兰颐;王景雁;陶野;茹庆国;王逸飞;于竞新;刘艳;吴清;
LAN Yi;WANG Jing-yan;TAO Ye;RU Qing-guo;WANG Yi-fei;YU Jing-xin;LIU Yan;WU Qing;School of Chinese Materia Medica,Beijing University of Chinese Medicine;Ovation Health Science and Technology Co.,Ltd.,ENN Group;Qingdao Eye Hospital,Shandong Eye Institute,Shandong Academy of Medical Sciences;

• 1:北京中医药大学中药学院
• 2:新奥集团新绎健康科技有限公司
• 3:山东省医学科学院山东省眼科研究所青岛眼科医院

摘要(Abstract)：

该文拟探讨并比较薄荷油与薄荷醇对中药复杂成分的经皮促透作用特征规律。选择系列不同logP(油水分配系数)中药有效成分作为模型药物,即蛇床子素(logP=3.85)、川芎嗪(logP=2.34)、阿魏酸(logP=1.26)、葛根素(logP=-0.35)、京尼平苷(logP=-1.01),简化并表征中药复杂成分体系,采用体外透皮试验,对比分析薄荷油与薄荷醇的经皮促透作用特征。同时,采用傅利叶变换红外光谱(FTIR)技术进一步比较薄荷油与薄荷醇对皮肤角质层内在分子结构的影响。研究结果显示,适宜浓度的薄荷油与薄荷醇均可促进不同logP药物成分的经皮吸收,薄荷醇作用下药物经皮促透倍数对数值与药物logP向于负线性关系,薄荷油作用趋向于呈抛物线关系,但都表现出对logP较低药物(即亲水性药物)具更佳的经皮促透效果,其作用趋势相似。红外光谱研究显示,薄荷油与薄荷醇主要通过影响角质层脂质而影响皮肤屏障功能,且作用强度相近,与体外透皮试验结果一致。可知,薄荷油与薄荷醇的体外经皮促透作用特征相似,且对角质层内在分子结构影响相同,因此,作为经皮促透剂应用条件下,可以考虑选择成分单一的薄荷醇代替组成复杂的薄荷油。
The aim of this paper was to investigate and compare the penetration-enhancing characteristics of menthol and essential oil from Mentha haplocalyx( M. haplocalyx oil) on the transdermal absorption of the complex traditional Chinese medicine( TCM) components. A series of TCM components were selected as model drugs based on their lipophilicity( logP value),namely osthole( OT,logP = 3. 85),tetramethylpyrazine( TMP,logP = 2. 34),ferulic acid( FA,logP = 1. 26),puerarin( PR,logP =-0. 35) and geniposide( GP,logP =-1. 01),in order to simply and characterize the TCM complex components system. Transdermal experiment in vitro was employed to investigate and compare the penetration-enhancing characteristics of menthol and M. haplocalyx oil on the transdermal absorption of these model drugs. Meanwhile,Fourier transform infrared spectroscopy( FTIR) was used to further compare the effect of menthol and M. haplocalyx oil on the molecular structure of stratum corneum( SC). The results showed that both of menthol and M. haplocalyx oil at proper concentration could promote the transdermal absorption of the selected model drugs. After application of menthol,the drug logP values gradually tended to have negative linear relationship with the logarithm of penetration enhancement ratio( ER); while after application of M. haplocalyx oil,the logP values tended to have parabolic relationship with the logarithm of ER.However,both menthol and M. haplocalyx oil exhibited higher efficiency for the drugs with relative low lg P value( ie hydrophilic drugs),with similar penetration-enhancing characteristics between these two. Infrared spectroscopy results showed that menthol and M. haplocalyx oil could affect the skin barrier functions mainly via stratum corneum lipids,with similar effect intensity,and this was consistent with the results of transdermal experiment in vitro. Thus,Menthol had similar penetration-enhancing characteristics with M. haplocalyx oil,and had same effect on the SC molecular structure. Therefore,as transdermal penetration enhancer,the menthol with single composition could be considered to replace M. haplocalyx oil with complex compositions.

关键词(KeyWords)： 薄荷油;薄荷醇;经皮促透剂;经皮吸收;傅利叶变换红外光谱
essential oil from Mentha haplocalyx;menthol;transdermal penetration enhancer;transdermal absorption;FTIR

Abstract:

Keywords:

基金项目(Foundation): 国家自然科学基金项目(81473365);; 北京中医药大学创新团队发展计划项目(2011-CXTD-13)

作者(Authors): 兰颐;王景雁;陶野;茹庆国;王逸飞;于竞新;刘艳;吴清;
LAN Yi;WANG Jing-yan;TAO Ye;RU Qing-guo;WANG Yi-fei;YU Jing-xin;LIU Yan;WU Qing;School of Chinese Materia Medica,Beijing University of Chinese Medicine;Ovation Health Science and Technology Co.,Ltd.,ENN Group;Qingdao Eye Hospital,Shandong Eye Institute,Shandong Academy of Medical Sciences;

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