环淫羊藿苷元微乳的制备及肠吸收研究

Study on preparation of CIT microemulsion and its Absorption in intestine

目的:制备环淫羊藿苷元(CIT)微乳,考察其理化性质及大鼠在体肠吸收特性。方法:采用伪三元相图得到空白微乳的优化处方,制备CIT微乳;采用透射电镜及激光粒度分析仪考察CIT微乳的形态、粒径分布和Zeta电位;采用葡聚糖凝胶柱色谱法测定CIT微乳的包封率;通过大鼠在体肠灌流模型,采用高效液相色谱法测定灌流液中CIT的含量,分析其肠吸收特性。结果:CIT微乳的最佳处方为肉豆蔻酸异丙酯/丙三醇-水-油酸乙酯体系,其比例为3∶3∶4∶2;透射电镜观察乳滴呈圆球形,大小均匀;平均粒径61.7 nm,Zeta电位-46.3 mV,平均包封率(92.1±1.74)%(n=3);CIT及其微乳在大鼠各肠段均有吸收,CIT微乳在各肠段的吸收较原料药显著增加(P<0.01)。结论:CIT微乳的制备工艺可行,微乳能促进CIT在大鼠小肠的吸收。

Objective： To prepare CIT microemulsion and to investigate its properities and the Absorption character in rat intestine in situ.Method： The optimum formulation of the blank microemulsion was selected by pseudo tertiary phase diagrams and the CIT microemulsion was prepared based on the blank microemulsion.The appearance,particle diameter distribution and Zeta potential were investigated by electron microscopy and grainsize analyzer.The entrapment efficiency was determined by sephadex column chromatography.An in situ single pass intestine perfusion method was used to investigate the intestinal Absorption of CIT microemulsion.HPLC method for determination of CIT in the intestinal flux was established.Result： The formulation was OP-glycerol-water-ethylis oleas（3∶3∶4∶2）.CIT microemulsion in electron microscopy was consisted of small spherical drop.The mean diameter was 61.7 nm,Zeta potential was-46.3 mV.The Entrapment efficiency was（92.1±1.74）%（n=3）.Both CIT and CIT microemulsion had been Absorbed in general intestinal tract,and the Absorption of CIT microemulsion was significantly high compared with CIT in duodenum,colon,jejunum and ileum（P〈0.01）.Conclusion： The preparation technology of CIT microemulsion was feasible,and the microemulsion system might improve the Absorption of CIT in the intestinal tract.