Comparative bioavailability of lornoxicam as single doses of quick-release tablet, standard tablet and intramuscular injection: a randomized, open-label, crossover phase I study in healthy volunteers.
OBJECTIVE
Lornoxicam is an NSAID used to obtain short-term relief of acute mild to moderate pain and symptomatic relief of pain and inflammation in rheumatoid arthritis and osteoarthritis. The aim of this study was to compare and evaluate the pharmacokinetic parameters of lornoxicam 8 mg as quick-release (QR) tablet, standard tablet (ST) and intramuscular injection (IM).


METHODS
Eighteen healthy volunteers (9 male, 9 female; average age 26.9 (SD 3.0) years; average body mass index 21.8 (SD 2.3) kg/m2 were randomized to three different treatment groups. Subjects received a single 8-mg dose of each lornoxicam formulation in a three-way crossover design on days 1, 8 and 15. Lornoxicam plasma concentrations were obtained from baseline to 24 hours using high-pressure liquid chromatography. The pharmacokinetic parameters area under the plasma concentration-time curve from zero to infinity (AUCinfinity), maximum plasma concentration (Cmax), time to maximum plasma concentration (tmax), terminal half-life (t1/2)) and mean residence time (MRT) were calculated.


RESULTS
Lornoxicam-QR was comparable with lornoxicam-ST and lornoxicam-IM regarding AUCinfinity, t1/2 and MRT. The AUCinfinity ratio (90% CI) was 1.07 (0.94, 1.20) for lornoxicam-QR/lornoxicam-ST and 1.10 (0.97, 1.24) for lornoxicam-QR/lornoxicam-IM. Cmax and tmax did not differ between lornoxicam-QR and lornoxicam-IM (p=0.66 and 0.07, respectively). Both lornoxicam-QR and lornoxicam-IM showed significantly shorter tmax and significantly higher Cmax values than lornoxicam-ST.


CONCLUSIONS
Lornoxicam-QR and lornoxicam-IM did not differ with respect to AUCinfinity, Cmax and tmax, but both lornoxicam-QR and lornoxicam-IM showed significantly shorter tmax and significantly higher Cmax values than lornoxicam-ST.
Radhofer-Welte
Susanna
S
Medical Scientific Strategy and Medical Marketing, Nycomed Group, Roskilde, Denmark and Linz, Austria.
Dittrich
Peter
P
Simin
Marija
M
Branebjerg
Poul Erik
PE
D000328:Adult; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D005260:Female; D006801:Humans; D007273:Injections, Intramuscular; D008297:Male; D010894:Piroxicam / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D013607:Tablets
D000894:Anti-Inflammatory Agents, Non-Steroidal; D013607:Tablets; D010894:Piroxicam; C059451:lornoxicam