pH敏感型黄芩苷眼用原位凝胶剂的体外研究

In vitro study on baicalin pH-triggered ophthalmic in situ gel system

目的:研究pH敏感型黄芩苷眼用原位凝胶剂。方法:采用桨法进行处方的体外释药试验,建立UV法测定体外释药量;应用离体角膜进行体外渗透试验,建立HPLC法测定离体角膜渗透量。结果:凝胶基质黏度随pH值的增大而增大,其拐点在pH 5.8～6.0之间;在一定范围内,亲水凝胶材料用量越大,凝胶基质的缓释作用越好;凝胶体外释放符合Ritger-Peppas方程;离体角膜渗透行为符合零级释放规律。结论:pH敏感型黄芩苷眼用原位凝胶剂达到了缓释释放的目的。

Objective：To prepare baicalin pH-triggered ophthalmic in situ gel.Methods：Release behavior of baicalin from pH-triggered in situ gel was explored in a dissolution apparatus with paddle method.The released amount of baicalin from pH-triggered gel was determined by UV;the cornea permeation of gel formulations was determined in rabbit corneas.The permeated amount of baicalin was determined by high performance liquid chromatography.Results：The viscosity of gel increased with increasing pH value.The inflexion of viscosity was from 5.8 to 6.0.The in vitro release behavior of the formulation followed Ritger-Peppas equation.The in vitro permeation behavior followed the zero-order kinetic equation.Conclusion：The release time of baicalin from pH-sensitive ophthalmic in situ gel is longer than eye-drops.