Pharmacokinetic study in man with the non-steroidal antiinflammatory drug flunoxaprofen. Serum concentration-time profile after oral or topical preparations.
A clinical study on normal volunteers was performed in order to establish the pharmacokinetic pattern of the non-steroidal antiinflammatory drug S-(+)-2-(4-fluorophenyl-a-methyl-5-benzoxazole-acetic acid (flunoxaprofen, Priaxim, FLU) after oral administration or after transcutaneous absorption. Six subjects (3 men and 3 women) received FLU orally (a single dose of 200 mg) and 6 subjects (4 men and 2 women) were treated by cutaneous application on the shoulder of 1.5 g of a gel preparation containing FLU 5%. Blood samples were withdrawn before and at several time intervals after the treatments up to 48 h after oral administration and up to 24 h after cutaneous application. Serum FLU concentrations were determined by a HPLC method. The results show that a single oral dose of FLU 200 mg follows a kinetic pattern very similar to that obtained with a 100 mg dose as referred to in the literature, without significant differences of t1/2 beta, Vd and clearance values in comparison with those after FLU 100 mg. The dose-related parameters (Cmax and AUC) were higher after FLU 200 mg than after FLU 100 mg. The cutaneous application of a flunoxaprofen gel preparation did not cause detectable systemic absorption of the drug. In conclusion FLU shows favourable pharmacokinetic parameters after 200 mg oral dose, since serum values of the drug exclude the risk of accumulation; moreover the topical application of a FLU gel preparation is a safe transcutaneous treatment for inflammation and pain due to lacking systemic absorption of the drug.
Bareggi
S R
SR
Department of Pharmacology, University of Milan, Italy.
Pedrazzini
S
S
De Angelis
M
M
D000284:Administration, Oral; D000287:Administration, Topical; D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D001583:Benzoxazoles / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D006207:Half-Life; D006801:Humans; D008297:Male; D008875:Middle Aged
D000894:Anti-Inflammatory Agents, Non-Steroidal; D001583:Benzoxazoles; C045356:flunoxaprofen