环孢菌素A自乳化半固体骨架胶囊的制备

Preparation of self-microemulsifying semi-solid matrix hard capsules of cyclosporine A

目的考察环孢菌素A自乳化半固体骨架胶囊的处方。方法制备药物的饱和溶液用以测定药物在不同油相中的溶解度;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相图;采用体外乳化实验筛选处方,并制备环孢菌素A自乳化半固体骨架胶囊。结果该胶囊中的乳化剂为Tween 80-聚氧乙烯(40)氢化蓖麻油(质量比为1∶1),助乳化剂为聚乙二醇-8-甘油辛酸/葵酸脂(labrasol),油相为辛酸/癸酸三甘油酯,半固体载体为泊洛沙姆188-硬脂酸聚烃氧(40)酯(质量比为1∶1)。该处方所形成的微乳平均粒径为40 nm。结论按优化处方制得的环孢菌素A自乳化半固体骨架胶囊能够提高环孢菌素A在水中的溶出度。

Objective To develop the formulation of cyclosporine self-microemulsifying hard capsules drug delivery system. Methods A supersaturated solution of cyclosporine A was prepared to measure the solubility, self-microemulsification in vitro, and pseudoternary phase diagrams were used to evaluate the self-microemulsification existence area. The optimum formulation was determined for cyclosporine A self-microemulsifying hard capsules. The cyclosporine A self-microemulsifying hard capsules and the dissolution was measured. Results In the optimum formulation, Tween80-RH40（mass ratio is 1：1）, labrasol, miglyol 812N and poloxamer 188-S-40 （mass ratio is 1：1）were seleted as emulsifier, co-emulsifier, oil phase and semi-solid matrix, respectively. Microemulsion droplets with a mean droplet size of 40 nm were formed by using this formulation. Conclusions The dissolution of cyclosporine A in water is significantly increased by using optimized formula of cyclosporine A self-microemulsifying hard capsules drug delivery system.