摘 要 目的：考察不同pH介质对双氯芬酸钠缓释片体外释放度有无影响及评价体外释放与体内吸收的相关性，为其质量控制提供实验依据。方法：在3种不同pH介质中进行体外释放度试验，计算相应时间内的累积释放百分数，用反相高效液相色谱法测定口服双氯芬酸钠缓释100 mg后血浆药物浓度，按Wagner-Nelson公式计算一定时间内双氯芬酸钠缓释片的体内吸收百分数。结果: 双氯芬酸钠缓释片在蒸馏水、pH6.8和pH7.4的磷酸缓冲液中的释放未受影响。双氯芬酸钠缓释片的体内吸收分数与体外释药分数具有良好的相关性 结论:用 pH6.8和pH7.4的磷酸缓冲液测定8小时作为双氯芬酸钠缓释片体外溶出度试验的释放介质是可行的。

    关键词 双氯芬酸钠；缓释片；释放度；释药介质；体外

    Release traits of diclofenac sodium sustained-release tablet in vitro and in vivo

    Abstract Objective: To study the effect of three different pH mediums on the in vitro releasing of diclofenac sodium sustained-release tablet and evaluate the relativity between absorption in vivo and dissolution rate in vitro. Methods: Tests of dissolution rate of diclofenac sodium sustained-release tablet in vitro were taken by adopting three different mediums. Plasma concentration after eight men po diclofenac sodium sustained-release tablet 100 mg was measured by means of reverse phase HPLC. Results: Dissolution rate of diclofenac sodium sustained-release tablet was not related to buffer pH. Good relativity was shown between absorption in vivo and dissolution rate in vitro. Conclusion: Eight hours test with buffer of pH6.8 and pH7.4 might be suitable medium of dissolution of diclofenac sodium sustained-release tablet. ......