Formulation, In-vitro Evaluation and Optimization of Directly Compressible Glibenclamide Orodispersible Tablets
No Thumbnail Available
Date
2016-12
Authors
Journal Title
Journal ISSN
Volume Title
Publisher
Addis Ababa University
Abstract
Glibenclamide (GLM) is an orally active hypoglycaemic agent which belongs to sulphonylurea
group. It controls blood glucose level primarily acting on beta cells, which are the insulinproducing
cells of pancreatic islet tissue to increase their sensitivity to glucose and to stimulate the
production and release of more insulin. It is used for the treatment of noninsulin dependent diabetes
mellitus (NIDDM). It shows poor absorption and low bioavailability from a conventional tablet,
which is attributed to its poor water solubility. In this study crospovidone and sodium bicarbonateas
disintegration agent and dissolution enhancer, respectively, were used to formulate and optimize
orodispersible tablets (ODT) of GLM in order to minimize absorption lag time, hasten the onset of
action, improve bioavailability and compliance. Tablets were prepared by direct compression
technique at different levels of compression force and evaluated for physicochemical properties.
Those formulations of tablets which showed better performance were optimized using central
composite design. The optimized tablets were compared for their release propertieswith marketed
products.
The results showed simultaneous optimization of the dependent variables offered the most
desirable representative optimum formulation, within the common optimum section, with hardness
of 5.75 Kg/cm2, friability of 0.2%, wetting time of 16.5 sec, disintegration time of 9.4 sec and
cumulative drug release of 98.0%in 30min at concentration of 9.73mg crospovidone, 30.33mg
sodium bicarbonate and 16.3KN compression force. The validity of obtained optimal point was
confirmed by the low magnitude of percent prediction errors of the response variables.
Comparative study of the cumulative drug release of GLM within 60 min between marketed
conventional tablet of GLM (Daonil®) and the optimized ODT with the model independent
method revealed that there was a significant difference between the two formulations with a
dissimilarity factor ƒ1value of 73.25% and similarity factor ƒ2value of 9.01%.Thus, the results of
this study showed ODT of GLM possess significantly rapid disintegration and enhanced
dissolution profiles.
Keywords:Glibenclamide, Orodispersible tablets, crospovidone, Sodium bicarbonate,
Direct compression, central composite design, Optimization
Description
Keywords
Glibenclamide, Orodispersible tablets, Crospovidone