Metabolic chiral inversion of ibuprofen in isolated rat hepatocytes.
Ibuprofen was used to demonstrate that isolated rat hepatocytes offer a suitable in vitro model to investigate the metabolic chiral inversion of anti-inflammatory 2-arylpropionic acids (profens). The inversion of the pharmacologically inactive (-)-(R)-ibuprofen to the active (+)-(S)-ibuprofen was shown to obey apparent first-order kinetics during 5 h and to increase linearly with increasing hepatocyte concentration up to 4 x 10(5) cells/ml. No elimination of (R)-ibuprofen by routes other than inversion was seen, whereas the elimination of (S)-ibuprofen appeared to be saturable.
Ecole de Pharmacie, Université de Lausanne, Switzerland.
S
S
Müller
J M
JM
Mayer
J C
JC
Etter
B
B
Testa
D000818:Animals; D007052:Ibuprofen / Q000378:metabolism* / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008099:Liver / Q000166:cytology / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D013237:Stereoisomerism
D007052:Ibuprofen