Cid E, Mella F, Lucchini L, Cárcamo M, Monasterio J
Biopharm Drug Dispos. 1986 Nov-Dec;7(6):559-66. doi: 10.1002/bdd.2510070605.
Eight normal male volunteers received 80 mg doses of propranolol by the oral and rectal routes and 2.2 mg by intravenous administration in a crossover fashion. Plasma concentrations of propranolol were measured by a gas chromatographic method using an electron capture detector. Individual subject concentration-time data were analysed and results indicated that the data fit a two compartment model with first order absorption. An approximately two-fold higher plasma propranolol concentration was observed after rectal administration as compared with oral dosing. Statistical analysis of the difference in the total AUCs indicates a significantly higher bioavailability of propranolol administered by the rectal route. The reduced bioavailability after oral administration indicates a substantial first pass effect but that it is possible to bypass the liver, at least partially, by giving the drug rectally to man.
八名正常男性志愿者以交叉方式经口服和直肠途径接受了80毫克剂量的普萘洛尔，并经静脉注射了2.2毫克。使用电子捕获检测器的气相色谱法测定普萘洛尔的血浆浓度。对个体受试者的浓度-时间数据进行分析，结果表明这些数据符合具有一级吸收的二室模型。与口服给药相比，直肠给药后观察到血浆普萘洛尔浓度大约高出两倍。对总AUC差异的统计分析表明，经直肠途径给药的普萘洛尔生物利用度显著更高。口服给药后生物利用度降低表明存在显著的首过效应，但通过对人体直肠给药至少可以部分绕过肝脏。
