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Crystallization method of biapenem

A crystallization technology of biapenem, which is applied in the field of crystallization of biapenem, can solve the problems of large amount of acetone, long crystallization time, low dissolved concentration, etc., and achieve improved yield, good color grade, and reduced material loss Effect

Pending Publication Date: 2022-01-11
石药集团中诺药业(石家庄)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the low dissolution concentration and slow precipitation, the crystallization time is long, the amount of acetone is large, the yield is low, and the color grade is high

Method used

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  • Crystallization method of biapenem

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Add 10 g of crude biapenem (purity 98.2%) to 100 ml of water, heat up to 40-50° C. in 10-15 minutes, stir and dissolve until clear and translucent. Add 1.5g of activated carbon and stir for 10 minutes to decolorize, then filter with a 0.45 micron filter membrane to obtain the filtrate; cool down to 10-20°C within 5 minutes to precipitate biapenem crystals, then add 300ml of acetone for further dissolution After crystallization for 2 hours, 9.30 g of biapenem was obtained, with a yield of 93.0%, a purity of 99.4%, and a color grade of 1#.

[0030] Compared with Comparative Example 1, the yield increased by 11%, the purity increased by 0.5%, and the color level decreased from 2# to 1#.

Embodiment 2

[0032] Add 9 g of crude biapenem (purity: 98.2%) into 100 ml of water, heat up to 40-50°C in 10-15 minutes, stir, dissolve and become transparent. Add 1.2g of activated carbon and stir for 10 minutes to decolorize, then filter with a 0.45 micron filter membrane to obtain the filtrate; cool down to 10-20°C within 5 minutes to precipitate biapenem crystals, then add 300ml of acetone for further dissolution Crystallized to obtain 8.01 g of biapenem, with a yield of 89.0%, a purity of 99.5%, and a color grade of 1#. Compared with Comparative Example 1, the yield increased by 9%, the purity increased by 0.8%, and the color level decreased by 1#.

Embodiment 3

[0034] Add 11g of crude biapenem (purity: 98.2%) to 110ml of water, heat up to 40-50°C in 10-15 minutes, stir, dissolve and become transparent. Add 1.5g of activated carbon for decolorization for 10 minutes, then filter with a 0.45 micron filter membrane to obtain the filtrate; rapidly cool down to 10-20°C within 5 minutes to precipitate biapenem crystals, then add 300ml of acetone for further dissolution Crystallized to obtain 10.1 g of biapenem with a yield of 91.9%, a purity of 99.3%, and a color grade of 1#. Compared with Comparative Example 1, the yield increased by 11.9%, the purity increased by 0.6%, and the color level decreased by 1#.

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Abstract

The invention discloses a crystallization method of biapenem, which comprises the following steps of: (1) dissolving: adding crude biapenem into water (the weight ratio of biapenem to water is 1: 10), quickly heating to 40-50 DEG C, and stirring for dissolving the crude biapenem until the solution is transparent; (2) decarburization: adding 1% of activated carbon for decolorization for 10 minutes, and then filtering by using a 0.45-micron filter membrane to obtain filtrate; and (3) rapidly cooling to 10-20 DEG C, separating out biapenem crystals, then adding acetone of which the volume is 3 times that of the biapenem crystals, and further carrying out solvent-out crystallization to obtain biapenem with high purity and better color grade. The crystallization method disclosed by the invention is simple and convenient to operate, short in period and environment-friendly, the purity of the biapenem product is improved, the color grade is reduced, the quality is better, and the medication is safer.

Description

technical field [0001] The invention relates to the technical field of crystallization of biapenem, in particular to a crystallization method of biapenem. Background technique [0002] Biapenem is a synthetic carbapenem antibiotic, which is more stable to renal dehydropeptidase than meropenem, and does not require combined enzyme inhibitors. The activity against Gram-negative bacteria, especially Pseudomonas aeruginosa, is stronger than that of imipenem; the antibacterial activity against Gram-positive bacteria is slightly lower than that of imipenem; the activity against anaerobic bacteria is the same as that of imipenem. [0003] The strains sensitive to apenem are: Staphylococcus, Streptococcus, Pneumococcus, Enterococcus (except Enterococcus faecium), Moraxella, Escherichia coli, Citrobacter, Klebsiella , Enterobacter, Serratia, Proteus, Haemophilus influenzae, Pseudomonas aeruginosa, Actinomyces, Peptostreptococcus, Bacteroides, Prevotella, Fusobacterium, etc. [0004...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D519/06
CPCC07D519/06
Inventor 徐永龙薛军芳袁国强李世成马文婵邱增会李敏谢子龙姚慧涛张娜李泽岚
Owner 石药集团中诺药业(石家庄)有限公司
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