奈福泮缓释胶囊体内外试验的相关性研究

Evaluation of the correlation between in vitro release and in vivo absorption characteristics of nefopam sustained release capsules

目的 :评价奈福泮缓释胶囊的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 :用反相高效液相色谱法测定血浆中的奈福泮浓度 ,按Wagner -Nelson公式计算一定时间内奈福泮缓释胶囊的体内吸收百分率。在释放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率。结果 :奈福泮缓释胶囊在体外缓慢释放 ,体内血药浓度维持时间长。结论

OBJECTIVE:To evaluate the correlativity between in vitro release and in vivo absorption of nefopam sustained release capsules.METHODS:The nefopam concentration in human plasma was determined by a high performance liquid chromatography method.According to the Wagner-Nelson formula,the percentage of in vivo absorption of two nefopam sustained release capsules were calculated.In vitro release of nefopam in 3 mediums of different pH was tested and the accumulated release percentage was calculated.RESULTS:The variation of pH of mediums were no significant affect on in vitro release rate of nefopam.CONCLUSION:A good correlativity was showed between in vivo absorption and in vitro release of nefopam sustained release capsules.