Chen Xin-Min, Li Jun-Song, Li Wen, Han Lei, Liu Xun-Hong, Di Liu-Qing, Cai Bao-Chang
School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing 210046, China.
Yao Xue Xue Bao. 2010 May;45(5):652-8.
The aim of the study is to investigate rat intestinal absorption behavior of three main active components, schisandrol A, schisandrin A and schisandrin B in Schisandra chinensis Baill extracts in intestine of rats. With phenol red as the indicator, in situ single pass intestinal perfusion (SPIP) model was used and the concentrations of three main active components in perfusion solution of different intestinal segments (duodenum, jejunum, ileum, and colon) were determined by HPLC in combination with diode array detection. The results showed that the absorption rate constant (Ka) and effective permeability values (Peff) of three main active components in Schisandra chinensis Baill extracts had significant difference (P < 0.05) at different concentrations of perfusion solution, the Ka and Peff first increased and then decreased with the increase of drug concentration, the middle concentration was higher than those of the other two concentrations. The saturate absorption phenomena were observed, and it suggested that the transport mechanisms of three main active components in vivo were similar to active transport or facilitated diffusion. Three active components can be well absorbed in all of the intestinal segments, while duodenum is the best absorption region. The Ka and Peff of three active components in jejunum and ileum had no significant difference (P > 0.05). The absorption of the three active components displayed significant difference (P < 0.05) at different intestinal segments of rats. Schisandrin A had the best absorption in duodenum. The Ka and Peff among three active components were sequenced as follows: schisandrin A > schisandrin B > schisandrol A in other intestinal segments, and there is significant difference (P < 0.05) between them.
本研究旨在考察大鼠肠道对五味子提取物中三种主要活性成分五味子醇甲、五味子甲素和五味子乙素的吸收行为。以酚红为指示剂,采用原位单向肠灌流(SPIP)模型,结合二极管阵列检测的高效液相色谱法测定不同肠段(十二指肠、空肠、回肠和结肠)灌流液中三种主要活性成分的浓度。结果表明,五味子提取物中三种主要活性成分的吸收速率常数(Ka)和有效渗透率(Peff)在不同灌流液浓度下有显著差异(P<0.05),Ka和Peff随药物浓度的增加先升高后降低,中间浓度高于其他两个浓度。观察到饱和吸收现象,提示三种主要活性成分在体内的转运机制类似于主动转运或易化扩散。三种活性成分在所有肠段均可良好吸收,其中十二指肠是最佳吸收部位。空肠和回肠中三种活性成分的Ka和Peff无显著差异(P>0.05)。三种活性成分在大鼠不同肠段的吸收存在显著差异(P<0.05)。五味子甲素在十二指肠中的吸收最佳。三种活性成分之间的Ka和Peff排序如下:在其他肠段中五味子甲素>五味子乙素>五味子醇甲,且它们之间存在显著差异(P<0.05)。