Unlock instant, AI-driven research and patent intelligence for your innovation.

Method for preparing cefuroxime-L-arginine hydrate

A technology of cefuroxime acid and cefuroxime, applied in the field of medicine, can solve problems such as instability and easy discoloration, and achieve the effect of improving stability

Active Publication Date: 2012-08-22
南昌立健药业有限公司
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In view of the above-mentioned deficiencies in the prior art, the object of the present invention is to provide a method for preparing a highly stable cefuroxime compound, specifically a method for preparing cefuroxime-L-arginine hydrate. Solving the problems of easy discoloration and instability of the existing cefuroxime sodium salt in the process of production, storage and use

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Method for preparing cefuroxime-L-arginine hydrate
  • Method for preparing cefuroxime-L-arginine hydrate

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0033] Process: Dissolve cefuroxime acid in L-arginine aqueous solution, the molar ratio of cefuroxime acid to L-arginine is 5:1, then add into acetone solution for recrystallization, and finally obtain a pharmaceutical compound containing crystal water.

[0034] Detection:

[0035] 1. Elemental analysis (C 22 h 30 N 8 o 10 S·H 2 O): C 42.81%; H 5.21%; N 18.13%; S 5.15%. (Theory: C 42.85%; H 5.23%; N 18.17%; S 5.20%)

[0036] 2. The water content in the material is 2.8~3.5% (theoretical: 2.9%) measured by Karl Fischer method; the result of thermogravimetric analysis shows that it is characteristic of monohydrate.

[0037] 3. Content analysis (HPLC method): the content of cefuroxime was 75.1%; the yield was 65.2%.

[0038] 4. Place the sample at a high temperature of 60°C for 10 days, and take samples to test the color of the sample and the solution at 5 days and 10 days respectively. The results show that the sample is white at 5 days, and the color of the solution is e...

example 2

[0040] Process: Dissolve cefuroxime acid in L-arginine aqueous solution, the molar ratio of cefuroxime acid to L-arginine is 4:1, then add into acetone solution for recrystallization, and finally obtain a pharmaceutical compound containing crystal water.

[0041] Detection:

[0042] 1. Elemental analysis (C 22 h30 N 8 o 10 S·H 2 O): C 42.83%; H 5.22%; N 18.13%; S 5.17%. (Theory: C 42.85%; H5.23%; N 18.17%; S 5.20%)

[0043] 2. The water content in the material is 2.8~3.5% (theoretical: 2.9%) measured by Karl Fischer method; the result of thermogravimetric analysis shows that it is characteristic of monohydrate.

[0044] 3. Content analysis: (HPLC method) the content of cefuroxime was 75.6%; the yield was 72.3%.

[0045] 4. Place the sample at a high temperature of 60°C for 10 days, and take samples to test the color of the sample and the solution at 5 days and 10 days respectively. The results show that the sample is white at 5 days, and the color of the solution is equi...

example 3

[0047] Process: Dissolve cefuroxime acid in L-arginine aqueous solution, the molar ratio of cefuroxime acid to L-arginine is 3:1, then add into acetone solution for recrystallization, and finally obtain a pharmaceutical compound containing crystal water.

[0048] Detection:

[0049] 1. Elemental analysis (C 22 h 30 N 8 o 10 S·2H 2 O): C 41.54%; H 5.20%; N 17.67%; S 5.03%. (Theory: C 41.64%; H 5.40%; N 17.66%; S 5.05%)

[0050] 2. The moisture content in the substance was measured by Karl Fischer method to be 5.5~6.0% (theory: 5.7%); the result of thermogravimetric analysis showed that it was the characteristic of dihydrate.

[0051] 3. Content analysis: (HPLC method) the content of cefuroxime was 73.6%; the yield was 86.8%.

[0052] 4. Place the sample at a high temperature of 60°C for 10 days, and take samples to test the color of the sample and the solution at 5 days and 10 days respectively. The results show that the sample is white at 5 days, and the color of the so...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention discloses a method for preparing a cefuroxime-L-arginine hydrate. The method comprises: dissolving cefuroxime in an L-arginine aqueous solution, with cefuroxime and the L-arginine added in proportion, then freeze-drying the solution or adding an organic solvent for recrystallization, thus finally obtaining a cefuroxime-L-arginine hydrate containing crystal water. The compound of theinvention includes crystal water able to enhance cefuroxime stability. In the invention, the structural particularity of the compound is utilized to improve the disadvantages of easy discoloring and unstability in production, storage and usage of cefuroxime sodium, and the stability of cefuroxime is improved, so that medical products of high efficiency and stability can be prepared.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a method for preparing a highly stable cefuroxime compound, in particular to a method for preparing cefuroxime-L-arginine hydrate. Background technique [0002] Cefuroxime is a broad-spectrum second-generation cephalosporin, and its mechanism of action is to inhibit the synthesis of bacterial cell walls by binding to bacterial proteins. Cefuroxime has broad antibacterial activity against pathogenic bacteria and is stable to many β-lactamases, especially plasmid-mediated enzymes common in Enterobacteriaceae. Animal experiments in vitro and clinical infection treatment have confirmed that cefuroxime is effective against aerobic Gram-positive bacteria such as Staphylococcus aureus (including β-lactamase-producing bacteria), Streptococcus pneumoniae, and Streptococcus pyogenes, as well as Escherichia coli, influenzae (including β-lactamase producing bacteria), Haemophilus parainfluenzae, Kle...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D501/34C07D501/04C07C279/14C07C277/08
Inventor 杨鹏博宋珊珊张超何成光刘竟飞黄晓军
Owner 南昌立健药业有限公司