Preparation method of high-purity natural ursodesoxycholic acid and application thereof in medicament

Abstract

The invention belongs to the technical field of medical biology, in particular to a preparation method of high-purity natural ursodesoxycholic acid. The high-purity natural ursodesoxycholic acid is obtained by separating and purifying bear gall powder prepared from a manual drained bear gall, and the high performance liquid chromatography purity is not lower than 98 percent. The preparation method comprises the following steps of: firstly, separating and purifying by applying a cation exchange medium to prepare tauroursodeoxycholic acid with purity not lower than 90 percent; and then thoroughly hydrolyzing the tauroursodeoxycholic acid into ursodesoxycholic acid and taurine in the presence of alkali and separating and purifying by applying a silica gel adsorption chromatography technology to prepare the ursodesoxycholic acid with purity not lower than 98 percent. The natural ursodesoxycholic acid prepared by the invention has the effects on treating primary biliary cirrhosis and primary sclerosing cholangitis.

Description

technical field [0001] The invention belongs to the technical field of medicine and biology, and in particular relates to a preparation method of high-purity natural ursodeoxycholic acid and its application in medicine. Background technique [0002] Ursodeoxycholic acid (UDCA) is an active ingredient of bear bile, a rare medicine, which has the functions of clearing away heat, calming the liver, and improving eyesight. It has a unique curative effect on cholesterol gallstones. The preparation method of existing patent or bibliography UDCA at home and abroad mainly contains three aspects, the one is that the bear bile powder that natural bear bile or artificial drainage bear bile is prepared is that raw material extracts and refines (referring to literature: Shi Lixia etc., drainage bear bile Comparison of active ingredient content before and after powder refining, Chinese Materia Medica. 2000, 23(6): 334; Shi Lixia et al., Development and Clinical Application of Bear Bile I...

AI Technical Summary

Problems solved by technology

The preparation method of existing patent or bibliography UDCA at home and abroad mainly contains three aspects, the one is that the bear bile powder that natural bear bile or artificial drainage bear bile is prepared is that raw material extracts and refines (referring to literature: Shi Lixia etc., drainage bear bile Comparison of active ingredient content before and after powder refining, Chinese Materia Medica. 2000, 23(6): 334; Shi Lixia et al., Development and Clinical Application of Bear Bile Injection, Chinese Patent Medicine. 1989, 11(6): 12), the obtained products are mainly Bear bile powder extracts with low UDCA content are mainly used as raw materials of some traditional Chinese medicines or natural health products, which cannot meet the quality standards and requirements of high-end preparations of traditional Chinese medicines and natural medicines, such as raw materials for injections; Deoxycholic acid is the semi-synthetic preparation of UDCA as a raw material (referring to literature: EP, 88637, 1983, etc.), this method is the main preparation process of pharmaceutical UDCA now, but the reaction yield is low, and relevant impurities such as reaction by-products are not easy Control; the third is to carry out the total synthesis of UDCA with other chemical raw materials as starting materials (referring to literature: Li Liang, Chinese patent 98105020.4, etc.), the synthetic route of this invention does not need high temperature and high pressure reaction conditions, and the reaction yield of each step is high. It has high industrial production value. In the UDCA synthesis research, a relatively optimized synthetic route was obtained. This route is a new process, but it is still in the laboratory research stage

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