Abstract: AIM: To study pharmacokinetics and bioavailability of chlorpheniramine maleate tablets in young healthy volunteers.METHODS: The chlorpheniramine concentrations in plasma were determined by HPLC method with UV detectoraftera single oral dose 8 mg of the reference formulation and the tested formulation were respectively given to 18 volunteers in randomized cross-overtest.The pharmacokinetics parameters were calculated by 3P97 software.RESULTS AND CONCLUSION:The concentration-time curves of two formulations fitted to a one-compartment open model.The C_max was 15.74±7.06μg·L^-1 and 14.88±4.40μg·L^-1,t_max was 3.9±1.2 h and 4.5±0.8 h,t_1/2ke was 15.54±3.76 h and 14.49±3.24 h,AUC_0-t was 248.86±78.52μg·h·L^-1 and 245.09±90.77μg·h·L^-1,AUC_0-∞ was 292.64±99.21μg·h·L^-1 and 282.04±98.64μg·h·L^-1,respectively.The pharmacokinetic parameters obtained from ourstudies showed no significant difference between two formulations (P>0.05).The relative bioavailability of F_0-t and F_0∞ of tested formulation were (104.1±36.1) % and (103.2±35.6) %,respectively.The two formulations are bioequivalent.

Key words: chlorpheniramine, HPLC, pharmacokinetics, bioavailability, bioequivalence