Development and Characterization of Floating Microspheres of Dexrabeprazole Sodium for the Treatment of Peptic Ulcer

Abstract

Dexrabeprazole sodium (DEX) is R (+)-isomer of rabeprazole. DEX has been used in the treatment of gastroesophageal reflux disease by suppressing gastric acid secretion. It acts as a proton pump inhibitor of the H+ /K+ ATPase enzyme. The purpose of this research was to prepare a floating drug delivery system of DEX. The floating microspheres can be prepared for the improvement of absorption and bioavailability of DEX by retaining the system in the stomach for prolonged period of time. Floating microspheres of DEX were prepared using different polymers like ethyl cellulose, hydroxy propyl methyl cellulose by solvent diffusion-evaporation method. The drug to polymer ratio used to prepare the different formulations was 1:7. The prepared floating microspheres were characterized for shape and surface morphology, size, percent drug loading, floating behavior, percentage yield and in vitro drug release. Formulation F1 showed good results with respect to the various evaluation parameters among various batches (F1-F8). The particle size increased with increase in polymer concentration. The drug entrapment efficiency was increased with increase in concentration of polymers. Buoyancy and the in vitro drug release decreased with respect to increase in concentration of polymers. In-vitro release and release kinetics data was subjected to different dissolution models. It was concluded that developed floating microspheres of DEX offers a suitable and practical approach for prolonged release of drug over an extended period of time and thus oral bioavailability, efficacy and patient compliance is improved.
 Keywords: Dexrabeprazole sodium, Floating drug delivery system, Microspheres, Solvent diffusion-evaporation method