直肠给药甲硫酸噻嗪铵后的首过效应。

First-pass effect after rectal administration of thiazinamium methylsulfate.

作者信息

Jonkman J H, van Bork L E, Wijsbeek J, Bolhuis-de Vries A S, de Zeeuw R A, Orie N G, Cox H L

出版信息

J Pharm Sci. 1979 Jan;68(1):69-72. doi: 10.1002/jps.2600680121.

Abstract

The absorption and metabolism of the quaternary ammonium compound thiazinamium methylsulfate were studied in humans using plasma concentration data and urinary excretion measurements. After giving a dose of 150 mg in suppositories, the relative bioavailability was 5.8 +/- 3.2 (SD) % of the dose, comparable to the values obtained following oral administration. The degree of first-pass effect observed after rectal administration was comparable with that after oral administration.

摘要

利用血浆浓度数据和尿排泄测量，在人体中研究了季铵化合物甲硫酸噻嗪铵的吸收和代谢。以栓剂形式给予150mg剂量后，相对生物利用度为剂量的5.8±3.2（标准差）%，与口服给药后获得的值相当。直肠给药后观察到的首过效应程度与口服给药后相当。