Alpha crystal form of obeticholic acid as well as preparation method, medicine composition and application thereof

A technology of obeticholic acid and crystal form, which is applied in the field of α crystal form of obeticholic acid and its preparation, can solve problems such as low melting temperature, unsuitability, and potential safety hazards, and achieve simple process operation and good stability , low-cost effect
CN105859818AInactive Publication Date: 2016-08-17SICHUAN RUIXIKANG BIOLOGICAL MEDICINE CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SICHUAN RUIXIKANG BIOLOGICAL MEDICINE CO LTD
Publication Date
2016-08-17
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to an alpha crystal form of obeticholic acid and a preparation method thereof. The preparation method comprises the following steps: (a) fully dissolving obeticholic acid under a backflow state in a mixed solvent of toluene or toluene and another kind of solvent forming a homogeneous system; (b) cooling the obtained obeticholic acid solution, so the alpha crystal form of the obeticholic acid precipitates out from the solution; (c) separating the alpha crystal form of the obeticholic acid out from the solution; and (d) placing the alpha crystal form of the obeticholic acid under 30-70 DEG C and drying for 3-30 hours at reduced pressure or ordinary pressure. The prepared alpha crystal form of obeticholic acid has the characteristics of better stability, higher purity, stable moisture content and the like. Furthermore, the invention also relates to a medicine composition of the alpha crystal form and the application of the alpha crystal form in preparing medicines for treating hepatic diseases such as biliary atresia, cholestatic liver disease, chronic liver disease, primary biliary cirrhosis, alcoholic fatty liver, non-alcoholic fatty liver disease and the like.
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Description

field of invention

[0001] The present invention relates to an α-crystal form of obeticholic acid and a preparation method thereof, and its preparation method for treating biliary atresia, cholestatic liver disease, chronic liver disease, primary biliary cirrhosis, alcoholic fatty liver, non-alcoholic Application in liver disease drugs such as chronic fatty liver disease. In addition, the present invention also provides a pharmaceutical composition containing this specific crystal form of obeticholic acid. Background of the invention

[0002] The chemical name of obeticholic acid (Ⅰ) is: 3α, 7α-dihydroxy-6α-ethyl-5β-cholan-24 acid, also known as: 6α-ethylchenodeoxycholic acid. The CAS registration number of obeticholic acid is: 459789-99-2. Obeticholic acid is a farnesoid X receptor agonist, which indirectly inhibits the gene expression of cytochrome 7A1 (CYP7A1) by activating farnesoid X receptor. Since CYP7A1 is the rate-limiting enzyme of bile acid biosynthesis, obetich...

Claims

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