基于皮肤电阻动力学技术快速比较6种温里药挥发油的透皮促进效果
Comparative Study on the Transdermal Penetration Enhancement Effect of Essential Oils of Interior-Warming Drugs Based on Electrical Resistance of Skin
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摘要: 目的 建立一种简便实用的快速评价中药挥发油透皮吸收促进效果的方法,并比较温热药性对温里药挥发油的作用差异。方法 以香附四物活性组分群为透皮促进对象,测定了其油水分配系数。以6种温里药挥发油为研究对象,采用Franz扩散池方法测定了其对香附四物活性组分群的透皮吸收促进效果,采用细胞电阻仪和Transwell装置测定了其对皮肤屏障功能的影响,并比较了皮肤电阻动力学测定结果与体外透皮吸收促进结果的相关性。结果 香附四物活性组分群中阿魏酸、芍药内酯苷、芍药苷、四氢非洲防己碱在pH7.4条件下的油水分配系数分别为-0.93、-0.59、-0.38、1.97和2.15。6种温里药挥发油对香附四物活性组分的透皮吸收均有明显的促进作用,尤其是对极性较强的成分,并且热性温里药挥发油(肉桂油、干姜油、高良姜油)的效果优于温性温里药挥发油(荜澄茄油、花椒油、丁香油)。对于不同极性组分,采用皮肤电阻动力学评价的促渗效果与采用体外透皮吸收实验评价的效果基本平行(r=0.748 1~0.812 9)。结论 温热药性对温里药挥发油透皮吸收促进作用有显著影响。采用皮肤电阻动力学可以快速评价中药挥发油体外透皮吸收促进效果。Abstract: OBJECTIVE To evaluate and establish a method for rapid comparison of transdermal penetration enhancement effect of essential oils (EOs) from Chinese materia medica (CMM). METHODS The active components (ferulic acid,albiflorin,paeoniflorin,tetrahydrocolumbamine,tetrahydropalmatine) in Xiangfu Siwu Decotion (XFSWD)were used as model drugs for transdermal permeation study. The oil/water partition coefficient values of the above active components were measured. Six EOs of interior-warming drugs were used as penetration enhancer (PE). The Franz diffusion cell method was applied to investigate the effects of EOs on transdermal permeation of active components in XFSWD. The impact of EOs on skin integrity was evaluated by electrical resistance (ER) of the skin. Finally,the correlation between the results of skin resistance dynamics and in vitro transdermal permeation experiment was assessed. RESULTS The oil-water partition coefficients of ferulic acid,albiflorin,paeoniflorin,tetrahydrocolumbamine,tetrahydropalmatine were measured to be -0.93,-0.59,-0.38,1.97, 2.15. Six EOs of interior-warming drugs as PE could significantly enhance the permeation of active components in XFSWD,especially the polar components. The EOs with hot nature possess better penetration ability than that of warm nature. Besides,there was a good correlation between the results of skin resistance dynamics and in vitro transdermal permeation experiments for above drugs with different polarity(r=0.748 1-0.812 9). CONCLUSION The penetration enhancing effect of EOs of interior-warming drugs are affected by drug four nature property characteristics of CMM.The ER method can effectively identify the penetration enhancing effect of EOs.
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