Formulation In-vitro Evaluation And Optimization Of Directly Compressible Glibenclamide Orodispersible Tablets

Glibenclamide (GLM) is an orally active hypoglycaemic agent which belongs to sulphonylurearngroup. It controls blood glucose level primarily acting on beta cells, which are the insulinproducingrncells of pancreatic islet tissue to increase their sensitivity to glucose and to stimulate thernproduction and release of more insulin. It is used for the treatment of noninsulin dependent diabetesrnmellitus (NIDDM). It shows poor absorption and low bioavailability from a conventional tablet,rnwhich is attributed to its poor water solubility. In this study crospovidone and sodium bicarbonateasrndisintegration agent and dissolution enhancer, respectively, were used to formulate and optimizernorodispersible tablets (ODT) of GLM in order to minimize absorption lag time, hasten the onset ofrnaction, improve bioavailability and compliance. Tablets were prepared by direct compressionrntechnique at different levels of compression force and evaluated for physicochemical properties.rnThose formulations of tablets which showed better performance were optimized using centralrncomposite design. The optimized tablets were compared for their release propertieswith marketedrnproducts.rnThe results showed simultaneous optimization of the dependent variables offered the mostrndesirable representative optimum formulation, within the common optimum section, with hardnessrnof 5.75 Kg/cm2, friability of 0.2%, wetting time of 16.5 sec, disintegration time of 9.4 sec andrncumulative drug release of 98.0%in 30min at concentration of 9.73mg crospovidone, 30.33mgrnsodium bicarbonate and 16.3KN compression force. The validity of obtained optimal point wasrnconfirmed by the low magnitude of percent prediction errors of the response variables.rnComparative study of the cumulative drug release of GLM within 60 min between marketedrnconventional tablet of GLM (Daonil®) and the optimized ODT with the model independentrnmethod revealed that there was a significant difference between the two formulations with arndissimilarity factor ƒ1value of 73.25% and similarity factor ƒ2value of 9.01%.Thus, the results ofrnthis study showed ODT of GLM possess significantly rapid disintegration and enhancedrndissolution profiles.rnKeywords:Glibenclamide, Orodispersible tablets, crospovidone, Sodium bicarbonate,rnDirect compression, central composite design, Optimization

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