Abstract

MUCOADHESIVE BUCCAL DRUG DELIVERY SYSTEMS CONTAINING ROSIGLITAZONE MALEATE FOR TREATMENT OF TYPE II DIABETES: FORMULATION DESIGN AND IN -VITRO EVALUATION

Abstract

Mucoadhesive buccal drug delivery systems of Rosiglitazone maleate were fabricated with objective of avoiding extensive first pass metabolism and to prolong its duration of action with reduction in dosing frequency. The mucoadhesive polymers used in the formulations were Carbopol 934P and HPMC. Tablets were prepared by direct compression method using polymer in different ratios. The tablets were evaluated for thickness, hardness, weight variation, uniformity of content, surface pH study, in-vitro swelling study, matrix erosion study, Mucoadhesive strength and mucoadhesion time, in-vitro drug release study and subjected to stability study. The stability studies shown that all the formulation were stable as there was no significant change in any values under study. Formulation (F4) containing Carbopol 934P and HPMC in the ratio of (0.28571:1) shown good buccoadhesive force and maximum drug release of 99.0219% in 8 hours. The surface pH of all tablets was found to be satisfactory (pH= 5.13 � 6.19), close to buccal pH, hence no irritation would observe with these tablets. It was observed that the best formulation F4 shown surface pH 6.12 and follows release kinetics First order >Higuchi order>Korsemeyer-Peppas >zero order>Hixson Crowell order. Although majority of the formulations followed non-fickian (anomalous) diffusion mediated drug release, the release exponent �n� for formulation F8 is 0.964 (i.e., > 0.89) , which indicates that when the Carbopol 934P and HPMC ratio is 0.8, the release mechanism is undergoing a change from non-Fickian to Case II transport. The results indicate that the mucoadhesive buccal tablets of Rosiglitazone maleate may be a good choice to bypass the extensive hepatic first pass metabolism with an improvement in the bioavailability of Rosiglitazone maleate through buccal mucosa for the treatment of type II Diabetes Mellitus.

Keywords: Mucoadhesive drug delivery, buccal tablets, rosiglitazone maleate.