Pharmacokinetics of dexketoprofen trometamol in healthy volunteers after single and repeated oral doses

The pharmacokinetics of dexketoprofen trometamol were evaluated in two stud ies using healthy volunteers. In the first study, the relative bioavailabil ity of a single oral capsule of dexketoprofen free acid 25 mg or dexketopro fen trometamol 25 mg (given as 37 mg of the trometamol salt) was compared t o ketoprofen 50 mg in 18 healthy volunteers. In the second study, the pharm acokinetics and tolerability of oral dexketoprofen trometamol in tablet for m were evaluated after either a single 25 mg dose (24 volunteers) or a repe ated dose of 25 mg twice daily for 7 days (12 volunteers). The absorption o f dexketoprofen from dexketoprofen trometamol capsules was bioequivalent to that of ketoprofen. On the other hand, the extent of absorption of dexketo profen free acid was significantly lower than that for ketoprofen. Dexketop rofen trometamol showed the most rapid absorption rate, with highest C-max and shortest t(max) values, whereas dexketoprofen free acid had the slowest absorption rate, and ketoprofen had an intermediate absorption rate. After repealed-dose administration of dexketoprofen trometamol, the pharmacokine tic parameters were similar to those obtained after single doses, indicatin g that no drug accumulation occurred. Dexketoprofen trometamol was well tol erated, with no clinically relevant adverse events reported. Journal of Cli nical Pharmacology, 1998;38:33S-40S (C) 1998 The American College of Clinic al Pharmacology.