Pharmacokinetic properties and clinical efficacy of once-daily sustained-release naproxen.
The pharmacokinetics and clinical efficacy of a once-daily sustained-release formulation of naproxen (sodium salt) have been compared with those of conventional-release agents. In a single dose pharmacokinetic study, the rate of absorption of the sustained-release preparation was less than that of a conventional-release preparation but the extent of absorption was the same. As is the case with conventional-release naproxen, food decreased the rate but not the extent of absorption of the sustained-release formulation. On multiple dose administration for 7 days, the AUC and average concentrations of the sustained release preparation (1 g daily) were the same as those for conventional release preparations of naproxen sodium (250 mg four times daily) and naproxen free acid (500 mg daily). The conventional-release sodium salt was absorbed more quickly with no differences in bioavailability. A double-blind clinical comparison in patients with osteoarthritis showed the sustained-release preparation (1 g daily) to be equivalent in efficacy to conventional naproxen capsules (500 mg twice daily) but to have a significantly lower incidence of gastrointestinal side-effects. The results suggest that sustained-release naproxen sodium has potential for use as a once-daily treatment for inflammatory disease.
Kelly
J G
JG
Institute of Biopharmaceutics, Athlone, Ireland.
Kinney
C D
CD
Devane
J G
JG
Mulligan
S
S
Colgan
B V
BV
D000293:Adolescent; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D002986:Clinical Trials as Topic; D003692:Delayed-Action Preparations; D004311:Double-Blind Method; D006801:Humans; D008297:Male; D008875:Middle Aged; D009288:Naproxen / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000627:therapeutic use; D010003:Osteoarthritis / Q000503:physiopathology; D010146:Pain / Q000188:drug therapy; D011897:Random Allocation
D003692:Delayed-Action Preparations; D009288:Naproxen