Pharmacokinetics of bromfenac in healthy subjects after single oral administration of three different doses.
The pharmacokinetic profile of bromfenac (2-amino-3-(4-bromobenzoyl) benzeneacetic acid, CAS91714-93-1) has been investigated in 12 healthy subjects (6 male and 6 female) after single oral doses of 25, 50 and 75 mg. Plasma concentrations were determined by a sensitive HPLC method with spectrophotometric detection. Sampling was performed up to 300 min after drug ingestion. Linear pharmacokinetics could be verified for this dose-range; there was a clear, positive dose-plasma concentration relationship. Bromfenac exhibits a cmax of 3.49 +/- 1.65-8.81 +/- 3.45 micrograms/ml at tmax 52 +/- 27-42 +/- 15 min. The elimination half-life 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 (Vd/f) 6.82 +/- 2.88-6.64 +/- 2.29 l. The results obtained show a fast absorption and rapid elimination of bromfenac when administered orally. The short plasma half-life of bromfenac apparently presents no direct relationship to its clinical effectiveness.
Högger
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Institute of Pharmaceutical Chemistry, Westfälische Wilhelms-Universität Münster, Fed. Rep. of Germany.
Rohdewald
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D000284:Administration, Oral; D000328:Adult; D000700:Analgesics / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics; D001577:Benzophenones / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001969:Bromobenzenes / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D013056:Spectrophotometry, Ultraviolet
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D001577:Benzophenones; D001969:Bromobenzenes; C053083:bromfenac