Tse F L, Sanders T M, Reo J P
Arch Int Pharmacodyn Ther. 1980 Dec;248(2):180-9.
The pharmacokinetics of propranolol in a fasted dog was examined following single oral, intraportal and intravenous doses. Extensive tissue uptake of propranolol occurred after intravenous dosing, the overall distribution volume was 11 liters/kg. Biological half-life was 1.5 hr, but was prolonged after oral and intraportal drug administration. Following oral doses, the absorption efficiency of propranolol as unchanged drug was 71%, while first-pass metabolism accounted for a further loss of 62% prior to its reaching the systemic circulation. Accordingly, the overall oral bioavailability was 27%.
在禁食犬中,分别单次口服、门静脉注射和静脉注射普萘洛尔后,对其药代动力学进行了研究。静脉给药后,普萘洛尔出现广泛的组织摄取,总体分布容积为11升/千克。生物半衰期为1.5小时,但口服和门静脉给药后延长。口服给药后,普萘洛尔以原形药物形式的吸收效率为71%,而在其到达体循环之前,首过代谢又导致了62%的损失。因此,总体口服生物利用度为27%。