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Method for preparing ceftizoxime sodium

A technology of ceftizoxime sodium and ceftizoxime acid, which is applied in the field of medicine, can solve the problems of increasing operating procedures, production costs, and long reaction steps, and achieve the effects of health and environmental protection, crystallization state improvement, and quality improvement.

Active Publication Date: 2011-04-13
哈药集团股份有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This route has long reaction steps, which increases the operating procedures and production costs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] I. the preparation of ceftizoxamic acid:

[0027] Dichloromethane 1000L, purified water 5L, add 7-ANCA (7-amino-3-H-cephem-4-carboxylic acid) 100Kg, stir to dissolve, cool down to -5 / 5℃, add organic base triethylamine 68Kg to dissolve , add AE active ester (2-(2-amino-4-thiazolyl)-2-methoxyimine-acetyl-benzothiazole thioester) 195 kg, maintain the reaction temperature -5 / 5°C and stir for 5 hours. Add 530L of purified water to stir and extract, add 500L of dichloromethane to the water phase to wash twice, add 0.01mol / l hydrochloric acid to the water phase feed solution, adjust the pH value to 5.5-6.0, and add 5.0Kg of 303 activated carbon to the water phase and Al2O3 (model XFA-75150, particle size 150 mesh ≥ 90%) 20.0Kg, stirred and decolorized for 20 minutes, filtered respectively in turn, added 350L of dispersant pharmaceutical ethanol, and added dropwise 3mol / l hydrochloric acid aqueous solution until a large amount of crystallization Precipitate, the pH value at th...

Embodiment 2

[0031] The influence of hydrochloric acid to adjust the pH value on the product content

[0032] When preparing ceftizoxamic acid in the prior art, hydrochloric acid is usually used to adjust the pH value to 2.0-2.5. In the preparation process of ceftizoxamic acid in the present invention, 0.01mol / l Hydrochloric acid, adjust the pH value to 5.5-6.0, and the content of the intermediate product ceftizoxamic acid (HPLC method) is increased by more than 2% on average compared with the control. The data of the control effect determined by the laboratory are as follows (6 batches in parallel):

[0033] .

Embodiment 3

[0035] In the preparation process of ceftizoxime sodium, the solvent crystallization operation of the original process uses a certain speed to continuously add the crystallization solvent. Although the product yield is high, the crystal grains are small, the crystal form is not uniform, the product stability is relatively poor, and the efficiency of a certain batch is relatively poor. During the period, the clarity exceeded the standard. At the same time, there was feedback in the sub-packaging process of the sterile raw powder, and it was difficult to sub-package certain batches.

[0036] The preparation method of the present invention is as follows: slowly add the crystallization solvent until the crystallization liquid becomes slightly cloudy, stop adding the solvent, slowly stir and grow the crystal for 0.5 hours, then continue to add the remaining solvent, and then stir and grow the crystal for 1 hour after the addition. Although the product yield of the optimized process ...

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PUM

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Abstract

The invention relates to synthetic ceftizoxime acid and a method for preparing ceftizoxime sodium from the synthetic ceftizoxime acid. The preparation process comprises the following steps: slowly adding a crystallization solvent in a crystallization liquid until the crystallization liquid becomes slightly turbid, stopping adding the solvent, slowly stirring and growing crystals for 0.5 hour, continuously adding the residual solvent, and stirring and growing the crystals for 1 hour after the residual solvent is completely added. The product prepared by the optimized process in the invention has remarkably improved quality although the yield is lowered by 1.0-1.5%; and the product crystallization state is obviously improved and the product quality problem of clarity stability in the period of validity is solved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a method for synthesizing ceftizoxime acid and preparing ceftizoxime sodium therefrom. Background technique [0002] Ceftizoxime sodium has a complex antibacterial effect and is stable against broad-spectrum β-lactamases produced by a variety of Gram-positive and Gram-negative bacteria. The process parameters used in the current process are not optimal process parameters, crystallization temperature, solvent Factors such as dropping speed and stirring speed have an impact on the crystal form of the finished product. [0003] Ceftizoxime Sodium was first developed by Japan Fujisawa Pharmaceutical Co., Ltd., and was first listed in Japan in 1982. The trade name is epocelin (Yibao Shiling). This product belongs to the third generation cephalosporin antibiotic. It has broad-spectrum, It has the characteristics of high efficiency, enzyme resistance, low toxicity and abil...

Claims

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Application Information

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IPC IPC(8): C07D501/20C07D501/06C07D501/04C07D501/12
Inventor 马杰陈玉山韩东胜崔嵘徐淑明李国峰余威
Owner 哈药集团股份有限公司
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