چکیده (انگلیسی):

The purpose of this research was to develop and evaluate buccal mucoadhesive controlled
release tablets of lercanidipine hydrochloride using polyethylene oxide and different viscosity grades of
hydroxypropyl methylcellulose individually and in combination. Effect of polymer type, proportion and
combination was studied on the drug release rate, release mechanism and mucoadhesive strength of the
prepared formulations. Buccal mucoadhesive tablets were made by direct compression and were
characterized for content uniformity, weight variation, friability, surface pH, thickness and mechanism of
release. In order to estimate the relative enhancement in bioavailability one optimized formulation was
evaluated in rabbits. Further, placebo tablets were also evaluated for acceptability in human subjects.
Results indicated acceptable physical characteristics of designed tablets with good content uniformity and
minimum weight variation. Drug release and mucoadhesive strength were found to depend upon
polymer type, proportion and viscosity. The formulations prepared using poly ethylene oxide gave
maximum mucoadhesion. The release mechanism of most formulations was found to be of anomalous
non-Fickian type. In vivo studies of selected formulation in rabbits demonstrated significant enhancement
in bioavailability of lercanidipine hydrochloride relative to orally administered drug. Moreover, in human
acceptability studies of placebo formulations, the designed tablets adhered well to the buccal mucosa for
more than 4 h without causing any discomfort. It may be concluded that the designed buccoadhesive
controlled release tablets have the potential to overcome the disadvantage of poor and erratic oral
bioavailability associated with the presently marketed formulations of lercanidipine hydrochloride.