Design and Development of Rebamipide Solid Dispersion-Loaded Floating Beads for Ameliorated Therapeutics

Abstract

Objectives Rebamipide, a gastroprotective drug, is used for preventing and treating ulcers but it has low aqueous solubility leading to poor bioavailability (10%). It acts both locally and systemically to provide gastroprotection and ulcer healing effects. The therapeutics of Rebamipide can be improved by enhancing its aqueous solubility and by sustaining its release in the stomach. Materials and Methods The above objective was fulfilled by preparing solid dispersion of Rebamipide by solvent evaporation method for aqueous solubility enhancement which was incorporated in floating beads by emulsion gelation method using different concentrations of sodium alginate and olive oil for prolonged gastroretention. The beads were characterized for size, swelling, entrapment efficiency, floating lag time, floating time and in-vitro drug release. Results and Discussion The solubility of rebamipide in solid dispersion was found to be 18.66 mg/mL which was much greater than its normal value (1.3 µg/mL). The size of beads varied between 2.03 mm-2.52 mm. The swelling index was found to be 12-28%. Entrapment efficiency was 90.1-96.9% proving excellent entrapment of drug by the method chosen. Floating lag time of optimized formulation (F6) was 3 sec with 90.2% drug release at12 hr showing adequate sustenance of drug release. Conclusion The solid dispersion loaded floating beads would prove effective in preventing and treating stomach ulcers because of enhanced aqueous solubility of drug in solid dispersion form resulting in higher drug concentration in gastric fluid, sustained release of drug and greater gastroretention time, giving improved therapeutics both locally and systemically.

Keywords: Peptic Ulcer; Rebamipide; Poloxamer 407; Solid Dispersion; Floating Beads