依诺沙星眼用缓释凝胶剂的体外研究

Study on enoxacin sustained-release ophtfaabnic gel in vitro

目的 研究依诺沙星眼用缓释凝胶剂。方法 建立UV法测定制剂的含量及体外释药量,建立HPLC测定制剂离体角膜渗透量,采用溶出度法进行处方的体外释药试验,应用离体角膜进行体外渗透试验。结果 亲水凝胶材料含量越小,依诺沙星从凝胶基质中释放越快,体外释药符合一级释放动力学方程;亲水凝胶含量高,体外释放符合Higuchi方程;离体角膜渗透行为符合零级释放规律。结论 依诺沙星眼用凝胶达到了缓慢释放的目的。

OBJECTIVE: To study enoxacin sustained-release ophthalmic gel. METHODS: The release test of formulation was conducted with permeable membrane. The content and the release amount of enoxacin from gel base were determined by UV. The cornea permeation test of formulation was studied with rabbit corneas. The permeant amount of enoxacin was determined by high performance liquid chromatography. RESULTS: The formulation release behavior in vitro followed the first-order kinetic equation with the less amount of polymer (2.0% & 3.0%) in the formulation; otherwise, it followed Higuchi equation with the higher amount of polyer (4.0%) in the formulation. The permeability of enoxacin was raised significantly with the less amount of polyer in the formulation. The formulation permeation behavior in vitro followed the zero-order kinetic equation. CONCLUSION: The release time of enoxacin ophthalmic gel-forming solution was longer than that of eye-drops.