水飞蓟宾磷脂复合物自微乳给药系统研究  

Study of SLB phospholipid complex Self-microemulsifying Drug Delivery System

作　　者：丁沐淦[1] 龙晓英[2] 李岩[1] 何琳[2] 

机构地区：[1]广东岭南职业技术学院,广州510663 [2]广东药学院,广州510006

出　　处：《海峡药学》2010年第6期19-23,共5页Strait Pharmaceutical Journal

基　　金：广东省科技厅重点引导项目(2005B10401004)

摘　　要：目的研制水飞蓟宾(SLB)磷脂复合物自微乳化胶囊并对其进行体外评价。方法通过单因素考察结合正交设计将SLB制成磷脂复合物,测定了该复合物的溶解度和油水分配系数,进一步制成自微乳给药系统。结果 SLB磷脂复合物的最佳工艺条件为,反应温度50℃,反应时间2 h,比例1∶2。按此最佳工艺条件制备SLB磷脂复合物,复合率为100%,其溶解度和油水分配系数分别为126.3μg.mL-1,166.64,其最佳自微乳给药系统(PMC)组成及比例为,复合物∶油酸乙酯∶吐温80∶丙二醇=12∶30∶45∶13。按最佳处方制备的SLB磷脂复合物-PMC在人工胃液中36 min内累积溶出百分率已达到80%。结论将水飞蓟宾制成磷脂复合物自微乳化胶囊能显著提高其体外溶出度。OBJECTIVE The formulation design and vitro evaluation of selfmicroemulsifying drug delivery system（SMEDDS） for silibinin（SLB） phospholipid complex.METHODS SLB was prepared into phospholipid complex by single factor investigation and orthogonal design.The solubility and O/W coefficient of SLB phospholipid complex were determined.Further,the SLB phospholipid complex was formulated into SMEDDS.RESULTS The best productive condition of SLB phospholipid complex were 50℃ reaction temperature,2h reaction time,the ratio of SLB and phospholipid was 1∶2.the complex ratio was 100% following above to prepared.The solubility and O/W coefficient of distribution of SLB phospholipid complex were 126.3 μg·mL-1 and 166.64,respectively.the optimum formulations of SLB phospholipid complex-SMEDDS were composed of complex,ethyl oleate,tween 80 and propylene glycol,with the ratio of 12∶30∶45∶13.The dissolution of the SLB complex-PMC in artificial gastric juice was 80% in 36 min.CONCLUSION SLB phospholipid complex-SMEDDS can improve the dissolution of SLB.

关 键 词：水飞蓟宾 磷脂复合物 自微乳化释药系统 溶解度 油水分配系数溶出度 

分 类 号：R282.71[医药卫生—中药学]