Single- and multiple-dose pharmacokinetic comparison of a sustained-release tablet and conventional tablets of naproxen in healthy volunteers.
The pharmacokinetics of a new sustained-release tablet of naproxen (500 mg once daily) were compared with a conventional tablet (250 mg twice daily) after single- or multiple-dose oral administration in healthy volunteers using an open, randomized two-way crossover experimental design. Naproxen was well absorbed from the sustained-release tablet (approximately 97%) compared with the conventional tablet. Pharmacokinetic data showed that the sustained-release formulation reached significantly delayed mean peak plasma levels (Cmax) in both single- and multiple-dose studies and lower Cmax in a single-dose study than the conventional formulation. However, there were no statistically significant differences in other pharmacokinetic parameters, including area under the concentration-time curve (AUC), elimination half-life (t1/2), and elimination rate constant (Ke), in either single- or multiple-dose studies between the two treatments. In addition, there were no significant differences between formulations in Cmax, minimum plasma concentration (Cmin), and fluctuation index in the multiple-dose study.
Department of Pharmaceutics, School of Pharmaceutical Sciences, Beijing Medical University, Republic of China.
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Zhou
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Zhang
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Lu
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Xia
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Wei
D000328:Adult; D000704:Analysis of Variance; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D006207:Half-Life; D006801:Humans; D008297:Male; D009288:Naproxen / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D013607:Tablets
D000894:Anti-Inflammatory Agents, Non-Steroidal; D003692:Delayed-Action Preparations; D013607:Tablets; D009288:Naproxen