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新型潜在抗心律失常药物“物质H + B”的水解稳定性及动力学研究

Study of the stability and the kinetics of hydrolysis on the new potential antiarrhythmic "substance H + B".

作者信息

Stankovićová M, Bachratá M, Bezáková Z, Blesová M, Cizmárik J, Sveda P

机构信息

Department of Pharmaceutical Chemistry, Pharmaceutical Faculty, Comenius University, Bratislava, Slovakia.

出版信息

Pharmazie. 1994 Aug;49(8):579-83.

PMID:7938147
Abstract

"Substance H + B", N-[2-(2-heptyloxyphenylcarbamoyloxy)-ethyl]-N- benzylpiperidine chloride (1) is a new potential antiarrhythmic, prepared by quarternization of the local anesthetic, antiarrhythmic and antimicrobial heptacaine, N-[2-(2-heptyloxyphenylcarbamoyloxy)-ethyl]-piperidine chloride. The content of the work was a study of the stability of 1 based on the short-time stability tests of aqueous solutions, the observation of long-time storing of the substance and study of the kinetics of hydrolysis in aqueous, ethanolic buffer solutions. The conclusions of the presented results are: 1 is stable in acidic and neutral media, the alkaline hydrolysis is faster from the start compared to the hydrolysis of heptacaine, but later obtains an equilibrium character.

摘要

“H物质+B”,N-[2-(2-庚氧基苯基氨基甲酰氧基)乙基]-N-苄基哌啶氯化物(1)是一种新型潜在抗心律失常药物,通过对局部麻醉药、抗心律失常药和抗菌药庚卡因N-[2-(2-庚氧基苯基氨基甲酰氧基)乙基]哌啶氯化物进行季铵化反应制备而成。该研究工作的内容是基于水溶液的短期稳定性试验、该物质的长期储存观察以及在水性、乙醇缓冲溶液中的水解动力学研究,对1的稳定性进行研究。所呈现结果的结论是:1在酸性和中性介质中稳定,碱性水解从一开始就比庚卡因的水解更快,但后来呈现出平衡特征。

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