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

Background and 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 lornoxicani 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/m(2) 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 (AUC(infinity)), maximum plasma concentration (C(max)), time to maximum plasma concentration (t(max)), terminal half-life (t(1/2)) and mean residence time (MRT) were calculated. Results: Lornoxicam-QR was comparable with lornoxicam-ST and lornoxicam-IM regarding AUC(infinity), t(1/2), and MRT. The AUC(infinity) 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 t(max) and significantly higher C(max) values than lornoxicam-ST. Conclusion: Lornoxicam-QR and lornoxicam-IM did not differ with respect to AUC(infinity), C(max) and t(max), but both lornoxicam-QR and lornoxicam-IM showed significantly shorter t(max) and significantly higher C(max) values than lornoxicam-ST.