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Cefuroxime sodium new crystal type compound and preparation adopting particle process crystal product molecular assembly and form optimizing technology

A technology of cefuroxime sodium and compound, applied in the field of medicine, can solve the problems of cefuroxime sodium, such as deep color, instability, content reduction and the like

Inactive Publication Date: 2016-06-15
HAINAN LINGKANG PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The cefuroxime sodium color and luster that all exists in above-mentioned method preparation is darker, the problem of poor stability
[0006] The conventional crystal form of cefuroxime sodium has poor stability, and is unstable to heat, acidic environment, and alkaline environment. It is manifested in problems such as easy discoloration of appearance, decrease in content, and occurrence of degradation products.

Method used

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  • Cefuroxime sodium new crystal type compound and preparation adopting particle process crystal product molecular assembly and form optimizing technology
  • Cefuroxime sodium new crystal type compound and preparation adopting particle process crystal product molecular assembly and form optimizing technology
  • Cefuroxime sodium new crystal type compound and preparation adopting particle process crystal product molecular assembly and form optimizing technology

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Example 1: Preparation of Cefuroxime Sodium New Crystal Form Compound

[0026] (1) Dissolve 54.4g of 7-ACA in 1000ml of chloroform, under stirring, add 60.6g of triethylamine to the above solution, stir for 30min, slowly add 50.1g of SMIF-Ts, keep warm at 0-5°C, and react 2h, add 500ml of distilled water, stir and react for 10min, take the water layer, decolorize with 5g of activated carbon at room temperature for 10min, filter, cool the filtrate to 0-5°C, slowly add 2mol / L hydrochloric acid solution, adjust the pH value to 3.0, precipitate crystals, and stir for 1h , filtered, washed with ice water until neutral, and dried under vacuum at 40°C to obtain 74.9g of 7-FCA.

[0027] (2) Add 70.0g of 7-FCA and 600ml of methanol to the reaction bottle, cool to 0-5°C under stirring, slowly add 700ml of 4% NaCO3 aqueous solution, after the addition, warm up to 10°C for 30min, and extract with ethyl acetate 2 times, 1000ml each time, combined the organic layers, washed 2 times ...

Embodiment 2

[0037] Embodiment 2: Preparation of new crystal form compound of cefuroxime sodium

[0038] (1) Dissolve 53.8g of 7-ACA in 1000ml of chloroform, and add 61.5g of triethylamine to the above solution under stirring. After stirring for 30min, slowly add 52.1g of SMIF-Ts, keep warm at 0-5°C, and react 2h, add 500ml of distilled water, stir and react for 10min, take the water layer, decolorize with 5g of activated carbon at room temperature for 10min, filter, cool the filtrate to 0-5°C, slowly add 2mol / L hydrochloric acid solution to adjust the pH to 3.1, precipitate crystals, stir for 1h, filter , washed with ice water until neutral, and dried under vacuum at 40°C to obtain 75.8g of 7-FCA.

[0039] (2) Add 70.5g of 7-FCA and 600ml of methanol into the reaction bottle, cool to 0-5°C under stirring, slowly add 700ml of 4% NaCO3 aqueous solution, after the addition, warm up to 10°C for 30min, and extract with ethyl acetate 2 times, 1000ml each time, combine the organic layers, wash ...

Embodiment 3

[0043] Embodiment 3: Preparation of new crystal form compound of cefuroxime sodium

[0044] (1) Dissolve 50.5g of 7-ACA in 1000ml of chloroform, and add 51.5g of triethylamine to the above solution under stirring. After stirring for 30min, slowly add 51.1g of SMIF-Ts, keep warm at 0-5°C, and react 2h, 500ml of distilled water was added, and the reaction was stirred for 10min. Take the water layer, decolorize with 5g of activated carbon at room temperature for 10min, filter, cool the filtrate to 0-5°C, slowly add 2mol / L hydrochloric acid solution to adjust the pH value to 3.3, precipitate crystals, stir for 1h, filter, wash with ice water until neutral, 40 °C and vacuum-dried to obtain 74.9 g of 7-FCA.

[0045] (2) Add 70.1g of 7-FCA and 600ml of methanol to the reaction bottle, cool to 0-5°C under stirring, slowly add 700ml of 4% NaCO3 aqueous solution, after the addition, warm up to 10°C for 30min, and extract with ethyl acetate 2 times, 1000ml each time, combine the organi...

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Abstract

The invention discloses a cefuroxime sodium new crystal type compound and a crystallizing preparation method thereof. The cefuroxime sodium new crystal type compound is prepared through a particle process crystal product molecular assembly and form optimizing technology. A stability test proves that the new crystal type compound has the advantages of being high in purity, low in impurity content, low in hygroscopicity and good in stability. Meanwhile, the invention discloses a preparation, cefuroxime sodium for injection. The preparation is prepared from cefuroxime sodium.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new crystal form compound and preparation of cefuroxime sodium prepared by particle process crystal product molecular assembly and shape optimization technology. Background technique [0002] The chemical name of Cefuroximesodium is: (6R,7R)-7-[2-furyl(methoxyimino)acetamido]-3-carbamoyloxymethyl-8-oxo-5- Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt. Molecular formula: C 16 h 15 N 4 NaO 8 S, molecular weight: 446.37. Its chemical structural formula is: [0003] [0004] Cefuroxime sodium belongs to the second generation of broad-spectrum cephalosporins, which was first developed and marketed by the British Glaxo company in 1975 under the trade name Xilixin. It was approved by the US FDA on December 28, 1987, and was launched in the US in 1988. It is effective against a wide variety of Gram-positive and Gram-negative bacteria and is sta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/34C07D501/12C07D501/06A61K31/546A61K9/14A61P31/04
CPCC07D501/12C07D501/34A61K9/14C07B2200/13C07D501/06
Inventor 陶灵刚王静康尹秋响郝红勋
Owner HAINAN LINGKANG PHARMA CO LTD
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