Multiple-dose pharmacokinetics of ceftibuten in healthy volunteers.
The pharmacokinetics of ceftibuten, a new cephalosporin antibiotic, and its conversion product, ceftibutentrans, were studied in healthy male volunteers following daily oral administration of a 400-mg capsule for 7 days. Mean concentrations of ceftibuten in plasma obtained on day 5 were similar to those obtained on day 7. Analysis of variance indicated that the concentrations in plasma on days 5 and 7 were at steady state. The mean accumulation factor was 1.14 for day 5 and 1.13 for day 7. The half-life (2.4 h) was independent of the duration of drug administration, and the mean maximum concentration of drug in plasma was 18 to 19 micrograms/ml. Urinary excretion was the major elimination route for ceftibuten, by which 57 to 59% of the drug was excreted unchanged over a 24-h period. The amounts of ceftibuten-trans in plasma and urine were low.
Lin
C
C
Department of Drug Metabolism and Pharmacokinetics, Schering-Plough Research Institute, Kenilworth, New Jersey 07033, USA.
Radwanski
E
E
Affrime
M
M
Cayen
M N
MN
D000328:Adult; D000077722:Ceftibuten; D002511:Cephalosporins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male
D002511:Cephalosporins; D000077722:Ceftibuten