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目的：酮洛芬缓释片与常释片单次给药的生物利用度和多次给药的峰谷浓度波动大小。方法：采用以萘普生（ｎａｐｒｏｘｅｎ）为内标的ＨＰＬＣ测定方法，测定健康男性受试者按交叉试验单剂量和多剂量服用酮洛芬缓释片和常释片后的血中酮洛芬浓度。结果：单剂量服用酮洛芬缓释片和常释片后，常释片的Ｃｍａｘ显著高于缓释片（Ｐ＜００１），缓释片给药后的Ｔｍａｘ延迟，ｔ１／２ｋｅ显著延长，相对生物利用度为９７１３％。缓释片在稳态时的Ｃｍｉｎ为０４０１μｇ·ｍＬ－１，而常释片为０１９０μｇ·ｍＬ－１（Ｐ＜００１）。在稳态时缓释片的峰谷浓度波动度（ＤＦ）、峰谷比（ＰＴＲ）都显著小于常释片，说明缓释片的峰谷浓度波动程度优于常释片。结论：经统计学检验表明这两种制剂具有生物等效性，该缓释片具有峰谷浓度差异小，波动幅度小的特点，显示出缓释特征。
OBJECTIVE: To investigate the bioavailability of single dose of ketoprofen sustained-release tablets and regular release tablets and the fluctuation of peak-to-valley concentration in multiple doses. Methods: Naproxen was used as the internal standard of HPLC to determine the concentration of ketoprofen in healthy male subjects after taking ketoprofen sustained-release tablets and regular-release tablets in single or multiple doses . Results: After a single dose of ketoprofen sustained-release tablets and regular release tablets, the Cmax of the tablets was significantly higher than that of the sustained-release tablets (P <001), the delayed release of Tmax was delayed and t1 / 2ke was significant Extended, the relative bioavailability was 97.13%. The Cmin of the sustained-release tablets was 0401μg · mL-1 at steady-state, while it was 0.19μg · mL-1 (P <001). At steady state, the peak-to-peak concentration fluctuation (DF) and peak-to-valley ratio (PTR) of sustained-release tablets were significantly lower than those of conventional tablets, indicating that the peak- Conclusion: The results of statistical tests show that the two preparations have bioequivalence. The sustained-release tablets have the characteristics of small difference in peak-to-valley concentration and small fluctuation range, showing the characteristics of sustained release.