Abstract

DESIGN AND IN VITRO AND IN VIVO EVALUATION OF FLOATING MICROSPHERES OF METFORMIN HYDROCHLORIDE FOR ORAL CONTROLLED RELEASE

*Aftab Alam, Dr. Mateen Hasan Khan, Hitesh Kumar and Dr. Sudhansu Ranjan Swain

Abstract

The floating microspheres have been utilized to obtained prolonged and uniform release in stomach for development of a once daily formulation. The major advantage of preparation technique includes short processing time, lake of exposure of ingredients to high temperature, and high encapsulation efficiencies. In the present study, preparation of metformin hydrochloride floating microspheres, evaluation of Floating Drug Delivery System in vitro release, optimization of floatation and drug release pattern to match target release profile was investigated. Floating microspheres were prepared by Single Emulsion Solvent Evaporation Method using Eudragit RS100 controlling polymer and 250 mg of metformin hydrochloride per batch and its in vitro release performance was evaluated by the usual pharmacopoeial and other tests such as yield(%), particle size analysis, floating ability, drug entrapment efficiency, surface topography and release studies. The result showed that mixing ratio of components in organic phase affected the size distribution (206.3-469.8 μm), drug entrapment efficiency (58.27-40.06(% wt/wt), % yield (78.27-75.44%wt/wt), floating ability (82.67-60.84 %) and drug release of floating microspheres (53.06-74.84% after 12 hrs), floating duration (8-12 hrs) and the best results were obtained at the ratio of drug: polymer, stirring speed, droplet stabilizer(1:5, 700rpm, 10%wt/wt). In case of floating microspheres of metformin hydrochloride, the reduction in glucose levels was slower and found to be 106.00±0.54mg/dl reached 8 hours after oral administration. The sustain hypoglycemic effect observed over longer periods of time in the case of floating microspheres is due to the controlled release and absorption of metformin hydrochloride over longer period of time.

Keywords: floating microspheres, metformin hydrochloride, controlled release.