Zhou D, Zhang Q, Lu W, Xia Q, Wei S
Department of Pharmaceutics, School of Pharmaceutical Sciences, Beijing Medical University, Republic of China.
J Clin Pharmacol. 1998 Jul;38(7):625-9. doi: 10.1002/j.1552-4604.1998.tb04469.x.
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.
在健康志愿者中，采用开放、随机双向交叉实验设计，比较了萘普生新型缓释片（每日一次，500毫克）和常规片（每日两次，250毫克）单剂量或多剂量口服给药后的药代动力学。与常规片相比，萘普生从缓释片中的吸收良好（约97%）。药代动力学数据表明，在单剂量和多剂量研究中，缓释制剂的平均血浆峰浓度（Cmax）显著延迟，且在单剂量研究中Cmax低于常规制剂。然而，在单剂量或多剂量研究中，两种治疗之间的其他药代动力学参数，包括浓度-时间曲线下面积（AUC）、消除半衰期（t1/2）和消除速率常数（Ke），均无统计学显著差异。此外，在多剂量研究中，两种制剂在Cmax、最低血浆浓度（Cmin）和波动指数方面也无显著差异。
