Cefazolin sodium pentahydrate compound and preparation method and medicine composition thereof

A technology of cefazolin sodium and compound, applied in the field of medicine, can solve problems such as poor stability of cefazolin sodium pentahydrate, and achieve the effects of less impurity content, high safety performance and good storage stability

Inactive Publication Date: 2013-09-11
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

[0005] The stability of cefazolin sodium pentahydrate is relatively poor, and it is more sensitive to high temperature and light, and needs to be kept away from light under low temperature conditions. The prior art...

Method used

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  • Cefazolin sodium pentahydrate compound and preparation method and medicine composition thereof
  • Cefazolin sodium pentahydrate compound and preparation method and medicine composition thereof
  • Cefazolin sodium pentahydrate compound and preparation method and medicine composition thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0038] Preparation of cefazolin sodium pentahydrate compound

[0039] Dissolve cefazolin sodium pentahydrate in N,N-dimethylformamide, slowly add water at 40°C under stirring condition, the volume of said N,N-dimethylformamide is equal to that of cefazolin sodium pentahydrate The mass ratio of N,N-dimethylformamide to water is 1ml:35mg, the volume ratio of N,N-dimethylformamide to water is 3:1, adjust to pH 5.0, stir for 35 minutes to obtain a clear liquid medicine, and move the liquid medicine into the reaction kettle , put it at 130°C for 24 hours, take it out, let it stand, and cool it down to 60°C at a rate of 10°C / min, open the kettle, add ethanol dropwise, and stir, the volume of ethanol is 5 times the volume of the liquid medicine , After the dropwise addition, cool to 0°C, filter, wash twice with ethanol, then wash twice with water, and then dry under reduced pressure for 2h to obtain. Yield 64.4%, HPLC content 99.79%. mp: 238-242°C.

[0040] The X-ray powder diffra...

Embodiment 2

[0042] Preparation of cefazolin sodium pentahydrate compound

[0043]Dissolve cefazolin sodium pentahydrate in N,N-dimethylformamide, slowly add water at 50°C under stirring condition, the volume of said N,N-dimethylformamide is equal to that of cefazolin sodium pentahydrate The mass ratio of N,N-dimethylformamide to water is 1ml:50mg, the volume ratio of N,N-dimethylformamide to water is 2:1, adjust to pH5.5, stir for 25min to obtain a clear liquid, and move the liquid into the reaction kettle , put it at 150°C for 48 hours, take it out, let it stand, and cool it down to 70°C at a rate of 5°C / min, open the kettle, add ethanol dropwise, and stir, the volume of ethanol is 8 times the volume of the liquid medicine , After the dropwise addition, cool to 5°C, filter, wash twice with ethanol, then wash twice with water, and then dry under reduced pressure for 4h to obtain. Yield 65.5%, HPLC content 99.80%. mp: 238-242°C.

[0044] The X-ray powder diffraction pattern obtained by ...

Embodiment 3

[0046] Preparation of Cefazolin Sodium Pentahydrate Sterile Powder Injection

[0047] Weigh 999 g of cefazolin sodium pentahydrate and 1 g of sodium benzoate prepared in Example 1 under aseptic conditions, place them in a solid powder mixer and mix them uniformly, and the raw materials obtained are transferred to a sterile preparation workshop for precision metering and subpackaging, each bottle Contains vinpocetine 0.25g, stoppered and capped, and the finished product is packaged for storage and sent for inspection.

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Abstract

The invention provides a cefazolin sodium pentahydrate compound. The structural formula of the cefazolin sodium pentahydrate compound is shown in the specification, the X-ray powder diffraction pattern of the cefazolin sodium pentahydrate compound measured by means of Cu-Ka ray is shown in Figure 1. The invention also provides a preparation method of the cefazolin sodium pentahydrate compound and a medicine composition containing the cefazolin sodium pentahydrate compound. The preparation of the cefazolin sodium pentahydrate medicine is sterile powder injection. Compared with the prior art, the cefazolin sodium pentahydrate compound and the medicine composition of the cefazolin sodium pentahydrate compound provided by the invention are better in storage stability, and medication safety of a patient is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a cefazolin sodium pentahydrate compound, a preparation method of the cefazolin sodium pentahydrate compound and a pharmaceutical composition containing the cefazolin sodium pentahydrate compound. Background technique [0002] Cefazolin sodium pentahydrate, chemical name: (6R,7R)-3-[[(5-methyl-1,3,4-thiadiazol-2-yl)sulfur]methyl]-7-[ (1H-tetrazol-1-yl)acetamido]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt pentahydrate; molecular formula: C 14 h 13 N 8 NaO 4 S 3 ·5H 2 O; molecular weight: 566.57. [0003] Cefazolin is a first-generation cephalosporin with a broad antibacterial spectrum. The mechanism of action is to bind to the penicillin-binding protein on the cell membrane, acylate the transpeptidase, inhibit the growth of bacteria, and even lyse and die. Except for Enterococcus and methicillin-resistant Staphylococcus, this prod...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/12A61K31/546A61P31/04
Inventor 梁宏平闫晓晔
Owner 四川省惠达药业有限公司
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