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An eutomer/distomer ratio near unity does not justify non‐enantiospecific assay methods in bioequivalence studies
Author(s) -
GarcíaArieta Alfredo,
AbadSantos Francisco,
RodríguezMartínez M. Angeles,
VarasPolo Yolanda,
Novalbos Jesús,
Laparidis Nikos,
GallegoSandín Sonia,
Orfanidis Kyriakos,
Torrado Juan
Publication year - 2005
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.20186
Subject(s) - bioequivalence , enantiomer , bioanalysis , chemistry , ibuprofen , chromatography , pharmacokinetics , stereoselectivity , chiral stationary phase , stereochemistry , pharmacology , organic chemistry , medicine , catalysis
The aim of the present investigation was to compare the pharmacokinetics of two tablet formulations of 600 mg of racemic ibuprofen obtained using enantiospecific and non‐enantiospecific assays, in order to explore if chiral assays should be employed in bioequivalence studies of chiral active substances. The stereoselective assay showed that, for both formulations, there was an initial phase where ( R )‐ibuprofen was the predominant enantiomer followed by a final phase where ( S )‐ibuprofen was the predominant one. Results from both analytical methods proved that the two formulations were bioequivalent. However, the chiral bioanalytical method detected a larger difference in the eutomer than that showed by the nonchiral bioanalytical method. In conclusion, although the exposure ratios of enantiomers are near unity, the measurement of unresolved ibuprofen alone is not an adequate measure of bioequivalence since it may mask the actual difference in the eutomer exposure among formulations. © 2005 Wiley‐Liss, Inc. Chirality 17:470–475, 2005.