Aim:To study the pharmacokinetics of oral administration of fudosteine in healthy volunteers.Methods:36 healthy volunteers were randomly grouped into three pools,each of with consisted of 12,and were orally given 600,400,and 200 mg of fudosteine tablets in a single of multiple modes.After plasma sampling,plasma concentration of fudosteine were determined by HPLC equipped with a fluorescence detector.Results:For the groups receiving 600,400,and 200 mg in a single mode,c_(max) were found to be(22.44±7.61),(12.91±2.93),(6.53±1.61)μg/mL;t_(max) were(0.52±0.37),(0.44±0.15),(0.40±0.21)h.Following oral dosing of 400 mg of fudosteine tablets in multiple modes,c_(max) and t_(max) were found to be(13.64±4.39)μg/mL,(0.55±0.50)h respectively.And c_(ss) was estimated to be(3.67±0.95)μg/mL.After co-administration of 200 mg of fudosteine tablet with a meal,c_(max) was found to be(3.37±0.68)μg/mL and t_(max) was(1.40±0.78)h. Conclusion:For the three groups given three doses of fudosteine,pharmacokinetics parameter such as t_(max),K,t_(1/2),MRT were similarly.However,both magnitudes of c_(max) and AUC_(0-τ)were dose-dependent.Mode of administration didn′t result in significant difference in the pharmacokinetic parameters(P>0.05).Moreover,parameters,c_(max) and t_(max),had significant difference between the fasting and fed groups(P<0.01).