石杉碱甲缓释微球的体外释放度及其体内外相关性研究

目的建立体内外相关性良好的石杉碱甲缓释微球的体外释放度测定方法。方法采用直接释药法和透析释药法测定石杉碱甲缓释微球的体外释放度，考察加入吐温的量和透析袋内递质的体积对释药速度的影响;采用高效液相色谱法测定石杉碱甲缓释微球在大鼠注射部位的残留量，计算微球在体内的释药速度。通过相关性评价确定最佳的体外释放度测定方法。结果透析释药法可获得良好的体内外相关性(r＝0.990 2)。结论透析释药法可用于测定石杉碱甲缓释微球的体外释放度。

In Vitro Release Experiment of Huperzine A Sustained-release Microspheres and Its Correlation Evaluation between In Vivo and In Vitro

Objective To establish a method for the determination of in vitro release of huperzine A sustained-release micro-spheres with a good correlation between in vivo and in vitro. Method Immediate release and dialysis release methods were used to determine the in vitro release rate of huperzine A microspheres.Effects of tween concentration and the medium volume in dialysis bag on release rate were studied.The residue huperzine A in the injection site was determined by HPLC,and in vivo release rate of huperzine A microspheres was caculated.The optimal release solution was chosen based on the correlation evaluation between the in vivo and in vitro results. Results Dialysis release method had a good in vitro and in vivo correlation(r=0.990 2). Conclusion Dialysis release method could be used to determine the in vitro release of huperzine A from microspheres.