betadex and Joint-Diseases

The efficacy of nonsteroidal anti-inflammatory drugs (NSAIDs) in rheumatic diseases depends on their concentrations within the joint. We determined piroxicam concentrations in plasma and synovial fluid (SF) after a single oral dose of 20 mg in the form of one tablet of piroxicam-beta-cyclodextrin.. 45 patients, aged 21 to 84 years, presenting with an effusion of the knee, related to degenerative or inflammatory joint disease, were included in this study after having given their written consent. One blood and one SF sample were drawn concomitantly in each patient from 0.5 to 48 h after NSAID administration. Piroxicam assays were performed by high performance liquid chromatography. Pharmacokinetic parameters were obtained from the mean plasma and synovial concentrations measured at various sampling times.. The peak concentration was higher in plasma (2.51+/-0.25 microg/ml) than in SF (1.31+/-0.76 microg/ml), but the elimination half-life was much longer in SF (90.7 h) than in plasma (32.5 h). The SF/plasma area under the concentration-time curve ratio (evaluating the quantity of NSAID transferred from the blood to the joint) was equal to 0.39.. Piroxicam contained in piroxicam-beta-cyclodextrin diffused well into the SF where its pharmacokinetic profile corresponded to that of a long half-life NSAID.

Topics: Administration, Oral; Adult; Aged; Aged, 80 and over; Anti-Inflammatory Agents, Non-Steroidal; Area Under Curve; Arthritis, Rheumatoid; beta-Cyclodextrins; Cyclodextrins; Drug Combinations; Female; Half-Life; Humans; Joint Diseases; Knee Joint; Male; Middle Aged; Piroxicam; Synovial Fluid

A study was carried out to assess the analgesic efficacy and the safety of piroxicam and to compare them with those of a piroxicam derivative, piroxicam beta-cyclodextrin, in chronic pain caused by arthritis of the neck and lower back. The drugs in question were administered for two weeks at the dose of 20 mg/die per os to 63 patients, 32 of whom were treated with the original molecule and the remaining subjects with its derivative. The study protocol scheduled assessments of pain and its reduction at baseline and after three, seven, and fourteen days of treatment. At the end of the two weeks of treatment, the drugs' efficacy and safety were evaluated. The results confirmed piroxicam's efficacy and safety in pain of the neck and lower back caused by osteoarthritis and did not show any differences, for the parameters examined, between the original molecule and its derivative.

Topics: Adult; Aged; beta-Cyclodextrins; Cervical Vertebrae; Chronic Disease; Cyclodextrins; Drug Evaluation; Female; Humans; Joint Diseases; Lumbar Vertebrae; Male; Middle Aged; Pain; Piroxicam; Randomized Controlled Trials as Topic