THE EFFICACY AND RELATIVE BIOAVAILABILITY OF DICLOFENAC RESINATE IN RHEUMATOID-ARTHRITIS PATIENTS

The pharmacodynamics and pharmacokinetics of 75 mg resin-bound diclofe nac (resinate) were compared with enteric-coated tablets containing 75 mg of diclofenac in a double-blind randomized crossover trial in 16 p atients suffering from rheumatoid arthritis. Diclofenac was significan tly faster absorbed from the resinate than from the enteric coated for mulation (t(lag) = 0.454 h vs. 0.998 h, t(max) = 1.41 h vs. 2.56 h) an d reached lower peak concentrations (C-max = 1.64 mu g/ml vs. 2.59 mu g/ml). No significant differences were found concerning the area under the plasma level-time curves and the mean residence times. Smaller va riances were found for the tmax and the mean residence times in the gr oup treated with diclofenac resinate. Onset and duration of analgesia, as assessed by visual analogue scales were similar in both treatment groups, but did not correlate with the plasma concentrations. Four pat ients experienced adverse effects including gastric pain, transaminase increases, proteinuria and plasma creatinin increase. No uncommon adv erse effects were observed with the new preparation.