DESIGN AND EVALUATION OF BUCCOADHESIVE CONTROLLED RELEASE FORMULATIONS OF PROCHLORPERAZINE MALEATE

Objective: The Purpose of this work was to design mucoadhesive tablets of prochlorperazine maleate to release the drug in buccal cavity for an extended period of time in order to avoid the first-pass metabolism.Methods: Six formulations were prepared using different polymer like Xanthan gum, Locust bean gum, Carbopol 974P NF, HPMC K100MCR, Polyox-WSR301 and Gantrez AN139 as a mucoadhesive and controlled release agents. The formulations were tested for content uniformity, thickness, weight variation, friability, in vitro drug release, in-vitro bio-adhesion, swelling index and residence time.Results: Drug excipient compatibility studies performed using DSC. The DSC studies revealed endothermic peak at 200o–205oC for Prochlorperazine maleate. Similarly endothermic peaks were obtained for separate excipient when heated in the range of 50-300 °C indicating their melting points. There was no separate peak observed when the drug was mixed with the different polymers like Xanthan gum, locust bean gum, Carbopol 974 P, HPMC K100 MCR, Gantrez AN139 and Polyox-WSR301 in ratio (1:1) indicating that no interaction took place between drug and polymers used in the study. Dissolution studies of the tablets of the optimized batch (BDS-6) containing Carbopol 974P (CP) and HPMC K100 MCR showed extended release 90.65% up to 24 hr. The bioadhesive force of optimized formulation is 12.18±.011 gm and the maximum swelling index was observed in 3.87±.0057 h.Conclusion: From the study it can be concluded that formulation BDS-6 containing Carbopol and HPMC K100 MCR give a promising result for sustained release action of PrM. Â