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阿伏苯唑代谢物(M-11)在大鼠体内的药代动力学

[Pharmacokinetics of afobazole metabolite (M-11) in rats].

作者信息

Bastrygin D V, Viglinskaia A O, Kolyvanov G B, Litvin A A, Bochkov P O, Mozhaeva T Ia, Zherdev V P

出版信息

Eksp Klin Farmakol. 2011;74(7):22-6.

Abstract

Pharmacokinetics of compound M-11 (main metabolite of afobazole) after administration via different routes was studied in rats. After oral and intravenous administration, M-11 exhibited weakly pronounced bioconversion with the formation of a few metabolites that could be detected in plasma samples for about 3 hours. The absolute bioavailability of M-11 after oral administration was 68.3%. It was found that M-11 was completely absorbed from gastrointestinal tract of rats and characterized by "the first pass effect", after which approximately 70% of administered dose entered the circulation. The parent substance was determined neither in urine nor in feces.

摘要

在大鼠中研究了化合物M-11(阿伏苯唑的主要代谢产物)经不同途径给药后的药代动力学。口服和静脉给药后,M-11表现出微弱的生物转化,形成少量代谢产物,这些代谢产物可在血浆样本中检测约3小时。口服给药后M-11的绝对生物利用度为68.3%。发现M-11从大鼠胃肠道完全吸收,并具有“首过效应”,之后约70%的给药剂量进入循环。在尿液和粪便中均未检测到母体物质。

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