西罗莫司滴丸的研制及其体外性质考察

Preparation and Properties in vitro of Sirolimus Dropping Pills

目的:研制西罗莫司(SRL)滴丸,以期改善其溶解性能。方法:对SRL滴丸的基质进行筛选;用正交试验优选SRL滴丸的最佳处方及工艺;对其平衡溶解度、吸湿性及体外释药特性进行考察。结果:选用PEG6000为SRL滴丸的基质;优选出的最佳处方及制备条件为:SRL与基质的用量为1∶10,滴速为65滴/min,滴制温度为95℃,冷却剂温度为5℃;在不同溶剂中,SRL滴丸的平衡溶解度均较SRL有显著增加,吸湿性较强,与市售SRL纳米结晶片相比,SRL滴丸释药迅速而完全,无显著性差异。结论:SRL滴丸可显著提高SRL溶解度及改善溶出性能,值得进一步研究。

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 equilibrium 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 solubility 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 release. Conclusion： SRL dropping pills exhibit increased solubility and improved dissolution,which are valuable to be studied further.