Cefazolin sodium compound and aseptic powder injection thereof

A technology of cefazolin sodium and sterile powder injection, applied in the field of medicine, can solve the problems of cefazolin sodium pentahydrate easily hygroscopic, no solution proposed, long reaction time, etc., and achieves improved hygroscopicity and simple preparation method , the effect of low hygroscopicity

Active Publication Date: 2014-08-06
YOUCARE PHARMA GROUP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This invention has the following problems: 1) the reaction time is long; 2) the particle size of the product obtained is small, and practice has proved that the average particle size of the product obtained in the above-mentioned embodiment in the method is about 15 microns; 3) the chelate obtained in the above-mentioned embodiment in the method Cefazolin sodium crystals are monoclinic crystals with space group P21
[0008] However, the cefazolin pentahydrate prepared by the method of the prior art is easy to get wet, so that there are certain problems in storage
However, the prior art does not propose a corresponding solution

Method used

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  • Cefazolin sodium compound and aseptic powder injection thereof
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  • Cefazolin sodium compound and aseptic powder injection thereof

Examples

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Effect test

Embodiment 1

[0035] [embodiment 1] the preparation of cefazolin sodium compound

[0036]Get cefazolin sodium bulk drug 50g, add ethanol, wherein the consumption ratio of cefazolin sodium bulk drug and ethanol is 1g: 6ml, heat and reflux until cefazolin sodium dissolves completely, obtain solution; Stop heating then, in gained solution In the horizontal direction of the liquid surface, the applied magnetic field intensity is in the constant magnetic field of 0.4T, and under the condition of the constant magnetic field, the mixed solvent of acetone, chloroform and N, N-dimethylformamide is added dropwise to the solution, wherein The volume ratio of the mixed solvent to ethanol is 3:1, and the volume ratio of acetone, chloroform and N,N-dimethylformamide in the mixed solvent is 2:3:1; After standing still for 6 hours, a white crystalline powder was obtained, which was filtered, the filter cake was washed with ethanol, and vacuum-dried for 2 hours to obtain the cefazolin sodium compound.

[0...

Embodiment 2

[0038] [embodiment 2] the preparation of cefazolin sodium compound

[0039] Get cefazolin sodium bulk drug 50g, add ethanol, wherein the consumption ratio of cefazolin sodium bulk drug and ethanol is 1g: 8ml, heat and reflux until cefazolin sodium dissolves completely, obtain solution; Stop heating then, in the gained solution In the horizontal direction of the liquid surface, the applied magnetic field intensity is in the constant magnetic field of 1.2T, and under the condition of the constant magnetic field, the mixed solvent of acetone, chloroform and N, N-dimethylformamide is added dropwise to the solution, wherein The volume ratio of the mixed solvent to ethanol is 5:1, and the volume ratio of acetone, chloroform and N,N-dimethylformamide in the mixed solvent is 4:5:1; After standing still for 10 hours, a white crystalline powder was obtained, which was filtered, the filter cake was washed with ethanol, and vacuum-dried for 4 hours to obtain the cefazolin sodium compound....

Embodiment 3

[0041] [embodiment 3] the preparation of cefazolin sodium compound

[0042] Get cefazolin sodium bulk drug 50g, add ethanol, wherein the consumption ratio of cefazolin sodium bulk drug and ethanol is 1g: 7ml, heat and reflux until cefazolin sodium dissolves completely, obtain solution; Stop heating then, in the gained solution In the horizontal direction of the liquid surface, the applied magnetic field intensity is in the constant magnetic field of 0.8T, and under the condition of this constant magnetic field, the mixed solvent of acetone, chloroform and N, N-dimethylformamide is added dropwise in the solution, wherein The volume ratio of the mixed solvent to ethanol is 4:1, and the volume ratio of acetone, chloroform and N,N-dimethylformamide in the mixed solvent is 2:5:1; After standing still for 8 hours, the obtained white crystalline powder was filtered, the filter cake was washed with ethanol, and vacuum-dried for 3 hours to obtain the cefazolin sodium compound.

[0043...

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Abstract

The invention belongs to the technical field of medicine, and in particular relates to a cefazolin sodium compound and an aseptic powder injection thereof. The structural formula of the cefazolin sodium compound is as shown in Formula (I); the compound is measured by a powder X-ray diffraction measurement method; and the X-ray powder diffraction diagram represented by a diffraction angle of 2 theta +/- 0.2 degrees is as shown in Fig . 1. The cefazolin sodium provided by the invention has a relatively low hygroscopicity; and the clinical effect and the bacteriological effect of the aseptic powder injection prepared from the cefazolin sodium provided by the invention are significantly better than those of the prior art. (the formula is shown in the specification).

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a cefazolin sodium compound and its sterile powder injection. 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 sodium is the first-generation broad-spectrum cephalosporin antibiotic. Except Enterococcus and methicillin-resistant Staphylococcus, this product has good antibacterial activity against other Gram-positive cocci. Streptococcus pneumoniae and hemolytic streptococcus Highly sensitive to this product. Diphtheria, Bacillus anthracis, Listeria and Clostridium are also very sensitive to this product. This product has good antibacterial activity against some...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/12A61K31/546A61K9/14A61P31/04
CPCC07D501/12C07D501/36
Inventor 李琦杨磊
Owner YOUCARE PHARMA GROUP
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