Preparation and Properties in vitro of Sirolimus Dropping Pills / 中国药师

ABSTRACT

Objective:To prepare sirolimus ( SRL) dropping pills to improve SRL solubility and dissolution. Methods:The base of SRL dropping pills was screened. The optimal formula and preparation process were also optimized by orthogonal design. The equi-librium solubility, hygroscopicity and drug release in vitro of SRL dropping pills were studied. Results: PEG6000 was chosen as the base. The optimal preparation conditions of SRL dropping pills were as follows the ratio of SRL and base was 1∶10, the dropping speed was 65 drops/min, the dropping temperature was 95℃ and the temperature of cooling solvent was 5℃. The equilibrium solubili-ty of SRL dropping pills in different solvents was increased significantly compared with that of SRL. The hygroscopicity of the dropping pills was notable. The drug release in vitro of SRL dropping pills was similar to that of the marketed tablets with quick and complete re-lease. Conclusion:SRL dropping pills exhibit increased solubility and improved dissolution, which are valuable to be studied further.