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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-效应面法筛选最优处方,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13 s;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5.58 cm·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。
Pearl eyesight eye drops in the eye a short time, affecting the curative effect. This article attempts to make it ophthalmic temperature-sensitive gel in situ, looking forward to prolong the drug in the eye retention time. Poloxamer 407 and poloxamer 188 were used as the gel matrix and carbomer 934 as the bioadhesive material. The best prescriptions were screened by the star design-response surface method and the rheological properties, In vitro dissolution and release mechanism, isolated corneal permeability and retention time were evaluated. The results showed that the formulation was Newtonian at 25 ℃ and formed a gel with a certain strength at 35 ℃. The gel had the property of pseudoplastic fluid, and the gelation time was 13 s. The gel dissolution and drug release all met the zero-order kinetic Learning equation; corneal apparent transmission coefficient of 5.58 cm · s-1; residence time is 7 times the commercially available eye drops. The resulting pearl eyesight good in situ gel gel, can extend the role of drug purposes.