Effect of food and relative bioavailability following single doses of diclofenac 150 mg hydrogel bead (HGB) capsules in healthy humans.

The effect of food on the bioavailability of diclofenac from a 150 mg diclofenac hydrogel bead (HGB) capsule was evaluated in 12 healthy male subjects in a fed and fasted state. Additionally, the fasting bioavailability of diclofenac from a 150 mg diclofenac HGB capsule relative to diclofenac sodium in buffered aqueous solution was evaluated in these same 12 subjects. The study was designed as an open-label, randomized, single-dose, 3 x 3 Latin-square crossover trial balanced for residual effects. A 2-week washout period was maintained between treatments. Blood samples were collected at frequent intervals over a 24-h period with plasma being separated and analyzed for diclofenac using a validated HPLC method. The administration of the 150 mg diclofenac HGB capsule dose within 30 min following a standardized breakfast minimally affected the bioavailability of diclofenac relative to administration under fasted conditions (7 per cent decrease in AUC(0-24), p greater than 0.05). There was, however, a 38 per cent decrease (p less than 0.05) in the Cmax and a three-fold increase (p less than 0.05) in Tmax for the fed HGB capsule administration. Under fasted conditions, significant differences in mean pharmacokinetic parameters were found between the 150 mg diclofenac HGB capsule and diclofenac sodium in buffered aqueous solution. The extent of availability of diclofenac from the HGB capsule was only 59 per cent relative to that from the solution (p less than 0.05).(ABSTRACT TRUNCATED AT 250 WORDS)

RCT Entities:   Population Interventions Outcomes