional functional long circulation material, the proportion of the total lipid to a drug, and the type and the concentration of a salt solution in an inner aqueous phase, a liposome, which has high encapsulation efficiency, good storage stability, and high filtering performance, is not easy to leak, is stable and controllable to release, prolongs the half-life remarkably, improves the therapeutic effect, and reduces toxic and side effects, is prepared. In addition, the provided liposome prescription and preparation process are simple, and scaled-up production and clinical popularization and application are facilitated.

IPC Classes  ?

• A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 47/28 - Steroids, e.g. cholesterol, bile acids or glycyrrhetinic acid
• A61K 47/02 - Inorganic compounds
• A61P 35/00 - Antineoplastic agents

Abstract

A continuous delivery preparation capable of being stably released and a preparation method therefor. The preparation comprises an active pharmaceutical ingredient and a gel carrier, and the gel carrier comprises a biodegradable polymer, an organic solvent, a hydrophobic additive, and an optional hydrophilic gel matrix material. Compared with an in-situ gel prepared by means of a conventional Atrigel technology, the delivery preparation has the effect of slowing down in vitro and vivo burst release of the drug after a small amount of the hydrophobic additive and the optional hydrophilic gel matrix material are added, and the in-vivo blood drug concentration can be maintained for more than one week in a safe and effective range. The preparation method of the preparation is simple.

IPC Classes  ?

• A61K 9/00 - Medicinal preparations characterised by special physical form
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers

Abstract

Disclosed is a method for preparing a progesterone particulate, especially a crystal or powder. The method comprises: step 1, dissolving progesterone in a solvent to provide a progesterone solution; step 2, pumping the progesterone solution into a high-speed shearing progesterone precipitation solvent at a predetermined speed to precipitate progesterone; and step 3, separating the precipitate and freeze-drying same to obtain the progesterone particulate, wherein the progesterone particulate being a progesterone crystal or progesterone powder. By using the method of the present invention, a micron-sized progesterone crystal or powder having good stability can be obtained. The progesterone injection prepared by using same not only achieves a sustained release effect of at least 5 days, but also has good stability. The method of the present invention is simple to operate, has low cost, and is easily scaled up for industrial production.

IPC Classes  ?

• A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
• C07J 7/00 - Normal steroids containing carbon, hydrogen, halogen, or oxygen, substituted in position 17 beta by a chain of two carbon atoms