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Crystal form VII of sofalcone and preparation method and application thereof

A sofalone and crystal form technology, which is applied to the separation/purification of medical preparations containing active ingredients, pharmaceutical formulas, and carboxylic acid compounds, and can solve problems that do not involve the crystal form of sofalone

Inactive Publication Date: 2010-07-21
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The preparation method of this product has been reported at home and abroad, such as document Chem.Pharm.Bull.1979, 27 (12): 2943~2953 and document U.S.4085135, Chinese patent CN1733682A, record the preparation method of sofalone in CN101434533A, The pharmaceutical composition containing them and the application of preparing medicine for treating gastric ulcer and chronic gastritis, but none of them involve the crystal form of sofadone

Method used

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  • Crystal form VII of sofalcone and preparation method and application thereof
  • Crystal form VII of sofalcone and preparation method and application thereof
  • Crystal form VII of sofalcone and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Weigh 10.0 g of sofalone, add 150 mL of tetrahydrofuran, heat to 65°C, stir to dissolve, filter while hot, and cool the filtrate to room temperature naturally, and let it stand for 4 days. A solid was precipitated and filtered to obtain light yellow flaky crystals.

Embodiment 2

[0045] Weigh 10.0 g of sofalone, add 180 mL of tetrahydrofuran, heat to 60°C, stir to dissolve, filter while hot, and cool the filtrate to room temperature naturally, and let it stand for 5 days. A solid was precipitated and filtered to obtain light yellow flaky crystals.

Embodiment 3

[0047] Weigh 10.0 g of sofalone, add 200 mL of tetrahydrofuran, heat to 30 ° C, stir and dissolve, filter while hot, and cool the filtrate to room temperature naturally, and let it stand for 6 days. A solid was precipitated and filtered to obtain light yellow flaky crystals.

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PUM

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Abstract

The invention relates to a crystal form VII of sofalcone and a preparation method thereof, and a medicinal composition prepared from the crystal form VII of the sofalcone obtained by the invention and application thereof. The crystal form VII of the sofalcone is characterized by a single crystal X-ray diffraction pattern of the crystal form VII of the sofalcone.

Description

technical field [0001] The invention belongs to the field of drugs against gastric ulcer and acute and chronic gastritis, more specifically, relates to sofalcone (sofalcone) or [5-(3-methyl-2-butenyl)oxyl group of formula (I) -Crystal form VII of 2-[3-[4-(3-methyl-2-butenyl)oxy]phenyl-1-oxo-2-propenyl]phenoxy]acetic acid and its preparation method , a pharmaceutical composition containing it and its use in the manufacture of anti-gastric ulcer and acute and chronic gastritis drugs. Background technique [0002] Sofalcone (sofalcone), the chemical name is [5-(3-methyl-2-butenyl)oxy-2-[3-[4-(3-methyl-2-butenyl)oxyl ]phenyl-1-oxo-2-propenyl]phenoxy]acetic acid is a gastric mucosal protective agent and tissue repair agent, which can be used for the treatment of gastric ulcer and acute and chronic gastritis, developed by Japan Taisho Pharmaceutical Company , listed in Japan in March 1984. [0003] Chemical structure: [0004] [0005] Molecular formula: C 27 h 30 o 6 ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C59/90C07C51/43A61K31/192A61P1/04
Inventor 刘登科刘颖刘冰妮刘默祁浩飞王景阳王平保
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH