非诺贝特自乳化半固体骨架胶囊的制备

Preparation of Self-microemulsifying Semi-solid Matrix Hard Capsules of Fenofibrate

目的制备非诺贝特自乳化半固体骨架胶囊并进行处方优化。方法以药物在不同油相中的溶解情况选择油相;采用伪三元相图法考察不同乳化剂形成微乳的能力和区域,绘制不同处方组成的伪三元相图;以体外乳化速率为评价指标筛选处方,并制备非诺贝特自乳化半固体骨架胶囊。结果该胶囊中的油相为油酸乙酯,乳化剂为Tween 80,助乳化剂为丙二醇,半固体载体为泊洛沙姆188,按优化处方制得的非诺贝特自乳化半固体骨架胶囊固化较快,37℃轻微搅拌条件下约2 min即可形成粒径(30±4)nm的微乳。结论成功制备非诺贝特自微乳半固体骨架胶囊,且工艺简单,易于工业化生产,具有良好的应用前景。

Objective To develop the formulation of fenofibrate self-microemulsifying semi-solid matrix hard capsules drug delivery system. Methods The solubility of fenofibrate in oil was investigated to choose the oil. Pseudoternary phase diagrams were used to evaluate the self-microemulsification existence area for different emulsifier and co-emulsifier. The rate of self-microemulsification in vitro as the index, the optimum formulation was determined for fenofibrate self-microemulsifying semi-solid matrix hard capsules. Results In the optimum formulation, ethyl oleate, Tween 80, propanediol and poloxamer 188 were seleted as oil phase, emulsifier, co-emulsifler, and semi-solid matrix, respectively. The fenofibrate self-microemulsifying semi-solid matrix hard capsules prepared according to the optimized formulation could form fine microemultion with the particle size of （32±4） nm within 2 rain, under gentle stirring at 37℃. Conclusion Enofibrate self-microemulsifying semi-solid matrix hard capsules was prepared successfully with a simple process. And it would be a promising formulation in the future.