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Method for preparing medicine ceftibuten crystal compound for treating surgical infection

A crystalline compound, the technology of cefbutene, applied in the field of medicine, can solve the problems of impurities, high polymer content, poor stability, etc., and achieve the effects of low polymer content, good stability and good clarity

Inactive Publication Date: 2017-02-22
临沂草之美医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The pharmaceutically acceptable excipients that can be used in the preparation of the present invention can include disintegrants, glidants, lubricants and binders. The capsules made by it have a higher dissolution rate, but it is found that the impurities , high polymer content, and poor stability

Method used

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  • Method for preparing medicine ceftibuten crystal compound for treating surgical infection
  • Method for preparing medicine ceftibuten crystal compound for treating surgical infection
  • Method for preparing medicine ceftibuten crystal compound for treating surgical infection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] The preparation of embodiment 1 ceftibuten crystal compound

[0041] 1) Prepare mixed solution A by mixing dimethylformamide and water at a volume ratio of 4:1;

[0042] 2) Take the ceftibuten raw material, add the mixed solution A prepared in step 1), wherein the ratio of the volume of the mixed solution A to the mass of ceftibuten is 8ml:1g, stir to dissolve it all and pour it into the obtained solution Add activated carbon for decolorization and filtration to obtain a clear solution;

[0043] 3) Prepare mixed solution B with isopropyl ether and isopropanol at a volume ratio of 3.5:1;

[0044] 4) At room temperature, add mixed solution B to the clear solution obtained in step 2) under an ultrasonic field with a power of 0.5KW, wherein the volume of mixed solution B is 6 times the volume of mixed solution A, and turn off the ultrasonic field after adding. The temperature was lowered to 3° C. and allowed to stand for 2 hours to precipitate crystals, which were then dr...

Embodiment 2

[0048] The preparation of embodiment 2 ceftibuten crystal compound

[0049] 1) Prepare mixed solution A by mixing dimethylformamide and water at a volume ratio of 4:1;

[0050] 2) Take the ceftibuten raw material, add the mixed solution A prepared in step 1), wherein the ratio of the volume of the mixed solution A to the mass of ceftibuten is 9ml:1g, stir to dissolve it all, and pour it into the obtained solution Add activated carbon for decolorization and filtration to obtain a clear solution;

[0051] 3) Prepare mixed solution B with isopropyl ether and isopropanol at a volume ratio of 3.5:1;

[0052] 4) At room temperature, add mixed solution B to the clear solution obtained in step 2) under an ultrasonic field with a power of 0.6KW, wherein the volume of mixed solution B is 7 times the volume of mixed solution A, and turn off the ultrasonic field after adding. The temperature was lowered to 3° C. and allowed to stand for 2 hours to precipitate crystals, which were then d...

Embodiment 3

[0054] The preparation of embodiment 3 ceftibuten crystal compound

[0055] 1) Prepare mixed solution A by mixing dimethylformamide and water at a volume ratio of 4:1;

[0056] 2) Take the ceftibuten raw material, add the mixed solution A prepared in step 1), wherein the ratio of the volume of the mixed solution A to the mass of ceftibuten is 10ml:1g, stir to dissolve it all, and pour it into the obtained solution Add activated carbon for decolorization and filtration to obtain a clear solution;

[0057] 3) Prepare mixed solution B with isopropyl ether and isopropanol at a volume ratio of 3.5:1;

[0058] 4) At room temperature, add mixed solution B to the clear solution obtained in step 2) under an ultrasonic field with a power of 0.6KW, wherein the volume of mixed solution B is 8 times the volume of mixed solution A, and turn off the ultrasonic field after adding. The temperature was lowered to 3° C. and allowed to stand for 2 hours to precipitate crystals, which were then ...

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Abstract

The invention belongs to the technical field of medicine and discloses a method for preparing a medicine ceftibuten crystal compound for treating surgical infection. The structural formula of the medicine ceftibuten crystal compound prepared through the method is as shown in the formula (I). The crystal compound is measured through the powder X-ray diffraction determination method, and an X-ray powder diffraction spectrum represented by the diffraction angle of 2theta+ / -0.2 degrees is as shown in the figure 1. The medicine ceftibuten crystal compound prepared through the method is high in purity, low in polymer content, good in stability, not likely to absorb moisture and good in flowability, and solubility of the compound is greatly improved. Please see the formula (I) in the description.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a method for preparing a crystal compound of ceftibuten, a medicine for treating surgical infection. Background technique [0002] Ceftibuten (Ceftibuten) is a third-generation oral broad-spectrum cephalosporin developed by Shionogi Company in Japan. It has strong antibacterial effect on most Gram-negative bacilli and some positive cocci. -Lactamase is highly stable and has post-antibiotic effects; it has the characteristics of broad antibacterial spectrum, strong antibacterial activity, and high bioavailability, and is used to treat various infections caused by sensitive strains, including upper respiratory tract infection, lower respiratory tract infection, phlegm Urinary system infection, enteritis and gastroenteritis, etc. [0003] The chemical name of ceftibuten is (+)-(6R,7R)-7β-[(Z)-2-(2-amino-4-thiazole)-4-carboxy-2-(Z)-butenamide] -8-oxo-5-thio-1-nitrobicy...

Claims

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Application Information

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IPC IPC(8): C07D501/22C07D501/12A61K31/546A61P31/04A61K9/14
CPCC07D501/22A61K9/0019A61K9/143A61K31/546C07B2200/13C07D501/12
Inventor 范明富路明华
Owner 临沂草之美医药科技有限公司
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