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Obeticholic acid compound and pharmaceutical composition thereof

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: 2016-08-17
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 pharmaceutical composition thereof
  • Obeticholic acid compound and pharmaceutical composition thereof
  • Obeticholic acid compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Embodiment 1 Preparation of obeticholic acid crystal form

[0041] Dissolve 5g of obeticholic acid sample in a mixed solvent of chloroform / n-heptane (100mL / 150mL) in a water bath at 60°C, keep it for 30 minutes, then cool it naturally in a water bath to room temperature, precipitate a flocculent solid, filter and dry to obtain a new crystal type. X-ray powder diffraction (XRD) collection of illustrative plates, differential scanning calorimetry (DSC) collection of illustrative plates, thermogravimetric analysis (TGA) collection of illustrative plates are respectively as attached figure 1 , 2 , 3 shown.

Embodiment 2

[0042] Embodiment 2 Preparation of obeticholic acid crystal form

[0043] In a water bath at 60°C, 15g of obeticholic acid sample was dissolved in 300mL of chloroform, and was added dropwise into 500mL of n-heptane solvent under stirring to precipitate a flocculent solid, which was filtered and dried to obtain a new crystal form. X-ray powder diffraction (XRD) pattern attached figure 1 basically the same.

Embodiment 3

[0044] Embodiment 3 Preparation of obeticholic acid crystal form

[0045]At room temperature, 15g of obeticholic acid sample was dissolved in 300mL of dichloromethane, and was added dropwise into 500mL of n-hexane solvent under stirring to precipitate a flocculent solid, which was filtered and dried to obtain a new crystal form. X-ray powder diffraction (XRD) pattern attached figure 1 basically the same.

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PUM

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Abstract

The invention provides a crystal-form obeticholic acid compound, and a preparation method and a pharmaceutical composition thereof. A crystal form of the obtained obeticholic acid compound is investigated in the aspects of hygroscopicity, stability and the like, and the crystal form is found out to be in compliance with medicine requirements. The preparation process provided by the invention is stable, has good reproducibility, and meets the requirements of industrialized mass production.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to an obeticholic acid compound in crystal form, a pharmaceutical composition and a preparation method thereof. Background technique [0002] Fatty liver disease has now replaced viral hepatitis as the world's number one liver disease. 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%, which is about three times higher in men than in women, and there is a trend of younger age development. 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 that unhealthy lifestyles and behaviors (weight loss, alcohol abstinence, etc.) should be corrected first. For patients with NAFLD accompanied by diabetes, hypertension, and hyperlipidemia, the main focus is to control the asso...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00A61K31/575A61P1/16
Inventor 赵俊宗在伟赵骞李建国
Owner JIANGSU AOSAIKANG PHARMA CO LTD
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