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Sulbenicillin sodium, and preparation method of preparation thereof

A technology of sulfobenicillin sodium and monohydrate, applied in the field of drug synthesis, can solve the problem of less research on hydrate, and achieve the effects of high production efficiency, high purity and good stability

Active Publication Date: 2014-04-09
SUZHOU ERYE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the research on sulbenicillin sodium mainly focuses on its sodium salt, and less research on its hydrate

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The preparation of embodiment 1 sulbenicillin sodium

[0030] (1) Preparation of Sulbenicillin Silane

[0031] Put 132Kg of dichloromethane, 20Kg of 6-APA and 42Kg of BSA into the reaction tank, stir until the solution is clear, continue to react for 1 hour, and cool to -5°C for use. Put 200Kg of dichloromethane and 29.4Kg of triethylamine sulfophenylacetic acid into the reaction tank, cool, put in 9.6Kg of triethylamine, cool down to -3°C, add 11.4Kg of pivaloyl chloride, control the temperature not to exceed 0°C, add After completion, the reaction was continued for 1 hour by keeping below 0°C. Combine the feed liquids, control the reaction temperature from -5°C to 5°C, and react for 1 hour. Concentrate the feed solution to dryness under reduced pressure in a water bath not exceeding 50°C, lower the temperature to below 30°C and put in 64Kg of acetone, concentrate to dryness under reduced pressure according to the above method, lower the temperature to below 30°C, pu...

Embodiment 2

[0039] The preparation of embodiment 2 sulbenicillin sodium monohydrate

[0040]Dissolve 100g of sulfbenicillin sodium in 500mL of water for injection, stir until completely dissolved, and prepare an aqueous solution with a mass concentration of 20%. Sulbenicillin sodium aqueous solution was filtered sequentially with filter paper and a sterilizing microporous membrane, and the filtrate was heated to 65°C, kept at room temperature for 40 minutes, and then filtered through a microporous membrane again to obtain the filtrate. Add 10 g of glucose into the filtrate as a freeze-drying protection agent, fully shake to dissolve the glucose, and filter to remove insoluble matter. Put the above materials into the freeze dryer, turn on the refrigeration, and quickly cool down to -40°C within 1 hour, and the material liquid becomes a block structure. The above block material was heated to -5°C within 3h, and then rapidly cooled to -30°C within 0.5h. Then raise the temperature to -2...

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Abstract

The invention relates to a sulbenicillin sodium monohydrate. The sulbenicillin sodium monohydrate is prepared through a step of dissolving sulbenicillin sodium in water and a step of lyophilizing. A preparation method of the sulbenicillin sodium monohydrate has a high production efficiency, and the sulbenicillin sodium monohydrate has a high purity and a good stability, and is especially suitable for being exploited to form a powder injection.

Description

Technical field [0001] The present invention is a drug synthesis field, which involves sodium sodium sodium and its preparation methods. Background technique [0002] Sulfin sodium sodium is a broad -spectrum semi -gyanicillin antibiotic, which is the symbolic bacteria, genus, enterococci, germine, Salmonella, and Chika bacteria, and other enterophchism bacteria, as well asCopper -green counterp molic bacteria, influenzaessiam, and Naacerobacteria have antibacterial effects.Hemorrhoids, pneumonia, and glycopylase without penicillinase also have antibacterial activity.Insidant bacteria, including digestive splin bacteria and scatterobacteria, also have certain effects.The mechanism of sodium sodium sodium sodium is to play a bactericidal effect by inhibiting the combination of bacterial cell walls. [0003] The chemical name of sodium sulfurin sodium (2S, 5R, 6R) -3, 3-two-based-6- (2-phenyl-2-sulfonium acetyamin) -7-oxygen generation-4-sulfur miscellaneous-1-Nitrogen Miscellaneou...

Claims

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Application Information

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IPC IPC(8): C07D499/62C07D499/16
CPCC07D499/16C07D499/62
Inventor 张健陈学文朱炜
Owner SUZHOU ERYE PHARMA CO LTD
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