The objectives of this study were to elucidate factors affecting the bioadhesion property of compressed tablets consisting of hydroxypropylmethyl cellulose and carbomer and to evaluate the bioavailability and pharmacokinetics of the formulated buccal adhesive captopril tablets. Buccal adhesive controlled-release systems for the delivery of captopril were prepared by compression of hydroxypropylmethyl cellulose with carbomer, which served as the bioactive adhesive compound. The interpolymer complex formation between hydroxypropylmethyl cellulose and carbomer was characterized in an acidic medium by turbidity, viscosity and FT-IR measurements. The kinetics of buccal adhesive and conventional tablets (Kapril) of captopril were examined in eight healthy volunteers. A single dose of captopril (50 mg) was administered as buccal adhesive and commercially available conventional (Kapril) tablets on two different occasions in a randomized crossover fashion. The release behaviour of the systems containing 50 mg of captopril and two polymers at different ratios was found to be non-Fickian. The mean pharmacokinetic parameters after buccal adhesive tablet administration were: C(max), 70.6 ng/ml; t(max), 3.4 h; AUC0-8, 352.7 ng.h/ml, and after conventional tablet administration were: C(max), 310.7 ng/ml; t(max), 1.2 h; AUC0-8, 890.1 ng.h/ml. This study demonstrated that the formulated buccoadhesive therapeutic system is suitable for buccal administration of captopril.