基于微透析技术的花椒挥发油在体经皮促透作用研究(1)
[摘要]該文拟采用经皮微透析技术测定花椒挥发油对不同脂溶性中药成分皮肤药动学行为的影响，评价其在体经皮促透特征。选择川芎嗪和葛根素作为亲脂性和亲水性模型药物，采用浓差法考察微透析探针体外回收率与传递率，采用反向渗析法测定药物探针在体回收率；以常用化学促透剂氮酮为阳性对照，测定不同浓度花椒挥发油对川芎嗪和葛根素的皮肤药动学行力影响。结果显示，2种模型药物探针回收率与传递率相等，药物在渗析膜间无相互作用，川芎嗪和葛根素的在体相对回收率分别为5917%，1985%。在体经皮试验表明花椒挥发油对川芎嗪具良好促透效果，且呈浓度依赖性关系，5%花椒挥发油的在体促透倍数(ER)为9864，比氮酮最佳浓度的促透效果更好(3%氮酮，ER=8911)；同时，花椒挥发油也可显著增加葛根素的在体经皮吸收，也表现出浓度依赖性关系。因此，该研究进一步证实花椒挥发油作为经皮促透剂的良好促透性能，为其在中药外用制剂中的应用提供了数据支持。
[关键词]花椒挥发油； 微透析； 促透剂； 在体经皮吸收； 反向渗析法
, 百拇医药
[Abstract]The aim of this paper is to investigate the topical pharmacodynamics behavior of different lipophilic model drugs after treatment with essential oil from Zanthoxyli Pericarpium by using the cutaneous microdialysis technique， and then evaluate its in vivo transdermal penetration enhancing properties Two traditional Chinese medicine active components， namely tetramethylpyrazine and puerarin， were chosen as lipophilic and hydrophilic model drugs， respectively Firstly， the concentration difference method was employed to measure the in vitro recovery rate and loss of the microdialysis probe， and the in vivo recoveries of two model drugs were determined by using the retrodialysis method Secondly， the skin pharmacodynamics behaviors of two model drugs were studied after treatment with different concentrations of the essential oil， and the wellestablished and standard penetration enhancer Azone was selected as a positive control It was found that the recovery of microdialysis probe was equal to its loss for two model drugs， with no interaction between drugs in dialysis membranes The retrodialysis studies revealed that the in vivo recovery of tetramethylpyrazine and puerarin were 5917%， 1985%， respectively The skin pharmacodynamics studies showed that the essential oil could facilitate the transdermal absorption of tetramethylpyrazine in a concentrationdependent manner， and the enhancement ratio (ER) for 5% essential oil was 9864， which was higher than that of the optimum concentration of Azone (3% Azone， ER=8911) Meanwhile， the Zanthoxyli Pericarpium could effectively promote the transdermal permeation of the puerarin in a concentrationdependent manner Hence， this study further confirmed that the Zanthoxyli Pericarpium had excellent penetrationenhancing activity as a natural transdermal penetration enhancer， providing data support for its application in traditional Chinese medicine external preparations
[Key words]essential oil from Zanthoxyli Pericarpium； microdialysis； penetration enhancer； in vivo transdermal absorption； retrodialysis method, 百拇医药(兰颐 杨琳 史大勇 王英新 吴学萍 谢璇 吴清)
[关键词]花椒挥发油； 微透析； 促透剂； 在体经皮吸收； 反向渗析法
, 百拇医药
[Abstract]The aim of this paper is to investigate the topical pharmacodynamics behavior of different lipophilic model drugs after treatment with essential oil from Zanthoxyli Pericarpium by using the cutaneous microdialysis technique， and then evaluate its in vivo transdermal penetration enhancing properties Two traditional Chinese medicine active components， namely tetramethylpyrazine and puerarin， were chosen as lipophilic and hydrophilic model drugs， respectively Firstly， the concentration difference method was employed to measure the in vitro recovery rate and loss of the microdialysis probe， and the in vivo recoveries of two model drugs were determined by using the retrodialysis method Secondly， the skin pharmacodynamics behaviors of two model drugs were studied after treatment with different concentrations of the essential oil， and the wellestablished and standard penetration enhancer Azone was selected as a positive control It was found that the recovery of microdialysis probe was equal to its loss for two model drugs， with no interaction between drugs in dialysis membranes The retrodialysis studies revealed that the in vivo recovery of tetramethylpyrazine and puerarin were 5917%， 1985%， respectively The skin pharmacodynamics studies showed that the essential oil could facilitate the transdermal absorption of tetramethylpyrazine in a concentrationdependent manner， and the enhancement ratio (ER) for 5% essential oil was 9864， which was higher than that of the optimum concentration of Azone (3% Azone， ER=8911) Meanwhile， the Zanthoxyli Pericarpium could effectively promote the transdermal permeation of the puerarin in a concentrationdependent manner Hence， this study further confirmed that the Zanthoxyli Pericarpium had excellent penetrationenhancing activity as a natural transdermal penetration enhancer， providing data support for its application in traditional Chinese medicine external preparations
[Key words]essential oil from Zanthoxyli Pericarpium； microdialysis； penetration enhancer； in vivo transdermal absorption； retrodialysis method, 百拇医药(兰颐 杨琳 史大勇 王英新 吴学萍 谢璇 吴清)