Comparative pharmacokinetic evaluation of extended release itopride HCI pellets with once daily tablet formulation in healthy human subjects: a two treatment, four period crossover study in fasted and fed condition

摘要

Objective: In this study, pharmacokinetics (PKs) and bioavailability of newly developed extended release (ER) Itopride HCI 150mg encapsulated ER pellets (test) and 150mg Ganaton ER once-daily (OD) tablets (reference) were compared and evaluated under fasted and fed conditions. Methods: Twelve healthy human subjects were enrolled in a single dose, randomized; two treatments, two sequences, four period crossover study. A modified and validated liquid chromatographic method was used for the estimation of Itopride HCI in plasma samples. The data were analyzed through non-compart-mental model using PK software Phoenix Winnonlin version 7. The outcome was measured on logarithmically transformed data, where p > 0.05 was considered as non-significant with 90% Cl limit of 0.8-1.25. Results: The Cmax, AUC0_f, and AUC0-oo values of Itopride HCI 150mg ER pellets versus that of OD 150mg tablets, in fed and fasted states, were within the limits specified by FDA to establish bioequivalence. The relative bioavailability of Itopride HCI 150mg ER pellets were 1.019 (fed) and 1.081 (fasted). The 90% CIs of AUC values for Itopride HCI 150mg ER pellets and OD 150mg tablets in fed versus fast were significantly greater and were not within 80-125% limit. Conclusion: The test and reference formulations had similar pharmacokinetic parameters in each condition studied. However, an increase in the amount of drug was observed in the fed state.