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A kind of preparation method of sulfbenicillin sodium and preparation thereof

A technology of sulbenicillin sodium and monohydrate, which is applied in the field of drug synthesis, can solve the problems of less research on hydrates, and achieve the effects of high production efficiency, high product purity and good stability

Active Publication Date: 2014-10-08
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 again with a microporous membrane 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 -20°C wit...

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PUM

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Abstract

The invention relates to a sulfbenicillin sodium monohydrate, which is prepared by dissolving sulfbenicillin sodium in water and then freeze-drying. The method has high production efficiency, and the obtained sulfbenicillin sodium monohydrate has high purity and good stability, and is very suitable for being developed into a powder injection preparation.

Description

technical field [0001] The invention belongs to the field of drug synthesis, in particular to sulfbenicillin sodium monohydrate and a preparation method thereof. Background technique [0002] Sulbenicillin sodium is a broad-spectrum semi-synthetic penicillin antibiotic, which is effective against Enterobacteriaceae bacteria such as Escherichia coli, Proteus, Enterobacter, Citrobacter, Salmonella and Shigella, and Pseudomonas aeruginosa, Haemophilus influenzae, Neisseria and other Gram-negative bacteria have antibacterial effect. It also has antibacterial activity against hemolytic Streptococcus, Streptococcus pneumoniae and non-penicillinase-producing Staphylococcus. It also has a certain effect on anaerobic bacteria including Peptostreptococcus and Clostridium. The mechanism of action of sulbenicillin sodium is to play a bactericidal effect by inhibiting the synthesis of bacterial cell walls. [0003] The chemical name of sulfbenicillin sodium is (2S,5R,6R)-3,3-dimethyl-...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D499/62C07D499/16
CPCC07D499/16C07D499/62
Inventor 张健陈学文朱炜
Owner SUZHOU ERYE PHARMA CO LTD