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作 者:赖筱娟[1] 刘汉清[1] 李俊松[2] 狄留庆[1] 蔡宝昌[2]
机构地区:[1]南京中医药大学药学院,江苏南京210046 [2]江苏省中药炮制重点实验室,江苏南京210046
出 处:《药学学报》2010年第12期1576-1581,共6页Acta Pharmaceutica Sinica
基 金:江苏省"青蓝工程"科技创新团队支持计划
摘 要:为了考察药物浓度、肠段及配伍冰片对丹酚酸肠吸收的影响,本文应用大鼠在体单向肠灌流法,以酚红为标示物,研究丹酚酸提取物中迷迭香酸、丹酚酸B和丹酚酸A在不同浓度下大鼠十二指肠、空肠及回肠的吸收情况及配伍不同浓度冰片后的吸收情况。实验结果发现,丹酚酸在弱酸条件下较为稳定,肠道酶对丹酚酸稳定性有影响;在不同浓度下,迷迭香酸、丹酚酸B的Ka和Peff值具有显著性差异,存在高浓度饱和现象,由此可推断迷迭香酸和丹酚酸B可能存在主动转运或协助扩散;丹酚酸A的Ka和Peff值并无显著性差异,无自身浓度抑制作用,符合Ficks扩散原理,由此可推断丹酚酸A可能以被动扩散方式吸收;丹酚酸在回肠Ka和Peff值均显著大于其他肠段,由此可推断回肠是丹酚酸的最佳吸收部位;随着冰片浓度的增加,促吸收作用有所增加,但当冰片到达一定的量时,促吸收作用减弱,中浓度冰片的促吸收效果最好,由此推断冰片可以促进丹酚酸的肠吸收,且冰片浓度对促吸收强度有一定影响。This study aimed to investigate the effects of concentration,intestinal section and borneol on the intestinal absorption of salvianolic acids.The experiment not only studied the intestinal absorption properties of three concentrations of rosmarinic acid,salvianolic acid B and salvianolic acid A at duodenum,jejunum and ileum,but also of salvianolic acids compatible with borneol at different concentrations using single-pass intestinal perfusion model in rat with phenol red as the marker.The results showed that salvianolic acids was stable under weak-acid condition and affected by metabolism enzyme;The Peff and Ka significantly different among three concentrations of rosmarinic acid and salvianolic acid B,whose intestinal absorption were saturated in high concentration,suggesting that the transport mechanisms of rosmarinic acid and salvianolic acid B were similar to active transport or facilitated diffusion;However,there was inconspicuousness in the Peff and Ka of salvianolic acid A at different concentrations,whose absorption was not saturated in high concentration,indicating that the transport mechanisms of salvianolic acid A was passive diffusion;The Peff and Ka in the ileum obviously higher than those in the duodenum and jejunum,namely the ileum was the best absorption section;When concentration of borneol increased,the enhancing effect of intestinal absorption of salvianolic acids increased,but significantly decreased when borneol increased to some degree.The enhancing effect of midium borneol concentration was the optimum.This implied that borneol can enhance the intestinal absorption of salvianolic acids,and the capacity of enhancing effect was influenced by the concentration of borneol.
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