PHARMACOKINETICS OF BROMFENAC IN HEALTHY-SUBJECTS AFTER SINGLE ORAL-ADMINISTRATION OF 3 DIFFERENT DOSES

The pharmacokinetic profile of bromfenac (2-amino-3-(4-bromobenzoyl) b enzeneacetic acid, CAS91714-93-1) has been investigated in 12 healthy subjects (6 male and 6 female) after single oral doses of 25, 50 and 7 5 mg. Plasma concentrations were determined by a sensitive HPLC method with spectrophotometric detection. Sampling was performed up to 300 m in after drug ingestion. Linear pharmacokinetics could be verified for this dose-range; there was a clear, positive dose-plasma concentratio n relationship. Bromfenac exhibits a c(max) of 3.49 +/- 1.65-8.81 +/- 3.45 mug/ml at t(max) 52 +/- 27-42 +/- 15 min. The elimination half-li fe was 39.8 +/- 7.3 - 34.2 +/- 8.0 min with a clearance (Cl/f) of 120. 6 +/- 51.6 - 135.3 +/- 34.6 ml/min and a volume of distribution (V(d)/ f) 6.82 +/- 2.88 - 6.64 +/- 2.29 l. The results obtained show a fast a bsorption and rapid elimination of bromfenac when administered orally. The short plasma half-life of bromfenac apparently presents no direct relationship to its clinical effectiveness.