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High efficient preparation method of azlocillin sodium for injection

A technology for azlocillin sodium and injection, which is applied in the directions of medical preparations containing active ingredients, pharmaceutical formulations, active ingredients of heterocyclic compounds, etc., can solve the problems of reducing the medicinal effect of azlocillin sodium, etc. Reduce solvent residue, good buffering effect

Inactive Publication Date: 2017-09-05
SICHUAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

And the preparation technology of existing azlocillin sodium for injection can cause the medicinal effect of azlocillin sodium for injection to reduce

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The efficient preparation method of azlocillin sodium for injection of the present invention comprises the following process steps:

[0021] (1) Azlocillin preparation: add 1 part of ampicillin to 7 parts of pure water, then add sodium carbonate until the ampicillin is completely dissolved;

[0022] (2) Slowly add 0.5 parts of imidazole chloride to the solution obtained in step (1), add dropwise sodium carbonate and / or sodium bicarbonate to adjust the pH of the solution to 7.0, filter, add acetone and / or ethanol to the filtrate, adjust with HCl PH to 3.5, filter;

[0023] (3) The solid obtained in step (2) is first washed with pure water, then washed with acetone or ethanol, and then dried;

[0024] (4) Mix and stir the azlocillin and water for injection prepared in step (3), add dropwise sodium carbonate solution until the azlocillin is completely dissolved, add activated carbon for decolorization, filter, fill, and freeze-dry to obtain azlocillin for injection sodiu...

Embodiment 2

[0026] The efficient preparation method of azlocillin sodium for injection of the present invention comprises the following process steps:

[0027] (1) Azlocillin preparation: add 1 part of ampicillin to 7 parts of pure water, then add sodium carbonate until the ampicillin is completely dissolved;

[0028] (2) Slowly add 0.5 parts of imidazole chloride to the solution obtained in step (1), add dropwise sodium carbonate and / or sodium bicarbonate to adjust the pH of the solution to 6.5, filter, add acetone and / or ethanol to the filtrate, adjust with HCl PH to 2.0, filter;

[0029] (3) The solid obtained in step (2) is first washed with pure water, then washed with acetone or ethanol, and then dried;

[0030] (4) Mix and stir the azlocillin and water for injection prepared in step (3), add dropwise sodium carbonate solution until the azlocillin is completely dissolved, add activated carbon for decolorization, filter, fill, and freeze-dry to obtain azlocillin for injection sodiu...

Embodiment 3

[0032] The efficient preparation method of azlocillin sodium for injection of the present invention comprises the following process steps:

[0033] (1) Azlocillin preparation: add 1 part of ampicillin to 7 parts of pure water, then add sodium carbonate until the ampicillin is completely dissolved;

[0034] (2) Slowly add 0.5 parts of imidazolyl chloride to the solution obtained in step (1), add dropwise sodium carbonate and / or sodium bicarbonate to adjust the pH of the solution to 6.8, filter, add acetone and / or ethanol to the filtrate, adjust with HCl PH to 2.5, filter;

[0035] (3) The solid obtained in step (2) is first washed with pure water, then washed with acetone or ethanol, and then dried;

[0036] (4) Mix and stir the azlocillin and water for injection prepared in step (3), add dropwise sodium carbonate solution until the azlocillin is completely dissolved, add activated carbon for decolorization, filter, fill, and freeze-dry to obtain azlocillin for injection sodi...

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PUM

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Abstract

The invention discloses a high efficient preparation method of azlocillin sodium for injection. According to the preparation method, ampicillin and imidazole acyl chloride carry out condensation reactions in a water phase, then the reaction product is crystallized in an acetone / water, ethanol / water, or acetone / ethanol / water system, then the crystals directly carry out salt forming reactions with sodium carbonate and / or sodium bicarbonate, and the reaction product is freeze-dried to obtain azlocillin sodium. The pharmaceutical effect of azlocillin sodium is effectively improved; and the problem that in a conventional technology, the pharmaceutical effect of azlocillin sodium is reduced is solved.

Description

technical field [0001] The invention relates to the field of medicine preparation, in particular to a high-efficiency preparation method of azlocillin sodium for injection. Background technique [0002] Azlocillin sodium, its chemical name is: (2S, 5R, 6R)-3,3-dimethyl-6-[(R)-2-(2-oxo-1-imidazolidinecarboxamido)- 2-benzacetylamino]-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid sodium salt. [0003] Azlocillin sodium was first developed by Bayer Company of Germany. It went on the market in May 1977. Since the 1980s, it has been used in the United States, Britain and other countries. In 1983, it was included in the supplementary volume of the 20th edition of the US Pharmacopoeia. However, it is recorded that its bactericidal effect on Pseudomonas aeruginosa is about ten times greater than that of carbenicillin, and it also has the effect of ampicillin on Gram-positive bacteria, and it retains the activity of carbenicillin on intestinal bacteria, so from Since the...

Claims

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Application Information

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IPC IPC(8): C07D499/68C07D499/16A61K9/14A61K31/431A61P31/04
CPCC07D499/68A61K9/0019A61K31/431C07D499/16
Inventor 刘焘陈玉红
Owner SICHUAN PHARMA
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