西罗莫司片的制备及溶出度考察

Preparation and Dissolution of Sirolimus Tablets

目的研制西罗莫司片并考察其溶出度。方法用固体分散技术和薄膜包衣技术制备西罗莫司片,采用差示扫描量热分析和X-射线衍射分析方法鉴别西罗莫司在载体中的存在状态。建立溶出度检查方法 ,对西罗莫司片和市售Rapamune^(?)片溶出考察。结果西罗莫司在载体中以非晶体状态存在,西罗莫司固体分散物提高西罗莫司片的溶出度,西罗莫司片和市售Rapamune^(?)片溶出相近。结论研制的西罗莫司片的溶出符合中国药典要求。

OBJECTIVE To prepare sirolimus tablets and evaluate its dissolution. METHODS The sirolimus tablets were prepared by the technique of solid dispersions and the film coating. Differential scanning calorimeter （DSC） and X-ray diffraction were used to determine the status of sirolimus in carriers. The method for analysis of dissolution was established and the dissolution of sirolimus tablets and Rapamune tablets were determined. RESULTS The sirolimus existed in amorphous form in solid dispersions. The sirolimus solid dispersions increased the dissolution of sirolimus tablets obviously. The dissolution of sirolimus tablets and Rapamune tablets is similar. CONCLUSION The dissolution of sirolimus tablets accorded with the demands of Chinese Pharmacopeia.