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Cefoxitin sodium crystal compound and cefoxitin sodium composition powder injection

A technology of cefoxitin sodium and compound, applied in the field of medicine, can solve the problems of high price and the like, and achieve the effects of improving bioavailability, improving drug safety, good bioavailability and drug safety

Active Publication Date: 2013-11-06
SHANDONG LUOXIN PHARMA GRP CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, the domestic cephalosporin market is mainly imported except for the first-generation cephalosporins, and the price is expensive.

Method used

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  • Cefoxitin sodium crystal compound and cefoxitin sodium composition powder injection
  • Cefoxitin sodium crystal compound and cefoxitin sodium composition powder injection
  • Cefoxitin sodium crystal compound and cefoxitin sodium composition powder injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044]Preparation of cefoxitin sodium crystalline compound: get 1 kg of cefoxitin sodium crude product, add volume ratio of 7:2.8:0.2 methanol:ethanol:water mixed solution that is 15 times of the weight of cefoxitin sodium crude product, and heat to reflux; After the crude product of cefoxitin sodium is dissolved, add activated carbon decolorizing with 0.3 times the weight of the crude product of cefoxitin sodium, and filter; Be the ethyl acetate of 0.8 times of the crude product weight of cefoxitin sodium, described stirring is 18rmp, and described dropping is to control dropping time 10 minutes and uniform speed dropwise; Cool down to 61°C for 5min, then cool down to 23°C for 10min under stirring at 10rmp, let stand for 19 hours, filter, wash twice with 6:4 methanol:ethyl acetate solution, 0.25 times each time, and dry to obtain the cephalosporin Citine sodium crystalline compound, the yield is 92.5%, and the HPLC content is 99.95%.

[0045] The X-ray powder diffraction pat...

Embodiment 2

[0047] Preparation of cefoxitin sodium crystalline compound: get 2 kg of cefoxitin sodium crude product, add volume ratio of 7: 2.8: 0.2 methanol: ethanol: water mixed solution that is 20 times the weight of cefoxitin sodium crude product, and heat to reflux; After the crude product of cefoxitin sodium is dissolved, add 0.3 times of the weight of the crude product of cefoxitin sodium for decolorization, filter; the filtrate is added with ethyl propionate whose volume is 1.8 times of the weight of the crude product of cefoxitin sodium, stop heating, and add dropwise the volume under stirring. Ethyl acetate that is 1.2 times the weight of the crude product of cefoxitin sodium, the stirring is 18rmp, and the dripping is to control the dripping time for 10 minutes at a constant speed; dropwise, stirring and cooling, the stirring cooling is under stirring at a rotating speed of 28rmp Cool down to 61°C for 5min, then cool down to 23°C for 10min under stirring at 10rmp, let stand for ...

Embodiment 3

[0050] Preparation of cefoxitin sodium crystalline compound: get 10 kg of cefoxitin sodium crude product, add volume ratio of 7:2.8:0.2 methanol:ethanol:water mixed solution that is 18 times of the weight of cefoxitin sodium crude product, and heat to reflux; After the cefoxitin sodium crude product is dissolved, add 0.5 times of the weight of the cefoxitin sodium crude product for decolorization, and filter; add ethyl propionate whose volume is 2.0 times the weight of the cefoxitin sodium crude product, stop heating, and add dropwise Ethyl acetate that is 1.0 times the weight of the crude product of cefoxitin sodium, the stirring is 20rmp, and the dripping is to control the dripping time for 12 minutes and drop at a constant speed; after dropping, stir and cool down, and the stirring and cooling is under stirring at a rotating speed of 29rmp. Cool down to 58°C for 5 minutes, then cool down to 25°C for 10 minutes under stirring at a rotating speed of 8rmp, let stand for 20 hour...

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Abstract

The invention relates to a cefoxitin sodium crystal compound. The method of powder X-ray diffractometry is utilized to determine the cefoxitin sodium crystal compound, and an X-ray powder diffraction pattern represented by the diffraction angle of 2theta+-0.2 degrees has characteristic diffraction peaks at 5.3 degrees, 8.6 degrees, 11.9 degrees, 13.2 degrees, 15.5 degrees, 16.1 degrees, 19.0 degrees, 22.3 degrees and 24.4 degrees. The invention also relates to a cefoxitin sodium composition powder injection containing the cefoxitin sodium crystal compound, and the cefoxitin sodium composition powder injection comprises 95 to 100 parts of the cefoxitin sodium crystal compound and 0.1 to 1 part of sodium benzoate.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a cefoxitin sodium crystalline compound and its composition powder for injection. Background technique [0002] Cefoxitin sodium is a cephamycin antibiotic, which is produced by Streptomyces lactamdurans. It is a new type of antibiotic produced by semi-synthesis. Its mother nucleus is similar to cephalosporins. , and the antibacterial properties are also similar, and are also customarily included in the second-generation cephalosporins. Cefoxitin acts antibacterially by binding to one or more penicillin-binding proteins (PBPs), inhibiting cell wall biosynthesis in actively dividing cells of bacteria. Cefoxitin sodium is effective against Gram-negative bacteria Haemophilus influenzae, Klebsiella, Escherichia coli, Morganella morganii, Mirabilis proteus, Providencia rettgeri and Neisseria gonorrhoeae. Strong antibacterial effect. [0003] Cefoxitin sodium is especially suitable for preve...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/57C07D501/12A61K31/546A61K9/14A61P31/04
Inventor 李明杰范丽王春艳
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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