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Method for removing impurity compounds in lidocaine and obtained product

A lidocaine and compound technology, applied in the field of drug detection and impurity control, can solve the problems affecting the sustainable and healthy development of the pharmaceutical industry, the quality assurance of drug products, and the discovery of unknown impurities that affect the safety of public medication, and achieve strong specificity, Ease of operation and control, and the effect of ensuring drug safety

Pending Publication Date: 2022-06-21
SHANGHAI VIWIT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] At present, in the preparation or production of lidocaine, the related research on impurity control is still very shallow, and it is still in the initial stage of indirectly realizing the impurity control in drugs by controlling the purity of API, for example: CN 102070483 A, CN105294477 A, CN 110590590 A, etc. These are still unable to realize the qualitative and / or quantitative detection of impurities in the lidocaine production process, which is not conducive to the discovery of new unknown impurities in its preparation or production process and to find ways to control them, nor is it conducive to the product quality of the drug Guarantee, which in turn will affect the safety of public medication and the sustainable and healthy development of my country's pharmaceutical industry

Method used

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  • Method for removing impurity compounds in lidocaine and obtained product
  • Method for removing impurity compounds in lidocaine and obtained product
  • Method for removing impurity compounds in lidocaine and obtained product

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0097] 1. Preparation of chloroacetyl-2,6-dimethylaniline

[0098]

[0099] Include the following steps:

[0100] A, inert gas (nitrogen) protection, add 16kg (about 132mol) 2,6-dimethylaniline, 11.09kg (about 132mol) sodium bicarbonate and 96L methylene dichloride in the reactor, stir, add 16.4kg ( About 145mol) chloroacetyl chloride (control the temperature in the kettle -5~15℃), stir the reaction at -5~15℃ for 1h, GC (gas chromatography) or TLC (thin layer chromatography) monitor the reaction is basically complete (2,6- The residual amount of dimethylaniline≤2wt%) ends after;

[0101] b. Add 16kg of purified water to the kettle, stir evenly, then distill under reduced pressure (vacuum degree≤-0.09MPa, temperature 40~45°C) until no distillate is produced, then add 176kg of purified water to the kettle, at 15~35 After stirring at °C for 2 h, centrifugation, and drying by blasting (50-60 °C), chloroacetyl-2,6-dimethylaniline was obtained as a white powdery solid with a yi...

Embodiment 2 and 3

[0160] The same content as Example 1 will not be repeated, the difference is that in the step a of preparing chloroacetyl-2,6-dimethylaniline, the consumption of chloroacetyl chloride is changed to 132mol and 158.4mol respectively, namely: 1 equivalent , 1.2 equivalents, and finally obtain chloroacetyl-2,6-dimethylaniline, white powdery solid, the yield is all ≥90% (calculated as 2,6-dimethylaniline), the HPLC purity is all ≥98%, impurity The content of A is in the range of 0.6% to 1.5%.

Embodiment 4～6

[0162] The same content as Example 1 is not repeated, the difference is that in the step a of preparing chloroacetyl-2,6-dimethylaniline, the consumption of sodium bicarbonate is changed to 106mol, 158.4mol, 198mol respectively, namely: 0.8 equivalents, 1.2 equivalents, and 1.5 equivalents, and finally chloroacetyl-2,6-dimethylaniline was obtained as a white powdery solid, the yields were all ≥95% (calculated as 2,6-dimethylaniline), and the HPLC purity was uniform. ≥98%, the content of impurity A is in the range of 0.6% to 1.5%.

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Abstract

The invention discloses a method for removing impurity compounds in lidocaine and an obtained product, and the method comprises the following steps: using or not using inert gas protection, using hydrogen chloride gas to adjust the pH value of a reaction liquid system of lidocaine, hydrochloric acid and acetone to 2.5-3.8, and then separating and purifying. Wherein the lidocaine comprises a compound as shown in a formula II in the specification. According to the method, lidocaine can form hydrochloride and / or hydrate to improve water solubility and bioavailability, a small amount of newly found impurity compounds in lidocaine can be effectively removed, impurity limit control is carried out on lidocaine, and then it is guaranteed that the quality of a raw material medicine product is controllable; moreover, the process conditions are mild, the obtained product is high in yield and purity, low in impurity content, small in toxic and side effects and higher in safety, and the safety, effectiveness and stability of lidocaine hydrochloride (and / or hydrate thereof) and a preparation thereof can be remarkably improved.

Description

technical field [0001] The invention belongs to the field of drug (or its intermediate product) detection and impurity control, in particular to a method for removing impurity compounds in lidocaine and a product obtained therefrom. Background technique [0002] Medicines, including APIs and preparations, are special commodities for the prevention, treatment and / or diagnosis of diseases, and their quality is related to the health and safety of the public. Therefore, ensuring its safety, effectiveness and quality control is the top priority throughout the entire process of research and development, production, storage, and clinical application. Whether various impurities in a drug can be accurately identified and controlled is directly related to the quality controllability and safety of the drug. It is a key link in its quality assurance and an important part of drug consistency evaluation. index. [0003] Impurities refer to other substances that appear in the drug due to...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C231/24C07C237/04A61K31/167A61P9/06
CPCC07C231/24A61K31/167A61P9/06C07C237/04
Inventor 魏彦君刘金飞杜文峰宋于强刘希望徐青景邢艳平殷亮
Owner SHANGHAI VIWIT PHARMA CO LTD
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