Abstract
Author(s): M. Sunitha1*, A. Padma1, B. Balaji1, V.Ravi Krishna2and M. Vamshi krishna
Buccal drug delivery system is used to improve oral bioavailability by avoiding first pass metabolism. Chlorpheneramine maleatea Histamine H1 antagonist used in allergic reactions, hay fever, rhinitis, urticaria, and asthma. It is absorbed rapidly but incompletely when given orally and undergoes first pass metabolism resulting in a low absolute bioavailability .The objective of this study was to develop effective mucoadhesive buccal tablets of Chlorpheneramine maleate to improve its bioavailability. Buccal tablets of Chlorpheneramine maleate were prepared by direct compression method using bioadhesive polymers like Xanthan gum, HPMCK4M by taking polymers in different ratios with drug. Then these were evaluated for different parameters such as thickness, hardness, weight variation, content uniformity, swelling index, and surface pH, ex vivobioadhesive strength, in vitrodrug release, ex vivo drug permeation and ex vivoresidence time. In vitroassembly was used to measure the bioadhesive strength of tablets with fresh porcine buccal mucosa as model tissue. The tablets were evaluated for in vitrorelease in pH 6.6phosphate buffer for 6 hrs in standard dissolution apparatus. In order to determine the mode of release, the data was subjected to Zero order, first order, Higuchi, Korsmeyer and Peppas diffusion model. The formulation Fa3 (HPMCK4M in 1:15 ratio with drug) followedFirst order and Korsmeyer and Peppas release kinetics governed by Non-Fickian mechanism, i.e. the drug release proceeded by both diffusion as well as erosion of the polymer. Therefore, the release of drug from the prepared tablets is controlled by the initial swelling of the polymer, followed by drug diffusion through the swollen polymer and slow erosion of the polymer