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Cefpirome sulfate compound and composition thereof

A technology of cefpirome sulfate and its compound, which is applied in the field of medicine, can solve the problems of insignificant improvement of stability and curative effect, and achieve the effects of improving drug safety, improving stability, and simplifying prescriptions

Inactive Publication Date: 2012-11-28
JIANGXI KANGHUA MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] Above-mentioned two kinds of technical schemes all belong to the refinement of cefpirome sulfate, although its purity can be further improved, the improvement of stability and curative effect is not significant

Method used

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  • Cefpirome sulfate compound and composition thereof
  • Cefpirome sulfate compound and composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Cefpirome sulfate of the present invention is prepared by the following method:

[0051] (1) Dissolve the crude cefpirome sulfate in purified water to form a 0.2 g / ml cefpirome sulfate aqueous solution;

[0052] (2) Add 0.4 times the amount of activated carbon to decolorize the crude product of cefpirome sulfate, filter, and heat the filtrate to 38°C;

[0053] (3) Add the ethanol / isopropanol / acetone mixed solution whose volume is 8 times of the weight of the cefpirome sulfate crude product to the filtrate twice; in the ethanol / isopropanol / acetone mixed solution, ethanol:isopropanol : The amount of acetone is 12:4.5:4.5; for the first time, at a stirring speed of 12rmp, add 1 / 14 ethanol / isopropanol / acetone mixed solution dropwise to the filtrate at a constant speed within 20 minutes, and dropwise at 1°C Cool the filtrate to 12°C at a speed of 1 / min; for the second time, at a stirring speed of 7rmp, add the remaining ethanol / isopropanol / acetone mixed solution to the filt...

Embodiment 2

[0057] (1) Dissolve the crude cefpirome sulfate in purified water to form a 0.02g / ml cefpirome sulfate aqueous solution;

[0058] (2) Add activated carbon of 0.1 times the amount of crude cefpirome sulfate for decolorization, filter, and heat the filtrate to 35°C;

[0059] (3) Add the ethanol / isopropanol / acetone mixed solution whose volume is 4 times the weight of the cefpirome sulfate crude product to the filtrate twice; in the ethanol / isopropanol / acetone mixed solution, ethanol:isopropanol : The amount of acetone is 8:3:3; for the first time, at a stirring speed of 8rmp, add 1 / 16 ethanol / isopropanol / acetone mixed solution dropwise to the filtrate at a constant speed within 5 minutes, and drop it at 0.5°C Cool the filtrate to 10°C at a speed of / min; for the second time, at a stirring speed of 4rmp, add the remaining ethanol / isopropanol / acetone mixed solution to the filtrate at a constant speed for 20 minutes;

[0060] (4) Stop stirring, under the ultrasonic field of 0.05KW,...

Embodiment 3

[0063] (1) Dissolve the crude cefpirome sulfate in purified water to form a 0.3g / ml cefpirome sulfate aqueous solution;

[0064] (2) Add 0.5 times the amount of activated carbon to decolorize the crude product of cefpirome sulfate, filter, and heat the filtrate to 40°C;

[0065] (3) Add an ethanol / isopropanol / acetone mixed solution whose volume is 12 times the weight of the cefpirome sulfate crude product to the filtrate twice; in the ethanol / isopropanol / acetone mixed solution, ethanol:isopropanol : The amount of acetone is 16:6:6; for the first time, at a stirring speed of 16rmp, add 1 / 12 ethanol / isopropanol / acetone mixed solution to the filtrate at a constant speed within 30 minutes, and drop it at the same time at 1.5℃ Cool the filtrate to 15°C at a speed of / min; for the second time, at a stirring speed of 10rmp, add the remaining ethanol / isopropanol / acetone mixed solution to the filtrate at a constant speed for 30 minutes;

[0066] (4) Stop stirring, under the ultrasonic...

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Abstract

The invention relates to a cefpirome sulfate compound and a composition thereof. The cefpirome sulfate compound is measured with a power X-ray diffraction measuring method. The X-ray powder diffraction represented by the diffraction angle of 2theta+ / -0.2 degrees shows characteristic peaks at the angles of 8.92 degrees, 10.55 degrees, 11.12 degrees, 11.98 degrees, 15.23 degrees, 16.80 degrees, 19.59 degrees, 20.88 degrees, 22.40 degrees, 23.32 degrees, 23.54 degrees, 24.11 degrees, 26.52 degrees, 26.88 degrees, 27.47 degrees, 29.18 degrees, 31.76 degrees and 33.76 degrees. The composition contains arginine; the molar ratio of cefpirome sulfate to arginine is 1:1-1:3, and is preferably 1:1.5-1:2; and the arginine is preferably L-arginine. The stability of the cefpirome sulfate compound provided by the invention is enhanced remarkably, the cefpirome sulfate compound does not change easily after standing for a long time, and the administration safety of a patient is enhanced greatly.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a cefpirome sulfate compound and a composition thereof. Background technique [0002] Cefpirome sulfate is the fourth-generation cephalosporin jointly developed by Hoechst Company of Germany and Roussel Company of France. Compared with the first, second, and third-generation cephalosporins, the fourth-generation cephalosporins have a wider antibacterial spectrum, are more stable to β-lactamase, have high blood drug concentrations, and can penetrate the blood-brain barrier. Cefpirome is an excellent new variety among the fourth-generation cephalosporins. It has strong antibacterial effect and wide antibacterial spectrum. Lanella, Pseudomonas) and anaerobic bacteria have a broad antibacterial spectrum and strong bactericidal effect. [0003] Due to the instability of the structure of cefpirome sulfate, it is easy to degrade when it meets water, so it cannot be taken orally, and because it...

Claims

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Application Information

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IPC IPC(8): C07D501/46C07D501/12A61K31/546A61K47/18A61P31/04
Inventor 周晓东
Owner JIANGXI KANGHUA MEDICAL TECH
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