关键词: 吗氯贝胺缓释片, 吗氯贝胺缓释片, 吗氯贝胺缓释片, 高效液相色谱法, 高效液相色谱法, 高效液相色谱法, 药代动力学, 药代动力学, 药代动力学, 多剂量, 多剂量, 多剂量

Abstract: Aim To investigate the pharmacokinetic characteristics of moclobemide sustained release tablets after multiple oral dose administration in healthy Chinese volunteers. Methods Moclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg once daily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide in plasma were determined by reversed-phase high performance liquid chromatography. The partial pharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results The concentration-time profile fitted an one-compartment model best. The steady-state pharmacokinetic parameters of moclobemide sustained release tablets after multiple oral doses were as follows: Cmax was (1 950±156)μg·L^-1, Tmax was (6.00±1.55) h, T1/2(kel) was (3.14±0.12) h, AUCss0-24 was (22836±1842) μg·h·L^-1, MRT was (7.68±0.36) h, CL/F(s) was (20.2±2.1) L·h^-1, and V/F(c) was (91.4±9.4) L, respectively. No marked adverse events were noted during this study. Conclusion The formulation has a sustained-release effect and good tolerance in the healthy volunteers, which provides useful information for clinical practice.

Key words: moclobemide sustained release tablets, moclobemide sustained release tablets, high performance liquid chromatography, high performance liquid chromatography, pharmacokinetics, pharmacokinetics, multiple dose, multiple dose