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Purification method of anidulafungin

A technology of anidulafungin and purification method, applied in the direction of peptides, etc., can solve the problems of difficult purification of the final product, low purity of anidulafungin, etc., and achieve the effects of controllable quality, easy recovery, and convenient operation.

Inactive Publication Date: 2017-02-22
TIANJIN LINGSHI BIOTECH DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The starting materials of the above-mentioned semi-synthetic drugs are all obtained by microbial fermentation, and contain a large number of by-products with similar structures, which brings great difficulties to the subsequent purification of the final product.
As a medicine, the purity and impurities of its Anifungin have relatively high requirements to ensure the effectiveness and safety of the drug, but at present the purity of Anifungin is relatively low, so a new Anifungin is urgently needed. Purification method of Fenjing

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] A kind of purification method of Anifungin, the steps are as follows:

[0023] (1) Dissolution and decolorization: Add the crude product of Anifungin into the crystallization solvent to completely dissolve the solid, add activated carbon to stir for decolorization, and filter out the decolorization to obtain a solution; the crystallization solvent is formed by mixing two solvents, the first The solvent is alcohol, and the second solvent is any one of halogenated hydrocarbons, ketones, nitriles or ethers; wherein, the volume ratio of the two solvents is 4:1;

[0024] (2) Take the solution of Anifungin, load the sample on the macroporous adsorption resin, wash the resin column with an acidic or neutral aqueous solution under the condition of 3-5bar, and then use an acidic aqueous solution with a volume percentage of 40%-60% organic solvent Pressurize and wash the resin column, and then use an acidic aqueous solution with a volume percentage of 60%-80% organic solvent to e...

Embodiment 2

[0028] A kind of purification method of Anifungin, the steps are as follows:

[0029] (1) Dissolution and decolorization: Add the crude product of Anifungin into the crystallization solvent to completely dissolve the solid, add activated carbon to stir for decolorization, and filter out the decolorization to obtain a solution; the crystallization solvent is formed by mixing two solvents, the first The solvent is alcohol, and the second solvent is any one of halogenated hydrocarbons, ketones, nitriles or ethers; wherein, the volume ratio of the two solvents is 6:1;

[0030] (2) Take the solution of Anifungin, apply it to polystyrene resin, wash the resin column with acidic or neutral aqueous solution under the condition of 6-7bar, and then use an acidic solution with a volume percentage of 40%-60% organic solvent The aqueous solution washes the resin column under pressure, and then uses an acidic aqueous solution with a volume percentage of 60%-80% organic solvent to elute the ...

Embodiment 3

[0034] A kind of purification method of Anifungin, the steps are as follows:

[0035] (1) Dissolution and decolorization: Add the crude product of Anifungin into the crystallization solvent to completely dissolve the solid, add activated carbon to stir for decolorization, and filter out the decolorization to obtain a solution; the crystallization solvent is formed by mixing two solvents, the first The solvent is alcohol, and the second solvent is any one of halogenated hydrocarbons, ketones, nitriles or ethers; wherein, the volume ratio of the two solvents is 8:1;

[0036] (2) Take the solution of Anifungin, load the sample on the macroporous adsorption resin, wash the resin column with an acidic or neutral aqueous solution under the condition of 7-9bar, and then use an acidic aqueous solution with a volume percentage of 40%-60% organic solvent Pressurize and wash the resin column, and then use an acidic aqueous solution with a volume percentage of 60%-80% organic solvent to e...

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PUM

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Abstract

The invention relates to a purification method of anidulafungin. The purification method of anidulafungin comprises the steps of 1, dissolving and distaining, wherein, an anidulafungin crude product into a crystal solvent is added to make the solid completely dissolve, activated carbon is added to distain by stirring, and the dissolved solution is obtained after discoloring by filtering; 2, sampling the anidulafungin dissolved solution, loading the sample in macroporous adsorption resin, and increasing the pressure to wash the resin column with an acid or neutral water solution under the condition of 3-9bar; 3, concentrating, wherein, the eluent is concentrated until the eluent is dry, so that an anidulafungin pure product with content of more than 99.5% is obtained. The purification method of the anidulafungin is simple in technology, convenient to operate, and less in adopted amount of solution, and the isomer impurities with similar structural properties can be effectively removed. The product is high in purity and safe and controllable in quality, can be applicable to a refining method of the anidulafungin for industrial production, and the purity can be increased to 99.5% or above.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, in particular to a method for purifying Anifungin. Background technique [0002] In recent years, with the increase in the incidence of cancer chemotherapy, organ transplantation, AIDS, etc., the incidence of deep fungal infection and the resulting mortality continue to rise, which has become one of the more difficult clinical problems. Anifungin is the third listed echinocandin antifungal drug for the treatment of candida bacteremia and abdominal abscess, peritonitis, esophageal candida and other types of candida infection. This product is produced by biological fermentation and transformation to remove the original side chain to obtain the echinocandin B nucleus, and then chemically synthesized to insert a new side chain. Such compounds can be further modified into semi-synthetic drugs, and micafungin, caspofungin and anidifungin are listed in sequence. The starting materials of the above-me...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07K7/56C07K1/16
Inventor 闻建华傅红闻铭远梁少雄
Owner TIANJIN LINGSHI BIOTECH DEV CO LTD
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