Abstract
The present investigation is concerned with formulation and evaluation of Mucoadhesive buccal tablets containing antidiabetic drug, Glimepiride to circumvent the first pass effect and to improve its bioavailability with reduction in dosing frequency and dose related side effects. The tablets were prepared by direct compression method. Six formulations were developed with varying concentrations of polymers like Carbopol 934P, HPMCK4M and Chitosan. The tablets were tested for weight variation, hardness, surface pH, drug Content uniformity, percentage swelling index, bioadhesive strength, ex-vivo residence time in-vitro drug dissolution study, In-vitro drug release kinetic study, ex-vivo permeation study and Stability study. FTIR studies showed no evidence on interactions between drug, polymers and excipients.The best in-vitro drug release profile was achieved with the formulation FIII which contains the drug, Carbopol 934p and HPMC K4M in the ratio of 1:3.75:10. The surface pH, bioadhesive strength, ex-vivo residence time and swelling index of formulation FIII was found to be 6.88±0.5, 41.6±0.15g, 330min and 191.94±0.71%, respectively. The formulation FIII, containing 4 mg of Glimepiride exhibited 6 h sustained drug release i.e. 99.32±0.5% with desired therapeutic concentration. The drug permeation from the formulation FIII was slow and steady and 3.56 mg of Glimepiride could permeate through sheep buccal membrane with a flux of 0.27 mg hr-1 cm-2.The in-vitro release kinetics studies reveal that all formulations fits well with zero order kinetics and followed non-Fickian diffusion mechanism. As in-vitro dissolution studies and in-vitro buccal permeation study showed satisfactory results, it can be further subjected to in-vivo studies in normal and diseased volunteers to find out the adverse effects, by pharmacodynamics andPharmacokinetic parameters.
