Abstract: AIM: To determine the plasma concentration of itopride hydrochloride granule and study its pharmacokinetics and bioequivalence in healthy volunteers. METHODS: A reversed-phase high performance liquid chromatography (RP-HPLC)method was established for the determination of itopride hydrochloride in human plasma after a single oral dose administration of 100 mg itopride hydrochloride granule (test preparation) and itopride hydrochloride tablet (reference preparation) in a crossover design.RESULTS: The main pharmacokinetic parameters after a single oral dose administration of 100 mg itopride hydrochloride granule and tablet were as follows:C_max 594.8 ±152.3 and 628.6 ±261.4 μg·L^-1 ,T_max 0.766 ±0.213 and 0.900 ±0.392 h, T_12ke 3.21 ±0.86 and 3.49 ±0.77 h, AUC_0-152266.0 ±1340.9 and 2339.4 ± 1831.7 μg·L^-1 ·h^-1, respectively.CONCLUSION: The relative bioavailability of itopride hydrochloride granule is 106.9 %±27.3 %.The results of statistical analysis for C_max, AUC_0-15 and AUC_0-∞ show that itopride hydrochloride granule and itopride hydrochloride tablet are bioequivalent.

Key words: reversed-phase high performance liquid chromatography, itopride hydrochloride, plasma concentration, pharmacokinetics, bioavailability, bioequievence