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关于地他唑在人体中的代谢

On the metabolism of ditazole in man.

作者信息

Maurer H, Kleff I

机构信息

Institute of Pharmacology and Toxicology, University of Saarland, Homburg/Saar, Fed. Rep. of Germany.

出版信息

Arzneimittelforschung. 1988 Dec;38(12):1843-5.

PMID:2907728
Abstract

This paper describes mass spectrometric studies on the metabolism of 4,5-diphenyl-2-bis-(2-hydroxyethyl)-amino-oxazole (ditazole, Ageroplas) in man. The metabolites were identified after cleavage of conjugates, extraction and derivatisation in urine of healthy volunteers orally administered with 400 mg of ditazole each. Besides the unchanged ditazole the following 7 metabolites could be detected: N-desalkyl and N,N-bisdesalkyl ditazole, hydroxy ditazole, N-desalkyl-hydroxy and N,N-bisdesalkyl-hydroxy ditazole as well as benzil and hydroxy benzil. Therefore, two main metabolic pathways, the aromatic hydroxylation and the N-desalkylation, can be postulated. Ditazole and its metabolites (with the exception of benzil) are excreted in urine partly in a conjugated form.

摘要

本文描述了对4,5 - 二苯基 - 2 - 双 -(2 - 羟乙基) - 氨基 - 恶唑(双苯恶唑,阿格罗普拉斯)在人体代谢的质谱研究。在给健康志愿者口服400mg双苯恶唑后,对其尿液中的代谢物进行结合物裂解、提取和衍生化处理后进行鉴定。除了未变化的双苯恶唑外,还能检测到以下7种代谢物:N - 去烷基和N,N - 双去烷基双苯恶唑、羟基双苯恶唑、N - 去烷基 - 羟基和N,N - 双去烷基 - 羟基双苯恶唑以及联苯甲酰和羟基联苯甲酰。因此,可以推测出两条主要的代谢途径,即芳环羟基化和N - 去烷基化。双苯恶唑及其代谢物(联苯甲酰除外)部分以结合形式从尿液中排出。

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