Jiangsu Hengrui Medicine Company Ltd.

Jiangsu Hengrui Pharmaceuticals Co., Ltd.

Yun Lu

Xinhua Zhang

Guaili Wu

Chenyang Wang

Hao Chen

Daimei Zhang

Changshan Guo

Tonghui Liu

Piaoyang Sun

Jun Feng

Qiyun Shao

Zhenjun Qiu

Lingjia Shen

Yuxia Wu

Xi Lu

Liang Zhong

Jiajia Xu

Xiaochen Pan

Disclosed is a pharmaceutical composition containing a bicyclo-substituted pyrazolone azo derivative or a salt thereof and a preparation method thereof. In particular, the pharmaceutical composition disclosed in the present invention contains (Z)-5-(2-hydroxyl-3-(2-(3-methyl-5-oxo-1-(5,6,7,8-tetrahydronaphthalene-2-yl)-1H-pyrazol-4(5H)-ylidene)hydrazino)phenyl)furan-2-carboxylic acid or a pharmaceutically acceptable salt thereof, and at least one filler optionally selected from cellulose, microcrystalline cellulose, lactose and starch. The composition has a good stability, dissolution rate and bioavailability, and the preparation process is simple, economical and quick.

Pharmaceutical composition comprising bicyclo-substituted pyrazolon azo derivative or salt thereof and preparation method thereof

The present invention provides a pharmaceutical composition containing a quinoline derivative or a salt thereof. Specifically, the invention provides a pharmaceutical composition containing (R,E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)-propeneamide or a pharmaceutically acceptable salt thereof, a cross-linked polyvinylpyrrolidone, and at least one pharmaceutically acceptable excipient. The pharmaceutical composition has a property of rapid dissolution.

Pharmaceutical composition comprising quinoline derivative or salt thereof

A pharmaceutically acceptable salt as a renal outer medullary potassium channel (ROMK) inhibitor, specifically an L-tartrate and a crystal form I and crystal form II thereof, is described. The pharmaceutically acceptable salt of the ROMK inhibitor, specifically the L-tartrate, has improved bioavailability and stability.

Pharmaceutically acceptable salt as renal outer medullary potassium channel inhibitor

The present invention provides a pharmaceutical composition containing a pyrrolo-fused six-membered heterocyclic compound or a pharmaceutically acceptable salt of the compound. Specifically, the invention provides a pharmaceutical composition containing 5-(2-diethylamino-ethyl)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidene-methyl)-3-methyl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one or a pharmaceutically acceptable salt thereof, and at least one water soluble filler. The pharmaceutical composition of the invention features a rapid dissolution and good stability.

Pharmaceutical composition comprising pyrrolo-fused six-membered heterocyclic compound

The present invention provides a method for preparing a pharmaceutical composition containing a pyrrolo-fused six-membered heterocyclic compound or a pharmaceutically acceptable salt thereof. Specifically, the invention provides a preparation method of a pharmaceutical composition, the method containing: mixing 5-(2-diethylamino-ethyl)-2-(5-fluoro-2-oxo-1,2-dihydro-indol-3-ylidene-methyl)-3-methyl-1,5,6,7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one or a pharmaceutically acceptable salt thereof with at least one filler, and then granulating the mixture. The pharmaceutical composition of the invention features a rapid dissolution and good stability.

Method for preparing pharmaceutical composition comprising pyrrolo-fused six-membered heterocyclic compound

Provided in the present invention is a pharmaceutical composition containing a JAK kinase inhibitor or a pharmaceutically acceptable salt thereof. In particular, provided in the present invention is a pharmaceutical composition containing (3aR, 5s, 6aS)-N-(3-methoxy-1,2,4-thiadiazol-5-yl)-5-(methyl(7H-pyrrolo [2,3-d] pyrimidin-4-yl) amino) hexahydrocyclopenta [c] pyrrol-2 (1H)-carboxamide, or a pharmaceutically acceptable salt thereof, and cellulose ether. The pharmaceutical composition of the present invention is characterized by a rapid dissolution rate and good stability.

Pharmaceutical composition containing JAK kinase inhibitor or pharmaceutically acceptable salt thereof

The present invention provides a method for preparing a pharmaceutical composition containing a quinoline derivative or a salt thereof. Specifically, the invention provides a method for preparing a pharmaceutical composition containing (R,E)-N-(4-(3-chloro-4-(pyridin-2-ylmethoxy)phenylamino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)-propeneamide or a pharmaceutically acceptable salt thereof. The method uses a wetting agent containing at least one organic solvent for a wet granulation in a preparation process of the pharmaceutical composition. The pharmaceutical composition prepared using the method has a uniform distribution of grain sizes during the preparation process and a property of rapid and uniform dissolution.

Method for preparing pharmaceutical composition comprising quinoline derivative or salt thereof

The present invention relates to a crystalline form of a BTK kinase inhibitor and the preparation method thereof. In particular, the present invention relates to a crystal form I of (R)-4-amino-1-(1-(but-2-ynoyl)pyrrolidin-3-yl)-3-(4-(2,6 -difluorophenoxy)phenyl)-1 H-pyrrolo[2,3-d]pyridazin-7(6H)-one (the compound of formula (I)) and the preparation method thereof. The crystal form I of the compound of formula (I) obtained by the present invention has a good crystalline stability and chemical stability, and the crystallization solvent used has a low toxicity and low residue, thus making it more suitable for use in clinical treatment.

Crystalline form of BTK kinase inhibitor and preparation method thereof

Provided in the present invention is a pharmaceutical composition containing an imidazoline derivative. In particular, the pharmaceutical composition provided in the present invention contains (S)-4-(3-(4-(2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-carbonyl-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile and cellulose ether; and the composition has a good stability, dissolution rate and bioavailability.

Pharmaceutical composition containing imidazoline derivative

Provided are an L-proline complex of a sodium-glucose cotransporter 2 inhibitor, and a monohydrate and a crystal of the L-proline complex. Specifically, provided are 1,6-dehydrated-1-C{4-chloro-3-[(3-fluoro-4-ethoxyphenyl)methyl]phenyl}-5-C-(hydroxymethyl)-&#x3b2;-L-idopyranose L-proline (a compound of formula (I)), a monohydrate and a type A crystal thereof, and a preparation method therefor. The obtained type A crystal of the compound of formula (I) has good chemical stability and crystal stability, and the crystallization solvent used has low toxicity and low residue, so the type A crystal can be better used in clinical treatment. 

L-proline complex of sodium-glucose cotransporter 2 inhibitor, monohydrate and crystal form thereof

Disclosed is a pregabalin sustained-release preparation, wherein the sustained-release tablet contains a pharmaceutically active ingredient containing pregabalin or a salt or hydrate thereof, a gel framework material containing alginic acid, and a swellable material containing polyoxyethylene.

Pregabalin sustained-release preparation

A crystalline form of an androgen receptor inhibitor and its preparation method are provided. In particular, provided are crystal form I of (S)-4-(3-(4-(2,3-dihydroxypropoxy)phenyl)-4,4-dimethyl-5-carbonyl-2-thioimidazolin-2-yl)-2-(trifluoromethyl)benzonitrile (a compound of formula (I)) and its preparation method. The method includes (a) adding any crystal form or amorphous form of the compound of formula (I) to an organic solvent to obtain a solution and heating the solution until it is clear, followed by cooling the solution to precipitate a crystal; and (b) filtering, washing, and drying the crystal. The obtained crystal form I of the compound of formula (I) has good chemical stability and crystal form stability, and the crystallization solvent used has low toxicity and residue, and is thus better for use in clinical treatment.

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Jiangsu, China

Yun Lu