阿奇霉素原位凝胶滴眼液的制备及体外释放机制考察

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。

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

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 azithromy...