甘草次酸醇质体水凝胶贴剂的制备与透皮给药研究  

Preparation and in vitro percutaneous permeation profile of glycyrrhetinic acid ethosome hydrogel patch

作　　者：闫菁华[1] 豆婧婧[1] 徐坤[1] 陈贵[1] 惠先[1] 鞠大宏[2] 郝保华[1] 

机构地区：[1]西北大学生命科学学院中药学教研室,西安710069 [2]中国中医科学院中医基础理论研究所,北京100700

出　　处：《第二军医大学学报》2011年第7期763-766,共4页Academic Journal of Second Military Medical University

基　　金：陕西省教育厅产业化中试项目(2010jc20);国家重大新药创制科技重大专项(2009ZX09502-019)~~

摘　　要：目的探讨甘草次酸醇质体水凝胶贴剂的制备方法,并考察其体外透皮给药的规律与特点。方法注入法制备甘草次酸醇质体,考察其包封率、粒径与表面电位,再制备成水凝胶贴剂;采用改良Franz立式扩散池,HPLC法测定甘草次酸含量,评价甘草次酸醇质体水凝胶贴剂的体外透皮给药规律与特点。结果甘草次酸醇质体外观为圆球形或椭球形,具有层状结构;其对于甘草次酸的包封率为(75.63±1.86)%,粒径为(106.2±20.54)nm,表面电位为(-41.3±2.8)mV。与甘草次酸水凝胶贴剂比较,甘草次酸醇质体水凝胶贴剂的透皮给药速率与累积渗透量高于甘草次酸水凝胶贴剂,24 h时甘草次酸醇质体水凝胶贴剂的累积渗透量是甘草次酸水凝胶贴剂的5.55倍,二者之间差异有统计学意义(t-test,P<0.01)。结论甘草次酸制备成醇质体后能够显著提高水凝胶贴剂的透皮给药效果,表明醇质体水凝胶贴剂是甘草次酸透皮给药的一个理想的载体。Objective To explore the preparation method of glycyrrhetinic acid ethosome（GAE） hydrogel patch and to evaluate its characteristics during in vitro transdermal drug delivery.Methods GAE was prepared by ethanol infusion method,and its entrapment efficiency,size and surface potential were investigated.Then GAE was used to prepare the hydrogel patch.The amount of penetrated glycyrrhetinic acid was determined by HPLC on modified Franz diffusion cells,and then the in vitro transdermal drug delivery of the prepared hydrogel patch was evaluated.Results GAE had a spherical or ellipsoidal appearance and a layered structure,with an encapsulation efficiency of（75.63±1.86）%,a particle size of（106.2±20.54） nm,and a surface potential of（-41.3±2.8） mV.The percutaneous delivery rate and accumulative infiltration quantity of GAE hydrogel patch were significantly higher than those of glycyrrhetinic acid hydrogel patch.The 24 h accumulative infiltration quantity of GAE hydrogel patch was 5.55 times that of the glycyrrhetinic acid hydrogel patch（t-test,P0.01）.Conclusion Compared with glycyrrhetinic acid,GAE can significantly improve the in vitro transdermal delivery of hydrogel patch,demonstrating that ethosome hydrogel patch might be an ideal vector for transdermal delivery of glycyrrhetinic acid.

关 键 词：甘草次酸 醇质体 水凝胶贴剂 皮肤投药 

分 类 号：R943.43[医药卫生—药剂学]