A kind of preparation method of amoxicillin sodium

A technology of amoxicillin sodium and amoxicillin, applied in the field of drug synthesis, can solve the problems of unfavorable labor protection and environmental protection, complex solvent system, strong toxic and side effects, etc., and achieves improved dissolution rate, reduced residual content, and small toxic and side effects. Effect

Inactive Publication Date: 2011-12-07
HARBIN PHARMA GRP CO LTD GENERAL PHARMA FACTORY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method has made a great leap in product quality compared with the freeze-drying method and the spray-drying method, it also has the disadvantages of complex solvent system, high cost, strong toxic and side effects, and is not conducive to labor protection and environmental protection.
[0004] Chinese patents 00100579.0 and 02100123.5 respectively disclose methods for preparing amoxicillin sodium from three substances and five substances, which are costly and complicated

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] (1) Preparation of acid anhydride: In dichloromethane, add hydroxydung salt, then add dimethylacetamide, pyridine and 1 / 3 pivalic acid, keep the temperature at -20°C, add pivaloyl chloride, keep the temperature and stir Make the hydroxydung salt dissolve clear for later use; add 2 / 3 special acid, the proportion of parts by weight of the components is: 3 parts of dichloromethane, 1 part of hydroxydung salt, 1 part of dimethylacetamide, 1 part of pyridine , 3 parts of pivalic acid, 3 parts of pivaloyl chloride;

[0024] (2) Preparation of 6-APA solution: Dissolve 6-APA in dichloromethane, stir at room temperature, add 1 / 2 triethylamine and purified water, cool to 0°C, add 1 / 2 triethylamine, wait for 6 -After the APA is completely dissolved, it is cooled for later use; the weight ratio of the components is: 1 part of 6-APA, 1 part of dichloromethane, 1 part of triethylamine, and 1 part of purified water;

[0025] (3) Condensation: transfer the 6-APA salt solution into the...

Embodiment 2

[0030] (1) Preparation of amoxicillin solution, in absolute ethanol, add the amoxicillin prepared in Example 1, then add diisopropylamine, keep the temperature at 10-15° C., amoxicillin is completely dissolved, add gac, and Carbon-removal filtration and sterilization filtration, and the pipeline through which the reaction liquid passes during the filtration is rinsed with absolute ethanol, and the filtrate and washing liquid are combined; the specific weight ratio is: 1 part of amoxicillin, 4 parts of absolute ethanol, diiso Propylamine 0.5 part;

[0031] (2) Preparation of sodium isooctanoate absolute ethanol solution: Add sodium isooctanoate to absolute ethanol to dissolve it completely, keep the temperature at 10-15°C, add activated carbon, filter through carbon removal and sterilize, and use anhydrous The pipeline through which the reaction liquid passes through ethanol flushing and filtration, and the filtrate and washing liquid are combined; the specific weight ratio is:...

Embodiment 3

[0034] (1) Preparation of amoxicillin solution, in absolute ethanol, add the amoxicillin prepared in Example 1, then add diisopropylamine, keep the temperature at 10-15° C., amoxicillin is completely dissolved, add gac, and Carbon-removal filtration and sterilization filtration, and the pipeline through which the reaction liquid passes through the filter is rinsed with absolute ethanol, and the filtrate and washing liquid are combined; the specific weight ratio is: 1 part of amoxicillin, 6 parts of absolute ethanol, diiso 0.3 parts of propylamine;

[0035] (2) Preparation of sodium isooctanoate absolute ethanol solution: Add sodium isooctanoate to absolute ethanol to dissolve it completely, keep the temperature at 10-15°C, add activated carbon, filter through carbon removal and sterilize, and use anhydrous The pipeline through which the reaction liquid passes through ethanol washing and filtration, and the filtrate and washing liquid are combined; the specific weight ratio is:...

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PUM

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Abstract

The present invention relates to the field of drug synthesis, in particular to a method for preparing amoxicillin sodium. The method of the present invention comprises the following steps: (1) preparation of acid anhydride; (2) preparation of 6-APA solution; (3) condensation: Move the 6-APA salt solution into the mixed acid anhydride reaction bottle, and time it for 3 hours; (4) Hydrolysis: add the condensation solution of step (3) to the hydrolyzed solution; (5) Crystallization: Leave the crystal to grow for 1 hour and then stir to grow the crystal for 1 hour (6) Suction drying: wash with water first, then wash with acetone, and dry in vacuum at 40° C. for 3 hours to obtain amoxicillin.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a production method of antibacterial drug amoxicillin sodium. Background technique [0002] Amoxicillin sodium is a broad-spectrum penicillin antibiotic known to be clinically widely used, and it has a strong and rapid killing effect on both Gram-negative bacteria and positive bacteria. [0003] There are currently three main production methods for amoxicillin sodium, one is freeze-drying, the other is spray-drying, and the other is solvent crystallization. The first two methods have great deficiencies in product quality, the content of the product is low, and the content of related substances is relatively high, which is prone to allergic reactions in clinical application. At the same time, due to rapid crystallization and small crystal form, it is easy to degrade rapidly during storage, which reduces its curative effect. The solvent crystallization method makes up for the shortc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/68C07D499/16
Inventor 赵玉新白铁忠姚远韩东胜黄宇红尹丽温海波魏莉徐丹李国峰
Owner HARBIN PHARMA GRP CO LTD GENERAL PHARMA FACTORY
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