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Medicine composition comprising bexarotene

A bexarotene and composition technology, applied in the field of pharmaceutical compositions and preparations containing bexarotene

Active Publication Date: 2020-09-29
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There is no report on the co-crystal of bexarotene

Method used

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  • Medicine composition comprising bexarotene
  • Medicine composition comprising bexarotene
  • Medicine composition comprising bexarotene

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Preparation method of pharmaceutical composition containing bexarotene 1

[0060] Weigh 50 mg of bexarotene crystal type I, 88 mg of bexarotene and ligustrazine eutectic, and 100 mg of co-amorphous bexarotene and polyvinylpyrrolidone 1:1, and physically mix them uniformly according to conventional methods. get.

[0061] Preparation method of pharmaceutical composition containing bexarotene 2

[0062] Weigh 50 mg of bexarotene crystal type I, 440 mg of bexarotene and ligustrazine eutectic, and 500 mg of co-amorphous bexarotene and polyvinylpyrrolidone 1:1, and physically mix them uniformly according to conventional methods. get.

Embodiment 2

[0064] Preparation method of bexarotene and ligustrazine cocrystal 1:

[0065] According to the table below, take appropriate amounts of bexarotene and ligustrazine into a mortar, add an appropriate amount of organic solvent, manually grind for an appropriate time, and dry at high temperature. Its powder X-ray diffraction analysis was carried out, and its diffraction pattern was the same as figure 1 Consistent, indicating that the obtained sample is a co-crystal of bexarotene and ligustrazine.

[0066]

[0067] Preparation method 2 of bexarotene and ligustrazine cocrystal:

[0068] As shown in the table below, take an appropriate amount of bexarotene and ligustrazine into a ball mill jar, add an appropriate amount of organic solvent, select an appropriate ball-to-material ratio, set an appropriate rotation speed, grind for an appropriate time, and dry at high temperature. Its powder X-ray diffraction analysis was carried out, and its diffraction pattern was the same as f...

Embodiment 3

[0074] Preparation method of bexarotene and polyvinylpyrrolidone co-amorphous product 1:

[0075] According to the table below, take an appropriate amount of bexarotene and polyvinylpyrrolidone in a mass ratio of 1:1 and put them in a ball mill. Its powder X-ray diffraction analysis was carried out, and its diffraction pattern was the same as Figure 4 Consistent, indicating that the obtained sample is a co-amorphous product of bexarotene and polyvinylpyrrolidone.

[0076]

[0077] Preparation method 2 of co-amorphous substance of bexarotene and polyvinylpyrrolidone:

[0078] Take 3 parts of Bexarotene 20g, and weigh 4g, 20g, 100g of polyvinylpyrrolidone respectively according to the mass ratio of 5:1, 1:1, 1:5, put them into the ball mill respectively, and select the ball-to-material ratio of 6: 1. The rotation speed is 400 r / min, the grinding is stopped for 2 minutes every 15 minutes, and the ball is milled for 10 hours, 2 hours, and 0.5 hours, respectively, to obtain t...

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Abstract

The invention discloses a medicine composition comprising bexarotene, and a preparation method and a purpose of the medicine composition. Concretely, the invention discloses the medicine composition comprising the bexarotene, the preparation method of the medicine composition, and application of the medicine composition comprising the bexarotene as a medicine active ingredient to preparation of medicine for preventing and treating glioma, skin T-cell lymphoma, breast cancer, psoriasis, Kaposi's sarcoma, lung cancer and Cushing's diseases.

Description

technical field [0001] The invention discloses a pharmaceutical composition containing bexarotene, a preparation method and application. Specifically, the present invention discloses a pharmaceutical composition containing bexarotene and a preparation method; the pharmaceutical composition containing bexarotene is used as a pharmaceutical active ingredient in the preparation and prevention of glioma and cutaneous T-cell lymphoma , breast cancer, psoriasis, Kaposi's sarcoma, lung cancer and Cushing's disease drugs. Background technique [0002] The present invention adopts bexarotene as active substance, and its chemical name is 4-[1-(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthyl ) vinyl] benzoic acid, the molecular formula is C 24 H 28 O 2 , the structural formula is shown in a. The cocrystal former used in the invention is polyvinylpyrrolidone, and the structural formula is shown in the following formula b. [0003] [0004] Daiss et al. used 1,2-bis(chlorodi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K31/4965A61K31/79A61P35/00A61P17/06A61P5/38
CPCA61K31/192A61K31/4965A61K31/79A61P35/00A61P17/06A61P5/38A61K2300/00
Inventor 杜冠华吕扬杨世颖孙岚焦凌泰任淑月王海港张丽张宝喜周启蒙宋俊科
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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