Design, development, and biopharmaceutical properties of buccoadhesive compacts of pentazocine

Buccoadhesive compacts (BCs) of pentazocine (PZ) were prepared by the direc t compression method using polymers like carbopol 974P (CP 974P) and hydrox ypropyl methylcellulose (HPMC K4M) in ratios of 1 : 0 (batch B-1), 1 : 1 (B -2) 1 : 2 (B-3), 1 : 4 (B-4), and 0 : 1 (B-5). The compacts were evaluated for thickness uniformity, weight variation, drug content uniformity and swe lling index. Swelling was increased with an increase in HMPC K4M content in the compacts. An in vitro assem bly was developed to measure and compare t he bioadhesive strength of compacts. The maximum bioadhesive strength was o bserved in compacts formulated with a combination of CP 974P and HPMC K4M. The compacts were evaluated in vitro for 24 hr in pH 6.6 phosphate buffer u sing a standardized dissolution apparatus. The data were evaluated by a sim ple power equation (M-t/M-infinity = Kt(n)); it was observed that all the c ompacts followed non-Fickian release kinetics. Same of the buccoadhesive co mpacts were evaluated in vivo in rabbits. The compacts gave controlled bloo d level profiles with a twofold to threefold increase in area-under-the-cur ve (AUC) values in comparison to oral administration of aqueous drug soluti on.