Comparative Bioavailability of Lornoxicam as Single Doses of Quick-Release Tablet, Standard Tablet and Intramuscular Inj
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Clin Drug Invest 2008; 28 (6): 345-351 1173-2563/08/0006-0345/$48.00/0 © 2008 Adis Data Information BV. All rights reserved.
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 Susanna Radhofer-Welte,1 Peter Dittrich,2 Marija Simin1 and Poul Erik Branebjerg1 1 2
Medical Scientific Strategy and Medical Marketing, Nycomed Group, Roskilde, Denmark and Linz, Austria Department of Pharmacology and Toxicology, Institute of Pharmaceutical Sciences, University of Graz, Graz, Austria
Abstract
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 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 (AUC∞), 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 lornoxicamIM regarding AUC∞, t1/2 and MRT. The AUC∞ ratio (90% CI) was 1.07 (0.94, 1.20) for lornoxicam-QR/lornoxicam-ST and 1.10 (0.97, 1.24) for lornoxicamQR/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. Conclusion: Lornoxicam-QR and lornoxicam-IM did not differ with respect to AUC∞, Cmax and tmax, but both lornoxicam-QR and lornoxicam-IM showed significantly shorter tmax and significantly higher Cmax values than lornoxicamST.
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Background Lornoxicam is an NSAID used to obtain shortterm relief of acute mild to moderate pain and symptomatic relief of pain and inflammation in rheumatoid arthritis[1] and osteoarthritis.[2] Lornoxicam is slightly acidic with a pKa (acid dissociation constant) of 4.7 and hence has a limited dissolution in an acidic environment.[3] It is slightly lipophilic with an apparent partition coefficient of 1.8 (n-octanol/ buffer pH 7.4). Lornoxicam is commercially available in most European countries in formulations for intravenous (IV) and intramuscular (IM) injection as well as in tablet formulations. IV and IM formulations
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