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目的:制备多西他赛固体过饱和自乳化释药系统(DTX-S-sSEDDS),并对其体外特性进行评价。方法:比较了不同的多西他赛自乳化释药系统在理化性质和体外溶出度方面的差异。结果:采用2.5%羟丙基甲基纤维素(HPMC K100)为促过饱和物质,乳糖为固体载体,喷雾干燥法制备获得的多西他赛固体过饱和自乳化释药系统(DTX-S-sSEDDS1),与常规自乳化制剂(DTX-SEDDS2)相比,DTX-S-sSEDDS1处方中自乳化油辅料用量减少2/5,经水分散后的粒径(106.12nm)仍小于DTX-SEDDS2的粒径(119.84nm);水中2h累积溶出百分率(90.96%)显著大于DTX-SEDDS2(76.77%),是原料药(2.87%)的约32倍。结论:所制备的多西他赛固体过饱和自微乳化释药系统(DTX-S-sSEDDS)在减少自乳化辅料用量的同时,可大大提高药物DTX的溶解性和溶出度,为进一步研发安全性和稳定性好的多西他赛自乳化新制剂提供了理论和实验依据。
Objective: To prepare docetaxel solid supersaturated self-emulsifying drug delivery system (DTX-S-sSEDDS), and to evaluate its in vitro characteristics. Methods: The differences in physicochemical properties and in vitro dissolution of different docetaxel self-emulsifying drug delivery systems were compared. Results: The docetaxel solid supersaturated self-emulsifying drug delivery system (DTX-S-100) was prepared by spray-drying 2.5% hydroxypropyl methylcellulose (HPMC K100) Compared with DTX-SEDDS2, the amount of self-emulsifying oil excipients in DTX-S-sEDDS1 formulation decreased by 2/5 compared with conventional self-emulsifying formulation (DTX-SEDDS2) (119.84nm). The cumulative dissolution rate in water for 2h (90.96%) was significantly higher than that of DTX-SEDDS2 (76.77%), which was about 32 times that of API (2.87%). Conclusion: The docetaxel solid supersaturated self-microemulsifying drug delivery system (DTX-S-sSEDDS) can greatly improve the solubility and dissolution of drug DTX while reducing the amount of self-emulsifying excipients. In order to further develop safety Sexual and stable docetaxel self-emulsifying new formulations provide a theoretical and experimental basis.