[关键词]
[摘要]
目的 探讨自乳化释药系统(SEDDS)对多组分同时增溶的可行性。方法 以姜黄素类组分为模型药物,采用D-最优混料设计优化SEDDS处方,以对双去甲氧基姜黄素、去甲氧基姜黄素和姜黄素的载药量、SEDDS的粒径和乳化时间为指标对SEDDS进行优化并对其进行综合评价,探讨SEDDS对多成分同时增溶的可行性。结果 优化得SEDDS最佳处方为Obleique CC497-聚山梨酯20-Transcutol P(0.21∶0.50∶0.29),SEDDS粒径为(248.8±3.4)nm,乳化时间为(70±1)s。37 ℃时,SEDDS对双去甲氧基姜黄素、去甲氧基姜黄素和姜黄素的最大载药量分别为2.298、12.220、52.561 mg/g,在水中的溶解度分别为0.107、0.661、1.648 mg/mL。结论 SEDDS能实现对多组分的同时增溶。
[Key word]
[Abstract]
Objective To explore the feasibility of self-emulsifying drug delivery system (SEDDS) for multicomponents simuitaneous solubilization. Methods The curcumin (Cur) components were used as model drug, D-optimal mixture design was used to optimize SEDDS prescription, and the contents of bisdemethoxycurcumin (BDMC), demethoxycurcumin (DMC), and Cur, SEDDS particle size, and emulsifying time were made as indicators to select and evaluate SEDDS, so as to explore the feasibility of SEDDS for the multicomponents simuitaneous solubilization. Results The optimal SEDDS prescription was Obleique CC497-Tween 20-Transcutol P (0.21∶0.50∶0.29), SEDDS particle size was (248.8 ± 3.4) nm, and emulsifying time was (70 ± 1) s. At 37 ℃, the maximum loading capacities of SEDDS for BDMC, DMC, and Cur were 2.998, 12.220, and 52.561 mg/g, respectively, and the solubilities in water were 0.107, 0.661, and 1.648 mg/mL. Conclusion SEDDS can realize the solubilization of multicomponent simultaneously.
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[基金项目]
重庆市GLP中心能力提升建设(cstc2012pt-kyys10001);重庆自然科学基金课题(cstc2012jjA1415);中药新产品开发研究能力提升建设(cstc2012pt-kyys10004)