盐酸地匹福林眼用凝胶剂的研究

目的：研制了盐酸地匹福林眼用凝胶剂，进行了体外释放、体外渗透以及眼部刺激性实验。方法：建立了高效液相色谱法测定制剂的含量及体外释药量的方法，采用透析膜扩散法进行处方的体外释药实验，采用离体角膜进行体外渗透实验。结果：亲水凝胶材料含量越小，盐酸地匹福林从凝胶基质中释放越快，凝胶剂体外释药符合一级释放动力学方程。凝胶剂离体角膜渗透行为符合一级释放规律。盐酸地匹福林凝胶剂具有较低的眼部刺激性。结论：盐酸地匹福林眼用凝胶剂有较好的缓释行为，可以明显降低眼部刺激。

The Study of Dipivefrin Hydrochloride Ophthalmic Gel

Dipivefrin hydrochloride ophthalmic gel was prepared and the release test and the isolated cornea permeation test of the formulation in vitro were investigated. The release test of the formulation was studied by using permeable membrane. The content and the release amount of Dipivefrin hydrochloride from the gel base were measured by high performance liquid chromatography. The cornea permeation test of the formulation was studied by using isolated rabbit corneas. The formulation release behavior in vitro followed the first-order kinetic equation. The release amount of Dipivefrin hydrochloride raised significantly with less polymer in the formulation. The cornea permeation behavior of the drug in vitro followed the first-order kinetic equation. The eye irritancy of Dipivefrin hydrochloride gel is lower than that of eyedrops.