Chiral bioanalytical methods in bioequivalence studies of intravenous vs. oral formulations of ibuprofen.

Abstract:

:According to the Ibuprofen Product-Specific Bioequivalence Guidance of the European Medicines Agency, achiral bioanalytical methods are considered acceptable for demonstration of bioequivalence of ibuprofen-containing products. The aim of this investigation is to compare the bioequivalence outcomes obtained with individual R and S ibuprofen enantiomers and the sum of both enantiomers from bioequivalence studies in which new intravenous ibuprofen products were compared with oral ibuprofen products. Bioequivalence was assessed for S and R enantiomers of ibuprofen and the sum of both enantiomers, which was calculated to represent the results that would have been obtained with an achiral assay. The infusion rates of 15, 20, and 30 minutes modify the maximum concentration (Cmax ) of the intravenous administrations. In contrast, the time when the maximum concentration is observed (Tmax ) was insensitive to detect differences in input rate within this range of infusion times. The eutomer S-ibuprofen is the least sensitive analyte to detect differences in input rate; therefore, the regulatory acceptance of achiral bioanalytical methods for ibuprofen bioequivalence studies is justified because the sum of both enantiomers is more discriminative than the chiral methods where only the eutomer is used for regulatory decisions.

journal_name

Chirality

journal_title

Chirality

authors

González-Rojano E,Marcotegui J,Laredo L,Gwaza L,Gordon J,Portolés A,Vargas E,Morales-Alcelay S,García-Arieta A

doi

10.1002/chir.23258

subject

Has Abstract

pub_date

2020-09-01 00:00:00

pages

1169-1177

issue

9

eissn

0899-0042

issn

1520-636X

journal_volume

32

pub_type

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