Bioinversion of ibuprofen enantiomers after administration in dogs: estimation of a novel index

Citation
R. Frihmat et al., Bioinversion of ibuprofen enantiomers after administration in dogs: estimation of a novel index, EUR J DRUG, 25(3-4), 2000, pp. 205-211
Citations number
17
Categorie Soggetti
Pharmacology & Toxicology
Journal title
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
ISSN journal
03787966 → ACNP
Volume
25
Issue
3-4
Year of publication
2000
Pages
205 - 211
Database
ISI
SICI code
0378-7966(200007/12)25:3-4<205:BOIEAA>2.0.ZU;2-C
Abstract
This study compares the pharmacokinetics and bioinversion of two chemical f orms of ibuprofen administered intravenously or orally. Dogs were given the free acid form of the S(+) isomer p.o. or i.v., or the racemate, as the fr ee acid or sodium salt, p.o., in a cross-over design. The main kinetic para meters were calculated and formation and bioinversion curves plotted. The v alues of C-max, T-max and AUC were higher for the S(+) isomer. The percenta ge bioinversion averaged between 35-70% according to the form. This study p roposes a new index for the calculation of bioinversion, independently of a ny i.v. administration, and confirms its self-limiting nature.