6种甘草酸盐乳膏中甘草酸的体外经皮渗透特性比较

摘要

OBJECTIVE:To compare in vitro percutaneous permeation characteristics of glycyrrhizic acid in 6 kinds of glycyrrhetate creams,and to provide reference for further development and utilization. METHODS:Modified Franz diffusion cell and isolated rat skin were adopted for in vitro percutaneous permeation test. 24 h accumulative permeation of glycyrrhizic acid in 6 kinds of glycyrrhetate creams(monoammonium glycyrrhizinate,diammonium glycyrrhizinate,monopotassium glycyrrhizinate, dipotassium glycyrrhizate,trisodium glycyrrhizinate,disodium glycyrrhetate)were determined by HPLC. The permeation characteristics of 6 kinds of glycyrrhetate creams were evaluated by calculating percutaneous absorption rate. RESULTS:24 h accumulative permeation of 6 kinds of glycyrrhetate in rat skin in descending order was as follows:trisodium glycyrrhizinate (23.933 μ g/cm2)>dipotassium glycyrrhizinate(22.952 μ g/cm2)>disodium glycyrrhizinate(15.424 μ g/cm2)>monopotassium glycyrrhizinate(10.703 μg/cm2)>diammonium glycyrrhizinate(9.557 μg/cm2)>monoammonium glycyrrhizinate(1.621 μg/cm2). The percutaneous permeation rate in descending order was as follows as trisodium glycyrrhizinate [1.010 2 μ g/(cm2·h)]>dipotassium glycyrrhizinate [0.974 5 μg/(cm2·h)]>disodium glycyrrhizinate [0.641 2 μg/(cm2·h)]>diammonium glycyrrhizinate [0.399 9 μg/(cm2·h)]>monopotassium glycyrrhizinate[0.362 8 μg/(cm2·h)]>monoammonium glycyrrhizinate[0.072 6 μg/(cm2·h)]. CONCLUSIONS:The permeation rate of trisodium glycyrrhizinate is the highest among 6 kinds of glycyrrhetate creams in vitro.%目的:比较6种甘草酸盐乳膏剂中甘草酸的体外经皮渗透特性,为其进一步开发利用提供参考.方法:以改良的Franz扩散池和离体大鼠皮进行体外经皮渗透试验,采用高效液相色谱(HPLC)法测定6种甘草酸盐(甘草酸单铵、甘草酸二铵、甘草酸单钾、甘草酸二钾、甘草酸三钠、甘草酸二钠)乳膏剂中甘草酸24 h累积渗透量,并计算其透皮吸收速率以评价6种甘草酸盐乳膏剂的透皮特性.结果:6种甘草酸盐在大鼠皮肤的24 h累积渗透量大小顺序为甘草酸三钠(23.933 μg/cm2)>甘草酸二钾(22.952 μg/cm2)>甘草酸二钠(15.424 μg/cm2)>甘草酸单钾(10.703 μg/cm2)>甘草酸二铵(9.557 μg/cm2)>甘草酸单铵(1.621 μg/cm2);经皮渗透速率快慢的顺序为甘草酸三钠[1.0102 μg/(cm2·h)]>甘草酸二钾[0.9745 μg/(cm2·h)]>甘草酸二钠[0.6412 μg/(cm2·h)]>甘草酸二铵[0.3999 μg/(cm2·h)]>甘草酸单钾[0.3628 μg/(cm2·h)]>甘草酸单铵[0.0726 μg/(cm2·h)].结论:6种不同甘草酸盐乳膏剂中,甘草酸三钠体外经皮渗透速率最高.