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High-purity tauro ursodesoxy cholic acid and preparation method thereof

A technology of tauroursodeoxycholic acid and taurourchenodeoxycholic acid, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, steroids, etc., to achieve a simple preparation process, environment-friendly, high-purity Effect

Active Publication Date: 2014-07-30
CHENGDU GUOHONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Moreover, the tauroursodeoxycholic acid synthesis method in the prior art cannot effectively remove the tauroursodeoxycholic acid brought into the raw material, which is tauroursodeoxycholic acid The use of sulfursodeoxycholic acid has brought certain safety hazards

Method used

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  • High-purity tauro ursodesoxy cholic acid and preparation method thereof
  • High-purity tauro ursodesoxy cholic acid and preparation method thereof
  • High-purity tauro ursodesoxy cholic acid and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] In this experiment, the liver toxicity of tauroursodeoxycholic acid samples containing different taurochenodeoxycholic acid impurities was studied.

[0060] 1. Materials and Methods

[0061] 1.1 Test drug: tauroursodeoxycholic acid containing 2% taurourchenodeoxycholic acid impurity (batch number: 100810), white powder, self-made; Sulfurursodeoxycholic acid (batch number: 100811), white powder, self-made; tauroursodeoxycholic acid (batch number: 100812), white powder, containing 0.7% taurodeoxycholic acid impurity; Tauroursodeoxycholic acid (batch number: 100813) with 0.5% impurity content of sulchenodeoxycholic acid, white powder, self-made; the above samples are all insoluble in water.

[0062] 1.2 Detection reagents: Liver function-related detection kits were purchased from Sichuan Mike Biotechnology Co., Ltd., mainly including: alanine aminotransferase (ALT) and aspartate aminotransferase (AST).

[0063] 1.3 Detection instrument: full-wavelength fluorescence and s...

Embodiment 2

[0079] The preparation of embodiment two high-purity tauroursodeoxycholic acid

[0080] a) The preparation of the crude product of tauroursodeoxycholic acid is carried out according to the following steps:

[0081] In the reaction kettle, add 4.0KG ursodeoxycholic acid, add 19KG acetone, add 1650ml triethylamine under stirring, turn on the jacket refrigeration, and lower the temperature of the mixture to -10°C. Add 1120ml of ethyl chloroformate, control the rate of addition of ethyl chloroformate, so that the temperature of the reaction solution is maintained between -5-0°C, the addition is completed in 30 minutes, continue to maintain the temperature and stir for 40 minutes to obtain ursodeoxy For the mixed anhydride of cholic acid and ethyl chloroformate, the above mixed anhydride reaction solution is filtered through a filter with nitrogen pressure to be equipped with 4.2KG purified water, 1.4KG taurine, and 0.4KG sodium hydroxide in a 50-liter reactor. The reaction was st...

Embodiment 3

[0086] The preparation method of embodiment three high-purity tauroursodeoxycholic acid

[0087] a) The preparation of the crude product of tauroursodeoxycholic acid is carried out according to the following steps:

[0088] In the reaction kettle, add 40.0KG of ursodeoxycholic acid, add 190KG of acetone, add 16.5L of triethylamine under stirring, turn on the jacket refrigeration, and lower the temperature of the mixture to -5°C. Add 11.2 L of ethyl chloroformate, control the rate of addition of ethyl chloroformate, so that the temperature of the reaction solution is maintained between 3-5 °C, the addition is completed in 30 minutes, and the temperature is continued to be stirred for 30 minutes to obtain ursodeoxy For the mixed acid anhydride of cholic acid and ethyl chloroformate, the above mixed anhydride reaction solution is filtered through a filter with nitrogen pressure into a 500-liter reactor equipped with 42KG purified water, 14KG taurine, and 4KG sodium hydroxide, and...

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Abstract

The invention relates to a high-purity tauroursodeoxycholic acid and a preparation method thereof. The content of tauroursodeoxycholic acid in the tauroursodeoxycholic acid of the present invention is less than 0.7%, which is safe and effective in clinical application and has no toxic or side effects; The reaction of cholic acid and ethyl chloroformate to form a mixed anhydride, through the control of reaction conditions and reaction solvents, not only realizes the advantages of simple process, low cost, environmental friendliness, and suitability for industrial production, but also can obtain high-purity taurine bear deoxycholic acid.

Description

technical field [0001] The present invention relates to a kind of raw medicine of medicine and its preparation method, in particular to a kind of high-purity tauroursodeoxycholic acid and its preparation method. technical background [0002] The chemical name of tauroursodeoxycholic acid is 2-[[(3α,5β,7β)-3,7-dihydroxy-24-oxocholestan-24-yl]amino]ethanesulfonic acid Dihydrate, discovered from bear bile in 1902, is the main bile acid in bear bile, and has antispasmodic, anticonvulsant, anti-inflammatory and gallstone-dissolving effects. Tauroursodeoxycholic acid can increase the secretion of bile acids, leading to changes in the composition of bile acids and increasing their content in bile. Tauroursodeoxycholic acid can also inhibit the synthesis of cholesterol in the liver, reduce the amount of cholesterol and cholesterol esters in bile and the saturation index of cholesterol, thereby facilitating the gradual dissolution of cholesterol in bile. [0003] Tauroursodeoxycho...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07J9/00A61K31/575A61P1/16A61P31/14
Inventor 郭礼新徐开辉
Owner CHENGDU GUOHONG PHARMA
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