大黄酸神阙穴给药经皮渗透性影响因素研究与初步机制探讨.docVIP

大黄酸神阙穴给药经皮渗透性影响因素研究与初步机制探讨 　　[摘要]采用VC扩散池，分别以新鲜的离体大鼠、家兔、小型猪的神阙穴及非穴位区皮肤为渗透屏障，以20%乙醇的生理盐水为接收液，进行渗透试验，HPLC测定大黄酸含量，以累积透过量、稳态透皮速率为指标；同时采用激光共聚焦显微镜可视化观察大黄酸经皮吸收差异，考察大黄酸经神阙穴和非穴位以及不同种属动物神阙穴皮肤的渗透特性。结果显示，在24 h内大黄酸经大鼠神阙穴皮肤的累积渗透量为（10263±960） μg?cm-2，稳态透皮速率为4307 μg?cm-2?h-1，均高于经非穴位区皮肤；大黄酸经不同种属动物神阙穴给药的累积渗透量和稳态透皮速率为大鼠家兔小型猪，两两比较，存在显著性差异；荧光吸收图显示皮肤中的药物含量为神阙穴非穴位，大鼠家兔小型猪。研究结果表明，大黄酸经皮渗透存在种属、穴位差异，经神阙穴位皮肤给药的透过量及速率显著高于非穴位皮肤，大黄酸神阙穴给药的初步机制可能是神阙穴为药物传递提供通道、载体，可视化验证了临床贴敷神阙穴治疗疾病具有特异性和优越性。 　　[关键词]大黄酸；神阙穴；种属；透皮特性 　　[Abstract]To study rhein′s permeative properties of acupoint and nonacupoint and different species′ transdermal administration in vitro Cumulative permeation amount and steadystate infiltration rate were taken as evaluative indexes to assess the permeability difference The ValiaChien diffusion cell method was used to conduct the permeability test， with fresh acupoint and nonacupoint skin of rat， rabbit and swine in vitro as permeation barriers， and blank 20% EtOH saline as absorption liquid HPLC was used to determine the rhein The absorption difference was observed by confocal laser scanning microscopy The 24hour cumulative permeation amount through acupoint skin in rats was （10263±960） μg?cm-2， the steadystate infiltration rate was 4307 μg?cm-2?h-1， both were higher than that through nonacupoint skin The thickness of acupoint skin in rat was thinner than that in rabbit and swine The cumulative permeation amount and steadystate infiltration rate of rhein in acupoint of rat were signally higher than those in rabbit and swine The absorption difference can be clearly observed through an accumulation of fluorescence In conclusion， species and acupoint all affect the permeability of rhein in vitro The permeation amount and rate of rhein on Shenque acupoint were better than that on nonacupoint skin， which could verify that treatment through Shenque acupoint is superior to that through nonacupoint The preliminary mechanism may be the drug delivery through Shenque acupoint as a channel and car