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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 develop sirolimus (SRL) dropping pills in order to improve its solubility. Methods: The matrix of SRL drip pills was screened. The orthogonal test was used to optimize the formulation and technology of SRL drip pills. The equilibrium solubility, hygroscopicity and in vitro release characteristics were investigated. Results: PEG6000 was selected as the substrate of SRL dropping pills. The best prescription and preparation conditions were as follows: the dosage of SRL and matrix was 1:10, the dropping speed was 65 drops / min, the dropping temperature was 95 ℃, the temperature of coolant At 5 ℃. In different solvents, the equilibrium solubility of SRL drops significantly increased compared with that of SRL, and the hygroscopicity was stronger. Compared with the commercially available SRL nanocrystals, SRL dropping pills released rapidly and completely, with no significant difference . Conclusion: SRL dropping pills can significantly improve the SRL solubility and improve the dissolution performance, worth further study.