各种吸收促进剂对黄芩苷鼻腔吸收的影响Enhancing effects of absorption enhancers on in situ nasal absorption of baicalin
黄惠锋,张淼,唐星
HUANG Hui-feng,ZHANG Miao,TANG Xing(School of pharmacy
摘要(Abstract)：
目的研究黄芩提取物中黄芩苷的鼻腔吸收规律和9种吸收促进剂对黄芩苷鼻腔吸收的促进作用,寻找有效的鼻腔吸收促进剂。方法采用大鼠在体鼻腔循环法考察黄芩苷鼻腔吸收,以鼻腔吸收的一级动力学常数来衡量各种吸收促进剂促吸收作用的强弱。结果黄芩苷鼻腔吸收需加入吸收促进剂,各种不同质量分数吸收促进剂的促进作用为:1%去氧胆酸钠0.5%壳聚糖≈0.5%冰片≈5%甲基化-β-环糊精>5%HP-β-CD>5%β-CD>1%Tween-80≈0.1%EDTA-Na2≈1%磷脂,其中加入最后三者的促吸收效果与不加吸收促进剂时无显著性差异。结论质量分数为1%去氧胆酸钠促吸收效果最好,但鼻黏膜毒性较大,0.5%壳聚糖、0.5%冰片、5%甲基化-β-环糊精和5%HP-β-CD可安全有效地促进黄芩苷的鼻腔吸收。
Objective To investigate the nasal absorption of baicalin and the enhancing activities of several absorption enhancers.Methods Nasal circulatory perfusion test in situ was employed to investigate the effects of absorption enhancers for nasal mucosa absorption of baicalin in rats.And the enchancing activities were evaluated by first-order nasal absorption rate constant k.Results Absorption enhancers were necessary to facilitate baicalin absorption by nasal mucosa.Among the absorption enhancers,the order of increasing absorption of baicalin caused by the enhancers was:1% sodium deoxycholate 0.5% chitosan≈0.5% borneol≈5% methyl-β-cyclodextrin>5% HP-βCD>5% β-CD>1% Tween-80≈0.1% EDTA-Na2≈1% lecithin.Conclusions 0.5% chitosan,0.5% borneol,5% methyl-β-cyclodextrin and 5% HP-β-CD are the promising candidates with good enhancing activities for nasal baicalin delivery.
关键词(KeyWords)：
黄芩苷;鼻腔吸收;吸收促进剂;在体鼻腔灌流法
baicalin;nasal absorption;absorption enhancers;in situ nasal recirculation method
基金项目(Foundation):
作者(Author):
黄惠锋,张淼,唐星
HUANG Hui-feng,ZHANG Miao,TANG Xing(School of pharmacy
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