Hengstmann J H, Steinkamp B
Arzneimittelforschung. 1981;31(5):843-8.
Pharmacokinetics and metabolism are described for 3H-labelled d,l,-1-(4-hydroxy-phenyl)-1-hydroxy-2-n-butylamino-ethan (bamethane, Vasculat) in man. Following i.v. injection and p.o. ingestion of tablets and aqueous solution identical amounts of 3H-activity are excreted in urine. This fact demonstrates complete enteric absorption. After i.v. injection 40%, after oral ingestion only 30% of dose are excreted unchanged in urine. Therefore, bioavailability is calculated as 75%. A similar result is seen when the areas under the serum level curve are compared. The biological half-life is 2.5 h. Absorption proceeded rapidly peak serum levels are observed at 30 min. There is, however, a considerable first-pass metabolism.
描述了人体中3H标记的d,l-1-(4-羟基苯基)-1-羟基-2-正丁氨基乙烷(巴美生,血管舒张剂)的药代动力学和代谢情况。静脉注射以及口服片剂和水溶液后,尿液中排出的3H活性量相同。这一事实表明肠道吸收完全。静脉注射后,40%的剂量,口服后只有30%的剂量以原形从尿液中排出。因此,生物利用度计算为75%。比较血清水平曲线下的面积时也得到了类似结果。生物半衰期为2.5小时。吸收迅速,30分钟时观察到血清峰值水平。然而,存在相当程度的首过代谢。