盐酸小檗碱离子型眼用原位凝胶的研究

Study of ion-activated in situ gel system containing berberine hydrochloride for ocular use

[目的]制备并评价眼用盐酸小檗碱离子敏感性原位凝胶剂。[方法]采用结冷胶作为离子敏感型高分子材料制备盐酸小檗碱离子敏感性原位凝胶剂;黏度计考察其流变学特征;采用荧光示踪法测定凝胶剂的眼部滞留时间;同体自身对照法考察凝胶剂的眼部刺激性。[结果]盐酸小檗碱离子敏感性原位凝胶剂为假塑性流体,对兔眼无刺激;该原位凝胶剂的滞留时间为3 h,比滴眼液增加了6倍。[结论]盐酸小檗碱离子敏感性原位凝胶剂的刺激性低,眼部滞留时间长,具有一定的缓释效果。

[Objective] To prepare and evaluate the ion-activated in situ gel system containing berberine hydroehloride for ocular use. [Methods] The ion-activated in situ gel of berberine hydrochloride was prepared by using gellan gum as ion-activating material. Rheological quality was investigated by examination of the viscosity. Ocular residence time was determined by fluorescence-labeled technique. [Results] The investigation of the rheological curve demonstrated that the ion-activated in situ gel of berberine hydroehloride represented a pseudoplastic flow type. Both ion-activated in situ gel of berberine hydrochloride and the eye-drop of Berberine had no irritation after ocular administration. Ocular residence time of ion-activated in situ gel of berberine hydrochloride was 6 times higher than that of eye-drop of Berberine. [Conclusion] As liquid ophthalmic delivery systems, ionactivated in situ gel of berberine hydrochloride can undergo in situ phase transition to form gels, which can prolong the residence time of in-situ gelling agent to enhance the effect of drug at the target site without irritation to the eye.