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当前位置: 首页 > 文章 > 手性药物经皮渗透对映体选择性机理的初步探讨 黑龙江畜牧兽医 2017 (7) 24-27+31
Position: Home > Articles > Preliminary study on the mechanism of enantioselectivity of the transdermal permeation of chiral drugs Heilongjiang Animal Science and Veterinary Medicine 2017 (7) 24-27+31

手性药物经皮渗透对映体选择性机理的初步探讨

作  者：
张亮;叶金翠
单  位：
浙江省医学科学院药物研究所;江苏农牧科技职业学院动物药学院
关键词：
手性药物;经皮渗透;对映体选择性;神经酰胺;手性促进剂;ATR-FTIR
摘  要：
为了研究神经酰胺和手性促进剂对于经皮渗透的影响,试验将经氯仿︰甲醇(2∶1,V/V)的混合溶剂提取角质层中的神经酰胺后的大鼠皮肤用于模型药物萘普生的经皮渗透研究,同时采用手性促进剂对皮肤角质层进行处理,探讨手性促进剂对角质层结构的影响。结果表明:采用去神经酰胺的大鼠皮肤,当加入萜烯类手性促进剂后,渗透速率反而下降,再观察不到促透效果。当对照供给液中加入1%的l-芳樟醇后,S-萘普生的经皮渗透速率由显著高于R-萘普生和RS-萘普生,变为显著地低于二者。说明萜烯类手性促进剂主要通过扰乱神经酰胺脂质起促透作用,神经酰胺在手性药物经皮渗透的对映体选择性上起着重要的作用。
译  名：
Preliminary study on the mechanism of enantioselectivity of the transdermal permeation of chiral drugs
作  者：
ZHANG Liang;YE Jincui;College of Animal Pharmaceutical Sciences,Jiangsu Agri-animal Husbandry Vocational College;Institute of Materia Medica,Zhejiang Academy of Medical Sciences;
关键词：
chrial drug;;transdermal permeation;;enantioselectivity;;ceramide;;chiral enhancer;;attenuated total reflection-Fourier transform infrared spectroscopy(ATR-FTIR)
摘  要：
To study the effects of ceramide and chiral enhancers on the transdermal permeation,ceramide was extracted from the stratum corneum of rat skin using a mixed solvent of chloroform/methanol(2∶1,V/V).The rat skin was further applied to the study on the transdermal permeation of model drug naproxen after the removal of ceramide.Meanwhile,the stratum corneum of rat skin was treated by chiral enhancers,and then the effects of chiral enhancers on the structure of the stratum corneum were investigated.The results showed that the permeation rate of the rat skin with the removal of ceramide was decreased after the addition of chiral terpene enhancers,meanwhile,no enhancing permeation effect was observed.The transdermal permeation rate of S-naproxen was significantly higher than that of both R-naproxen and RS-naproxen,while the transdermal permeation rate of S-naproxen was significantly lower than that of R-naproxen and RS-naproxen when the addition of1% l-linalool was added to the control supply liquid.The results indicate that chiral terpene enhancers play a role in enhancing permeation mainly through disrupting ceramide lipids,and ceramide play an important role in the enantioselectivity of transdermal permeation of chiral drugs.

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