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Highly-water-soluble amoxicillin and preparation method thereof

A technology for amoxicillin and amoxicillin crude products, applied in the field of highly water-soluble amoxicillin, can solve the problem of low dissolution rate of amoxicillin, and achieve the effects of fast dissolution rate, high water dissolution rate, and simple and fast operation.

Active Publication Date: 2019-06-11
上海朝瑞化工有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] In order to solve the problem of low dissolution rate of amoxicillin prepared by enzymatic method in the prior art, the present invention provides a preparation method of highly water-soluble enzymatic amoxicillin, and also provides a high Water soluble amoxicillin

Method used

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  • Highly-water-soluble amoxicillin and preparation method thereof
  • Highly-water-soluble amoxicillin and preparation method thereof

Examples

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Embodiment

[0036] Adjust the pH of the crude amoxicillin aqueous solution to 0.8 with 30wt% hydrochloric acid aqueous solution at 25°C to obtain a dissolved aqueous solution of the crude amoxicillin, and pass through a 0.45um filter membrane to remove impurities; ammonia water, directly adjust the pH to 5.5, the temperature of the solution will drop from 24°C to 1°C within 1h during the whole cooling process, filter through a Buchner funnel, wash with water, put in a vacuum drying oven (-0.09MPa), and dry at 40-45°C for 2h , to get amoxicillin finished product.

[0037] Example IV

[0038] Adjust the pH of the crude amoxicillin aqueous solution to 2.2 with 30wt% hydrochloric acid aqueous solution at 30°C to obtain the dissolved crude amoxicillin aqueous solution, and pass through a 0.45um filter membrane to remove impurities; ammonia water, directly adjust the pH to 6.0, the temperature of the solution will drop from 27°C to 5°C within 1.5h during the whole cooling process, filter throu...

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Abstract

The invention provides a highly-water-soluble amoxicillin and a preparation method thereof. The preparation method comprises the following steps: adding an acidic solution into an aqueous solution ofcrude amoxicillin prepared by an enzymatic method, and performing dissolved clarification to obtain a dissolved-clarified aqueous solution of the crude amoxicillin; performing cooling on the dissolved-clarified aqueous solution of the crude amoxicillin from 18-30 DEG C to 0-5 DEG C within 0.5-1.5 h, and adjusting the pH to 5-6 in the cooling process; and when the temperature is reduced to 0-5 DEGC, performing filtration, and performing washing by using water. The highly-water-soluble amoxicillin provided by the invention has the characteristic of a rapid dissolution speed in water.

Description

technical field [0001] The invention relates to the technical field of crystallization technology of amoxicillin, in particular to a preparation method capable of obtaining highly water-soluble amoxicillin and the obtained highly water-soluble amoxicillin. Background technique [0002] Amoxicillin, molecular formula C 16 h 19 N 3 o 5 S·3H 2 O, the structural formula is as follows: [0003] [0004] Amoxicillin, also known as amoxicillin, mainly appears in preparations in the form of trihydrate. The main use of amoxicillin is as a broad-spectrum penicillin antibiotic for the treatment of Gram-negative and positive bacteria. [0005] A traditional way to obtain amoxicillin is: it is produced from penicillin V or penicillin G through a series of complex chemical transformation processes, which use solvents including but not limited to dichloromethane, butyl acetate, isopropanol, etc. , and chemicals including but not limited to triethylamine and pivalic acid. Therefo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/68C07D499/18
Inventor 许红磊
Owner 上海朝瑞化工有限公司
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