ArticlesPharmacokinetics of ketoprofen enantiomers in healthy subjects following single and multiple doses
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The market of chiral drugs: Chiral switches versus de novo enantiomerically pure compounds
2018, Journal of Pharmaceutical and Biomedical AnalysisCitation Excerpt :Therefore, the use of the single (S)-ibuprofen was thought that it would give faster onset of action at a lower dosage and would reduce the source of configurational individual variability. After ibuprofen, another “profen” drug (namely, ketoprofen, see Table 1) was submitted to chiral switching and marketed as the (S)-(+)-enantiomer in 1998 [4], and this time the switch has been more straightforward, since the metabolic (R) ⇋ (S) chiral inversion for ketoprofen was shown to be negligible in humans [8]. By merging the data taken from a paper reviewing the chiral switches launched from 1994 to 2002 [4] with those from a more recent review focusing on the period from 2001 to 2011 [9], it emerges that the US Food and Drug Administration (FDA) approved 15 single-enantiomer versions of racemic drugs, i.e., 15 chiral switches have been launched in the period from 1994 to 2011 (see Table 1).
Species comparison of enantioselective oral bioavailability and pharmacokinetics of ketoprofen
2011, Research in Veterinary ScienceCitation Excerpt :Inversion is usually unidirectional from R(−) to S(+) KTP except in CD-1 mice where a substantial bi-directional inversion was noted (Jamali et al., 1997). Proof of chiral inversion can only be furnished by the administration of pure enantiomers or if >50% of a racemic dose is recovered from the elimination pathways as one of the enantiomers (Foster et al., 1988). Hence, in this study recourse to literature data is needed.
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