The aim of this study was to evaluate drug release from a bisoprolol patch preparation containing 4 mg bisoprolol and its pharmacokinetics after an 8-h application. The residual drug in the preparation and the pharmacokinetics after removing the preparation were monitored in healthy voluneers and patients. In the first study, 11 volunteers were enrolled and the patch was applied for 8h. In the second study, 8 patients were enrolled and the patch was applied once daily for 24h. The amount of residual bisoprolol in the patch and serum concentration of bisoprolol were determined by high-performance liquid chromatography. Percentage of drug release from the patch was 82.6±8.1% in volunteers and 89.4±5.5% in patients, with no significant difference between two groups. Percentage of drug release in patients was similar to the value given in the drug interview form (88.3±3.7%). No difference in the time of reaching maximum drug concentration (Tmax) was abserved between volunteers and the interview form data (10.9±1.6h vs. 10.0±2.1h), but the maximum drug concentration ( Cmax) and elimination half-life (T1/ 2) were slightly lower in volunteers than in the interview form data (Cmax : 5.3±3.2 ng/mL vs. 6.5±2.5 ng/mL,T1/ 2 : 13.7±2.7h vs. 15.0±2.7h). These results suggest that there are no differences in drug release and pharmacokinetics of the bisoprolol patch preparation when the patch preparation was applied for 8 and for 24h.