Lo M W, Effeney D J, Pond S M, Silber B M, Riegelman S
J Pharmacol Exp Ther. 1982 May;221(2):512-5.
We studied whether or not propranolol underwent presystemic metabolism in the gastrointestinal wall in five dogs. The dogs were studied before and four weeks after creation of a portacaval transposition. Before surgery, systemic bioavailability of the oral dose was 8 +/- 8% (mean +/- S.D.), whereas after transposition the bioavailability was 102 +/- 9%. The systemic plasma clearance increased from 766 +/- 192 to 976 +/- 280 ml/min. The terminal half life and apparent volume of distribution after transposition were not significantly different from those obtained preoperatively. Our results indicate that there is complete absorption but no metabolism of propranolol by the gastrointestinal wall.
我们研究了普萘洛尔在五只狗的胃肠道壁中是否进行首过代谢。在建立门腔静脉转位术前和术后四周对这些狗进行了研究。手术前,口服剂量的全身生物利用度为8±8%(平均值±标准差),而转位术后生物利用度为102±9%。全身血浆清除率从766±192增加到976±280毫升/分钟。转位术后的终末半衰期和表观分布容积与术前获得的值无显著差异。我们的结果表明,普萘洛尔在胃肠道壁中能完全吸收但无代谢。