A study on the relative bioavailability of a sustained-release formulation of diclofenac sodium.
The bioavailability of an in vitro sustained-release formulation of diclofenac sodium was compared with a conventional product in six healthy male volunteers. The administration of a single dose (100 mg) of either formulation in a crossover design revealed significant differences in the extent of absorption as assessed by AUC. The relative bioavailability of the sustained-release formulation was found to be 53% compared with the conventional product. The Cmax for the sustained release formulation (0.54 +/- 0.29 micrograms ml-1) was significantly much lower than the corresponding value for the conventional formulation (4.12 +/- 0.91). However, the tmax for the sustained release formulation (3.6 +/- 2.1 h) was not significantly different from the corresponding value for the conventional formulation (2.5 +/- 0.4 h). Although the sustained release formulation showed serum concentration-time profiles characteristic of sustained products in vivo, it failed to attain therapeutic drug levels. The in vivo results were found inconsistent with the in vitro availability of the drug.
Suleiman
M S
MS
Department of Pharmaceutical Technology, Jordan University of Science and Technology, Irbid.
Najib
N
N
el-Sayed
Y
Y
Hasan
M
M
Abdulahameed
M
M
D000328:Adult; D001682:Biological Availability; D003692:Delayed-Action Preparations; D004008:Diclofenac / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006801:Humans; D008297:Male; D012995:Solubility
D003692:Delayed-Action Preparations; D004008:Diclofenac