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奥沙西泮在健康志愿者中的药代动力学。

Pharmacokinetics of oxazepam in healthy volunteers.

作者信息

Alván G, Siwers B, Vessman J

出版信息

Acta Pharmacol Toxicol (Copenh). 1977 Jan;40 Suppl 1(1):40-51.

PMID:300541
Abstract

The pharmacokinetics of oxazepam was studied in healthy volunteers. When oral doses of 15 mg were given to eight subjects on two occasions 2.5 years apart the individual areas under the plasma concentration time curves did not differ significantly. Plasma clearance ranged between 0.050 and 0.171 x kg-1 x h-1 and half-lives from 5.9 to 25 hours. The urinary recovery of oxazepam conjugates was 67 +/- 15 S.D.% of the dose given and the total recovery including faecal oxazepam was 70 +/- 15 S.D. %. On multiple dosing (5 mg t.i.d.) stable steady-state concentrations were established. There was a tendency for slightly lower steady-state concentrations than predicted from single oral doses. During steady-state 86 +/- 17 S.D. % of the dose was recovered in the urine over a 24 hour period.

摘要

在健康志愿者中研究了奥沙西泮的药代动力学。当在两次间隔2.5年的情况下给8名受试者口服15毫克剂量时,血浆浓度-时间曲线下的个体面积无显著差异。血浆清除率在0.050至0.171 x kg-1 x h-1之间,半衰期在5.9至25小时之间。奥沙西泮结合物的尿回收率为给药剂量的67±15标准差%,包括粪便中奥沙西泮的总回收率为70±15标准差%。多次给药(5毫克,每日三次)后建立了稳定的稳态浓度。稳态浓度有略低于单次口服剂量预测值的趋势。在稳态期间,24小时内86±17标准差%的剂量在尿液中回收。

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