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Obeticholic acid compound, and medicinal composition containing compound

A technology of obeticholic acid and its compounds, which is applied in the field of obeticholic acid compounds and their pharmaceutical compositions and preparations, can solve problems affecting the quality of medicines, and achieve good reproducibility and stable preparation processes

Inactive Publication Date: 2016-10-05
JIANGSU AOSAIKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It can be seen that various crystal forms of OCA have been disclosed in the prior art, but drug polymorphism is a common phenomenon in drug research and development, and is an important factor affecting drug quality

Method used

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  • Obeticholic acid compound, and medicinal composition containing compound
  • Obeticholic acid compound, and medicinal composition containing compound
  • Obeticholic acid compound, and medicinal composition containing compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Example 1 Preparation of crystal form of obeticholic acid

[0042] 3α,7α-dihydroxy-6α-ethyl-5β-cholan-24-acid methyl ester (65.9g, 0.152mol), methanol (152ml), 20% (mass fraction) sodium hydroxide aqueous solution (36ml) Mix and react at 55~60℃ for 2h. After the reaction was completed, methanol was evaporated under reduced pressure, the residue was dissolved in 150 ml of purified water, and concentrated hydrochloric acid was added dropwise with stirring to adjust the pH to 2-3. Ethyl acetate (200ml) was added to the solution, and the solution was extracted and separated. The organic phase was dried with anhydrous sodium sulfate for 2h and then spin-dried to obtain about 60.6g of yellow oil. Then n-butyl acetate (73ml) was added to dissolve it at 60°C. , after dropping to room temperature, a white solid was precipitated, filtered, and the filter cake was dried at 40° C. to obtain 41.9 g of obeticholic acid solid. The X-ray powder diffraction (XRD) pattern, differential...

Embodiment 2

[0043] Example 2 Preparation of crystal form of obeticholic acid

[0044]Add obeticholic acid (82g) to the reaction flask, add ethyl acetate (100ml) and heat to 60°C to dissolve all, stand and cool down to room temperature naturally, separate out white solids, filter, and dry the filter cake at 40°C to obtain 60g of solids . X-ray powder diffraction (XRD) pattern attached figure 1 basically the same.

Embodiment 3

[0045] Example 3 Preparation of crystal form of obeticholic acid

[0046] Add obeticholic acid (98.0g) to the reaction flask, add ethyl acetate (195ml) and heat to 60°C to dissolve, let stand and drop to room temperature to precipitate a white solid, filter, and dry the filter cake at 40°C to obtain Product 66.6 g. X-ray powder diffraction (XRD) pattern attached figure 1 basically the same.

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Abstract

The invention provides an obeticholic acid compound with a crystal form, and a preparation method and a medicinal composition thereof. A result of investigation of the crystal form of the obeticholic acid compound obtained in the invention from the hygroscopicity and the stability shows that the obeticholic acid compound accords with medicinal requirements. The preparation method has the advantages of stable process, good reappearance, and meeting of requirements of industrial large-scale production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a crystal form of obeticholic acid compound and its pharmaceutical composition and preparation method. Background technique [0002] Fatty liver disease has now replaced viral hepatitis as the number one liver disease in the world. More than 90% of fatty liver patients in my country are non-alcoholic fatty liver disease (NAFLD). The prevalence of NAFLD is about 12% to 24%. It is about three times higher in men than in women, and there is a trend of younger age. According to a survey of 23,965 adults, 1 / 5 of NAFLD progressed to steatohepatitis. There is still no effective treatment for NAFLD. The guidelines generally recommend correcting unhealthy lifestyles and behaviors (weight loss, alcohol abstinence, etc.) first, and for NAFLD patients with diabetes, hypertension, and hyperlipidemia, the control of accompanying diseases is the main priority. [0003] Primary b...

Claims

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Application Information

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IPC IPC(8): C07J9/00A61K31/575A61P1/16
Inventor 赵俊宗在伟赵骞杨瑞峰朱海溪李淦
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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