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Preparation method of freeze-dried preparation of cefozopran hydrochloride

A technology of cefazolam hydrochloride and freeze-dried preparations is applied in the field of preparation of freeze-dried preparations of cefazolam hydrochloride for injection, which can solve the problem that it is difficult to remove the solvent to a satisfactory level, the preparation method is complicated, and it is difficult to prepare qualified and high-quality preparations. Cefazolam hydrochloride freeze-dried preparation and other problems, to achieve the effect of excellent stability, purity and appearance, less impurities

Active Publication Date: 2014-10-15
珠海保税区丽珠合成制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the usual vacuum drying is difficult to remove the solvent to a satisfactory level without causing the decomposition of SCE-2787 (HCl) itself
[0022] In summary, in the currently reported technology for preparing lyophilized preparations of cefozopran hydrochloride, the preparation method is more complicated, and it is difficult to prepare qualified and high-quality lyophilized preparations of cefozopran hydrochloride

Method used

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  • Preparation method of freeze-dried preparation of cefozopran hydrochloride
  • Preparation method of freeze-dried preparation of cefozopran hydrochloride
  • Preparation method of freeze-dried preparation of cefozopran hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] (1) Dissolve 206g of anhydrous sodium carbonate and 120g of sodium chloride in 5L of water for injection at room temperature, and use CO 2 Adjust the pH value to about 9 to obtain the excipient solution;

[0072] (2) Add 5L of water for injection and 3L of absolute ethanol into a 20L reaction kettle, preheat to 50°C, add 1098.5g of cefazolam hydrochloride with 2.3% water and 0.3% ethanol content (ceftozolam C 19 h 17 N 9 o 5 S 2 Calculated as 1000g), stirred and dissolved to obtain cefzolam hydrochloride water-ethanol solution;

[0073] (3) Add the excipient solution prepared in step (1) dropwise to the cefzolam hydrochloride water-ethanol solution prepared in step (2), while using CO 2 Control the pH value to about 7.5, drop the temperature naturally after dropping to obtain a mixed solution, and control the temperature of the mixed solution to be 20°C to 25°C;

[0074] (4) Add 50 g of activated carbon to the mixed solution obtained in step (3) and stir for 20 mi...

Embodiment 2

[0097] (1) Dissolve 206g of anhydrous sodium carbonate and 120g of sodium chloride in 6L of water for injection at 35°C to 40°C, and use CO 2 Adjust the pH value to about 10 to obtain the excipient solution;

[0098](2) Add 6L of water for injection and 2L of anhydrous methanol into a 20L reaction bottle, preheat to 37°C, add 1095.1g of cefazolam hydrochloride with 2.1% water and 0.2% methanol content (ceftozolam C 19 h 17 N 9 o 5 S 2 Calculated as 1000g), stirred and dissolved to obtain cefzolam hydrochloride water-methanol solution;

[0099] (3) Add the excipient solution prepared in step (1) dropwise to the cefzolam hydrochloride water-methanol solution prepared in step (2), while using CO 2 Control the pH value to about 8.0 to obtain a mixed solution, and control the temperature of the mixed solution to be 25° C. to 30° C.

[0100] (4) Add 30 g of activated carbon to the mixed solution obtained in step (3) and stir for 30 minutes while maintaining CO 2 , control the...

Embodiment 3

[0124] (1) Dissolve 206g of anhydrous sodium carbonate and 120g of sodium chloride in 3.5L of water for injection at 20°C to 25°C, and use CO 2 Adjust the pH value to 8 to obtain the excipient solution;

[0125] (2) Add 3.5L of water for injection and 2.5L of absolute ethanol into a 20L reactor, preheat to 52°C, add 1183.1g of cefozopran hydrochloride ethanol solvate with 3.0% water and 7.5% ethanol C 19 h 17 N 9 o 5 S 2 Calculated as 1000g), stirred and dissolved to obtain cefzolam hydrochloride water-ethanol solution;

[0126] (3) Add the excipient solution prepared in step (1) dropwise to the cefzolam hydrochloride water-ethanol solution prepared in step (2), while using CO 2 The pH value is controlled to be 7 to obtain a mixed solution, and the temperature of the mixed solution is controlled to be 30° C. to 40° C.

[0127] (4) Add 30 g of needle activated carbon to the mixed solution obtained in step (3) and stir while maintaining CO 2 , the temperature of the mixe...

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Abstract

The invention relates to a preparation method of an injection-use freeze-dried preparation of cefozopran hydrochloride. The method includes following steps: (1) dissolving anhydrous sodium carbonate and sodium chloride in water at 20-40 DEG C and adjusting a pH value to 8.0-10.0 with carbon dioxide to obtain an auxiliary material solution; (2) dissolving cefozopran hydrochloride, or a solvate thereof, in an ethanol-water solution, or a methanol-water solution, to obtain a cefozopran hydrochloride solution, wherein the ethanol-water solution, or the methanol-water solution, is pre-heated to 35-55 DEG C; (3) adding dropwisely the auxiliary material solution prepared in the step (1) to the cefozopran hydrochloride solution prepared in the step (2) with the pH value being controlled within 7.0-8.5 through carbon dioxide to obtain a mixed solution; (4) adding needle-use activated carbon to the mixed solution with stirring with carbon dioxide being added; and (5) filtering a solution obtained through the step (4) to obtain a sterile filtrate and performing a freeze-drying process. By means of the method in the invention, the freeze-dried preparation of cefozopran hydrochloride is little in impurities, is high in quality and can satisfy, even is higher than a standard in the 15th version of the Japanese pharmacopoeia.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a preparation method of a freeze-dried preparation of cefozopram hydrochloride for injection. Background technique [0002] Cefozopran hydrochloride (cafozopran hydrochloride) is the fourth-generation cephalosporin for injection developed and marketed by Takeda Corporation of Japan. efficient. This product has good enzyme resistance and strong penetrating effect on bacterial cell walls, and is used to treat infections caused by sensitive bacteria. [0003] The chemical name of cefazolam hydrochloride is: [[(6R,7R)-7-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-methoxy Iminoacetamido]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]imidazo[1,2- b] Pyridazinium hydroxide inner salt monohydrochloride. CAS RN: 113981-44-5; its chemical structure is shown in formula (I): [0004] [0005] Molecular formula: C 19 h 17 N 9 o 5 S 2. HCl molecular weight: 551.99...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/546A61P31/04
Inventor 谢斌周成光
Owner 珠海保税区丽珠合成制药有限公司
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