OBJECTIVE To develop a rapid and sensitive HPLC-MS method for the analysis of rupatadine in human plasma,and study the pharmacokinetic characteristics of rupatadine fumarate tablets after a single oral dose of 10 mg in healthy volunteers.METHODS A single oral dose of 10 mg rupatadine fumarate tablets was given to 10 healthy volunteers.Blood samples were collected before dosing and at 0.25,0.5,0.75,1,1.5,2,3,4,6,8,10,12,16,24 h after a single oral dose of 10 mg.A HPLC-MS method was used to assay the concentration of rupatadine in plasma.The pharmacokinetic parameters were evaluated with PKS program.RESULTS The concentrations of rupatadine in plasma were discribed with a two-compartment model.The main pharmacokinetic parameters of rupatadine by oral administration were as follows:t_1/2(5.3±1.7)h,t_max(0.8±0.1)h,ρ_max(2.38±0.61)μg·L^-1,AUC_0-24(6.8±1.2)μg·h·L^-1,AUC_0-∞(7.3±1.3) μg ·h·L^-1.CONCLUSION The analytical method appeared to be accurate,sensitive and convenient.The pharmacokinetic profile of rupatadine fumarate tablet was similar to the published reports.