Comparative Pharmacokinetics of Cephalexin, Cefaclor, Cefadroxil, and CGP 9000

Abstract

In a randomized crossover study, the pharmacokinetics of three new cephalosporin antibiotics, cefaclor, cefadroxil, and CGP 9000, in comparison to cephalexin, were determined after oral administration, by capsules, of 1,000 mg on an empty stomach in 12 normal subjects. Serum concentrations were measured during a period of 8 h, and urine recovery was measured during 24 h. The significant parameters of bioavailability of an orally administered substance were determined. The maximal serum concentrations ( y _max ) for cephalexin, cefaclor, cefadroxil, and CGP 9000 (in milligrams per liter) were: 38.8 ± 8.1; 34.6 ± 7.8; 33.0 ± 5.4; and 23.3 ± 7.3, respectively. The areas under the curve (in hours × milligrams per liter) were: 93.0 ± 14.8; 74.5 ± 9.9; 70.1 ± 9.0; and 108.5 ± 18.4, respectively. In a further crossover study with six subjects, 1,000 mg of cephalexin and of cefadroxil were given during a standard breakfast. The y _max of cephalexin decreased to 23.1 ± 6.6 mg/liter, in contrast to cefadroxil, with an unchanged y _max of 32.7 ± 3.4 mg/liter.