FORMULATION AND EVALUATION OF BUCCAL PATCHES OF CARVEDILOL PHOSPHATE

Abstract

Carvedilol is a non - selective adrenergic antagonist with no intrinsic sympathomimetic activity widely used to treat essential hypertension and an gina pectoris. Although it is completely absorbed from the gastrointestinal tract, the systemic availability is approximately 2 5 - 35% because of high first pass metabolism. The aim of the present study was to develop the mucoadhesive buccal patches of carvedilol phosphate and to evaluate in vitro performance of buccal patches of carvedilol by using Chitosan, PVP K 30, PVP K 90, HPM C, and propylene glycol as plasticizer. IR spectra of carvedilol along with polymers indicated no interaction between carvedilol and all the four selected polymers. After optimizi ng the formula from the three combinations of polymeric patches, three formul as were selected for drug loading, respectively from each combination they were loaded with 30mg (D 1 ), 40mg (D 2 ), 50mg (D 3 ) and 60mg (D 4 ) carvedilol phosphate. The in vitro studies shows that there was an increase in the extend of duration of drug releas e with increase in concentration of chitosan in the formula. Kinetic of release of drug from all the drug loaded batches were found to follow first order. The formulated buccal patches of carvedilol phosphate was found to be suitable buccal delivery system to avoid the first pass metabolism of carvedilol phosphate which will have other added benefits like longer duration of action and quicker onset of a ction as compared to tablets of carvedilol phosphate.