Method for preparing tardocillin

Abstract

The invention discloses a preparing method of benzathine penicillin which comprises the following procedures: a, 50 percent to 75 percent of ethanol is added to a raw medicine of the N, N-dibenzyl ethylenediamine diacetate, and is prepared into solvent A; b, 50 percent to 75 percent of ethanol is added to the raw medicine of penicillin G salt, and is prepared into solvent B; c, the pre-applied solvent A is added to the solvent B for stirring, then the residual solvent A is added to the solvent B, thus obtaining nzathine benzylpenicillin suspension; d, filtering and then washing and drying are carried out on the nzathine benzylpenicillin suspension. The method has the advantages of improving yield coefficient of products, purity quotient and the controllability of particle size, reducing the toxicity of the residual solvent, improving the quality and safety of products and avoiding the harm of methanol to environment and human body at the same time.

Description

technical field [0001] The invention relates to a production and preparation method of pharmaceutical raw materials, in particular to a production and preparation method of benzathine penicillin. Background technique [0002] Benzathine penicillin, also known as long-acting penicillin, its English name is BenzathineBenzylpenicillin, its chemical name is (2S, 5R, 6R)-3,3-dimethyl-6-(2-phenylacetamido)-7-oxo-4 -Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid N,N'-dibenzyldiethylamine salt tetrahydrate. In 1950, the United States patent (US 2627491) disclosed the synthesis method of this compound for the first time. There are two kinds of processing routes for producing benzathine penicillin at present, and a kind of is the synthetic processing route of using water as solvent, is about to add N,N-dibenzylethylenediamine diacetate (hereinafter referred to as DBED) into appropriate amount of water and be mixed with solution A , Add penicillin G sodium to an appropriate amount...

AI Technical Summary

Problems solved by technology

Above-mentioned first kind of synthetic technique, its used solvent is nontoxic and harmless, but this method has the disadvantages that the reaction speed is difficult to control, the crystal particle size of the product is small, the loss when carrying out solid-liquid separation and washing and refining is large, and the product yield is low; Two kinds of synthetic techniques, although the yield of product, purity are improved relatively, and product particle size is controlled, but its effect is still not ideal enough

In particular, the controllable range of product granularity is narrow, and it is difficult to meet the needs of users for various granularities.

In order to solve this problem, the effective control of product particle size can only be achieved by increasing the amount of methanol or repeated grinding.

This greatly increases the manufacturing cost of the product

Furthermore, since methanol is a toxic solvent, the residual methanol in the final product not only has potential adverse effects on patients, but also causes great harm to operators and the ecological environment in the production process.

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