DESIGN AND EVALUATION OF SUSTAINED-RELEASE AND BUCCAL ADHESIVE PROPRANOLOL HYDROCHLORIDE TABLETS

The release of propranolol hydrochloride incorporated into sustained-r elease and buccal adhesive tablets was studied in vitro. The formulati on containing 20% hydroxypropyl methylcellulose (HPMC) yielded good su stained-release matrix tablets. Buccal adhesive controlled-release tab lets were prepared by compression of HPMC with polycarbophil (PAA), wh ich served as the bioactive adhesive compound. The release behaviour o f buccal adhesive tablets was found to be non-Fickian. The adhesion fo rce was significantly affected by the mixing ratio of HPMC and PAA in the tablet and the weakest adhesion force was observed at the ratio of 1:1 (HPMC:PAA). Interpolymer complex formation was confirmed between HPMC and PAA in acidic medium by turbidity, viscosity and FT-IR measur ements. The kinetics of sustained-release and buccal adhesive tablets of propranolol were examined in nine healthy volunteers. Conventional propranolol (Dideral(R)) was also studied for comparison purposes. As compared to conventional propranolol (40 mg), a single dose of 20% HPM C (160 mg) produced a smoother plasma level profile, with lower and de layed peak times. Dose corrected AUG(0-8) values were greater after Di deral(R) than after 20% HPMC (168.7 +/- 80.3 vs 97.3 +/- 36.1 ng h ml( -1) p < 0.05). The buccal delivery of propranolol caused ulceration an d serious irritation that took weeks to heal, There was no significant difference (p > 0.05) in the AUG(0-4) values between 20% HPMC and buc cal adhesive tablets.