甘草酸磷脂／胆盐混合胶束的制备及其体内评价  

Preparation and in Vivo Evaluation of Glycgrrhizin acid-Sodium Deoxycholate/Phospholipid-Mixed Micelles

作　　者：靳士晓[1,2] 靳世英[1,2] 李仙义[3] 吕青远[1] 付珊珊[1,2] 韩晋[1] 袁海龙[1] 

机构地区：[1]中国人民解放军第三O二医院药学部,北京100039 [2]成都中医药大学药学院,成都611730 [3]中国人民解放军总后勤部卫生部药品仪器检验所,北京100071

出　　处：《中国药学杂志》2013年第4期280-285,共6页Chinese Pharmaceutical Journal

基　　金：国家教育部留学归国人员科研启动基金(20101561);北京市自然科学基金资助项目(7122176)

摘　　要：目的制备甘草酸的磷脂/胆盐混合胶束,提高甘草酸口服生物利用度。方法采用薄膜分散法制备甘草酸的磷脂/胆盐混合胶束,并通过胶束理化性质的测定、在体肠吸收及药动学实验对其综合评价。结果制备的载药胶束平均粒径为(82.99±7.5)nm,Zeta电位为(-32.23±1.05)mV,分布均一且具有良好的稳定性;在体肠吸收与对照药物相比,有明显改善;药动学实验中,混合胶束的ρmax达到77.26μg·mL-1,是对照药物的2.82倍,显著提高甘草酸口服生物利用度。结论磷脂/胆盐混合胶束有望开发成为甘草酸的新型药物传递系统。OBJECTIVE To improve the oral bioavailability of glycyrrhizin by preparing glycyrrhizin-sodium deoxycholate/phospholipid-mixed micelles （GL-SI）C/PL-MMs）. METHODS GL-SDC/PL-MMs was prepared by a film dispersion method. In order toevaluate the property GL-SDC/PL-MMs comprehensively, physical and chemical properties determination, in situ intestinal absorption, and pharmaeokinetics test were carried out. RESULTS The average particle size of drug-loaded micelles prepared by film dispersion method was （ 82. 99± 7.5 ） nm and Zeta potential was （ - 32. 23 ± 1.05 ） mV. Compared with the control drug, glycyrrhizin loaded in SDC/PL-MMs significantly improved its in situ intestinal absorption. The oral bioavailability was markedly enhanced, indicated by the increase of Pmax to 77. 26 μ·gmL - 1, which was 2. 82 times of that of the control drug. CONCLUSION SDC/PL-MMs is expected to be developed into a new drug delivery systems of GL.

关 键 词：甘草酸 磷脂 胆盐混合胶束 在体肠吸收 药动学 

分 类 号：R944[医药卫生—药剂学]