OBJECTIVE To study pharmacokintics of domestic levofloxacin mesylate in healthy volunteers after oral administration of various dose. METHODS Thirty healthy volunteers were divided into 3 grops and given single oral dose of levofloxacin mesylate 100,200,300 mg.The levofloxacin concentrations in serum and urine were determined by HPLC methods.The 3P87(pharmacokinetics program) was used for analysis of metabolism process and parameters of kinetics. RESULTS It ws found that the serum concentrations-time curves were fitted to a two-compartment model.The main pharmacokinetic parameters were as following:t_peak(1.287±0.385) h,(1.121±0.316) h,(1.386±0.233) h;t_1/2β(7.669±1.697) h,(6.596±1.207) h,(6.187±0.972) h;and AUC(11.418±1.834) mg·h·L^-1,(21.502±4.805) mg·h·L^-1,and (32.764±3.564) mg·h·L^-1,respectively.There was no significant difference of main pharmacokinetic parameters among three dose groups. CONCLUSION The disposition of levofloxacin mesylate in healthy volunteers was dose-independent.This study will provide a scientific basis for the clinical applications.