环孢素A自微乳软胶囊的制备及质量控制

摘要

目的:制备环孢素A自微乳软胶囊,确定纳米粒径测定方法,控制产品质量.方法:通过测定环孢素A溶解度,以及以自微乳化后的粒径、自乳化时间和色泽为指标,对油相、潜溶剂、乳化剂、助乳化剂进行筛选,制备环孢素A自微乳软胶囊；通过稳定性、精密度等方法学试验,确定自微乳化后乳滴直径测定方法,控制产品质量.结果与结论:油相、潜溶剂、乳化剂、助乳化剂比例为1∶2∶2∶2时可获得优良的自乳化效果,软胶囊平均自微乳粒径为25 nm,因此提高了环孢素生物利用度,减少了服用量.%Objective:To prepare cyclosporine microemulsion soft gelatin capsules and to determine the nano-particle size for the quality of products.Methods:The cyclosporine A solubility,particle diameter after self-microemulsifying,self-emulsifying time and color were determined as indicators for the screening of oil phase,latent solvents,emulsifiers and co-emulsifiers to prepare a cyclosporine microemulsion soft capsule; stability,precision and other methodological tests were conducted to establish a method for the measurement of droplet size after microemulsifying to control the quality of products.Results and Conclusion:The oil phase,latent solvents,emulsifiers and coemulsifiers at the ratio of 1:2:2:2 obtained excellent selfemulsifying effects,the average particle diameter of self-microemulsifying in soft capsules was 25 nm.The resulted product can increase cyclosporine bioavailability and reduce the dosage.