依维莫司分散片的制备及质量考察

Preparation and Quality Control of Everolimus Dispersible Tablets

目的制备依维莫司分散片并建立其质量控制方法。方法用固体分散技术和流化床技术制备依维莫司分散片,采用高效液相色谱法测定其含量、有关物质和溶出度,建立依维莫司分散片质量控制方法。结果依维莫司分散片在1min内全部崩解,分散性均匀,45min溶出达85%以上。在高效液相色谱法含量测定中,依维莫司在100~1200μg·m L^(-1)范围线性良好,平均回收率为99.26%,RSD为0.52%;在溶出测定中,依维莫司在1.0~12.0μg·m L^(-1)范围线性良好,平均回收率为100.32%,RSD为0.67%。结论本品制备工艺简单,质量控制方法准确,质量符合药典要求。

OBJECTIVE To prepare everolimus dispersible tablets and establish a method for its quality control. Method：The everolimus dispersible tablets were prepared by the technique of solid dispersions and the fluidized-bed. The content,related substance and dissolution of the everolimus dispersible tablets were determined by HPLC,and its quality control method was established. RESULTS The everolimus dispersible tablets could completely disintegrate within 1 minute,and the dispersible uniform was excellent,and its dissolution was more than 85%with 45 minutes. A good linear relationship was obtained in the range of 100 ~ 1200μg·m L^（-1）with the average recovery of 99. 26%（ RSD = 0. 52%）. The dissolution sample showed a good linear relationship at a range of 1. 0 ~12. 0μg·m L^（-1）with the average recovery of 100. 32%（ RSD = 0. 67%）. CONCLUSIONS The preparing technique of the everolimus dispersible tablets is simple. The quality control method is accurate,and its quality meets the requirements of Pharmacopoeia.