A novel approach for dissolution enhancement of Ibuprofen by preparing floating granules

Abstract

Ibuprofen, a weekly acidic, non-steroidal anti inflammatory drug having high permeability through stomach but due to its solubility limitation it can’t enter in to systemic circulation and gastric empting time ranging from 30 min to 2 hr, after this time ibuprofen goes in to small intestine where it is solubilise but can’t permeate through its membrane. To improve dissolution of such drug is challenging and rational.  In present investigation, dissolution of ibuprofen improves by preparing floating granules. Floating is requiring for increasing residence time of granules in stomach. Ibuprofen must have to remain in stomach because it is mostly permeable through it. Multipurpose floating formulations was developed by preparing immediate release (for loading dose) granules containing gelucire 44/14 and sustained release floating granules containing gelucire 43/01 and small amount of gelucire 44/14.  Amount of gelucire 44/14 and gelucire 43/01 was optimized using factorial design. Amount of gelucire 44/14 (X1) and amount of Gelucire 43/01 (X2) selected as independed variable. t_100% (time require to dissolve 100 % drug) and total floating time chosen as response or depended variable. Release kinetic of ibuprofen studied by applying different model (zero order, first order, higuchi, korsmeyer-peppas, Hixson crowell and weibull).  In optimized formulation, Granules remain floated for 3 hrs. and gave 100% drug release in 150 minute. Highest R² and lowest Sum of square residual (calculated from AUC) was observed in Weibull model.