ABSTRACT

The purpose of this research was to develop and optimize buoyant beads containing lafutidine by ionic-gelation method for gastroretentive delivery. The effect of two independent process variables like NaHCO 3: Polymer, Drug: Polymer ratio on % drug entrapment, % swelling and % drug release of buoyant beads containing lafutidine was optimized using 32 factorial designs. The observed responses coincided well with the predicted values, given by the optimization technique. The optimized beads showed drug entrapment efficiency 78.76+0.27%, swelling 69.90+0.13%, cumulative drug release 69.00+0.36% after 8 h; the average size of all buoyant beads ranged from 1.35+0.01 to 1.56+0.05 mm. The buoyant beads were characterized by SEM, DSC and FTIR spectroscopy for surface morphology and excipient-drug interaction analysis, respectively. All these beads showed prolong release of lafutidine over 8 h in 0.1 N HCl (pH1.2) evaluation of buoyancy of the optimized formulation in vivo in human volunteers showed that the beads were buoyant in gastric fluid for 8 h both in fasted and fed state.