Human Bioavailability

Ibuprofen self-emulsified drug delivery system (IBSEDDS) has been prepared, characterized and optimized to release 100% drug in one hour. The optimal formulation was subjected to stability and bioavailability studies in human volunteers. The stability was conducted under different storage temperature (4oC, room temperature and 37oC) for 8 months and evaluated for in-vitro drug release, particle size and turbidity. Bioavailability was evaluated after administration of a single oral dose of two formulations, test (HPMC capsule containing IBSEDD) and reference (HPMC capsule containing 50 mg drug in soybean oil), by 6 health human volunteers. The results showed that IBSEDDS was stable under different storage temperatures and the drug was more stable at 4oC. The changes in particle size and turbidity were lesser at room temperature.  The pharmacokinetic parameters for test/reference were: the Cmax , 0.892/0.468 ug/ml,  the Tmax, 1/1.5hr and the AUC0-∞, 3.956/1.986 mg.hr/ml. The % RBof IBSEDDS was 199.114. In a conclusion, the IBSEDD formulation stored at 4oC were more stable regarding drug content but samples stored at room temperature were more stable regarding particle size and turbidity. The IBSEDD formulation showed higher rate and extent of drug absorption and higher bioavailability compared to the oily drug solution.