pH敏感型黄岑苷眼用原位凝胶剂的体外研究

摘要

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.%目的:研究pH敏感型黄岑苷眼用原位凝胶剂.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敏感型黄岑苷眼用原位凝胶剂达到了缓释释放的目的.