1988 Volume 3 Issue 2 Pages 199-209
Pharmacokinetics of bermoprofen, a new non-steroidal antipyretic agent, were evaluated in male healthy volunteers. The subjects were given single oral dose (5, 10, 20 and 40 mg, each of 5 subjects) and repeated oral dose (15 and 20 mg × 3/day for a day and 20 mg × 3/day for 5 days, each of 5 subjects). The results were as follows:
1. Mean plasma levels of the unchanged drug were maximal at 0.5-1 h and dose-related after single dosing of 5, 10, 20 and 40 mg with levels of 164, 247, 415 and 1325 ng/ml, respectively, followed by a biphasic decrease with apparent half-lives of 0.5-0.8 h (α-phase) and 1.9-2.1 h (β-phase). M 1, a 11-oxo-reduced metabolite, showed higer plasma levels and longer elimination half-lives than those of the unchanged drug. Plasma levels of M 2 and M 3 were less than 1/30 of that of the unchanged drug.
2. More than 99.5 % of bermoprofen and M 1 was bound to plasma protein.
3. A total amount excreted with urine for 48 h was 66-75 % of the dose after single dosing. The major excretion route was the glucuronidation of M 1 and bermoprofen, these conjugates being more than 80 % of the urinary excretion. The excretions of bermoprofen, M 1, M 2 and M 3 amounted to about 2-5 % of the dose.
4. There were no significant changes in the plasma concentration-time frofile and the fraction of urinary excretion between single and multiple doses, indicating that the pharmacokinetics of bermoprofen in man were not affected with its multiple administration.
