丹酚酸B磷脂复合物自乳化药物传递系统的制备及质量评价  

Optimization and Characterization of SalB-PC Loaded Self-emulsifying Drug Delivery System

作　　者：童廷德[1] 黄蕊[1] 孙逊[1] 张彦 龚涛[1] 张志荣[1] 

机构地区：[1]四川大学华西药学院靶向药物与释药系统教育部重点实验室,成都610041 [2]重庆药友制药有限公司研发中心,重庆401121

出　　处：《四川大学学报（医学版）》2013年第2期303-307,共5页Journal of Sichuan University(Medical Sciences)

摘　　要：目的制备丹酚酸B磷脂复合物(SalB-PC)自乳化药物传递系统(SEDDS),并对其进行质量评价。方法利用单因素筛选和伪三元相图法,根据乳化效率、乳化后样品的性状及其粒径等指标,筛选出最优处方,并对自乳化制剂的形态学、粒径和电位,以及在人工肠液中的释放特性等质量指标进行考察。结果最优处方:SalB-PC∶Lauroglycol FCC∶Cremophor EL∶Transcutol P的质量比为9∶45∶40∶15。SalB-PC自乳化制剂为黄色澄清液体,经过100倍稀释形成的乳剂粒径为(187.2±7.1)nm,多分散指数(PDI)为0.267±0.008,zeta电位为(-35.6±2.7)mV,在人工肠液中的释放速率比SalB溶液和SalB-PC溶液缓慢。结论水溶性药物丹酚酸B可以制备成自乳化给药系统,该剂型能减缓SalB在人工肠液中的释放速率。Objective To prepare self-emulsifying delivery system （SEDDS） of Salvianolic acid B phospholipid complex （SalB-PC） and evaluate its quality. Methods The best formulation was optimized using single-factor and pseudo-ternary phase diagrams, according to the emulsifying efficiency, the characteristics and partical size of the emulsion and other indicators. The morphology, particle size, zeta-potential and the release in artificial intestinal fluid of self-emulsifying formulation were evaluated. Results The weight ratio of SalB-PC Lauroglycol FCC ： Cremophor EL ： Transcutol P in the best formulation was 9 ： 45 ： 40 ： 15. SalB-PC loaded self- emulsifying formulation is yellow and transparent solution, with partical size about （187. 2 ± 7. 1 ） nm, polydispersity index （PDI） about 0. 267± 0. 008 and zeta-potential about （- 35.6 ± 2.7） mV after diluted about 100- fold. The self-emulsifying formulation released slower than the solution with only SalB or SalB-PC. Conclusion Water-soluble drug Salvianolic acid B can be prepared to SEDDS, and this formulation can slow down the release of SalB in artificial intestinal fluid.

关 键 词：水溶性药物 丹酚酸B磷脂复合物 自乳化给药系统 

分 类 号：R943[医药卫生—药剂学]