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Preparation method of tazobactam sodium

A technology of tazobactam sodium and tazobactam acid, which is applied in the field of synthesis of the β-lactam inhibitor tazobactam sodium, which can solve the problem of harsh intermediate steps and low purity affecting the safety of clinical medication and the stability of preparations issues such as sexual decline

Inactive Publication Date: 2012-03-21
海南美好西林生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The process is complicated, and the intermediate steps are harsh and easy to produce "three wastes", and the production cost is high
Because the purity of tazobactam sodium obtained by this traditional method is not high, the stability of the preparation is greatly reduced, which is not conducive to clinical application.
In addition, sulbactam and 6-aminopenicillanic acid are used as starting materials to further react to prepare tazobactam sodium, which also affects the safety of clinical medication due to the complicated preparation process and low purity.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] According to the preparation method of tazobactam sodium of this embodiment, it comprises the following steps successively: take the cooling water that temperature is 6~15 ℃ and add tazobactam acid to make 50% tazobactam acid solution, and 15 % sodium bicarbonate solution, stir until the solution is completely clear, filter and sterilize, and set aside; put the above filtrate in a freeze-drying tray with a liquid layer thickness of 10-15mm, put it in the cold trap of a freeze dryer, and store it at -45°C Pre-lyophilize for 2-3 hours, then vacuum freeze-dry (vacuum degree below 10Pa), the first stage: -45℃~0℃ for 2.5 hours, keep warm at 0℃ for 6 hours; the second stage: 0℃~5℃ , the time is 1.5 hours, heat preservation at 5°C for 6 hours; the third stage: heat up to 50°C at 5°C-10°C / h, heat preservation and drying for 5-7 hours, and freeze-drying is completed, and white tazobactam sodium is freeze-dried powder.

Embodiment 2

[0016] According to the preparation method of tazobactam sodium of the present embodiment, it comprises the following steps successively: (1) take the cooling water that temperature is 6~15 ℃ and add tazobactam acid to make 50% tazobactam acid solution , mix with 15% sodium carbonate solution, stir until the solution is completely clear, filter and sterilize, and set aside; (2) put the above-mentioned filtrate in a freeze-drying tray, the thickness of the liquid layer is 10-15mm, and put it in the cold trap of a freeze-drying machine , pre-lyophilized at -45°C for 2-3 hours, and then vacuum freeze-dried (vacuum degree below 10Pa), the first stage: -45°C to 0°C for 2.5 hours, and keep warm at 0°C for 6 hours; the second stage: 0℃~5℃, the time is 1.5 hours, keep warm at 5℃ for 6 hours; the third stage: heat up to 50℃ at 5℃~10℃ / h, keep warm and dry for 5-7 hours, and freeze-drying is completed to obtain white thazol Bactam sodium lyophilized powder.

Embodiment 3

[0018] According to the preparation method of tazobactam sodium of the present embodiment, it comprises the following steps successively: (1) take the cooling water that temperature is 6~15 ℃ and add tazobactam acid to make 50% tazobactam acid solution , mix with 15% sodium hydroxide solution, stir until the solution is completely clear, filter and sterilize, and set aside; (2) put the above-mentioned filtrate in a freeze-drying tray, the thickness of the liquid layer is 10-15mm, and put it in a freeze-drying machine cold trap Pre-freeze-dry at -45°C for 2-3 hours, then vacuum freeze-dry (vacuum degree below 10Pa), the first stage: -45°C to 0°C for 2.5 hours, keep warm at 0°C for 6 hours; the second stage : 0 ℃ ~ 5 ℃, the time is 1.5 hours, keep warm at 5 ℃ for 6 hours; the third stage: heat up to 50 ℃ at 5 ℃ ~ 10 ℃ / h, keep warm and dry for 5-7 hours, after lyophilization, white he Zobactam sodium lyophilized powder.

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Abstract

The invention relates to a preparation method of a beta-lactam inhibitor, namely tazobactam sodium. The preparation method comprises the following steps: dissolving tazobactan acid in 6-15 DEG C of cooling water, mixing with a salt forming agent solution under the condition of controlling the temperature, stirring to ensure that the solution is clear, and lyophilizing to obtain tazobactam sodium powder. The tazobactam sodium prepared by the method has high purity; and the entire technological operation is convenient, the cost is low and the production efficiency and yield are increased.

Description

technical field [0001] The invention relates to the technical field of synthesis of a β-lactam inhibitor tazobactam sodium. Background technique [0002] Tazobactam sodium is a β-lactamase inhibitor used clinically after clavulanic acid and sulbactam. It was developed by Japan Dapeng Pharmaceutical Company in the 1980s. Except for Neisseriaceae and Acinetobacter, it has no antibacterial activity against other bacteria, but tazobactam has irreversible inhibition of most important β-lactamases produced by β-lactam antibiotic-resistant strains effect. It can prevent drug-resistant bacteria from destroying penicillins and cephalosporins, and tazobactam has obvious synergistic effects with penicillins and cephalosporins. Clinically, it is often made into compound preparations with piperacillin. [0003] The traditional synthesis of tazobactam is to use 6-APA (6-aminopenicillanic acid) as raw material, after esterification and oxidation reaction to obtain the key intermediate,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D499/16
Inventor 魏雪纹李强魏西雨
Owner 海南美好西林生物制药有限公司
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