Corbo M, Liu J C, Chien Y W
Controlled Drug-Delivery Research Center, Rutgers University College of Pharmacy, Piscataway, NJ 08855-0789.
J Pharm Sci. 1990 Jul;79(7):584-7. doi: 10.1002/jps.2600790707.
The systemic bioavailability of propranolol was evaluated following oral and transdermal administration in rabbits. Using a four-way crossover study, the bioavailability of propranolol following oral administration was determined to be 12.3 +/- 5.9%, indicating that propranolol is subject to extensive hepatic first-pass metabolism in rabbits. Transdermal delivery of propranolol, via an adhesive delivery device, resulted in a bioavailability of 74.8 +/- 10.1%, indicating that the transdermal delivery of propranolol can significantly increase systemic bioavailability over oral administration. Skin irritation studies indicated that neither propranolol nor the adhesive used in the device caused any appreciable skin irritation.
在兔体内口服和经皮给药后,对普萘洛尔的全身生物利用度进行了评估。采用四交叉研究,口服给药后普萘洛尔的生物利用度测定为12.3±5.9%,表明普萘洛尔在兔体内经历广泛的肝脏首过代谢。通过粘性给药装置经皮递送普萘洛尔,生物利用度为74.8±10.1%,表明普萘洛尔经皮递送相比口服给药可显著提高全身生物利用度。皮肤刺激性研究表明,普萘洛尔及装置中使用的粘合剂均未引起任何明显的皮肤刺激。