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Method for preparing chenodeoxycholic acid and ursodesoxycholic acid by directly extracting and synthetizing from porcine bile paste or leftovers

A technique for chenodeoxycholic acid and ursodeoxycholic acid is applied in the field of preparation of directly extracting and synthesizing chenodeoxycholic acid and ursodeoxycholic acid, and can solve the problem of low yield, unsuitability for production, and ursodeoxycholic acid. The problem of high cost, to achieve the effect of simplifying the process and reducing the cost

Active Publication Date: 2012-05-16
郑州药凰中医药研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] It is also reported in the prior art to inoculate Eubacterium aerogenes and Escherichia coli from chicken bile, pH 9.8-10.2, cultivate for 12-23 hours, the conversion rate is 25-45%, and the content of chenodeoxycholic acid in chicken bile is 4- 5% (total bile acid content is 8-9% in chicken bile), be converted into 1.25-2.25% of ursodeoxycholic acid, extract again, and yield is 1-2%, and above-mentioned method produces ursodeoxycholic acid cost High, low output, not suitable for production

Method used

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  • Method for preparing chenodeoxycholic acid and ursodesoxycholic acid by directly extracting and synthetizing from porcine bile paste or leftovers
  • Method for preparing chenodeoxycholic acid and ursodesoxycholic acid by directly extracting and synthetizing from porcine bile paste or leftovers
  • Method for preparing chenodeoxycholic acid and ursodesoxycholic acid by directly extracting and synthetizing from porcine bile paste or leftovers

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Embodiment 1

[0035] Get 100 kilograms of pig bile paste, saponify, extract hyodeoxycholic acid (fusing point 175 ℃), after saponification, leftovers contain 30% chenodeoxycholic acid. Direct pretreatment, add 20 times of alkaline water, temperature 95°C, ph9 / 10, add 1+1 natural clarifier (Ⅲ-B, produced by Shandong Yaosheng Biotechnology Co., Ltd.) 5 / 10,000 (calculated based on mother liquor). Stir for 4 hours until clarification, cool down, press filter to obtain clarified mother liquor, adjust ph3-4. To obtain pretreated raw materials, add 10 times the amount of methanol, dissolve and cool down to 0°C, add 12.25 kg of bromine solution, stir for 8 hours, then add sodium carbonate 10% alkaline water to dissolve and wash to remove chenodeoxycholic acid in thin layer chromatography Impurity cholic acid. Apply macroporous weakly basic adsorption resin in ethanol solution to remove bromate and hypobromite to obtain 7-ketolithocholic acid, which contains a small amount of C3 and C7-diketone com...

Embodiment 2

[0037] Referring to Example 1, ursodeoxycholic acid was obtained by reduction with potassium metal.

Embodiment 3

[0039] Referring to Implementation 1, ursodeoxycholic acid was obtained by reduction with Raney nickel.

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Abstract

The invention provides a method for preparing chenodeoxycholic acid and ursodesoxycholic acid by directly extracting and synthetizing from porcine bile paste or leftovers, comprising the following steps: using lower content (15-35%) porcine bile paste or leftovers and pre-processing it to remove off non-cholic acids impurities; removing off cholic acid impurities below the chenodeoxycholic acid in the thin layer chromatography by bromine oxidation or chromium oxidation; removing off cholic acid impurities above the chenodeoxycholic acid or the ursodesoxycholic acid in the thin layer chromatography by conventional reduction method; directly preparing the chenodeoxycholic acid or the ursodesoxycholic acid.

Description

technical field [0001] The invention relates to a method for preparing chenodeoxycholic acid and ursodeoxycholic acid, in particular to a method for directly extracting and synthesizing chenodeoxycholic acid and ursodeoxycholic acid from pig bile paste or leftovers . Background technique: [0002] Ursodeoxycholic acid (UDCA), referred to as UDCA, is the main component of bear bile. Its chemical name is (3α, 7β)-dihydroxy-5βcholic acid, which is the 7- Hydroxy epimers. Since 1980s, when ursodeoxycholic acid was discovered to effectively dissolve cholesterol stones, new researches have shown that ursodeoxycholic acid has a positive effect on choleresis and liver protection. In recent years, it has been reported abroad that UDCA not only has a good effect on the treatment of primary biliary cirrhosis, primary sclerosing cholangitis, and chronic active hepatitis, but also can be used to treat chronic hepatitis and rejection after liver transplantation. At present, ursodeoxych...

Claims

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Application Information

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IPC IPC(8): C07J9/00
Inventor 周平宏叶亮毕小升吴茂芝曹雪松吴紫梦于露毕一天曹汝成毕思宾
Owner 郑州药凰中医药研究有限公司
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