Ogiso T, Iwaki M, Tanino T, Oue H
Faculty of Pharmaceutical Sciences, Kinki University, Osaka, Japan.
J Pharmacobiodyn. 1992 Jul;15(7):347-52. doi: 10.1248/bpb1978.15.347.
The percutaneous (p.c.) absorption of pindolol, a beta-blocker, through rabbit skin was examined by in vitro and in vivo studies. Additionally, for practical use of the transdermal system (TTS), a trial for sustaining a suitable plasma concentration of pindolol by using a rate-controlling membrane and for describing plasma drug levels after p.c. application by using a simple pharmacokinetic model was tested. As a result, the drug penetrated through rabbit skin in vitro at a zero-order rate. In vivo, the drug was also absorbed through the skin from a gel base with or without enhancers. The gel preparation with Azone (Rp. 2) gave high plasma levels of pindolol. The transdermal system produced with Rp. 2 and a rate-controlling membrane (Hipore 4050) provided relatively constant plasma levels for 48 h. The model presented could describe the time course of plasma pindolol concentrations following p.c. application of the systems.
通过体外和体内研究检测了β受体阻滞剂吲哚洛尔经皮（p.c.）透过兔皮肤的情况。此外，为了透皮系统（TTS）的实际应用，测试了使用速率控制膜维持吲哚洛尔合适血浆浓度的试验，以及使用简单药代动力学模型描述经皮给药后血浆药物水平的试验。结果，药物在体外以零级速率透过兔皮肤。在体内，药物也从含或不含促进剂的凝胶基质中经皮肤吸收。含氮酮（Rp. 2）的凝胶制剂使吲哚洛尔的血浆水平较高。用Rp. 2和速率控制膜（Hipore 4050）制成的透皮系统在48小时内提供相对恒定的血浆水平。所提出的模型可以描述经皮应用该系统后血浆吲哚洛尔浓度的时间过程。
