FLOATING MICROSPHERES ENCAPSULATING CARVEDILOL FOR EFFECTIVE MANAGEMENT OF HYPERTENSION

The objective of the present study was to formulate and evaluate floating microspheres of carvedilol. Carvedilol has a terminal half-life of 7-10 hr, but most of the drug is eliminated with a half-life of about 2hr.Besidesbeingabeneficialdrugcomparedtoother drugs of the same class, it has narrow absorption window in upper part of the gastro intestinal tract, hence a floating drug delivery system is preferred, such that the formulation will be available for a longer duration than usual for absorption. Floating microspheres were prepared by emulsion solvent diffusion method using ethanol and dichloromethane as solvents. Ethyl cellulose and Hydroxy propyl methyl cellulose, HPMC K 4 M, were used to prolong the release of the drug from microspheres. The prepared microspheres were subjected to various evaluatory studies. All the microspheres were found to have a size in the range of 20-40 μ and were nearly spherical in shape. For optimization of Formulation F1 (EudragitRS100), F2 (Acrycoat S 100) and F3 (Cellulose Acetate) was selected.  The formulation F1 prepared using EudragitRS100 showed 82.5±2.76 percentage drug release AFTER 24 Hrs. as compare to other formulations.

Key words: Carvedilol, Floating microspheres, Hypertension