6种甘草酸盐乳膏中甘草酸的体外经皮渗透特性比较
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摘要
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(23.933μg/cm~2)>甘草酸二钾(22.952μg/cm~2)>甘草酸二钠(15.424μg/cm~2)>甘草酸单钾(10.703μg/ccm~2)>甘草酸二铵(9.557μg/ccm~2)>甘草酸单铵(1.621μg/ccm~2);经皮渗透速率快慢的顺序为甘草酸三钠[1.010 2μg/(ccm~2·h)]>甘草酸二钾[0.974 5μg/(cm~2·h)]>甘草酸二钠[0.641 2μg/(ccm~2·h)]>甘草酸二铵[0.399 9μg/(ccm~2·h)]>甘草酸单钾[0.362 8μg/(ccm~2·h)]>甘草酸单铵[0.072 6μg/(ccm~2·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。
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/ccm~2)>dipotassium glycyrrhizinate(22.952 μ g/ccm~2)>disodium glycyrrhizinate(15.424 μ g/ccm~2)>monopotassium glycyrrhizinate(10.703 μ g/ccm~2)>diammonium glycyrrhizinate(9.557 μg/ccm~2)>monoammonium glycyrrhizinate(1.621 μg/ccm~2).The percutaneous permeation rate in descending order was as follows as trisodium glycyrrhizinate [1.010 2 μ g/(ccm~2·h)] >dipotassium glycyrrhizinate [0.974 5 μ g/(ccm~2·h)]>disodium glycyrrhizinate [0.641 2 μg/(ccm~2·h)]>diammonium glycyrrhizinate[0.399 9 μg/(ccm~2·h)]>monopotassium glycyrrhizinate [0.362 8 μg/(ccm~2·h)]>monoammonium glycyrrhizinate [0.072 6 μg/(ccm~2·h)].CONCLUSIONS:The permeation rate of trisodium glycyrrhizinate is the highest among 6 kinds of glycyrrhetate creams in vitro.
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/ccm~2)>dipotassium glycyrrhizinate(22.952 μ g/ccm~2)>disodium glycyrrhizinate(15.424 μ g/ccm~2)>monopotassium glycyrrhizinate(10.703 μ g/ccm~2)>diammonium glycyrrhizinate(9.557 μg/ccm~2)>monoammonium glycyrrhizinate(1.621 μg/ccm~2).The percutaneous permeation rate in descending order was as follows as trisodium glycyrrhizinate [1.010 2 μ g/(ccm~2·h)] >dipotassium glycyrrhizinate [0.974 5 μ g/(ccm~2·h)]>disodium glycyrrhizinate [0.641 2 μg/(ccm~2·h)]>diammonium glycyrrhizinate[0.399 9 μg/(ccm~2·h)]>monopotassium glycyrrhizinate [0.362 8 μg/(ccm~2·h)]>monoammonium glycyrrhizinate [0.072 6 μg/(ccm~2·h)].CONCLUSIONS:The permeation rate of trisodium glycyrrhizinate is the highest among 6 kinds of glycyrrhetate creams in vitro.
引文
[1]陈坤顺,李祥.复方甘草苷注射液的应用风险与防范[J].中国药物经济学,2013,8(8):32-33.
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[13]王森,朱卫丰,欧水平,等.促透剂对良肤乳膏中丹皮酚、白鲜碱、梣酮和甘草次酸的体外透皮吸收及皮肤滞留量的影响[J].中国中药杂志,2009,34(14):1178-1182.
[14]许景峰,赵维娟,张梅,等.100种药物透皮吸收行为的实验研究及经验回归方程的推论[J].中国药学杂志,1998,33(2):86-91.
[15]任立,丁平田,陈黎赟.甘草酸单铵凝胶的制备及含量的测定[J].中国药剂学杂志,2005,3(3):165-168.
[16]李昱晖,项蕾红.离子通道对皮肤屏障修复的影响[J].国际皮肤性病学杂志,2010,36(2):89-91.
[17]靳士晓.基于中药难溶性有效成分甘草酸的磷脂/胆盐混合纳米胶束新型给药系统的研究[D].成都:成都中医药大学,2013.
[18]金春英.水+混合溶剂体系的液液相平衡及在分离中的应用[D].泉州:华侨大学,2005.
[2]于辉,李春香,宫凌涛,等.甘草的药理作用概述[J].现代生物医学进展,2006,6(4):77-79.
[3]韩瑶聃,王彬,王政雨,等.甘草酸药理作用的研究进展[J].中国新药杂志,2012,21(21):81-82.
[4]郝飞.甘草酸国外研究进展[J].中国药房,2001,12(8):500-501.
[5]任立.甘草酸单铵凝胶剂的研究[D].沈阳:沈阳药科大学,2005.
[6]MANTOVANI A,RICCIARDI C,STAZI AV,et al.Teratogenicity study of ammonium glycyrrhizinate in the Sprague-Dawley rat[J].Food Chem Toxicol,1988,26(5):435-440.
[7]陈璐,曾明辉.不同基质的氟他胺凝胶剂中氟他胺体外透皮特性比较[J].成都医学院学报,2015,10(1):35-43.
[8]李育卿,魏玉辉.甘草酸单铵乙醇脂质体凝胶对小鼠湿疹的疗效[J].中成药,2012,34(4):640-645.
[9]杨金艳,吴诗惠,罗明霞.益肤凝胶透皮吸收促进剂的筛选研究[J].中药药理与临床,2011,27(2):115-118.
[10]田璐,张蜀,林华庆,等.经皮给药制剂体外透皮扩散试验方法的研究进展[J].中国药房,2012,23(29):2761-2764.
[11]兰颐,王琼,安静,等.接受液中的乙醇浓度对药物体外透皮试验的影响[J].中国中药杂志,2013,38(16):2597-2600.
[12]杨柳,王爱武,苗杰,等.6种透皮吸收促进剂对盐酸普萘洛尔乳膏透皮吸收性能的影响[J].中国药房,2013,24(29):2721-2723.
[13]王森,朱卫丰,欧水平,等.促透剂对良肤乳膏中丹皮酚、白鲜碱、梣酮和甘草次酸的体外透皮吸收及皮肤滞留量的影响[J].中国中药杂志,2009,34(14):1178-1182.
[14]许景峰,赵维娟,张梅,等.100种药物透皮吸收行为的实验研究及经验回归方程的推论[J].中国药学杂志,1998,33(2):86-91.
[15]任立,丁平田,陈黎赟.甘草酸单铵凝胶的制备及含量的测定[J].中国药剂学杂志,2005,3(3):165-168.
[16]李昱晖,项蕾红.离子通道对皮肤屏障修复的影响[J].国际皮肤性病学杂志,2010,36(2):89-91.
[17]靳士晓.基于中药难溶性有效成分甘草酸的磷脂/胆盐混合纳米胶束新型给药系统的研究[D].成都:成都中医药大学,2013.
[18]金春英.水+混合溶剂体系的液液相平衡及在分离中的应用[D].泉州:华侨大学,2005.