Abstract: The present work is aimed to study the pharmacokinetic parameters of optimized repaglinide floating drug delivery system (FDDS) by 2⁴ factorial designs, followed by comparison with a commercially available formulation. The main effects and interactions of formulation variables were studied by using normal and pareto charts. The optimized formulation shows a fickian diffusion drug release mechanism. Pharmacokinetic parameters of the designed drug delivery system were evaluated in rabbit models. Mean while a simple, specific high performance liquid chromatographic method was developed and validated as per biopharmaceutical specifications, the linearity was observed at the range of 110-550 ng/mL (r² = 0.999). By using methanol-phosphate buffer (pH 2.5) (70:30, v/v) as mobile phase at the flow rate of 1.0 mL/min the validation shows a better retention time of 5.2 min for repaglinide. And the same validation method was used for pharmacokinetic profile analysis of repaglinide marketed products and FDDS. The comparative pharmacokinetic results such as t_max, half-life, area under the curve, mean residence times were increased significantly for the repaglinide in FDDS than the marketed product of repaglinide except C_max and elimination rate constant.

Key words: Pharmacokinetic study, Floating drug delivery system, Rabbit model