阿奇霉素微乳滴眼液的体外释放度特性

Study on release in vitro characteristic of azithromycin microemulsion eye drops

目的研究考察阿奇霉素微乳滴眼液体外释放行为。方法采用HPLC法测定人工泪液中阿奇霉素的含量,用不同的考察方法研究阿奇霉素微乳滴眼液的释药特性并进行比较,以阐明其释放机制,同时考察体外释放度的影响因素。结果 HPLC法能够准确测定阿奇霉素在泪液中的体外释放度,在10 h内释放稳定,释放机制为扩散和凝胶溶蚀共同作用。研究也显示处方工艺因素中的油相、乳化剂、HPMC、壳聚糖、制备温度和p H对体外释放度有不同程度的影响。结论阿奇霉素微乳滴眼液适宜采用反向透析法考察其体外释放行为,且能够达到较好的缓释效果,体外释放稳定。

Objective To study the method for the determination of drug release behavior of azithromycin microemulsion eye drops in vitro. Methods The content of azithromycin in artificial tears were determined by HPLC,and the drug release behavior of azithromycin microemulsion were studied and compared by various methods,to study the in vitro release mechanism. And the influence factors of release rates in vitro were studied. Results HPLC method was able to analyze azithromycin quantity in artificial tears accurately. The release of azithromycin microemulsion was stable within 10 h,and resulted from a combination of diffusion and erosion. Studies showed that oil phases and emulsifiers,HPM C,chitosan,temperature and p H had different influences on the release rates of azithromycin microemulsion. Conclusion Drug release behavior of azithromycin microemulsion is adaptive to be investigated by reverse dialysis bag technique,the azithromycin microemulsion eye drops has advantages of better in vitro sustained release and more stable release profile.