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Cefuroxime axetil tablet composition and preparation method thereof

A technology of furoctyl tablets and furoctyl tablets, which is applied in pill delivery, organic chemistry, antibacterial drugs, etc., can solve the problems of content decrease and impurity increase, and achieve quality improvement, increase purity, and simplify the production process Effect

Inactive Publication Date: 2019-06-14
陕西卓力时代人力资源有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Cefepime is a thermally unstable and highly water-soluble neutral internal salt. Cefepime has carboxyl negative ions, which combine with protons in the aqueous solution to promote the ionization balance of water to generate more alkaline ions and make the solution It is weakly alkaline, but it is prone to degradation and ring-opening reactions under weakly alkaline conditions, resulting in a decrease in content and an increase in impurities

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] At room temperature, mix 500ml of water, 600ml of dimethylformamide and 1200ml of isopropanol evenly, add 150g of 7-MPCA and 200g of AE-active ester under effective stirring to form a fluid slurry system; drop 20% Sodium hydroxide until the pH of the solution system is between 5.5 and 6.5, react at 20°C for 4h; continuously extract three times with 3000ml of dichloromethane, and distill the water phase under reduced pressure at room temperature at 20°C to 25°C for 1.5h; then add 6mol / L of Adjust the pH value to 0.5-1.0 with hydrochloric acid, then add 2.5 L of acetone, stir for 2 hours, crystallize to obtain cefuroxime axetil tablets, filter with suction, wash the filter cake with acetone and dry for 1 hour to obtain 210 g of cefuroxime axetil tablets, which are detected by HPLC The purity is 99.5%.

Embodiment 2

[0027] Put 140g of 7-MPCA and 180g of AE-active ester in a mixed solvent of 1500ml of dimethylacetamide and 500ml of water, stir and homogenize; adjust the pH to 6.0-7.5 with triethylamine, and react at 15°C for 3h; add 2500ml Dichloromethane was extracted twice, and the water phase was distilled under reduced pressure at 10-20°C for 1.2h; then 6mol / L hydrochloric acid was added to control the pH value to 1.0-1.6, 2.6L acetone was added, stirred for 2.5h, and crystallized to obtain cephalosporin Fuocetin axetil tablets were suction filtered, and the filter cake was washed with acetone and dried for 1 h to obtain 295 g of cefepime hydrochloride, with a purity of 99.7% as determined by HPLC.

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PUM

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Abstract

The invention belongs to the field of medical intermediates, in particular to a cefuroxime axetil tablet composition and a preparation method thereof. The preparation method comprises the following steps: adding (6R,7R)-7-[2-(2-amino-4-thiazolyl)-2-(methoxyimino)acetylamino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid and AE-active esterinto a mixed solvent of water and a water-soluble organic solvent; adjusting the pH value to 5.5-7.5, and carrying out acylation reaction under the condition of heat preservation; conducting extracting after the reaction is finished, and recovering an organic phase through reduced pressure distillation; and adjusting the pH value of a water phase by using hydrochloric acid, and conducting crystallizing to prepare a cefuroxime axetil tablet. The method is mild in reaction, is an acidic and slightly neutral environment, has less influence on cefepime, is easy to control, reduces the probabilityof degradation and ring opening of cefuroxime axetil, increases the purity of a final product, improves the yield of cefepime, improves the quality of cefepime, and has an HPLC detection purity of higher than 99.5%.

Description

technical field [0001] The invention belongs to the field of pharmaceutical intermediates, in particular to a cefuroxime axetil tablet composition and a preparation method thereof. Background technique [0002] Cefmenoxime, also known as cefmenoxime (cefmenoxime), is nearly white or nearly yellow crystalline powder, also known as "cefotaxime tetrazole", "cefotaxime", "cefotaxime cephalosporin", "ammonium cephalosporin" Furoxetate Pitomycin "" Besterke" or "CMX" is a third-generation cephalosporin and belongs to semi-prepared antibiotics. The chemical formula is C16H17N9O5S3, the molecular weight is 511.55800, easily soluble in dimethyl sulfoxide, hardly soluble in water or methanol, almost insoluble in ethanol or acetone. Cephalosporins are broad-spectrum antibiotics with strong activity against Gram-negative bacteria and are stable against β-lactamase, and must be administered by injection. It is clinically used for respiratory tract infection, urinary tract infection, fe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/34C07D501/06C07D501/12A61K31/546A61K9/20A61P31/04
Inventor 程淑清牛清玲
Owner 陕西卓力时代人力资源有限公司
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