Mezlocillin sodium compound as well as preparation method and pharmaceutical composition thereof

A technology of mezlocillin sodium and compound, applied in the field of medicine, can solve the problems of slow dissolution rate and poor fluidity, and achieve the effects of fast dissolution rate, good fluidity and convenient compatibility

Inactive Publication Date: 2013-09-04
四川省惠达药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The mezlocillin sodium in the prior art has a slow dissolution rate and poor fluidity. In order to obtain a more excellent mezlocillin sodium compound, the present invention is specially proposed

Method used

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  • Mezlocillin sodium compound as well as preparation method and pharmaceutical composition thereof
  • Mezlocillin sodium compound as well as preparation method and pharmaceutical composition thereof
  • Mezlocillin sodium compound as well as preparation method and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] The preparation method of mezlocillin sodium compound:

[0047] N,N-dimethylformamide and methanol are formulated into a mixed solvent at a volume ratio of 2:1, the raw material drug of mezlocillin sodium is taken, and the mixed solvent of N,N-dimethylformamide and methanol is added, and the The ratio of the volume of the mixed solvent to the mass of mezlocillin sodium is 5ml: 1g, stir, adjust the pH of the solution to 6.5, add activated carbon for decolorization, the amount of added activated carbon is 0.2% g / ml of the total volume of the medicinal solution, stir After 30 minutes, filter to obtain a clear solution. Move the clear solution into a reaction kettle, place it in a 100°C oven for 48h, cool down to 70°C at a rate of 5°C / h, open the kettle, stir slowly and add ether dropwise. The stirring rate was 15 rpm, the amount of diethyl ether was 5 times that of the mixed solvent, the temperature was lowered to 0°C, filtered, washed 3 times with diethyl ether, and then ...

Embodiment 2

[0050] The preparation method of mezlocillin sodium compound:

[0051] N,N-dimethylformamide and methanol are formulated into a mixed solvent at a volume ratio of 3:1, and the raw material drug of mezlocillin sodium is taken, and the mixed solvent of N,N-dimethylformamide and methanol is added, and the The ratio of the volume of the mixed solvent to the mass of mezlocillin sodium is 8ml: 1g, stir, adjust the pH of the solution to 5.5, add activated carbon for decolorization, the amount of added activated carbon is 0.3% g / ml of the total volume of the medicinal solution, stir After 25 minutes, filter to obtain a clear solution. Move the clear solution into a reaction kettle, place it in a 120°C oven for 12h, cool down to 60°C at a rate of 10°C / h, open the kettle, stir slowly and add ether dropwise. The stirring rate was 8rpm, the amount of diethyl ether was 3 times that of the mixed solvent, the temperature was lowered to 5°C, filtered, washed 3 times with diethyl ether, and th...

Embodiment 3

[0054] Preparation of mezlocillin sodium sterile powder injection:

[0055] Weigh 99.5 g of mezlocillin sodium and 0.5 g of sodium benzoate prepared in Example 1 under aseptic conditions, place them in a solid powder mixer and mix them evenly, and the raw materials obtained are transferred to the aseptic preparation workshop for precise metering and subpackaging, each bottle Containing 1.5g of mezlocillin sodium, stoppered and capped, the finished product is packaged for storage and sent for inspection.

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a mezlocillin sodium compound. The structural formula of the mezlocillin sodium compound is as follows: with the adoption of Cu-K alpha ray measurement, the mezlocillin sodium compound obtains an X-ray powder diffraction spectrogram as shown in figure 1. The invention further provides a preparation method of the mezlocillin sodium compound, a pharmaceutical composition containing the mezlocillin sodium compound and a preparation method of the mezlocillin sodium compound. The dosage form of a mezlocillin sodium drug is a sterile powdered injection and a freeze-dried powder injection. The mezlocillin sodium compound is high in dissolution rate and good in fluidity, thereby facilitating subpackage and improvement on accuracy of packaging quantity.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a mezlocillin sodium compound, a preparation method thereof, a pharmaceutical composition containing the mezlocillin sodium compound and a preparation method of the pharmaceutical composition. Background technique [0002] Mezlocillin sodium, English name Mezloeillin Sodium, molecular formula C 21 h 24 N 5 NaO 8 S 2 , CAS No. 59798-30-0, chemical name 3,3-dimethyl-6-[(R)-2-[3-(methylsulfonyl)-2-oxo-1-imidazolidinecarboxamido] -Sodium 2-phenylacetamido]-7-oxo-4-thia-1-azabicyclo[3.2.0]-heptane-2-carboxylate. [0003] Mezlocillin sodium was discovered in 1968 by the Bayer Company of the Federal Republic of Germany in the study of ampicillin a-aminophthalated derivatives. It was first listed in the Federal Republic of Germany in 1977. In 1981, the US FDA officially approved the drug to be launched in the United States. Since the 1980s, it has been listed in the Un...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/68C07D499/16A61K31/431
Inventor 闫晓晔
Owner 四川省惠达药业有限公司
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