Metabolic chiral inversion of ibuprofen in isolated rat hepatocytes

Müller, Sylvia ; Mayer, Joachim M. ; Etter, Jean-Claude ; Testa, Bernard

New York, NY [u.a.] : Wiley-Blackwell
Published 1990
ISSN:
0899-0042
Keywords:
ibuprofen ; in vitro metabolism ; chiral inversion ; rat hepatocytes ; Chemistry ; Organic Chemistry
Source:
Wiley InterScience Backfile Collection 1832-2000
Topics:
Chemistry and Pharmacology
Notes:
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 × 105 cells/ml. No elimination of (R)-ibuprofen by routes other than inversion was seen, whereas the elimination of (S)-ibuprofen appeared to be saturable.
Additional Material:
2 Ill.
Type of Medium:
Electronic Resource
URL: