阿奇霉素原位凝胶滴眼液的制备及体外释放机制考察  

Preparation of ophthalmic thermosensitive in situ gel of azithromycin and the in vitro release mechanism

作　　者：常晓慧[1] 闫笑笑[1] 贺霞[1] 刘慧[1] 薛晓[1] 王东凯[1] 

机构地区：[1]沈阳药科大学药学院,沈阳110016

出　　处：《中国新药杂志》2011年第16期1577-1582,共6页Chinese Journal of New Drugs

摘　　要：目的:研制阿奇霉素温敏原位凝胶滴眼液。方法:以凝胶基质与泪液混合前后的相变温度变化筛选适宜的处方,基于阿奇霉素与硫酸显色的原理,建立UV法测定其体外释放度,以阐明其释放机制。结果:硫酸显色方法能够准确测定阿奇霉素在泪液中的体外释放度,该原位凝胶在8 h内能稳定释放,释放机制为扩散和凝胶溶蚀共同作用。结论:与普通阿奇霉素滴眼液相比较,原位凝胶滴眼液能够达到较好的缓释效果,体外释放稳定,有广泛的应用前景。Objective：To prepare azithromycin thermosensitive in situ gel for ophthalmic drug delivery.Methods：The formulation was screened based on the change in phase-transition temperature after mixing of gel and tear.Spectro-photometric method based on the colour reaction between sulfuric acid and azithromycin was applied to evaluate cumulative release of azithromycin and the in vitro release mechanism.Results：Sulfuric acid method was able to analyze azithromycin quantity in tear accurately.The release of azithromycin from in situ gel was stable within 8 h,and resulted from a combination of diffusion and erosion.Conclusion：Compared with ordinary eye drops,azithromycin in situ gel has advantages of better in vitro sustained release and more stable release profile.The thermosensitive in situ gels of azithromycin will have a wide range of applications.

关 键 词：阿奇霉素 眼部用药 温敏凝胶 硫酸显色反应 体外释放 

分 类 号：R943.41[医药卫生—药剂学] R978.15[医药卫生—药学]