淫羊藿苷元自微乳在Caco-2细胞模型的肠吸收特性初步研究  

Absorption characteristics in intestine of icaritin self-microemulsion via Caco-2 monolayer model

作　　者：王晋艳[1,2] 陈彦[1,2] 张振海[1] 贾东升[1,2] 贾晓斌[1,2] 

机构地区：[1]江苏省中医药研究院中药新型给药系统重点实验室国家中医药管理局中药释药系统重点研究室,江苏南京210028 [2]江苏大学药学院,江苏镇江212013

出　　处：《中草药》2012年第3期476-481,共6页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金资助项目(81173557);江苏省中医药领军人才项目(LJ200913);江苏省中医药局资助项目(LZ09063)

摘　　要：目的制备淫羊藿苷元自微乳,考察其理化性质及体外肠吸收特性。方法在考察淫羊藿苷元理化性质的基础上,以油酸乙酯为油相,聚山梨酯80为乳化剂,丙三醇为助乳化剂制备淫羊藿苷元自微乳,采用透射电镜及激光粒度分析仪测定其稀释后所得微乳的形态、粒径分布和Zeta电位,并采用Caco-2细胞模型初步分析其肠吸收特性。结果所制备的淫羊藿苷元自微乳稀释后,微乳平均粒径为55.6 nm,Zeta电位为30.8 mV,在Caco-2细胞模型上的表观渗透系数(Papp)为(3.52±0.3)×10 6cm/s。结论淫羊藿苷元自微乳制剂稳定,体外研究显示自微乳系统能够促进淫羊藿苷元在肠道的吸收。Objective To prepare icaritin self-microemulsion and investigate its properties and oral absorption characteristics in Caco-2 monolayer model.Methods To prepare icaritin self-microemulsion with ethyl oleate as oil phase,Polysorbate-80 as surfactant,and glycerol as cosurfactant.The appearance,particle diameter distribution,and Zeta potential of the diluted icaritin self-microemulsion were investigated by transmission electron microscopy and laser grain size analyzer,and the intestinal absorption was studied by using Caco-2 monolayer model.Results The mean particle diameter distribution of the diluted icaritin self-microemulsion was 55.6 nm,with Zeta potential of 30.8 mV.The apparent permeability coefficient（Papp） of the diluted microemulsion in Caco-2 monolayer model was（3.52 ± 0.3） × 10 6cm/s.Conclusion The icaritin self-microemulsion is stable and could significantly improve the absorption of icaritin in the intestinal tract.

关 键 词：淫羊藿苷元 自微乳 肠吸收 CACO-2细胞 表观渗透系数 

分 类 号：R283.6[医药卫生—中药学]