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Ceftezole sodium compound and novel method thereof

A technology of ceftezole sodium and ceftezole, which is applied in the medical field, can solve the problems of affecting the curative effect of clinical medication and the purity of ceftezole sodium is not very high, and achieve the effects of low cost, reduced toxic and side effects, and high yield

Inactive Publication Date: 2012-08-01
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The purity of ceftezole sodium obtained by these two synthetic routes is not very high, which directly affects the curative effect of clinical medication, and further research and improvement are needed on its purity

Method used

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  • Ceftezole sodium compound and novel method thereof
  • Ceftezole sodium compound and novel method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] The purification of embodiment 1 ceftizole sodium

[0028] (1) 100g of ceftizole sodium crude product was dissolved in 1000ml of water, then slowly adding 0.1mol / L hydrochloric acid, stirring and reacting until the pH of the solution was 1.5, i.e., ceftizole precipitation was produced, and suction filtration obtained ceftizole 83.9g;

[0029] (2) 83.9g of ceftiazole obtained in the previous step was dissolved in 400g of methanol, the activated carbon of the total solution volume 4.0g was added, the temperature was kept at 60°C and stirred for 30min, and the filtrate was collected by filtration and decarburization;

[0030] (3) The filtrate obtained in step (2) is treated with an anion / cation exchange membrane electrodialysis device: the anion exchange membrane uses the AHA anion exchange membrane provided by the Japanese Tokuyama Caoda company, and the cation exchange membrane is provided by the Japan Tokuyama Caoda company The CMB cation-exchange membrane, the solutio...

Embodiment 2

[0035] The purification of embodiment 2 ceftizole sodium

[0036] (1) 100g of ceftizole sodium crude product was dissolved in 1000ml of water, then slowly adding 0.5mol / L phosphoric acid, stirring and reacting until the pH of the solution was 1.8, i.e., ceftazole precipitation was produced, and suction filtration obtained ceftizole 82.1g;

[0037] (2) the 82.1g ceftiazole obtained in the previous step was dissolved in 350g methylene chloride, the gac of 3.5g was added, and the temperature was kept at 60°C and stirred for 20min, filtered and decarburized, and the filtrate was collected;

[0038] (3) The filtrate obtained in step (2) was treated with an anion / cation exchange membrane electrodialysis device: NEOSEPTA ACS anion exchange membrane produced by ASTOM Co., Ltd. was used for the anion exchange membrane, and NEOSEPTA CMX cation exchange membrane produced by ASTOM Co., Ltd. was used for the cation exchange membrane. Membrane, feeding the solution obtained in the step (2)...

Embodiment 3

[0044] Embodiment 3 Refining of ceftizole sodium

[0045] (1) 100g of ceftizole sodium crude product was dissolved in 1000ml of water, then slowly adding 0.5mol / L phosphoric acid, stirring and reacting until the pH of the solution was 2.5, i.e., ceftazole precipitation was produced, and suction filtration obtained ceftizole 80.9g;

[0046] (2) 80.9g of ceftiazole obtained in the previous step was dissolved in 300g of isopropanol, the activated carbon of 3.0g was added, the temperature was kept at 60°C and stirred for 30min, and the filtrate was collected by filtration and decarburization;

[0047] (3) The filtrate obtained in step (2) is treated with an anion / cation exchange membrane electrodialysis device: the anion exchange membrane uses the AHA anion exchange membrane provided by the Japanese Tokuyama Caoda company, and the cation exchange membrane is provided by the Japan Tokuyama Caoda company The CMB cation-exchange membrane, the solution obtained in step (2) is fed int...

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Abstract

The invention relates to a ceftezole sodium compound and a novel method thereof. The method provided by the invention achieves the refining aim by acidification reaction, activated carbon adsorption, electroosmosis device processing and preparation of chromatographic columns, so as to finally obtain a high-purity ceftezole sodium compound, overcomes the defects of low purity of the existing raw materials, improves the product quality of the preparation, reduces the toxic and side effects, and ensures the clinical safety of the medicine at the same time.

Description

technical field [0001] The invention relates to a ceftizole sodium compound and a new method thereof, belonging to the technical field of medicine. Background technique [0002] Ceftezole Sodium (Ceftezole Sodium), also known as Yitixin, the chemical name is 6R (trans)-8-oxo-7-[(1H-1-tetrazolyl acetyl)amino]-3- [[2-(1,3,4-thiadiazolyl)thio]methyl]-5-thia-1-azabicyclo[4,2,0]oct-2-ene-2-carboxylic acid Sodium salt, chemical formula: C 13 H 11 N 8 NaO 4 S 3 , the structural formula is: [0003] [0004] Ceftizole sodium is a semi-synthetic cephalosporin antibiotic synthesized and developed by Fujisawa Corporation of Japan, and was marketed under the trade name of Ceolslin in April 1978. Ceftezole sodium was used relatively late in my country. In 2002, Harbin Pharmaceutical and Tianjin Xinfeng had production of APIs and preparations. [0005] Ceftazole sodium is mainly used for the treatment of infections caused by Staphylococcus aureus, Streptococcus pyogenes, Pneumo...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/36C07D501/12
Inventor 胡建荣
Owner HAINAN LINGKANG PHARMA CO LTD
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