香附四物汤全方与组方药材挥发油经皮外用“药辅合一”作用研究

  目的  比较香附四物汤全方挥发油与组方药材挥发油经皮外用“药辅合一”作用。  方法  以水蒸气蒸馏法提取得到香附四物汤全方挥发油和当归油、川芎油、木香油、香附油等4种组方药材挥发油。采用GC-MS分析挥发油成分, 通过皮肤电阻法比较全方挥发油和各组方药材挥发油的透皮促渗效果, 以人角质形成细胞HaCaT评价挥发油的皮肤细胞毒性, 并采用大鼠离体子宫收缩模型评价全方挥发油和组方药材挥发油的生物效应。  结果  香附四物汤全方挥发油以藁本内酯为其最主要成分, 含量为43.54%;与各组方药材挥发油相比, 全方挥发油含有16种新成分。全方挥发油及4种组方药材挥发油均具有显著的透皮促渗效果(P < 0.05), 其中全方挥发油的促渗作用较强, 是氮酮的2.5倍。5种挥发油对人角质形成细胞的毒性均显著低于氮酮(P < 0.05), IC₅₀值为氮酮的1.98~6.25倍。5种挥发油均不同程度地抑制缩宫素诱导的离体子宫收缩, 其中全方挥发油对平滑肌收缩幅度、收缩频率和肌张力的抑制作用均最强, 分别为66.69%, 47.56%和66.98%。  结论  香附四物汤全方挥发油作为透皮促渗剂应用于中药外用制剂具有低毒、高促渗和生物活性强的特点, 更易发挥“药辅合一”作用。 

Study on the Function of "Unification of Medicines and Excipients" of Essential Oils from Xiangfu Siwu Decoction and Its Single Herbs for Percutaneous External Application

OBJECTIVE To compare the function of"unification of medicines and excipients"of essential oils(EOs)from Xiangfu Siwu decoction(XFSWD)and its single herbs for percutaneous external application.METHODS All the EOs of XFSWD and its single herbs(Angelica sinensis,Ligusticum chuanxiong,Saussurea lappa,Cyperus rotundus)were extracted by wet distillation and analyzed by GC-MS.Transdermal penetration enhancement of EOs was evaluated by electrical resistance of skin.Then the in vitro toxicity was evaluated by human keratinocyte(HaCaT)cytotoxicity.Oxytocin induced female rats uterine contraction animal model was applied to evaluate the bioactivity of EOs.RESULTS Ligustilide(43.54%)was the main component of XFSWD oil.Compaired with single herbs,16 new constituents were determined from XFSWD oil.EOs had significant transdermal penetration enhancement(P<0.05),of which the XFSWD oil presented 2.5 times higher effect than that of Azone.EOs showed lower skin cytotoxicity(P<0.05),with IC₅₀ value was 1.98~6.25 times that of Azone.The experiments showed that the activities of the EOs on inhibition of rats uterine contraction were increased in varying degrees.The activities of XFSWD oil was prior to that of EOs from single herbs on the contraction amplitude,contraction frequency and muscle tension of smooth muscle,which were 66.69%,47.56%and 66.98%,respectively.CONCLUSION XFSWD oil has the characteristics of low skin toxicity,high penetration promoting effect and strong pharmacological activity,which makes it easier to bring the superiority of"unification of medicines and excipients"into full play.