丹参双相载药乳剂的研制及其质量评价  

Development of biphasic drug-loading lipid emulsion of Salvia miltiorrhiza and its quality evaluation

作　　者：王银艳[1] 李曦[1] 赖秀俊 黎伟[1] 杨雅静[1] 储婷[1] 毛声俊[1] 

机构地区：[1]四川大学华西药学院靶向药物及释药系统教育部重点实验室,四川成都610041

出　　处：《中国中药杂志》2014年第19期3748-3752,共5页China Journal of Chinese Materia Medica

基　　金：四川省科技支撑计划项目(2011SZ0009)

摘　　要：探讨以乳剂同时载药丹参脂溶性与水溶性成分的可行性,为从制剂学方面综合利用丹参药效成分提供新思路。以丹参酮ⅡA,丹酚酸B为原料,大豆磷脂与帕洛沙姆188为混合乳化剂,甘油为等渗调节剂,采用星点设计-效应面法优选处方,高速剪切法制备初乳,续以高压均质机进行匀化,制备丹参双相载药静脉乳剂,进而考察其药剂学特性与稳定性。所制得产品外观为橙黄色乳状液,平均粒径241 nm,Zeta电位-35.3 m V,其中丹参酮ⅡA载药量为0.5 g·L-1,丹酚酸B载药量为1g·L-1,长期留样稳定性良好。结果表明研制的乳剂可同时载药脂溶性成分丹参酮ⅡA,水溶性成分丹酚酸B,可为充分发挥丹参的药效奠定制剂学基础。The feasibility of simultaneously loading both liposoluble and water-soluble components of Salvia miltiorrhiza in emulsion was discussed, in order to provide new ideas in comprehensive application of effective components in S. miltiorrhiza in terms of technology of pharmaceutics. With tanshinone ⅡA and salvianolic acid B as raw materials, soybean phospholipid and poloxamer 188 as emulsifiers, and glycerin as isoosmotic regulator, the central composite design-response surface method was employed to optimize the prescription. The coarse emulsion was prepared with the high-speed shearing method and then homogenized in the high pressure homogenizer. The biphasic drug-loading intravenous emulsion was prepared to investigate its pharmaceutical properties and stability. The prepared emulsion is orange-yellow, with the average diameter of 241 nm and Zeta potential of -35.3 mV. Specifically, the drug loading capacity of tanshinone II A and salvianolic acid B were 0. 5 g · L- 1 and 1 g · L- 1, respectively, with a good stability among long-term retention samples. According to the results, the prepared emulsion could load liposoluble tanshinone ⅡA and water-soluble salvianolic acid B simultaneously, which lays a pharmaceutical foundation for giving full play to the efficacy of S. miltiorrhiza.

关 键 词：丹参酮ⅡA 丹酚酸B 制备工艺 星点设计 质量评价 

分 类 号：R283[医药卫生—中药学]