Abstract:

Objective: To study the pharmacokinetics and bioequivalence of domestic and imported Flupentixol and Melitracen tablets in healthy subjects. Methods: Twenty-two healthy male subjects in a randomized crossover design were given a single oral dose of 10 mg domestic and imported Flupentixol and Melitracen tablets. Plasma concentrations of the subjects were determined by liquid chromatography-tandem mass spectrometry（LC-MS/MS）. The pharmacokinetic parameters were calculated applied SigmaPLot 2001 and Origin 6.0 software. Results: The main pharmacokinetic parameters of domestic and imported Flupentixol and Melitracen were as follows. Flupentixol: Cmax were 164.8 ±55.2 and 161.5 ±51.9 pg·mL^-1; Tmax were 9.0 ±4.5 and 9.6 ±3.9 h; AUC_0→t were 5 622 ±2 243 and 5 412 ±1 677 pg·h^-1, respectively. Melitracen: C_max were 10.9 ±6.2 and 9.6 4±.4 ng·mL^-1; T_max were 4.7 ±0.9 and 4.4 1.±1 h; AUC_0→t were 312 1±55 and 291 ±139 ng·h^-1, respectively. The statistic analysis of two formulations was conducted by analysis of variance, two one-sided tests and confidence intervals, which demonstrated that there were no significant differences between domestic and imported formulations in main pharmacokinetic parameters （P > 0.05）. The mean relative bioavailability of
domestic formulation of Flupentixol was 105.42 ±22.23%, and Melitracen was 107.29 ±20.40% （n=24）. Conclusion: The domestic Flupentixol and Melitracen are bioequivalent to the imported formulation.

Key words: Flupentixol, melitracen, LC-MS/MS, pharmacokinetics, bioequivalence