Cefmenoxime hydrochloride compound entity used for children and preparation thereof

A technology of cefmenoxime hydrochloride and compound, which is applied in the field of cefmenoxime hydrochloride compound entity and its preparation for children, can solve the problems such as difficulty in dissolving cefmenoxime hydrochloride, increase in impurities, poor stability, etc. good stability

Inactive Publication Date: 2015-10-28
ZHEJIANG CHANGDIAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the difficulty in dissolving cefmenoxime hydrochloride and the poor stability of cephalosporin products in solution, too long time in dissolution will cause degradation of cefmenoxime and increase of impurities

Method used

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  • Cefmenoxime hydrochloride compound entity used for children and preparation thereof
  • Cefmenoxime hydrochloride compound entity used for children and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] (1) Weigh 100g of cefmenoxime crude product, add 1000ml of water, stir and slowly add 4% sodium bicarbonate solution dropwise until clarification, add 10ml of ethyl acetate under stirring, transfer to a 1000ml pressure-resistant container, ensure that it is full and air bubbles are removed, and seal Container, shake, temperature control -18 ℃ and freeze for 3 hours, then take out;

[0023] (2) Remove the organic phase, and after the ice melts, add 10 g of activated carbon, stir and decolorize, and filter;

[0024] (3) Transfer the filtrate to a crystallization tank, control the temperature at 10-15°C, adjust the pH to 1.5 with dilute hydrochloric acid, continue to grow crystals for 1 hour, filter with suction, wash with water, and dry in vacuum at 40°C to obtain the final product. The maximum impurity is 0.13%, and the total impurity is 0.23%.

Embodiment 2

[0026] (1) Weigh 100 g of cefmenoxime crude product, add 1000 ml of water, stir and slowly add 4% sodium bicarbonate solution dropwise until clarification, add 10 ml of chloroform under stirring, transfer to a 1000 ml pressure-resistant container, ensure that it is full and air bubbles are removed, seal the container, Shake, and freeze at -18°C for 3 hours before taking out;

[0027] (2) Remove the organic phase, and after the ice melts, add 10 g of activated carbon, stir and decolorize, and filter;

[0028] (3) Transfer the filtrate to a crystallization tank, control the temperature at 10-15°C, adjust the pH to 1.7 with dilute hydrochloric acid, continue growing crystals for 1 hour, filter with suction, wash with water, and dry in vacuo at 40°C. The maximum simple impurity is 0.19%, and the total impurity is 0.29%.

Embodiment 3

[0030] (1) Weigh 100g of cefmenoxime crude product, add 1000ml of water, stir and slowly add 4% sodium bicarbonate solution dropwise until clarification, add 7ml of ethyl acetate under stirring, transfer to a 1000ml pressure-resistant container, ensure that it is full and air bubbles are removed, and seal Container, shake, temperature control -18 ℃ and freeze for 3 hours, then take out;

[0031] (2) Remove the organic phase, and after the ice melts, add 10 g of activated carbon, stir and decolorize, and filter;

[0032] (3) Transfer the filtrate to a crystallization tank, control the temperature at 10-15°C, adjust the pH to 1.5 with dilute hydrochloric acid, continue to grow crystals for 1 hour, filter with suction, wash with water, and dry in vacuum at 40°C. The maximum simple impurity is 0.17%, and the total impurity is 0.24%.

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Abstract

The invention provides a cefmenoxime hydrochloride compound entity used for children. The structural formula is as shown in specifications. The cefmenoxime hydrochloride compound entity is prepared through the steps that step1, water is added into a cefmenoxime hydrochloride crude product, sodium carbonate is added, stirring is performed for dissolving, an extracting agent is added, and then the cefmenoxime hydrochloride crude product is transferred into a pressure-resistant container in a filling mode, vibrated in a sealed mode after being defoamed and taken out after being frozen in a temperature control mode; step2, an organic phase is removed, after a solid is melted, active carbon is added, stirring is performed for discoloring, and filtering is performed; step3, pH of filtrate is adjusted to 1.5-2.3 through hydrochloride acid, and then crystal growing, filtering, washing with water and vacuum drying at 40 DEG C are performed to obtain the cefmenoxime hydrochloride compound entity. The cefmenoxime hydrochloride prepared through the method has the advantages of having few impurities, being high in purity and the like compared with a traditional technology.

Description

technical field [0001] The invention relates to a cefmenoxime hydrochloride compound entity and its preparation for children, belonging to the field of medicinal chemistry. Background technique [0002] The chemical name of cefmenoxime hydrochloride is (6R,7R)-7-[2-(2-amino-4-thiazolyl)(methoxyimino)acetamido]-3-[[(1-methyl-1H -tetrazol-5-yl)-thio]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate hydrochloride, also known as aminothiazide Oximazole cephalosporins and Besteke are third-generation cephalosporins, which have antibacterial effects on both Gram-negative and Gram-positive aerobic and anaerobic bacteria. Among Gram-negative bacteria, the antibacterial effect on Escherichia coli and Klebsiella pneumoniae is slightly stronger than that of cefotiam, and significantly stronger than that of the first-generation cefazolin. The antibacterial effect of Acidobacterium and Enterobacter is also relatively strong, and it also has a strong antibacterial effect on Bacte...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/12A61K9/19
CPCA61K9/0019A61K9/19C07D501/12C07D501/36
Inventor 陈宇东厉达中
Owner ZHEJIANG CHANGDIAN PHARMA
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