Preparation method of benzathine benzylpenicillin V

A technology of benzathine penicillin and penicillin V, which is applied in the field of compound preparation, can solve the problems of unsatisfactory industrial production and clean production, failure to achieve good results, poor product quality and yield, etc., so as to facilitate practical operation and control , Controllable crystal growth rate, reduce the difficulty of separation and washing

Active Publication Date: 2017-06-23
NORTH CHINA PHARM GRP SEMISYNTECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] At present, relevant patents and literature reports on the production and preparation methods of benzathine penicillin V have not yet been seen.
And when using the disclosed preparation method of benzathine penicillin G (publication number is 101357926A) to produce benzathine penicillin V, because the method uses the difference of raw materials, and the difference of final product physicochemical property, can not reach good effect, product quality And the yield is not good enough to meet the needs of industrialized production and clean production. New explorations and improvements are needed in process routes, technical methods and process parameters.

Method used

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  • Preparation method of benzathine benzylpenicillin V
  • Preparation method of benzathine benzylpenicillin V
  • Preparation method of benzathine benzylpenicillin V

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preparation example Construction

[0042] The preparation method of benzathine penicillin V of the present invention, concrete implementation steps are as follows:

[0043] (a) Preparation of reaction solution

[0044] At room temperature, add penicillin V salt into an organic solvent with a concentration range of 50-95%, and prepare a solution A with a mass volume ratio of 1:5-15;

[0045] Add N,N'-dibenzylethylenediaminediacetic acid into an organic solvent with a concentration range of 50-95%, and prepare a B solution with a mass-volume ratio of 1:5-15;

[0046] Water by volume: the amount of organic solvent (50~95%)=1:0.5~10 is configured into reaction solvent C; The volume of reaction solvent C is 0.5~20 times of total volume of A solution and B solution;

[0047] When the ratio of the amount of penicillin V salt to N,N'-dibenzylethylenediaminediacetic acid is about 2:1, the reaction can be more complete, and the double-flow operation is more convenient when the volumes of solution A and solution B are th...

Embodiment 1

[0055] (a) Preparation of reaction solution: at room temperature, add 10kg of penicillin V sodium crude drug into 50L of 50% ethanol solution to make penicillin V potassium ethanol solution, i.e. A solution; Benzyl ethylenediamine diacetic acid is added to 50L of ethanol solution with a concentration of 50% to make N, N'-dibenzyl ethylenediamine diacetic acid ethanol solution, i.e. solution B; by volume ratio water: ethanol solution (50% )=1:0.5 amount configuration 500L reaction solvent C;

[0056] (b) Pre-reaction: Take 2% of the respective total amounts of the A solution and the B solution and add it to the reaction solvent C at the same time, stir at a speed of 100 rpm until the crystals appear, and then grow the crystals for 10 minutes;

[0057] (c) Final reaction: After the crystal growth is completed, the remaining A solution and B solution are simultaneously added to the reaction solvent C after the pre-reaction within 1 hour, and then fully reacted for 1 hour at the s...

Embodiment 2

[0060] (a) Preparation of reaction solution: at room temperature, add 12kg of penicillin V potassium crude drug into 60L of 80% methanol solution to make penicillin V potassium methanol solution, namely A solution; Benzyl ethylenediamine diacetic acid is added into 50L of 70% ethanol solution to make N, N'-dibenzyl ethylenediamine diacetic acid ethanol solution, i.e. solution B; by volume ratio water: ethanol solution (concentration 60 %)=1:4 amount configuration 550L reaction solvent C;

[0061] (b) Pre-reaction: Take 2% of the respective total amounts of the A solution and the B solution and add it to the reaction solvent C at the same time, stir at a speed of 100 rpm until the crystals appear, and then grow the crystals for 10 minutes;

[0062] (c) Final reaction: After the crystal growth is completed, the remaining A solution and B solution are simultaneously added to the reaction solvent C after the pre-reaction within 1 hour, and then fully reacted for 1 hour at the same...

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Abstract

The invention discloses a preparation method of benzathine benzylpenicillin V, and belongs to the field of production of semi-synthetic antibiotics. The preparation method comprises the following steps of preparing of reaction liquid, pre-reacting, final reacting, and purifying, wherein the reaction liquid is prepared from a benzylpenicillin V salt solution prepared by an organic solvent, an N,N'-dibenzyl ethylenediamine diacetate solution and a reaction solvent. The preparation method has the advantages that the crystal form and crystal granularity of a product are more controllable, the yield rate and quality of the product are effectively improved, the operation is simple, and the preparation method is suitable for industrialized production.

Description

technical field [0001] The invention relates to a preparation method of a compound, specifically a preparation method of benzathine penicillin V, which belongs to the production and preparation process of semi-synthetic antibiotics. Background technique [0002] In a broad sense, penicillin refers to a class of antibiotics that contain penicillanic acid in the molecule, which can destroy the cell wall of bacteria and play a bactericidal role during the reproduction period of bacterial cells. It can be divided into natural penicillins and semi-synthetic penicillins. Semi-synthetic penicillin uses penicillanic acid as the parent in the molecular structure, and changes the side chain so that it can overcome many defects of natural penicillins, such as being not resistant to acid and alkali and enzymes. [0003] The benzathine penicillin V involved in the present invention belongs to the semi-synthetic penicillin. The chemical name of benzathine penicillin V is (2S,5R,6R)-3,3-d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/60A61P31/04
CPCC07B2200/13C07D499/60
Inventor 左丽华严正人刘欣刘慧勤王欣黄娟
Owner NORTH CHINA PHARM GRP SEMISYNTECH CO LTD
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