Gregg M R, Jack D B, Smith S R, Kendall M J
J Clin Pharm Ther. 1987 Apr;12(2):91-9. doi: 10.1111/j.1365-2710.1987.tb00513.x.
Plasma oxprenolol concentrations were measured in eight healthy volunteers who received equivalent oral doses of the drug in the form of an aqueous solution and a 10/170 oxprenolol Oros drug delivery system. Absorption from the lower gastrointestinal tract was assessed by measurement of plasma concentrations after rectal administration of the pre-equilibrated Oros systems. Because three of the first four volunteers suffered local irritation, however, the other four volunteers received Slow Trasicor 160 mg orally as a comparative preparation. The rate of in vivo absorption after oral administration of the Oros system closely mirrored its in vitro release rate. Drug availability from Oros was reduced, however, and was equivalent to 77% of that from the oral solution. Oxprenolol was well absorbed from the rectum while the system was present in this segment of the gut. The reduced systemic availability in three of the volunteers could be accounted for largely by drug loss when the system was expelled. Slow Trasicor produced higher peaks but lower 24 h plasma concentrations than the orally administered Oros system. As judged from the relative areas under the plasma concentration-time curve, however, the availability of the drug from the two dosage forms was comparable.
在八名健康志愿者中测量了血浆氧烯洛尔浓度，这些志愿者分别以水溶液和10/170氧烯洛尔渗透泵控释给药系统的形式接受了等效口服剂量的该药物。通过直肠给予预平衡的渗透泵控释系统后测量血浆浓度来评估下消化道的吸收情况。然而，由于前四名志愿者中有三名出现局部刺激，其他四名志愿者口服160 mg盐酸心得宁作为对照制剂。口服渗透泵控释系统后的体内吸收速率与其体外释放速率密切相关。然而，渗透泵控释系统的药物利用率降低，相当于口服溶液的77%。当渗透泵控释系统存在于肠道的这一部分时，氧烯洛尔从直肠吸收良好。三名志愿者全身利用率降低很大程度上可归因于系统排出时的药物损失。盐酸心得宁产生的峰浓度较高，但24小时血浆浓度低于口服渗透泵控释系统。然而，从血浆浓度-时间曲线下的相对面积判断，两种剂型的药物利用率相当。
