Chlorhexidine, which is a gold standard for antiplaque agents, was prepared (is a buccoadhesive controlled-release drug formulation. The released amount and effectiveness of the antibacterial properties of the formulations were determined in in vivo and in vitro studies. In laboratory studies, nearly 40% of the total amount of the drug was released over 4 h. Clinically, first day results up to 4 h showed a statistically significant reduction of the bacterial amount in the drug-loaded side of oral mucosa. The results for 1 and 4 days were not statistically significant in the tablet group. The usefulness of the tablet dosage form was also assessed in the subjects.