Abstract

DEVELOPMENT AND EVALUATION OF MUCOADHESIVE BENEDIPINE FORMULATION

V. V. B. K. Mishra*, S. Sethy, A.K. Rath

Abstract

The main objective of the present study was to extend the GI residence time of the dosage form and control the release of Benedipine using mucoadhesive tablet. The preparation was done to achieve controlled plasma level of the drug which is especially useful after 8 to 12 weeks of monotherapy. The method of preparation is direct compression by using simplex lattice design .It was was followed by optimization of various evaluation parameters. Taking into account these parameters final formulation was prepared. The tablets were evaluated for, hardness, thickness, weight variation, drug content mucoadesion and swelling index. The study on mucoadhesive strength and time was followed by in-vitro drug release study. Stability studies shows that all the formulation was stable as there was no significant change in any values under study. The Formulation (F4) which contains drug, Carbopol 934P and HPMC of ratio (1:6.5:18.5) shown good buccoadhesive force and maximum drug release at 99.0219% in 8 hours. The pH of surface of all tablets was found to be optimum (pH= 5.13 – 6.19), which is close to buccal pH .Irritation is least for these tablets. It was observed that the best formulation F4 shown surface pH 6.12 and follows release kinetics i.e., First order >Higuchi order>Korsemeyer-Peppas >zero order>Hixson Crowell order. Majority of the formulations followed non-fickian diffusion mediated drug release but the release exponent ‘n’ for formulation F8 (0.964 > 0.89), shows that when the Carbopol 934P and HPMC ratio is 0.8, the release mechanism undergoes a change from non-Fickian of Case II transport. The results indicates that the mucoadhesive buccal tablets of Benedipine may be a good choice to bypass the extensive hepatic first pass metabolism which improves in the bioavailability of Benedipine maleate through buccal mucosa to treat type II Diabetes Mellitus.

Keywords: Mucoadhesive drug delivery, Buccal tablets Benedipine, HPMC K4M, PEG 940.