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Cefathiamidine compound

A technology of cefathiamidine and compounds, which is applied in the field of cefathiamidine compounds, can solve problems such as unsatisfactory results, and achieve the effects of low incidence of adverse reactions, low polymer content, and significant antibacterial activity

Active Publication Date: 2015-09-16
SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the above-mentioned documents also improve its stability from aspects such as increasing the content and reducing impurities, and the results are not satisfactory in the investigation of the polymer content.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] [Example 1] Preparation of Cefathiamidine Compound

[0052] 1) Get 10kg of cefathiamidine crude product, add it in 30L mixed solvent A at 35°C, stir and dissolve to obtain the crude product solution, wherein said mixed solvent A is composed of propylene glycol, tetrahydrofuran and water in a volume ratio of 2:1: 5 prepared mixed solvent;

[0053] 2) The crude product solution obtained in step 1) was naturally cooled to room temperature, and then 60 L of ethanol was added to the crude product solution at a speed of 15 L / min under stirring at a speed of 55 r / min to form a turbid solution;

[0054] 3) Adjust the stirring speed to 15r / min, then add 90L of mixed solvent B to the turbid solution obtained in step 2) at a speed of 5L / min, after the addition is completed, cool down to 0°C, and crystals will precipitate out. Mixed solvent B is a mixed solvent prepared from acetone and N-methylpyrrolidone at a volume ratio of 3:1;

[0055] 4) Stand still in an environment with a...

Embodiment 2

[0060] [Example 2] Preparation of Cefathiamidine Compound

[0061] 1) Take 10kg of cefathiamidine crude product, add in 35L mixed solvent A at 45°C, stir and dissolve to obtain the crude product solution, wherein said mixed solvent A is composed of propylene glycol, tetrahydrofuran and water in a volume ratio of 3:1:7 Prepared mixed solvent;

[0062] 2) The crude product solution obtained in step 1) was naturally cooled to room temperature, and then 175 L of ethanol was added to the crude product solution at a speed of 25 L / min under stirring at a speed of 65 r / min to form a turbid solution;

[0063] 3) Adjust the stirring speed to 25r / min, then add 280L of mixed solvent B to the turbid solution obtained in step 2) at a speed of 10L / min, after the addition is completed, cool down to 5°C, and crystals are precipitated. Mixed solvent B is a mixed solvent prepared from acetone and N-methylpyrrolidone at a volume ratio of 8:1;

[0064] 4) Stand still in an environment with a tem...

Embodiment 3

[0068] [Example 3] Preparation of Cefathiamidine Compound

[0069] 1) Take 10kg of cefathiamidine crude product, add it in 32L mixed solvent A at 40°C, stir and dissolve to obtain the crude product solution, wherein said mixed solvent A is composed of propylene glycol, tetrahydrofuran and water in a volume ratio of 2.5:1: 6 mixed solvent prepared;

[0070] 2) The crude product solution obtained in step 1) was naturally cooled to room temperature, and then 96L of ethanol was added to the crude product solution at a rate of 20 L / min under stirring at a speed of 60 r / min to form a turbid solution;

[0071] 3) Adjust the stirring speed to 20r / min, and then add 160L of mixed solvent B to the cloudy solution obtained in step 2) at a speed of 8L / min. Mixed solvent B is a mixed solvent prepared from acetone and N-methylpyrrolidone at a volume ratio of 5:1;

[0072] 4) Stand still in an environment with a temperature of 2° C. for 3 hours, filter, wash the filter cake with absolute et...

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Abstract

The invention belongs to the technical field of medicines, and concretely relates to a cefathiamidine compound. The cefathiamidine compound is a cefathiamidine hydrate, the structure of the cefathiamidine compound is represented by formula (I), and the X-ray powder diffraction pattern of the cefathiamidine compound is represented by figure 1. The cefathiamidine compound is a novel crystal form compound of the cefathiamidine hydrate, and is different from cefathiamidine compounds reported in the prior art. A result of tests shows that the new crystal form compound of the cefathiamidne hydrate has lower content of high-molecular polymers than cefathiamidine in the prior art, and the content of the high-molecular polymers does not obviously increase with the prolongation of the storage time; and the compound has substantial antibiosis activity on Staphylococcus aureus, coagulase negative staphylococci and Enterococcus faecalis.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a cefathiamidine compound. Background technique [0002] Cefathiamidine is a β-lactam antibiotic and belongs to the first generation of cephalosporins for injection. Its chemical name is (6R,7R)-3[(acetyl)methyl]-7-[α-(N,N'-diisopropylamidinothio)-acetylamino]-8-oxo- 5-thia-1-azabicyclo[4,2,0]-oct-2-ene-2-carboxylate betaine, the molecular formula is C 19 h 28 N 4 o 6 S 2 , the structural formula is as follows: [0003] [0004] Cefathiamidine is the first-generation cephalosporin, and its antibacterial spectrum is similar to that of cephalothin. It has a strong effect on Staphylococcus aureus, Streptococcus viridans, and pneumococcus, and has unique antibacterial activity against Enterococcus. It is mainly used for Staphylococcus aureus , Respiratory tract infection caused by pneumococcus and streptococcus, biliary tract infection, urinary tract infection, gynecologic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/28C07D501/12A61K31/545A61P31/04A61K9/19
CPCA61K9/0019A61K9/19C07D501/12C07D501/28
Inventor 李俊广韩后良韩云龙龚红银
Owner SHANDONG LUOXIN PARMACEUTICAL GROUP STOCK CO LTD
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