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A kind of method of purifying telavancin crude product

A technology of telavancin and telavancin hydrochloride, applied in peptide preparation methods, chemical instruments and methods, organic chemistry, etc., can solve the problems of no purification of telavancin, achieve enhanced competitiveness, and simple process , the effect of low production cost

Active Publication Date: 2018-05-11
宁夏泰瑞制药股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, there are literature reports on the extraction and purification of vancomycin in China, but there is no literature report on the purification of telavancin

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] 10 kg of telavancin crude product was dissolved with 20% hydrochloric acid solution, pH to 5, telavancin concentration controlled at 60%, and then filtered to obtain 16.9 L of telavancin solution. Add 50 L of organic solvent, lower the temperature to 5° C., and adjust the pH to 9 with 15% ammonia water. Stir for 20 minutes and let stand for 60 minutes. After standing still, liquid-liquid separation was carried out. Extracted twice to obtain telavancin organic solvent solution 99.5L, the total extraction yield reached 95.8%.

[0034] Add 400L of deionized water to the telavancin extract, control the temperature at 10°C, start the stirring system, slowly and uniformly add 20% hydrochloric acid solution during the stirring process, adjust the pH to 4.5, continue stirring for 20 minutes, and let stand for 60 minutes. After standing still, liquid-liquid separation was carried out. Back extraction 2 times, telavancin solution volume is 800L, back extraction total yield rea...

Embodiment 2

[0040] 10kg of telavancin crude product was dissolved with 22% hydrochloric acid solution, the pH was 5.3, the concentration of telavancin was controlled at 62%, and then filtered to obtain 16.1L of telavancin solution. Add 53L of organic solvent, lower the temperature to 7.5°C, and adjust the pH to 9.3 with 18% ammonia water. Stir for 23min and let stand for 70min. After standing still, liquid-liquid separation was carried out. Extracted twice to obtain telavancin organic solvent solution 105.8L, the total extraction yield reached 96.0%.

[0041] Add 455L of deionized water to the telavancin extract, control the temperature at 11°C, start the stirring system, add 22% hydrochloric acid solution slowly and uniformly during the stirring process, adjust the pH to 4.8, continue stirring for 22 minutes, and let stand for 70 minutes. After standing still, liquid-liquid separation was carried out. Back extraction 2 times, telavancin solution volume is 905L, back extraction total y...

Embodiment 3

[0047]10 kg of telavancin crude product was dissolved with 25% hydrochloric acid solution, the pH was 5.5, the concentration of telavancin was controlled at 65%, and then filtered to obtain 15.4 L of telavancin solution. Add 54L of organic solvent, lower the temperature to 10°C, and adjust the pH to 9.5 with 20% ammonia water. Stir for 25 minutes and let stand for 80 minutes. After standing still, liquid-liquid separation was carried out. Extracted twice to obtain telavancin organic solvent solution 107.7L, the total extraction yield reached 96.2%.

[0048] Add 484L of deionized water to the telavancin extract, control the temperature at 12°C, start the stirring system, slowly and uniformly add 25% hydrochloric acid solution during the stirring process, adjust the pH to 5, continue stirring for 25 minutes, and let it stand for 80 minutes. After standing still, liquid-liquid separation was carried out. Back extraction 2 times, telavancin solution volume is 967L, back extract...

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PUM

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Abstract

The invention relates to a method for purifying telavancin crude product, a method for purifying telavancin crude product, characterized in that the process steps are: first acidifying and dissolving the telavancin crude product, filtering, and obtaining the filtrate with organic Solvent extraction, back extraction with hydrochloric acid solution, separation and extraction by ion exchange method to obtain telavancin hydrochloride solution, and then the telavancin hydrochloride solution is ultrafiltered, crystallized, washed with water and dried. The invention realizes the effective separation and purification of telavancin crude product, the effective content reaches 99%, improves the product quality, reduces the production cost, and is beneficial to enhance the domestic and foreign market competitiveness of telavancin.

Description

technical field [0001] The invention belongs to the technical field of antibiotic extraction, in particular to a method for purifying crude telavancin. Background technique [0002] Telavancin is a hydrophilic vancomycin derivative, and its activity against MRSA, MRSE and VanA enterococcus is higher than that of vancomycin and teicoplanin, and its activity is moderate among the second-generation glycopeptide antibiotics. However, its mechanism of action has remarkable characteristics: it can improve its bactericidal ability against Staphylococcus aureus, Streptococcus pneumoniae, and VanA type Staphylococcus aureus or enterococcus by interfering with bacterial lipogenesis, while breaking the cell membrane and destroying the integrity of the cell membrane. [0003] At present, there are domestic literature reports on the extraction and purification of vancomycin, but no literature reports on the purification of telavancin. Contents of the invention [0004] The object of t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K9/00C07K1/36C07K1/34C07K1/18
Inventor 任勇
Owner 宁夏泰瑞制药股份有限公司
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