反溶剂法制备甘草酸纳米粒的表征与体外透皮特性研究  

Representation and in vitro transdermal characteristics of glycyrrhizic acid nanoparticles prepared by antisolvent recrystallization method

作　　者：许文佳[1] 赵修华[1] 祖元刚[1] 李娜[1] 吴薇薇[1] 

机构地区：[1]东北林业大学森林植物生态学教育部重点实验室,黑龙江哈尔滨150040

出　　处：《中草药》2014年第8期1068-1071,共4页Chinese Traditional and Herbal Drugs

基　　金：国家科技支撑计划项目(2012BAD21B05)

摘　　要：目的以乙醇为溶剂,醋酸乙酯作为反溶剂制备甘草酸纳米粒(GAN),考察GAN作为皮肤给药载体的渗透情况。方法分别利用扫描电镜、激光粒度仪、红外光谱、溶出度等分析方法对原粉及纳米粒的性质进行表征;应用透皮扩散仪,采用改良Franz扩散池法,以离体大鼠皮肤进行体外经皮渗透实验,并以HPLC法测定接收液和皮肤组织中的药物浓度。结果获得的GAN为球形,平均粒径为220 nm;纳米化后甘草酸的释药速率得到极大提高;GAN同原粉相比,透皮性能大大增强,12 h的单位累积透过量分别是78.51、9.792μg/cm2。结论制备后的甘草酸粒径变小、分布均匀,化学结构未发生变化,而体外释药率和体外透皮性能均有提高,在医药产品开发上具有潜在的应用价值。Objective To prepare glycyrrhizic acid nanoparticles （GAN） using ethanol as solvent and ethyl acetate as the antisolvent, and to investigate the osmosis of GAN as carrier of dermal administration. Methods Using scanning electron microscope （SEM）, laser particle size analyzer, Fourier transform-infrared spectroscopy （FT-IR）, and release rate analysis, the untreated glycyrrhizic acid （GA） and GA powder were characterized; In vitro cutaneous permeation experiments were carried out on modified Franz diffusion cells, using excised mouse skin. The concentration of diammonium glycyrrhizinate in the receptor compartments and skin were determined by HPLC. Results The GAN was spherical, the average particle size was 220 nm, and the dissolution rate ofnanosized glycyrrhizinate was improved obviously. The transdermal rate ofnanosized glycyrrhizinate was better than the original glycyrrhizin, and the 12 h unit accumulation transmissibility of GAN and GA was 78.51 and 9.792 μg/cm2, respectively. Conclusion After preparing, the panicle size becomes smaller, the chemical structure does not change significantly, and both of dissolution rate and in vitro transdermal performance have been improved. The GAN has the potential application values in the development of pharmaceutical industry.

关 键 词：甘草酸 纳米粒 反溶剂 皮肤渗透 释放率 

分 类 号：R283.6[医药卫生—中药学]