多剂量萘普生缓释片及普通片的人体药代动力学和生物利用度研究

MULTIPLE DOSE PHARMACOKINETIC AND BIOAVAIL ABILITY STUDIES OF ORAL SUSTAINED RELEASE AND CONVENTIONAL FORMULATIONS OF NAPROXEN IN HEALTHY VOLUNTEERS

８名健康男性受试者连续６ｄ多剂量交叉口服萘普生缓释片和普通片的药代动力学和相对生物利用度研究。结果表明：萘普生缓释片和普通片的Ｔｍａｘ分别为３．５ｈ和１．３ｈ，表明缓释效果明显；经统计分析，萘普生缓释片（５００ｍｇ，ｑｄ）与萘普生普通片（２５０ｍｇ，ｂｉｄ）生物等效；萘普生缓释片的相对生物利用度为９７．０％；２种制剂的其他药代动力学参数如Ｃｍａｘ、Ｃｍｉｎ、ＡＵＣ２４０、ＡＵＣ∞０、ｔ１／２以及波动系数（ＦＩ）等均无显著性差异。

The pharmacokinetics of naproxen sustained release tablets (500 mg, qd) was investigated together with a conventional preparation (250 mg, bid) after multiple oral administration in eight healthy human subjects using an open, randomized two way crossover experimental design. Based on the area under the plasma concentration time curve ( AUC ), the two tablet formulations are judged to be bioequivalent, with a relative bioavailability of 97.0% for the sustained release formulation. The sustained release formulation reached significantly delayed mean peak plasma levels compared with the conventional one. But there was no statistically significant difference for other pharmacokinetic parameters, including C max , C min , AUC , t 1/2 and the fluctuation index ( FI ) between the two preparations.