Cefoperazone sodium compound and medicine composition thereof

A technology of cefoperazone sodium and its compound, which is applied in the field of cefoperazone sodium compound and its pharmaceutical composition, can solve problems such as poor stability, achieve good curative effect, improve medication safety, and achieve good dissolution stability

Active Publication Date: 2014-07-30
YOUCARE PHARMA GROUP +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] However, according to the recrystallization method of the prior art, although the cefoperazone sodium obtained can be dissolved in water, its stability is poor, and solids are separated out after being placed for a long time.

Method used

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  • Cefoperazone sodium compound and medicine composition thereof
  • Cefoperazone sodium compound and medicine composition thereof
  • Cefoperazone sodium compound and medicine composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1. Preparation of Cefoperazone Sodium Compound

[0034] Take 1kg of the crude cefoperazone sodium, add 15 times the volume of the crude cefoperazone sodium in a volume ratio of 7:2.8:0.2 water: methanol: ethanol mixture solution 15L, heat in a water bath, control the temperature at 32 ℃; after the crude cefoperazone sodium is dissolved, add cefoperazone sodium The activated carbon of 0.3 times the weight of the crude product was decolorized and filtered to obtain the filtrate; the filtrate was heated to control the temperature in a water bath to add ethyl propionate 1.5 times the weight of the crude cefoperazone sodium to the filtrate. After the addition, the heating was stopped and the volume was added dropwise under stirring. Ethyl acetate 0.8 times the weight of the crude cefoperazone sodium, the stirring is 18 rpm, and the dripping is to control the dripping time for 10 minutes at a uniform rate; after the dripping, the temperature is cooled by stirring, and the...

Embodiment 2

[0036] Example 2. Preparation of Cefoperazone Sodium Compound

[0037] Take 2 kg of the crude cefoperazone sodium, add 20 times the weight of the crude cefoperazone sodium to water: methanol: ethanol mixed solution with a volume ratio of 7:2.8:0.2, heat in a water bath, and control the temperature at 37℃; after the crude cefoperazone sodium is dissolved, add the crude cefoperazone sodium 0.3 times the weight of activated carbon was decolorized, filtered, and the filtrate was obtained; the filtrate was heated at 37°C and the volume of ethyl propionate was 1.8 times the weight of the crude cefoperazone sodium was added to the filtrate, the heating was stopped after the addition, and the volume was cefoperazone sodium dropwise under stirring The weight of crude product is 1.2 times of ethyl acetate, the stirring is 18 rpm, the dropping is to control the dropping time for 10 minutes, and the dropping is at a constant speed; after the dropping, the temperature is lowered by stirring, a...

Embodiment 3

[0039] Example 3. Preparation of Cefoperazone Sodium Compound

[0040] Take 10 kg of the crude cefoperazone sodium, add the volume of the crude cefoperazone sodium 18 times the volume ratio of 7:2.8:0.2 water: methanol: ethanol mixed solution, heated in a water bath, control the temperature at 35 ℃; after the crude cefoperazone sodium is dissolved, add the crude cefoperazone sodium 0.5 times the weight of activated carbon is decolorized, filtered, and the filtrate is obtained; the filtrate is heated at 35°C and the volume of ethyl propionate is 2.0 times the weight of the crude cefoperazone sodium is added to the filtrate, the heating is stopped after the addition, and the volume is cefoperazone sodium while stirring. The crude product weight 1.0 times of ethyl acetate, the stirring is 20 rpm, the dropping is to control the dropping time for 12 minutes, and the dropping is at a constant speed; after the dropping, the temperature is cooled by stirring, and the stirring and cooling ...

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to a cefoperazone sodium compound and a medicine composition thereof. The structure formula of the cefoperazone sodium compound is as shown in a formula (I). The compound is determined by using a powder X-ray diffraction determination method, and an X-ray powder diffraction spectrum shown by a diffraction angle of 2 theta +/- 0.2 degree is as shown in a figure 1. The cefoperazone sodium compound provided by the invention has good solubility and stability, and solids can not be separated out after the cefoperazone sodium compound is placed for a long time; and in addition, the cefoperazone sodium compound has a better curative effect and a better clearing effect on pathogenic bacteria.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a cefoperazone sodium compound and a pharmaceutical composition thereof. Background technique [0002] Cefoperazone sodium (cefoperazone sodium), its chemical name is: (6R, 7R)-3-[[(1-methyl-1H-tetrazol-5yl)sulfur]methyl]-7-[(R)-2- (4-Ethyl-2,3-dioxo-1-piperazinecarbamido)-2-p-hydroxyphenyl-acetamido]-8-oxo-5-thia-1-azabicyclo[ 4.2.0] Oct-2-ene-2-carboxylate sodium salt. It belongs to the third generation of cephalosporin antibiotics. It has the advantages of wide antibacterial spectrum and strong antibacterial effect. It is widely used in clinical practice. For example, cefoperazone sodium for injection, and the compound preparation made with sulbactam is cefoperazone sodium and sulbactam sodium for injection. [0003] CN1970561A discloses a stable new crystal form of cefoperazone sodium, which is composed of one or more of subtypes I, II and III of crystal form A. The in...

Claims

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Application Information

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