Abstract: AimTo study the pharmacokinetics of fudosteine in healthy volunteers after the single and multiple dose administration. MethodsThirty-six volunteers were divided into three groups randomly, each group included six men and six women. In the single dose design, the volunteers received either a single dose of 600 mg, 400 mg or 200 mg fudosteine. After a one-week wash out period, the volunteers of 400 mg group participated in the multiple dose design in which each volunteer received 400 mg fudosteine three times a day for five consecutive days. The plasma concentrations were determined by pre-column derivatization HPLC-FL method and the pharmacokinetic parameters of fudosteine were calculated. ResultsThe obtained pharmacokinetic parameters of fudosteine in single dose of 600 mg, 400 mg and 200 mg groups were as follows: T_1/2 were (2.8±0.5), (2.7±0.5) and (3.2±0.6) h, respectively. T_max were (0.51±0.22), (0.59±0.21) and (0.48±0.18) h, respectively. C_max were (16±4), (11±3) and (6.1±1.5) μg·mL^-1, respectively. The AUC_{0-10 h} and C_max correlated linearly with doses, respectively (r>0.99). The T_max, C_max and AUC values of fudosteine in healthy male volunteers were smaller than those in female volunteers, and the T_1/2 value was longer than that in female volunteers. The obtained multi-dose pharmacokinetic parameters of fudosteine were as follows: C_ss was (4.1±0.8) μg·mL^-1; DF was 3.0±0.7; T_1/2 was (2.5±0.4) h; T_max was (0.6±0.3) h; C_max was (13.2±1.3) μg·mL^-1. ConclusionThe values of pharmacokinetic parameters in healthy volunteers were linear in the range from 200 mg to 600 mg. Statistic analysis results showed that the differences of AUC and C_max between men and women were not resulted from sexual differences, but from the weight differences. There was no significant difference in pharmacokinetic parameters between single dose and multi-dose.