复方甲硫酸新斯的明眼用原位凝胶的处方工艺研究

目的 筛选用于治疗近视的复方甲硫酸新斯的明眼用原位凝胶处方。方法 温度敏感型凝胶以泊洛沙姆P407和泊洛沙姆P188为基质；离子敏感型凝胶以去乙酰结冷胶为基质；pH敏感型凝胶以卡波姆P934、卡波姆P940和羟丙基甲基纤维素为基质，以胶凝的黏度与成分的相溶性为考察指标，筛选最佳基质处方。采用美国药典溶出度测定法第三法的改良法，作缓释制剂的释放度考察。结果 以温度敏感型的泊洛沙姆P407 24%和P188 10%合用的基质制备复方甲硫酸新斯的明眼用原位凝胶最为适合。结论 本法制备眼用原位凝胶的工艺可行，并具有较好的缓释效果。

Study on the Formulation of Compound Neostigmine in Situ Ophthalmic Gel

OBJECTIVE To screen out the formulation of compound neostigmine in situ ophthalmic gel for myopia. METHODS Carbopol P934 and P940 were selected and researched as the matrixl of in situ pH-setting gel and its co-effect of combination with hydroxyl-propyl-methyl-cellulose(HPMC, K₄M). The formulation of base material of in situ ion-setting ophthalmic gel was gelrite. And the main matrix material of in situ thermo-setting gel was poloxamer P407 and P188. On the screening of the formulation, the viscosity of gel and the compatibility of ingredients were used as two indexes. RESULTS The applicative formulation of compound neostigmine in situ ophthalmic gel was thermo-setting gel which was including 24% poloxamer P407 and 10% poloxamer P188. CONCLUSION This formulation is feasibility, and this preparation has good properties of sustained release.