Lai Xiao-juan, Liu Han-qing, Li Jun-song, Di Liu-qing, Cai Bao-chang
School of Pharmacy, Nanjing University of Traditional Chinese Medicine, Nanjing 210046, China.
Yao Xue Xue Bao. 2010 Dec;45(12):1576-81.
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 medium 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.
本研究旨在考察浓度、肠段及冰片对丹酚酸肠吸收的影响。实验采用大鼠单通道肠灌流模型,以酚红为标记物,不仅研究了三种浓度的迷迭香酸、丹酚酸B和丹酚酸A在十二指肠、空肠和回肠的肠吸收特性,还研究了不同浓度冰片配伍丹酚酸的肠吸收特性。结果表明,丹酚酸在弱酸条件下稳定,受代谢酶影响;三种浓度的迷迭香酸和丹酚酸B的有效渗透系数(Peff)和吸收速率常数(Ka)有显著差异,其在高浓度时肠吸收饱和,提示迷迭香酸和丹酚酸B的转运机制类似于主动转运或易化扩散;然而,不同浓度丹酚酸A的Peff和Ka无明显差异,其在高浓度时吸收不饱和,表明丹酚酸A的转运机制为被动扩散;回肠的Peff和Ka明显高于十二指肠和空肠,即回肠是最佳吸收肠段;随着冰片浓度的增加,丹酚酸肠吸收的增强作用增强,但当冰片浓度增加到一定程度时显著降低。中等冰片浓度的增强作用最佳。这表明冰片可增强丹酚酸的肠吸收,且增强作用的大小受冰片浓度的影响。