Metabolic chiral inversion of ibuprofen in isolated rat hepatocytes

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Abstract
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.