Abrégé

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.

Classes IPC  ?

• A61K 9/10 - DispersionsÉmulsions
• A61K 9/14 - Préparations médicinales caractérisées par un aspect particulier à l'état particulaire, p. ex. poudres
• A61K 31/635 - Composés contenant des groupes para-N-benzènesulfonyl-N-, p. ex. sulfanilamide, p-nitrobenzènesulfonohydrazide contenant un hétérocycle, p. ex. sulfadiazine
• A61K 47/12 - Acides carboxyliquesLeurs sels ou anhydrides
• A61P 29/00 - Agents analgésiques, antipyrétiques ou anti-inflammatoires non centraux, p. ex. agents antirhumatismauxMédicaments anti-inflammatoires non stéroïdiens [AINS]

Abrégé

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.

Classes IPC  ?

• A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
• A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
• A61K 9/1278 - Chargement ultérieur, p. ex. par gradient ionique ou de pH
• A61P 35/00 - Agents anticancéreux

Abrégé

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.

Classes IPC  ?

• A61K 9/06 - OnguentsExcipients pour ceux-ci
• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 31/381 - Composés hétérocycliques ayant le soufre comme hétéro-atome d'un cycle ayant des cycles à cinq chaînons
• A61K 31/426 - 1,3-Thiazoles
• A61K 31/4985 - Pyrazines ou pipérazines condensées en ortho ou en péri avec des systèmes hétérocycliques
• A61K 47/14 - Esters d’acides carboxyliques, p. ex. acides gras monoglycérides, triglycérides à chaine moyenne, parabènes ou esters d’acide gras de PEG
• A61K 47/20 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant du soufre, p. ex. sulfoxyde de diméthyle [DMSO], docusate, laurylsulfate de sodium ou acides aminosulfoniques
• A61K 47/22 - Composés hétérocycliques, p. ex. acide ascorbique, tocophérol ou pyrrolidones
• A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères

Abrégé

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.

Classes IPC  ?

• A61K 9/16 - AgglomérésGranulésMicrobilles
• A61K 31/437 - Composés hétérocycliques ayant l'azote comme hétéro-atome d'un cycle, p. ex. guanéthidine ou rifamycines ayant des cycles à six chaînons avec un azote comme seul hétéro-atome d'un cycle condensés en ortho ou en péri avec des systèmes hétérocycliques le système hétérocyclique contenant un cycle à cinq chaînons ayant l'azote comme hétéro-atome du cycle, p. ex. indolizine, bêta-carboline
• A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères
• A61P 25/18 - Antipsychotiques, c.-à-d. neuroleptiquesMédicaments pour le traitement de la manie ou de la schizophrénie

Abrégé

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.

Classes IPC  ?

• A61K 9/06 - OnguentsExcipients pour ceux-ci
• A61K 47/36 - PolysaccharidesLeurs dérivés, p. ex. gommes, amidon, alginate, dextrine, acide hyaluronique, chitosane, inuline, agar-agar ou pectine
• A61K 31/381 - Composés hétérocycliques ayant le soufre comme hétéro-atome d'un cycle ayant des cycles à cinq chaînons
• A61L 2/02 - Procédés ou appareils de désinfection ou de stérilisation de matériaux ou d'objets autres que les denrées alimentaires ou les lentilles de contactAccessoires à cet effet utilisant des phénomènes physiques

Abrégé

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.

Classes IPC  ?

• A61K 9/127 - Vecteurs à bicouches synthétiques, p. ex. liposomes ou liposomes comportant du cholestérol en tant qu’unique agent tensioactif non phosphatidylique
• A61K 31/7068 - Composés ayant des radicaux saccharide et des hétérocycles ayant l'azote comme hétéro-atome d'un cycle, p. ex. nucléosides, nucléotides contenant des cycles à six chaînons avec l'azote comme hétéro-atome d'un cycle contenant des pyrimidines condensées ou non-condensées ayant des groupes oxo liés directement au cycle pyrimidine, p. ex. cytidine, acide cytidylique
• A61K 47/24 - Composés organiques, p. ex. hydrocarbures naturels ou synthétiques, polyoléfines, huile minérale, gelée de pétrole ou ozocérite contenant des atomes autres que des atomes de carbone, d'hydrogène, d'oxygène, d'halogènes, d'azote ou de soufre, p. ex. cyclométhicone ou phospholipides
• A61K 47/28 - Stéroïdes, p. ex. cholestérol, acides biliaires ou acide glycyrrhétinique
• A61K 47/02 - Composés inorganiques
• A61P 35/00 - Agents anticancéreux

Abrégé

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.

Classes IPC  ?

• A61K 9/00 - Préparations médicinales caractérisées par un aspect particulier
• A61K 47/34 - Composés macromoléculaires obtenus par des réactions autres que celles faisant intervenir uniquement des liaisons non saturées carbone-carbone, p. ex. polyesters, acides polyaminés, polysiloxanes, polyphosphazines, copolymères de polyalkylène glycol ou de poloxamères

Abrégé

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.

Classes IPC  ?

• A61K 31/57 - Composés contenant des systèmes cycliques du cyclopenta[a]hydrophénanthrèneLeurs dérivés, p. ex. stéroïdes substitués en position 17 bêta par une chaîne à deux atomes de carbone, p. ex. prégnane ou progestérone
• C07J 7/00 - Stéroïdes normaux contenant du carbone, de l'hydrogène, un halogène ou de l'oxygène, substitués en position 17bèta par une chaîne de deux atomes de carbone