“Design and Characterization of Porous Floating Beads of Lafutidine”

The aim of present research work was to design and characterize porous floating beads of lafutidine a second-generation H2–receptor antagonist. Using the emulsion gelation method, Lafutidine porous floating beads were meticulously crafted, incorporating hydrophilic polymers such as sodium alginate (serving as the gelling agent), along with hydroxypropyl methylcellulose K15M, hydroxypropyl methylcellulose K4M and Carbopol 934p as polymers. Calcium carbonate was introduced as the gas-generating agent, while calcium chloride played the crucial role of the cross-linking agent. The effect of different formulation variables was also studied. The beads were evaluated for particle size, surface morphology, percentage yield, drug entrapment efficiency, drug content, swelling index, buoyancy study and in-vitro drug release. Fourier-transform infrared spectroscopy and differential scanning calorimetry studies were carried out for compatibility studies. The micromeritic parameters of floating beads of lafutidine were within acceptable limits. The particle size was between 1210.53 ± 1.07 to 1249.46 ± 0.98 μm. When observed under scanning electron microscopy, the floating beads were spherical in shape with distinct pores inside. The percent yield was 76.04 ± 2.59 to 92.43±1.91%, entrapment efficiency was 70.91 ± 1.49 to 82.40 ± 2.41%, drug content was 71.85 ± 1.79 to 83.96 ± 1.83% and the swelling index was 67.34 ± 1.24 to 86.90 ± 1.51%. The buoyancy time was 43 ± 0.8 to 59 ± 0.5 s and the total buoyancy time was more than 12 h. The in-vitro dissolution studies showed 84.53 to 98.84% drug release in 12 h. F5 was selected as the optimized formulation as it released 98.84% of the drug in 12 h at a controlled rate, which is desired for diseases like peptic ulcer. All the formulations followed zero order kinetics indicating drug release by non-fickian release mechanism. Drug and excipient compatibility studies showed no interaction was observed.