北京中医药大学学报Issue(2)：155-161,7.DOI:10.3969/j.issn.1006-2157.2016.02.014
氮酮对不同亲脂性中药有效成分的经皮促透作用研究∗
Percutaneous penetration enhancement effects of azone on TCM active in-gredients with different lipophilicity
摘要
Abstract
Objective To investigate the effects of azone on transdermal absorption of TCM active ingre-dients with different lipophilicity, and further explore its percutaneous penetration enhancement effects on the complex TCM active ingredients. Methods Five model drugs, namely osthole, tetramethylpyrazine, ferulic acid, puerarin and geniposide, were selected based on their lipophilicity determined by logKo/w, and then tested using in vitro permeation studies in which Franz diffusion cellsand rat skin were em-ployed. Meanwhile, the association between the logKo/w values of model drugs and enhancement ratio ( ER) was established. Results Different concentrations of azone could significantly promote the trans-dermal absorption of all model drugs. The ER value gradually increased with the increase of the azone concentration withina certain concentration range. It, however, started to decrease when exceedinga cer-tain concentration level. The penetration enhancement ratio was roughly in parabolic curve relation with the drug lipophilicity after treatment with azone, and azone could achieve the optimal permeation effect for moderate hydrophilic drugs (an estimated logKo/w value of -0. 5). Conclusion azone could significant-ly promote the transdermal absorption of TCM components with different lipophilicity, and its penetration enhancement ratio was in parabolic curve relation with the drug lipophilicity.关键词
氮酮/不同亲脂性中药有效成分/促透剂/经皮吸收Key words
azone/TCM active ingredients with different lipophilicity/penetration enhancer/transdermal absorption分类
医药卫生引用本文复制引用
王景雁,兰颐,茹庆国,王逸飞,刘艳,于竞新,吴清..氮酮对不同亲脂性中药有效成分的经皮促透作用研究∗[J].北京中医药大学学报,2016,(2):155-161,7.基金项目
国家自然科学基金资助项目( No.81473365),北京市自然科学基金项目( No.7132127),北京中医药大学创新团队发展计划项目( No.2011-CXTD-13) （ No.81473365）
