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氟硝西泮对健康人体受试者单次及多次口服给药后的药代动力学

Pharmacokinetics of flunitrazepam following single- and multiple-dose oral administration to healthy human subjects.

作者信息

Boxenbaum H G, Posmanter H N, Macasieb T, Geitner K A, Weinfeld R E, Moore J D, Darragh A, O'Kelly D A, Weissman L, Kaplan S A

出版信息

J Pharmacokinet Biopharm. 1978 Aug;6(4):283-93. doi: 10.1007/BF01060092.

DOI:10.1007/BF01060092
PMID:29954
Abstract

Healthy human subjects received single and multiple oral doses of flunitrazepam. Absorption and disposition were first order and reproducible from administration. The oral doses were virtually completely available to the liver, and elimination from the body occurred entirely via metabolism. Assuming the liver to be the sole eliminating organ, hepatic blood clearance and extraction ratio were approximately 0.235 liter/hr/kg and 0.154, respectively. Steady-state blood volume of distribution averaged 3.76 liters/kg in the single-dose studies. Terminal exponential half-lives from the single- and multiple-dose studies (different subjects) averaged 13.5 and 19.2 hr, respectively; these differences were not due to clearance changes but were entirely attributable to variations in volumes of distribution.

摘要

健康人体受试者接受了氟硝西泮的单次和多次口服给药。吸收和处置呈一级动力学,给药后具有可重复性。口服剂量在肝脏中几乎完全可利用,且体内消除完全通过代谢进行。假设肝脏是唯一的消除器官,肝血清除率和提取率分别约为0.235升/小时/千克和0.154。单剂量研究中稳态血药分布容积平均为3.76升/千克。单剂量和多剂量研究(不同受试者)的终末指数半衰期分别平均为13.5小时和19.2小时;这些差异并非由于清除率变化,而是完全归因于分布容积的差异。

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Pharmacokinetics of flunitrazepam following single- and multiple-dose oral administration to healthy human subjects.氟硝西泮对健康人体受试者单次及多次口服给药后的药代动力学
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Classification of benzodiazepine hypnotics in humans based on receptor occupancy theory.基于受体占有率理论对人类苯二氮䓬类催眠药进行分类。

本文引用的文献

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