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Metabolic chiral inversion of ibuprofen in isolated rat hepatocytes
Author(s) -
Müller Sylvia,
Mayer Joachim M.,
Etter JeanClaude,
Testa Bernard
Publication year - 1990
Publication title -
chirality
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.43
H-Index - 77
eISSN - 1520-636X
pISSN - 0899-0042
DOI - 10.1002/chir.530020203
Subject(s) - ibuprofen , chemistry , inversion (geology) , in vitro , hepatocyte , kinetics , pharmacology , chromatography , biochemistry , biology , medicine , paleontology , physics , structural basin , quantum mechanics
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 × 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.