根皮苷在体大鼠肠吸收试验.docVIP

根皮苷大鼠在体肠吸收特性研究 翟秉涛，郭东艳*，史亚军，范妤，杨伟平，李佳 （陕西中医药大学，陕西咸阳，712046） [摘要] 采用大鼠在体单向肠灌流模型，运用HPLC测定灌流液中根皮苷的含量，研究根皮苷在小肠段和结肠的吸收情况，并考察药物浓度和P-糖蛋白（P-gp）抑制剂对根皮苷吸收的影响，得出根皮苷在体大鼠肠吸收的动力学特征。结果表明根皮苷在大鼠全肠段均有吸收，在空肠段和结肠段吸收较完全，在十二指肠段和回肠段难以吸收；其在不同肠段的吸收速率常数(Ka)和表观吸收系数（Papp）从大到小依次为 空肠 结肠 十二指肠 回肠；不同质量浓度的根皮苷（5.14、10.28、20.56 μg·mL-1Ka和Papp没有显著性差异（P 0.05），提示在实验浓度范围内，根皮苷在大鼠全肠段的吸收没有浓度依赖性，吸收机制可能属于被动扩散；含P-gp抑制剂组和不含P-gp抑制剂组比较，根皮苷的Ka和Papp有显著性差异（P 0.05），表明根皮苷可能是P-gp底物。 [关键词] 根皮苷；在体肠吸收；单向灌流模型；P-糖蛋白 In vivo intestinal absorption characteristics of phloridzin in rats ZHAI Bing-tao，GUO Dong-yan（ The Medicine College of Shaanxi University of Chinese Medicine, Xianyang 712046，China [Abstract] To study the in vivo intestinal absorption kinetics of phloridzin in rats. The absorption of phloridzin in the small intestines and colon of rats was investigated using an in vivo single-pass perfusion method and the drug concentration was measured by HPLC．The effects on intestinal absorption of different drug concentration and P-glycoprotein ( P-gp) inhibitor were conducted. The results showed that the phloridzin could be absorbed in whole intestine, but more fully in the jejunum and colon segment,poorly absorbed in the duodenum and ileum . The absorption rate constant (Ka) and the apparent absorption coefficient（Papp）of phloridzin decreased following the sequence of jejunum colon duodenum ileum. Absorption parameters of phloridzin had no significant difference at different concentration (5.14、10.28、20.56 μg·mL-1) . The saturate phenomena was not observed under the test range of drug concentration, and the absorption mechanism may be the passive diffusion transport.There had a significant difference in Ka and Papp values between P-gp inhibitor and no P-gp inhibitor groups. Phloridzin may be the substrate of P-gp. [Key words] phloridzin；in vivo intestinal absorption；a single-pass perfusion method；P-gp phloridzin 或phlorizin），化学名称为1-( 2-( beta-D-吡喃葡萄糖氧基) -4，6-二Caco-2细胞单层模型中的转运与吸收，本试验进一步采用大鼠在体单向灌流模型，考察根皮苷在大