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氯氮䓬在生理条件下对其N-亚硝基衍生物的反应性研究(作者译)

[Studies on the reactability of chlordiazepoxide to its N-nitrosos derivative in physiological conditions (author's transl)].

作者信息

Kinawi A, Onken A, Rozyczka B, König W

出版信息

Arzneimittelforschung. 1977 Feb;27(2):363-7.

PMID:16620
Abstract

It is shown that chlordiazepoxide readily reacts with sodium nitrite in an aqueous HCl solution as well as in human gastric juice to N-nitrosochlordiazepoxide with a high yield (up to 75%). For this reaction the pH optimum has been determined to be 1.4. After oral application of chlordiazepoxide alone or in combination with nitrite to rats, the drug as well as its N-nitroso derivative were recovered from serum and analysed by high-pressure liquid chromatography.

摘要

结果表明,氯氮䓬在盐酸水溶液以及人胃液中能与亚硝酸钠迅速反应,以高收率(高达75%)生成N-亚硝基氯氮䓬。已确定该反应的最佳pH值为1.4。单独给大鼠口服氯氮䓬或与亚硝酸盐联合给药后,从血清中回收药物及其N-亚硝基衍生物,并通过高压液相色谱法进行分析。

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