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A kind of highly water-soluble amoxicillin and preparation method thereof

A technology for amoxicillin and crude amoxicillin, applied in the field of highly water-soluble amoxicillin, can solve the problem of low amoxicillin dissolution rate, and achieve the effects of fast dissolution rate, small crystal particle size and high dissolution rate

Active Publication Date: 2021-08-17
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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  • A kind of highly water-soluble amoxicillin and preparation method thereof
  • A kind of highly water-soluble amoxicillin and preparation method thereof

Examples

Experimental program
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Effect test

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 to the aqueous solution of the crude amoxicillin prepared by an enzymatic method for dissolving to obtain the crude amoxicillin Aqueous solution; the dissolved crude amoxicillin aqueous solution is reduced from 18-30°C to 0-5°C within 0.5-1.5 hours, and the pH is adjusted to 5-6 during the cooling process; when the temperature drops to 0-5°C , filtered and washed with water. The highly water-soluble amoxicillin provided by the invention has the characteristics of fast dissolution rate 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 Patents(China)
IPC IPC(8): C07D499/68C07D499/18
Inventor 许红磊
Owner 上海朝瑞化工有限公司