Pharmacokinetics of FK027 (cefixime) in healthy volunteers after intravenous injection.

The pharmacokinetics of FK027 was investigated in 6 healthy male volunteers after intravenous injection of 100mg both without and with oral probenecid 1g by a two-way crossover design. The serum concentrations of FK027 without probenecid declined biphasically. The distribution half-life (t1/2α) was 0.148±0.015hr and the elimination half-life (t1/2β) was 2.519±0.070hr. The volume of distribution of the central compartment (Vc) was 4.032±0.379 L and the volume of distribution of the peripheral compartment (Vt) was 7.074±0.576 L. The total body clearance (Clbody) was 58.5±94.63ml/min and the renal clearance (Clr) was 37.40±1.82ml/min. The unchanged drug excreted in the 24-hr urine was 64.8±3.5%. When FK027 was given with probenecid, the serum concentrations and area under the concentration-time curve (AUC) increased significantly and t1/2β and the volume of distribution at steady state (Vdss) increased slightly, but Clbody and Clr decreased. These results indicate that FK027 is rapidly distributed to the tissues and thereafter gradually eliminated from the body, and it is excreted from the kidneys, mainly through glomerular filtration and to some extent through renal tubular secretion.