Preparation method and application of cefuroxime sodium

A technology of cefuroxime sodium and cefuroxime acid, which is applied in the field of medicine, can solve the problems of unsatisfactory stability and color of cefuroxime sodium, unsatisfactory dissolving effect of cefuroxime, large amount of water and acetone, and achieve residual solvent less, lower production costs, and reduced dosage

Inactive Publication Date: 2019-11-12
SHANGHAI LONGXIANG BIO MEDICINE DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But common problem at present is that the cefuroxime sodium stability (mainly color aspect) that makes is unsatisfactory
In addition, the organic solvents in the prior art are all selected acetone, and the dissolving effect of single acetone on cefuroxime is still unsatisfactory, and what have just add cosolvent isopropanol, acetonitrile, but still unsatisfactory, the consumption of water and acetone is big, and total solvent amount And the large amount of water makes post-processing difficult and costly

Method used

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  • Preparation method and application of cefuroxime sodium

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Dissolve 10.0g of cefuroxime acid in a mixed solution of 7ml of water and 70ml of acetone, stir until dissolved, add 1.0ml of 10.0% sodium sulfite aqueous solution, then add 0.5g of activated carbon and stir for 30 minutes, filter to remove carbon, and mix with appropriate amount of acetone and water Wash the charcoal with the solution, combine the filtrate and the charcoal washing solution, control the temperature at 30°C, stir the solution of 5.0g 60% sodium lactate and 50ml ethanol into the above combined solution, stir for 30 minutes after the addition, then add 100ml of acetone dropwise, continue stirring 60 minutes; filter, collect, wash the crystals, and vacuum-dry at 35° C. to obtain 10.10 g of stable cefuroxime sodium, with a yield of 96.0%.

[0036] Wherein the calculation method of yield is: yield (%)=mass of cefuroxime sodium obtained in experiment / theoretical quality of cefuroxime sodium. Specifically, the molecular weight of cefuroxime acid is 424.39, the ...

Embodiment 2

[0038] Dissolve 10.0g of cefuroxime acid in a mixed solution of 7ml of water and 70ml of acetone, stir until dissolved, add 1.0ml of 10.0% sodium metabisulfite aqueous solution, then add 0.5g of activated carbon and stir for 30 minutes, filter to remove charcoal, and use appropriate amount of acetone and water Wash the charcoal with the mixed solution, combine the filtrate and the charcoal washing solution, control the temperature at 30°C, stir the solution of 5.0g 60% sodium lactate and 30ml methanol into the above combined solution, stir for 30 minutes after the addition, then add 100ml of acetone dropwise, continue Stir for 60 minutes; filter, collect, wash the crystals, and vacuum-dry at 35° C. to obtain 9.8 g of stable cefuroxime sodium, with a yield of 93.2%.

Embodiment 3

[0040] Dissolve 10.0g of cefuroxime acid in a mixed solution of 7ml of water and 70ml of acetone, stir until dissolved, add 0.20ml of 10.0% sodium metabisulfite aqueous solution, then add 0.5g of activated carbon and stir for 30 minutes, filter to remove charcoal, and add appropriate amount of acetone and water Wash the charcoal with the mixed solution, combine the filtrate and the charcoal washing solution, control the temperature at 30°C, stir and add 12.0g of 20.0% sodium acetate aqueous solution into the above combined solution, stir for 30 minutes after the addition, then add 50ml of acetone dropwise, and continue to stir for 60 minutes; filter, collect, wash the crystals, and vacuum-dry at 35°C to obtain 10.45 g of stable cefuroxime sodium, with a yield of 99.3%.

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Abstract

The invention belongs to the technical field of medicines, and relates to a preparation method and application of cefuroxime sodium. The preparation method of the cefuroxime sodium comprises the following steps: dissolving cefuroxime acid in a solvent, adding a stabilizer aqueous solution, and adding a salt former to obtain the cefuroxime sodium. The cefuroxime sodium prepared by the method disclosed by the invention has good color stability. In addition, seldom residual solvent exists in the preparation method of the cefuroxime sodium; the yield is high; and water and total solvent consumption are reduced, production is facilitated, and the production cost is greatly reduced.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a preparation method and application of cefuroxime sodium. Background technique [0002] Cefuroxime sodium is a second-generation highly effective, safe and broad-spectrum semi-synthetic cephalosporin. Since it was developed and marketed by the British Glaxo company in 1975, due to its excellent curative effect on infections caused by most β-lactamase-producing pathogenic bacteria, it is not metabolized by the liver in the body and is excreted from urine through the kidneys in its original form. Kinetics and safety, currently widely used clinically, especially for the treatment of Gram-negative bacterial infections. Cefuroxime sodium is a national essential drug, and it is also one of the eight cephalosporin varieties that will be used without restriction in the catalog of hierarchical management of antibacterial drug use that will be released in my country in 2011. [0003] Alt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/34C07D501/04A61K31/546A61P31/04
CPCA61K31/546A61P31/04C07D501/04C07D501/34
Inventor 熊毅杨洪朱延亮
Owner SHANGHAI LONGXIANG BIO MEDICINE DEV CO LTD
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