珍珠水解液眼用温敏原位凝胶的制备及性质研究摘要-药学学报.pdfVIP

珠水解液眼用温敏原位凝胶的制备及性质研究 宋立娜，李鹤然，王宏宇，李贞，赵文畅，卢方正，李三鸣* （沈阳药科大学药学院，辽宁沈阳110016） 摘要：因珍珠明目滴眼液在眼部作用时间短，影响疗效。本文试图将其制成眼用 温度敏感型原位凝胶，期待延长药物在眼部滞留时间。以泊洛沙姆407 和泊洛沙姆 188 为凝胶基质，卡波姆 934 为生物黏附性材料；以星点设计-效 面法筛选最优处方，并 对最优处方进行流变学性质、体外溶蚀及释药机制、离体角膜透过性及滞留时间进行 评价。结果表明，在 25 ℃时制剂为牛顿流体，35℃时形成具有一定强度的凝胶，凝胶 具有假塑性流体的特征，胶凝时间为 13s；凝胶溶蚀及药物释放均符合零级动力学方 程；角膜表观透过系数为 5.58cm s-1 ；滞留时间是市售滴眼液的7 倍。所得珍珠明目眼 用原位凝胶性质良好，可达到延长药物作用时间的目的。 关键词：珍珠水解液；泊洛沙姆；温敏原位凝胶；流变学；角膜透过性；滞留时 间 收稿日期： 2016-05-24; 修回日期: 2016-06-02 基金项目：国家自然科学基金资助项目81273445 ） *通讯作者Tel / Fax: 86-24 E-mail: li_sanming@126.com 1 Preparation and properties of thermosensitive in situ gel for ophthalmic formulation containing pearlhydrolyzate * SONG Li-na, LI He-ran, WANG Hong-yu, LI Zhen, ZHAO Wen-chang, LU Fang-zheng, LI San-ming (Shool of Pharmmacy, Sheny ang Pharmaceutical University, Shenyang 110016, China) Abstract:The aim of this paper was to obtain an ophthalmic thermosensitive in situ gel with improved mechanical and mucoadhesive properties that could prolong the retention time and enhance the bioavalability of pearl hydrolyzate. In situ gel formulations comprised of poloxamer 407, poloxamer188 and Carbopol 934 were prepared and optimized by central composite design response surface methodology. The rheological properties, transcorneal permeability, retention time and in vitro release behaviors of the optimal gel formulation were investigated. The results indicated that ophthalmic in situ gel was Newtonian liquid at 25℃, while it performed a semisolid gel with non-newtonian liquid property with a gelation time of 13 s at 35℃. Compared with a conventional eye drops, the ophthalmic in situ gel represented a