Development of Fast Dissolving Tablets of Glibenclamide Using Crospovidone and its Kneading Mixture

Abstract:

Glibenclamide (GLB) is a second generation anti-diabetic drug used for the treatment of Type –II Diabetes. The drawback of the drug is, it is practically insoluble in water and so possesses poor solubility, GI absorption and bioavailability. Hence the objective of the work is to develop fast dissolving tablets of Glibenclamide using Crospovidone (CP) as super disintegrating agent. The kneading mixtures of glibenclamide were prepared with Crospovidone in the weight ratios of 1:0.5, 1:1 and 1:1.5. The mixture, GLB : CP (1:1.5) (KM) exhibited highest dissolution rate of 99.8% in 45 min. FTIR analysis of the selected kneading mixture indicated the absence of drugpolymer interaction. Hence the tablets were prepared by using the kneading mixture GLB: CP (1:1.5) (KM) by wet granulation method. Various formulations were tried and the FDT was selected which possessed optimum characteristics of disintegration time of 20 sec, hardness of 3.5 kg/cm2 and friability of 0.34±0.61%.There is 99.9% of drug release in 20 min. The FDTs were stable without any significant changes in their initial properties of hardness, friability, disintegration time and % drug release upon storage for 4 weeks.

Key words: Glibenclamide, FDTs, Crospovidone, kneading method, Disintegration, Dissolution.