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A kind of cefoxitin compound and composition thereof

A technology of cefoxitin and compounds, which is applied in the field of cefoxitin compounds and their compositions, can solve problems such as high price, and achieve the effects of improving drug safety, good dissolution stability, and excellent dissolution performance

Active Publication Date: 2011-12-28
江西新先锋医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] 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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  • A kind of cefoxitin compound and composition thereof
  • A kind of cefoxitin compound and composition thereof
  • A kind of cefoxitin compound and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] The preparation of described cefoxitin compound is: get 100g of cefoxitin crude product, add the volume ratio that is 7.5:2.5 methanol: ethanol solution that volume is 8 times of cefoxitin crude product weight, heat to reflux; Cefoxitin crude product dissolves clear Finally, add 0.5 times of activated carbon for decolorization for 30 minutes, filter; the filtrate stops heating, naturally cools down to 43 ° C, maintains the temperature and adds dropwise acetone with a volume ratio of 5 times the weight of the crude cefoxitin: aqueous solution of 9: 1, the resulting The dropwise addition is at a constant speed of 6 to 7 minutes at a stirring speed of 12 to 14rmp; after dropping, stir and cool down, the stirring and cooling is to cool down to room temperature for 10 minutes under stirring at a rotating speed of 17 to 18rmp, and then stir at a rotating speed of 11rmp for 20min Cool down to 12-13°C, let stand for 19 hours, filter, wash twice with 8:2 methanol:water solution, ...

Embodiment 2

[0061] The preparation of described cefoxitin compound is: get 100g of cefoxitin crude product, add the volume ratio that is 7.5:2.5 methanol: ethanol solution that volume is 8 times of cefoxitin crude product weight, heat to reflux; Cefoxitin crude product dissolves clear Finally, add 0.5 times of activated carbon for decolorization for 30 minutes, filter; the filtrate stops heating, naturally cools down to 43 ° C, maintains the temperature and adds dropwise acetone with a volume ratio of 5 times the weight of the crude cefoxitin: aqueous solution of 9: 1, the resulting The dropwise addition is at a stirring speed of 11 to 13rmp, and is added dropwise at a constant speed within 5 minutes; after dropping, stir and cool down. 11~12 ℃, stand still for 18 hours, filter, with 8: 2 methanol: aqueous solution washes 2 times, each dosage is 0.4 times of the volume of cefoxitin crude product weight, dry, obtain described cefoxitin compound, yield Yield 91.2%, HPLC content 99.52%, mp.1...

Embodiment 3

[0064] The preparation of described cefoxitin compound is: get 100g of cefoxitin crude product, add the volume ratio that is 7.5:2.5 methanol: ethanol solution that volume is 8 times of cefoxitin crude product weight, heat to reflux; Cefoxitin crude product dissolves clear Finally, add 0.3 times of activated carbon for decolorization for 30 minutes, filter; the filtrate stops heating, naturally cools down to 42 ° C, maintains the temperature and adds dropwise acetone with a volume ratio of 4 times the weight of the crude cefoxitin: aqueous solution of 9: 1, the resulting The dropwise addition is at a constant speed of 7 to 8 minutes at a stirring speed of 12 to 14rmp; after dropping, stir and cool down, the stirring and cooling is to cool down to room temperature for 10 minutes under stirring at a rotating speed of 15 to 17rmp, and then stir at a rotating speed of 10rmp for 20min Cool down to 10-11°C, let stand for 19 hours, filter, wash 3 times with 8:2 methanol:water solution...

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Abstract

The invention relates to a cefoxitin compound. The cefoxitin compound is determined by the method of powder X-ray diffractometry, and characteristic diffraction peaks appear at 5.8 degrees, 7.4 degrees, 8.6 degrees, 13.0 degrees, 14.8 degrees, 15.2 degrees, 16.5 degrees, 18.7 degrees, 23.1 degrees and 25.2 degrees in an X-ray powder diffraction spectrum which is represented by the angle of diffraction 2theta plus or minus 0.2 degree. The invention also relates to a composition of the cefoxitin compound, and the composition comprises 90 to 100 parts of the cefoxitin compound and 0 to 2000 parts of a pharmaceutically acceptable carrier, preferably 0.1 part to 1000 parts of the pharmaceutically acceptable carrier, more preferably 1 part to 500 parts, and most preferably 1 part to 5 parts.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a cefoxitin compound and a composition thereof. Background technique [0002] Cefoxitin (cefoxitin), the chemical name is (6R, 7S-3-carbamoyloxymethyl-7-methoxy-8-oxo-7-2[(2-thienyl)acetamido]-5 -Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, developed by Merk Company of the United States, and launched in 1994. Cefoxitin is semi-synthesized from methoxycephalosporin C produced by Streptomyces A new class of antibiotics. Because it inhibits the synthesis of bacterial cell walls to kill bacteria, and due to the structural characteristics of cefoxitin, it has high resistance to β-lactamase produced by bacteria, so it is resistant to β-lactamase Stable cefoxitin has huge market potential. [0003] Patent application 200910027790.1 discloses a synthesis method of cefoxitin, which uses 7-ACA as a starting material, and first reacts with thiophene acetyl chloride to obtain cephalotinic a...

Claims

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Application Information

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IPC IPC(8): C07D501/57C07D501/12A61K31/546A61P31/04
Inventor 夏智红
Owner 江西新先锋医药有限公司
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