Flurbiprofen is a
propionic acid-derived non-steroidal anti-inflammatory
drug (
NSAID) used widely in the treatment of
rheumatism and non-arthritic
pain. The pharmacokinetics of topically and orally administered
flurbiprofen were compared in a two-part, open study involving healthy adult volunteers. In the first (cross-over) part of the study, 12 Caucasians were randomized to receive either a single oral dose of 50 mg
flurbiprofen or a single topical application of a novel 40 mg
flurbiprofen-containing patch on the right wrist for 12 h. In the second part of the study, each subject applied a
flurbiprofen-containing patch twice daily to the same wrist for 7 days. Plasma concentrations of
flurbiprofen and urinary concentrations of the
NSAID and its metabolites were measured by high-performance liquid chromatography assay, to enable comparison of the pharmacokinetic parameters for delivery of the
drug by both routes. Maximum concentrations of the
NSAID in plasma (Cmax) were much lower after a single application of the topical 40 mg
flurbiprofen patch than after a single oral dose of 50 mg of the
NSAID (mean +/- SD: 43 +/- 16 ng/ml versus 5999 +/- 1300 ng/ml, respectively). After repeated application of the topical patch, Cmax increased only slightly to 103 +/- 57 ng/ml. The mean relative bioavailability of
flurbiprofen from the patch was 3.5 +/- 1.7%, calculated from plasma area under the curve data and 4.4 +/- 2.8% from urinary excretion data.(ABSTRACT TRUNCATED AT 250 WORDS)