硝酸毛果芸香碱温敏凝胶的研制及溶蚀性能研究

目的制备硝酸毛果芸香碱温敏凝胶,考察其载药凝胶溶蚀行为。方法以泊洛沙姆为温敏凝胶基质制备硝酸毛果芸香碱眼用凝胶,通过凝胶相变温度筛选最佳处方,采用无膜溶蚀实验研究凝胶释药特性。结果18%、19%、20%的泊洛沙姆407溶液在体温范围内发生相变形成凝胶,其pH≈7,凝胶中硝酸毛果芸香碱释放速度分别为0.462、0.393、0.294 mg.min-1。结论18%-20%泊洛沙姆407溶液适合作为眼部给药的温敏凝胶基质,凝胶中药物释放基本符合零级释放行为。

Preparation of pilocarpine thermosensitive gel and study on dissolution performance

Objective To prepare poloxamer 407-based in situ gel and to discover the relationship between temperature and concentration of polaxamer 407.Methods The pilocarpine-loaded in situ gel was prepared based on poloxamer 407,and the best concentration of poloxamer 407 was chosen according to the phase transfer temperature.Results Phase transfer temperature of gel with 1820% polaxamer 407 was below human temperature,and the pH≈7.The in vitro release experiment showed that the drug release velocity of 18%,19%,20% in situ gels were 0.462,0.393,and 0.294 mg·min^-1.Conclusion Dissolution of 1820% poloxamer solution was suitable for ophthalmic drug delivery as the thermosensitive gel.