Percutaneous absorption of pindolol and pharmacokinetic analysis of the plasma concentration.
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.
Ogiso
T
T
Faculty of Pharmaceutical Sciences, Kinki University, Osaka, Japan.
Iwaki
M
M
Tanino
T
T
Oue
H
H
D000279:Administration, Cutaneous; D000818:Animals; D066298:In Vitro Techniques; D007275:Injections, Intravenous; D008297:Male; D010869:Pindolol / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D011817:Rabbits; D012869:Skin Absorption
D010869:Pindolol