Study of relative bioavailability of chlorpheniramine maleate tablets in healthy volunteers

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 detector after a single oral dose 8 mg of the reference formulation and the tested formulation were respectively given to 18 volunteers in randomized cross-over test. 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 ± 7.06 μg·L -1 and 14.88 ± 4.40 μg·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 ± 78.52 μg·h·L -1 and 245.09 ± 90.77 μg·h·L -1 , AUC_ 0-∞ was 292.64 ± 99.21 μg·h·L -1 and 282.04 ± 98.64 μg·h·L -1 , respectively. The pharmacokinetic parameters obtained from our studies 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.