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齐哌丙醇(咳舒平)在人体内的生物转化。使用氨作为选择性反应气的气相色谱/质谱研究(作者译)

[Biotransformation of zipeprol (Mirsol) in humans. Gas chromatographic/mass spectrometric studies, using ammonia as a selective reactant gas (author's transl)].

作者信息

Gielsdorf W, Toffel-Nadolny P

出版信息

J Clin Chem Clin Biochem. 1981 Jan;19(1):25-30.

PMID:7205156
Abstract

After oral application of Zipeprol (Mirsol) the unchanged drug and nine degradation products were detected in human urine; six of them could be identified. All identified metabolites were detected in the alkaline urine fraction; after acid hydrolysis N-(2-hydroxyethyl)-piperazine was found as an artifact. With respect to the presented results, biotransformation of Zipeprol in man mainly follows three degradation routes: 1. alpha-cleavage leading to metabolite M4; 2. cleavage of the exocyclic N-C-bond of the piperazine ring leading to metabolites M3, M5, M6; 3. benzylic cleavage leading to benzylalcohol (M1); oxidation leading to 2-hydroxy-2-phenylacetic acid (mandelic acid, M2).

摘要

口服齐哌丙醇(米索)后,在人尿中检测到未变化的药物和9种降解产物;其中6种能够被鉴定出来。所有鉴定出的代谢产物都在碱性尿部分被检测到;酸水解后发现N-(2-羟乙基)-哌嗪是一种人为产物。根据所呈现的结果,齐哌丙醇在人体内的生物转化主要遵循三条降解途径:1. α-裂解生成代谢产物M4;2. 哌嗪环外环N-C键的裂解生成代谢产物M3、M5、M6;3. 苄基裂解生成苯甲醇(M1);氧化生成2-羟基-2-苯基乙酸(扁桃酸,M2)。

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