Relative bioavailability of levofloxac in hydrohloride capsulein healthy volunteers

Aim To investigate the pharmacokinetics and relative bioavailability of levofloxacin hydrochloride capsule.Methods A single 200 mg oral dose of either capsule or tablet was given to 12 healthy male volunteers in randomized self-crossover way.Plasma levofloxacin concentration was determined by high performance liquid chromatography. The concentration-time data of levofloxacin was fitted to two-compartment model with first-order absorption and the bioequivalence of the two formulations were evaluated by the analysis of variance and the two one-sided t-test. Results The pharmacokinetic parameters were as follows:capsule:Cmax=(3.18±0.57) mg·L-1, tmax=(0.83±0.33) h, AUC0～24=(19.95±2.86) mg·h·L-1,t1/2(β)=(7.75±2.04) h; tablet : Cmax=(2.96±0.43) mg·L-1,tmax=(0.96±0.33) h, AUC0～24=(21.49±1.88) mg·h·L-1,t1/2(β)=(6.82±0.84) h. Relative bioavailability of capsule was (93.0±11.8)% compared with tablet. Conclusion The two formulations are of bioequivalence.