利奥前列素在大鼠体内的药代动力学

Pharmacokinetics of rioprostil in rats.

作者信息

Petersen-von Gehr J K, Siefert H M, Steinke W

机构信息

Bayer AG, Institut für Pharmakokinetik, Wuppertal, FRG.

出版信息

Scand J Gastroenterol Suppl. 1989;164:46-50; discussion 50-1. doi: 10.3109/00365528909091185.

DOI:10.3109/00365528909091185

PMID:2510280

Abstract

The pharmacokinetics of rioprostil in rats has been investigated following a single intravenous or oral dose of rioprostil between 0.004 and 10 mg/kg. Rioprostil is eliminated from plasma following an intravenous dose rapidly (t1/2 = 0.22 h) and nearly exclusively by biotransformation. The high total clearance (CL = 5.4 l.h-1.kg-1) indicates an additional extrahepatic metabolism. A systemic bioavailability of 2%, in spite of a rapid and nearly complete absorption (fa = 90%), indicates an extended first-pass effect. Twenty-four hours after the administration of [3H]rioprostil the residual radioactivity in the animal amounted to less than 1% of the dose administered.

摘要

已对大鼠单次静脉注射或口服剂量为0.004至10 mg/kg的利奥前列素后的药代动力学进行了研究。静脉注射后，利奥前列素从血浆中迅速消除（t1/2 = 0.22小时），几乎完全通过生物转化消除。高总清除率（CL = 5.4 l·h-1·kg-1）表明存在额外的肝外代谢。尽管吸收迅速且几乎完全（fa = 90%），但系统生物利用度为2%，表明存在显著的首过效应。给予[3H]利奥前列素24小时后，动物体内的残留放射性低于给药剂量的1%。