The effects of gender and oral contraceptive steroids on the pharmacokinetics of (R)‐ibuprofen were studied in groups of healthy adult males, females and oral contraceptive steroid (OCS) using females. The values of AUC, CLpo, t1/2 and Vss, app did not differ significantly between the groups. Similarly, the percentage unbound of (R)‐ibuprofen in pooled plasma from the three groups was not statistically different. Since chiral inversion is the major determinant of (R)‐ibuprofen clearance in humans, it may be inferred from these data that gender and OCS have little or no effect on conversion of (R)‐ibuprofen to the pharmacologically active S‐ enantiomer. Moreover, it is unlikely that hormonal factors influence the activity of the human hepatic long‐chain fatty‐acid:CoA ligase, the enzyme mediating the rate limiting step of (R)‐ibuprofen inversion.
|Number of pages||4|
|Journal||British Journal of Clinical Pharmacology|
|Publication status||Published - Aug 1995|