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反复服用片剂和糖浆后左美丙嗪的药代动力学及相对生物利用度

Pharmacokinetics and relative bioavailability of levomepromazine after repeated administration of tablets and syrup.

作者信息

Dahl S G, Strandjord R E, Sigfusson S

出版信息

Eur J Clin Pharmacol. 1977 Apr 20;11(4):305-10. doi: 10.1007/BF00607681.

Abstract

Plasma levels of levomepromazine and its sulphoxide were measured in 8 psychiatric patients after repeated doses of levomepromazine tablets or syrup. The rate and extent of absorption of the drug were similar for the two dosage forms, although the extent of presystemic metabolism appeared to be slightly greater after administration of syrup than of tablets. The biological half-life of levomepromazine ranged from 16.5 h to 77.8 h, and a 13-fold variation was seen in the ratio of the total clearance to the absorbed fraction of the dose (Cl/Fpo). It is postulated that individual variation in the dose required for therapy was due in part to individual variation in the pharmacokinetics of the drug.

摘要

对8名精神科患者在重复服用左美丙嗪片或糖浆后测定了血浆中左美丙嗪及其亚砜的水平。两种剂型药物的吸收速率和程度相似,尽管糖浆给药后的首过代谢程度似乎略高于片剂。左美丙嗪的生物半衰期为16.5小时至77.8小时,剂量总清除率与吸收分数之比(Cl/Fpo)有13倍的差异。据推测,治疗所需剂量的个体差异部分归因于药物药代动力学的个体差异。

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