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A kind of telavancin purification method

A technology of telavancin and alumina, applied in the field of medicine, can solve problems such as separation and purification difficulties, and achieve the effects of simple treatment, reduction of hazardous waste emissions, and reduction of purification costs

Active Publication Date: 2022-02-01
福建康鸿生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are many active sites such as amino groups and hydroxyl groups in the structural formula of glycolipopeptide antibiotics. The introduction of the above groups will generate many impurities at the target position at the same time, making separation and purification difficult.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment example 1

[0048] Add 10 g of light yellow telavancin crude product to 300 ml of sodium carbonate aqueous solution (30 g of sodium carbonate, 10%), control the temperature not higher than 25 ° C, dissolve with ultrasonic stirring, filter a small amount of insoluble solids through a Buchner funnel, and discard the filter residue. Add 100ml of ethyl acetate to the filtrate, stir and separate the layers, continue to extract the water layer once with 100ml of ethyl acetate, combine the ethyl acetate layers, distill and recover the ethyl acetate, and keep the water layer for later use. Pack 300g of neutral alumina into the column, and rinse the column with 1000ml of purified water and 1000ml of 3% glacial acetic acid aqueous solution once. The extracted water layer was loaded with samples, and eluted successively with 15% ethanol aqueous solution and 17.5% ethanol aqueous solution, and the analysis solution was detected by TLC (reversed-phase thin-layer plate, developer: methanol / glacial aceti...

Embodiment example 2

[0050]Add 10 g of the light yellow telavancin crude product to 300 ml of aqueous sodium hydroxide solution (30 g of sodium hydroxide, 10%), control the temperature not higher than 25° C., and dissolve with ultrasonic stirring. A small amount of insoluble solids are filtered through a Buchner funnel, and the filter residue is discarded. Add 100ml of ethyl acetate to the filtrate, stir and separate the layers, continue to extract the water layer once with 100ml of ethyl acetate, combine the ethyl acetate layers, distill and recover the ethyl acetate, and keep the water layer for later use. Pack 300g of neutral alumina into the column, and rinse the column with 1000ml of purified water and 1000ml of 3% glacial acetic acid aqueous solution once. The extracted water layer was loaded with samples, and eluted successively with 15% ethanol aqueous solution and 17.5% ethanol aqueous solution, and the analysis solution was detected by TLC (reversed-phase thin-layer plate, developer: meth...

Embodiment example 3

[0052] Add 10 g of light yellow telavancin crude product to 300 ml of sodium carbonate aqueous solution (30 g of sodium carbonate, 10%), control the temperature not higher than 25 ° C, dissolve with ultrasonic stirring, filter a small amount of insoluble solids through a Buchner funnel, and discard the filter residue. Add 100ml of ethyl acetate to the filtrate, stir and separate the layers, continue to extract the water layer once with 100ml of ethyl acetate, combine the ethyl acetate layers, distill and recover the ethyl acetate, and keep the water layer for later use. Pack 300g of acidic alumina into the column, and wash the column once with 1000ml of purified water and 1000ml of 3% glacial acetic acid aqueous solution. The extracted water layer was loaded with samples, and eluted successively with 15% ethanol aqueous solution and 17.5% ethanol aqueous solution, and the analysis solution was detected by TLC (reversed-phase thin-layer plate, developer: methanol / glacial acetic ...

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PUM

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Abstract

The invention discloses a method for purifying telavancin. According to the characteristics of the structural formula of telavancin, telavancin is dissolved in an aqueous solution of inorganic alkali, and branched chain impurities are removed by extraction with an organic solvent. The aqueous phase is adsorbed by alumina and analyzed. The solution was eluted, the analysis solution was concentrated by nanofiltration membrane nanofiltration, the concentrated solution was adjusted with dilute acid to adjust the pH, and a large amount of white solid was precipitated, filtered with suction, the solid was beaten with an organic solvent, and the filter cake was dried under reduced pressure at low temperature to obtain the finished product of Telavancin , the present invention is easy to operate by adjusting the pH, and the cost is low. Aluminum oxide is used for impurity removal, and the purification cost is reduced without affecting the purification efficiency.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and in particular relates to a method for purifying telavancin. Background technique: [0002] Telavancin is a new type of lipoglycopeptide antibiotic, a new drug jointly developed by Schwann Corporation of the United States and Astellas Corporation of Japan. In 2009, the U.S. FDA approved telavancin for the treatment of skin infections caused by Gram-positive bacteria. In 2011, EMA approved it for the treatment of adult hospital-acquired pneumonia caused by MRSA. The activity is higher than that of vancomycin, and the half-life is longer than that of vancomycin, and the clinical administration is once a day. The abuse of antibiotics by humans leads to the emergence of superbugs. Antibiotics on the market have no therapeutic effect on superbugs. Telavancin has drug resistance and has been used to treat infections caused by sensitive bacteria for a long time. An important drug with broad marke...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07K9/00C07K1/34C07K1/14
CPCC07K9/008
Inventor 张茂华蒋永飞苏专专孙万树詹立都
Owner 福建康鸿生物科技有限公司