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甲基苯巴比妥在人体中的药代动力学和生物利用度

Pharmacokinetics and bioavailability of methylphenobarbital in man.

作者信息

Hooper W D, Kunze H E, Eadie M J

出版信息

Ther Drug Monit. 1981;3(1):39-44.

PMID:7233487
Abstract

The pharmacokinetics and bioavailability of mephobarbital have been studied in 2 volunteers. Plasma levels of mephobarbital and phenobarbital were measured by gas chromatography-mass spectroscopy with selected ion monitoring. Urinary output of phenobarbital and the p-hydroxy derivatives of both mephobarbital and phenobarbital was measured by high pressure liquid chromatography. The time course of these plasma and urinary levels was monitored following single 800-mg oral and 200-mg intravenous doses in the 2 patients. The major conclusions of the study were that mephobarbital is reasonably well absorbed following oral dosing and that some 35% or so of the dose (by either route) is converted to the recently identified metabolite, p-hydroxymephobarbital.

摘要

已在2名志愿者身上研究了美索比妥的药代动力学和生物利用度。采用气相色谱 - 质谱联用选择离子监测法测定血浆中美索比妥和苯巴比妥的水平。通过高压液相色谱法测定苯巴比妥以及美索比妥和苯巴比妥的对羟基衍生物的尿量。在2例患者单次口服800 mg和静脉注射200 mg剂量后,监测这些血浆和尿液水平的时间进程。该研究的主要结论是,口服给药后美索比妥吸收良好,约35%的剂量(无论何种给药途径)会转化为最近鉴定出的代谢产物对羟基美索比妥。

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