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A kind of cefoperazone sodium compound and pharmaceutical 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: 2016-04-27
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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  • A kind of cefoperazone sodium compound and pharmaceutical composition thereof
  • A kind of cefoperazone sodium compound and pharmaceutical composition thereof
  • A kind of cefoperazone sodium compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Embodiment 1, the preparation of cefoperazone sodium compound

[0035] Take 1 kg of the crude product of cefoperazone sodium, add 15 times the weight of the crude product of cefoperazone sodium, and add 15 L of 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 32°C; after the crude product of cefoperazone sodium is dissolved, add cefoperazone sodium Decolorize with active carbon of 0.3 times the weight of the crude product, filter to obtain the filtrate; add ethyl propionate whose volume is 1.5 times the weight of the crude product of cefoperazone sodium to the filtrate by heating in a water bath to control the temperature at 32 ° C, stop heating after adding, and add dropwise with stirring. Ethyl acetate of 0.8 times the weight of cefoperazone sodium crude product, the stirring is 18rmp, and the dripping is to control the dripping time for 10 minutes and drop at a constant speed; after dropping, ...

Embodiment 2

[0037] Embodiment 2, the preparation of cefoperazone sodium compound

[0038] Take 2 kg of the crude product of cefoperazone sodium, add a volume ratio of 20 times the weight of the crude product of cefoperazone sodium, water:methanol:ethanol mixed solution of 7:2.8:0.2, heat in a water bath, and control the temperature at 37°C; after the crude product of cefoperazone sodium is dissolved, add the crude product of cefoperazone sodium Activated carbon decolorizing with 0.3 times the weight, filtered to obtain the filtrate; heating in a water bath to control the temperature, adding ethyl propionate with a volume of 1.8 times the weight of the crude product of cefoperazone sodium to the filtrate at 37°C, stopping heating after adding, and adding dropwise a volume of cefoperazone sodium Ethyl acetate of 1.2 times the weight of the crude product, the stirring is 18rmp, and the dropping is to control the dropping time for 10 minutes and drop at a constant speed; after dropping, stir a...

Embodiment 3

[0040] Embodiment 3, the preparation of cefoperazone sodium compound

[0041]Take 10kg of the crude product of cefoperazone sodium, add a volume ratio of 18 times the weight of the crude product of cefoperazone sodium, water:methanol:ethanol mixed solution of 7:2.8:0.2, heat in a water bath, and control the temperature at 35°C; Decolorize with activated carbon with 0.5 times the weight, filter to obtain the filtrate; add ethyl propionate whose volume is 2.0 times the weight of the crude product of cefoperazone sodium to the filtrate by heating in a water bath at 35°C, stop heating after adding, and add dropwise with volume of cefoperazone sodium Ethyl acetate of 1.0 times the weight of the crude product, the stirring is 20rmp, and the dropping is to control the dropping time for 12 minutes and drop at a constant speed; after the dropping is completed, stir and cool down, and the stirring and cooling is to cool down to 10°C for 5 minutes under stirring at a rotating speed of 29r...

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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 medicines, and in particular relates to a cefoperazone sodium compound and a pharmaceutical composition thereof. Background technique [0002] Cefoperazone sodium (cefoperazonesodium), its chemical name is: (6R, 7R)-3-[[(1-methyl-1H-tetrazol-5 base) sulfur] methyl]-7-[(R)-2-( 4-Ethyl-2,3-dioxo-1-piperazinecarbonylamino)-2-p-hydroxyphenyl-acetylamino]-8-oxo-5-thia-1-azabicyclo[4.2 .0] Oct-2-ene-2-carboxylic acid sodium salt. It belongs to the third-generation cephalosporin antibiotics. It has the advantages of broad antibacterial spectrum and strong antibacterial effect. It is widely used in clinical practice, such as 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 the subtypes I, II, and III of t...

Claims

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Application Information

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Patent Type & Authority Patents(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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