Summary
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.
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Kelly, J.G., Kinney, C.D., Devane, J.G. et al. Pharmacokinetic properties and clinical efficacy of once-daily sustained-release naproxen. Eur J Clin Pharmacol 36, 383–388 (1989). https://doi.org/10.1007/BF00558300
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DOI: https://doi.org/10.1007/BF00558300