An eutomer/distomer ratio near unity does not justify non-enantiospecific assay methods in bioequivalence studies

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 substan...

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Published in:Chirality (New York, N.Y.) N.Y.), 2005, Vol.17 (8), p.470-475
Main Authors: García-Arieta, Alfredo, Abad-Santos, Francisco, Rodríguez-Martínez, M. Angeles, Varas-Polo, Yolanda, Novalbos, Jesús, Laparidis, Nikos, Gallego-Sandín, Sonia, Orfanidis, Kyriakos, Torrado, Juan
Format: Article
Language:English
Subjects:
Administration, Oral
Adult
Analysis of Variance
Anti-Inflammatory Agents, Non-Steroidal - administration & dosage
Anti-Inflammatory Agents, Non-Steroidal - blood
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Area Under Curve
bioequivalence
chirality
Cross-Over Studies
enantiomers
Female
Humans
ibuprofen
Ibuprofen - administration & dosage
Ibuprofen - blood
Ibuprofen - pharmacokinetics
Intestinal Absorption
Male
pharmacokinetics
Stereoisomerism
Tablets
Therapeutic Equivalency
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Summary: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.
ISSN:0899-0042
1520-636X
DOI:10.1002/chir.20186