Pharmacokinetics and absolute bioavailability of oral cefuroxime axetil in the rat.
The objectives of this study were to determine the oral bioavailability of cefuroxime (C) and to evaluate the pharmacokinetic model that best describes the plasma concentration behaviour following single intravenous (IV), intraperitoneal (IP) and oral single doses. The same dose of C was administered by IV, IP and oral routes to three separate groups of rats (2.02 mg of cefuroxime axetil (CA) by the oral route or 1.78 mg of cefuroxime sodium (CNa) by IV and IP route). A two-compartment open model without lag time can predict the C disposition kinetics. The influence of the administration route on the pharmacokinetic parameters and AUC values was investigated by means of a one-way analysis of variance test. The results indicated that the first-pass effect in the intestine and liver reduce oral bioavailability when the drug is administered orally. Cefuroxime bioavailability after oral and IP administration estimated from the plasma levels was nearly 24 and 75%, respectively.
Ruiz-Carretero
P
P
Department of Pharmaceutics, Faculty of Pharmacy, University of Valencia, Avda. Vicente Andrés Estellés s/n. 46100, Burjassot, Spain.
Nacher
A
A
Merino-Sanjuan
M
M
Casabo
V G
VG
D000284:Administration, Oral; D000818:Animals; D002444:Cefuroxime / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000493:pharmacokinetics; D008297:Male; D011355:Prodrugs / Q000008:administration & dosage / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar
D011355:Prodrugs; D002444:Cefuroxime; C040738:cefuroxime axetil