lornoxicam and Arthritis

Lornoxican (chlorotenoxicam) is a nonsteroidal anti-inflammatory drug (NSAID) of the oxicam class. Unlike other oxicams, lornoxicam has a relatively short plasma half-life (3 to 5 hours). Lornoxicam is eliminated following biotransformation to 5'-hydroxy-lornoxicam, which does not undergo enterohepatic recirculation. Glucoroconjugated metabolites are excreted in urine and faeces with a half-life of about 11 hours. Lornoxicam and its metabolites bind extensively to plasma albumin. Substantial concentrations of lornoxicam are attained in synovial fluid, the proposed site of action in chronic inflammatory arthropathies. The effects of lornoxicam concentration on its therapeutic and toxicological properties have not yet been extensively reported. Lornoxicam, like other NSAIDs, appears to interact with warfarin, sulphonylureas, digoxin and furosemide.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Arthritis; Drug Administration Routes; Drug Interactions; Half-Life; Humans; Piroxicam; Protein Binding; Serum Albumin; Synovial Fluid

To assess the safety of lornoxicam in subjects with G-6-PDH deficiency.. Open controlled 2-week in vivo study on lornoxicam 8 mg bid in subjects with G-6-PDH deficiency suffering from rheumatic diseases.. In 8 male patients with the Mediterranean form of G-6-PDH deficiency (mean age +/- SD, 54.3 years +/- 7.2) lornoxicam showed no influence on red blood cells (RBC) survival curve. The RBC half-life was the same before and after two weeks of treatment.. Lornoxicam caused no RBC damage and evidenced favourable safety in subjects with G-6-PDH deficiency, suffering from rheumatic diseases.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Arthritis; Erythrocyte Aging; Glucosephosphate Dehydrogenase Deficiency; Humans; Male; Middle Aged; Piroxicam; Time Factors

The focus of this study was to develop in situ injectable implants of Lornoxicam which could provide sustained drug release.. Biodegradable in situ injectable implants were prepared by polymer precipitation method using polylactide-co-glycolide (PLGA). An optimized formulation was obtained on the basis of drug entrapment efficiency, gelling behavior and in vitro drug release. The compatibility of the formulation ingredients were tested by Fourier transform infrared (FT-IR) spectroscopy, and differential scanning colorimetry (DSC). SEM study was performed to characterize in vivo behavior of in situ implant. Pharmacokinetic study and in vivo gelling study of the optimized formulation were performed on Sprague-Dawley rats. Stability testing of optimized formulation was also performed.. The drug entrapment efficiency increased and burst release decreased with an increase in the polymer concentration. Sustained drug release was obtained up to five days. SEM photomicrographs indicated uniform gel formation. Chemical interaction between the components of the formulation was not observed by FT-IR and DSC study. Pharmacokinetic studies of the optimized formulation revealed that the maximum plasma concentration (Cmax), time to achieve Cmax (Tmax) and area under plasma concentration curve (AUC) were significantly higher than the marketed intramuscular injection of lornoxicam. Stability study of optimized batch showed no change in physical and chemical characteristics.. Lornoxicam can be successfully formulated as in situ injectable implant that provides long-term management of inflammatory disorders with improved patient compliance.

Topics: Absorbable Implants; Animals; Anti-Inflammatory Agents, Non-Steroidal; Arthritis; Calorimetry, Differential Scanning; Delayed-Action Preparations; Drug Compounding; Drug Evaluation, Preclinical; Drug Stability; Excipients; Injections, Intra-Articular; Male; Microscopy, Electron, Scanning; Models, Animal; Piroxicam; Polylactic Acid-Polyglycolic Acid Copolymer; Rats; Rats, Sprague-Dawley; Spectroscopy, Fourier Transform Infrared

Lornoxicam is a potent non-steroidal anti-inflammatory drug (NSAID). It shows limited solubility in the gastric pH, delayed bioavailability and pharmacodynamic effects with aggravated gastric side effects (due to longer residence in the stomach wall).. To enhance dissolution of lornoxicam in the gastric fluid and expectedly absorption and pharmacological action, with less ulcerogenic effects.. Formulation of immediate release (IR) lornoxicam liquitablets containing both liquid and solid release modulators (wetting agent, solubilizers and microenvironmental pH modifiers). Beside the traditional direct compression technique employed for the preparation of liquitablets a new technique, blister molding, was also used. The effect of the two different manufacturing methods on the fast release characteristics (rapid disintegration and dissolution) was studied. Stability and pharmacological activity of the optimum formula were also explored.. Similarity factor pointed out the superiority of molding technique in enhancing dissolution of lornoxicam owing to significant crystallinity reduction (XRD). Optimum formula showed negligible change in drug content and dissolution profiles over 12 weeks, significantly improved anti-inflammatory activity and significantly reduced gastric ulcerative effect over pure lornoxicam and commercial formula.. Blister molded lornoxicam liquitablet of improved dissolution and pharmacological activity and less gastric erosion was successfully prepared.

Topics: Animals; Anti-Inflammatory Agents, Non-Steroidal; Arthritis; Delayed-Action Preparations; Drug Compounding; Drug Liberation; Drug Stability; Piroxicam; Rats; Solubility; Tablets; Ulcer