白头翁皂苷在大鼠体内的肠吸收研究(1)
[摘要]建立HPLC-ELSD 法对白头翁皂苷在大鼠体内的小肠吸收情况进行考察。结果显示5 种白头翁皂苷中B3和BD的吸收系数(Ka)，B3和B7的渗透系数 (Peff) 在不同肠段具有显著性差异(P<0.05)，5种白头翁皂苷的渗透系数(Peff)在不同肠段的吸收为十二指肠>空肠>结肠>回肠;0.05～2.5 g·L-1质量浓度内，5种白头翁皂苷随着浓度提高出现过饱和现象，该类皂苷在十二指肠的渗透系数(Peff)与浓度间的线性关系不明显 (0.600 7≤R2≤0.772 7);加入地高辛后，白头翁皂苷的渗透系数明显降低，而加入维拉帕米后，渗透系数明显提高，其中B3，BD，B7和B11有显著性差异 (P<0.05)。以上结果表明B3，BD，B7受吸收部位影响较大，十二指肠是该类皂苷的主要吸收部位;白头翁皂苷不完全依赖浓度梯度转运，细胞膜上的载体蛋白参与了药物的转运过程，其小肠吸收机制并不完全为被动转运;白头翁皂苷可能是P-gp底物。
[关键词]白头翁皂苷;肠吸收;吸收速率常数;渗透系数
, 百拇医药
[收稿日期]2014-07-18
[基金项目]国家自然科学基金项目(81460594);江西省自然科学基金项目(20122BAB215041);江西省教育厅科技计划项目(GJJ12529，GJJ13583);江西中医药大学博士启动基金项目(2010BS2037，2014BS019)
[通信作者]*苏丹，副教授，硕士生导师，主要从事药用植物有效成分和新药开发研究，Tel：13177859011，E-mail：Sud94@aliyun.com
[作者简介]刘亚丽，讲师，博士，主要从事中药药物代谢和新药开发研究，Tel：18007092727，E-mail：582685133@qq.comIntestinal absorption of pulchinenosides from Pulsatilla chinensis in rats
, 百拇医药
LIU Ya-li1， SONG Yong-gui1， GUAN Zhi-yu1， ZHANG Ling1， YANG Shi-lin1， WANG Meng1， CHEN Zhen-hua2， SU Dan1*
(1. Jiangxi University of Chinese Traditional Medicine， Nanchang 330025， China;
2. Pharmacy Department， Jiangxi Science and Technology Normal University， Nanchang 330013， China)
[Abstract]HPLC-ELSD was applied to explore the absorption mechanism of pulchinenosides(B3， BD， B7， B10， B11) in rats. The experimental results showed that the absorption rate constant， Ka value (B3， BD) and Permeability coefficient， Peff value (B3， B7) displayed significant difference(P<0.05) in various intestinal segments，The Ka value and Peff value of PRS was different from each other with the highest absorption in duodenum(duodenum>jejunum>colon>ileum); The PRS displayed excessive satuation as the concentration increased over 0.05-2.5 g·L-1. There were no obvious linear correlations between Peff values and concentrations in duodenum (0.600 7≤R2≤0.772 7);Ka and Peff value declined when the PRS was perfused with P-glycoprotein promoter digoxin， on the other hand， inclined when perfused with P-glycoprotein inhibitor verapamil with significant difference among PRS B3， BD， B7， B11 (P<0.05). All the above results demonstrated that B3， BD， B7 were greatly influenced by absorption sites， duodenum was the main absorption site; PRS didn′t entirely transported in a concentration dependent manner， and the transporter-protein involved the transportation， so the intestinal absorption of the five pulchinenosides was not entirely passive diffusion; and PRS might be the substrates of P-glycoprotein., 百拇医药(刘亚丽 宋永贵 关志宇 张凌 杨世林 王萌 陈振华 苏丹)
[关键词]白头翁皂苷;肠吸收;吸收速率常数;渗透系数
, 百拇医药
[收稿日期]2014-07-18
[基金项目]国家自然科学基金项目(81460594);江西省自然科学基金项目(20122BAB215041);江西省教育厅科技计划项目(GJJ12529，GJJ13583);江西中医药大学博士启动基金项目(2010BS2037，2014BS019)
[通信作者]*苏丹，副教授，硕士生导师，主要从事药用植物有效成分和新药开发研究，Tel：13177859011，E-mail：Sud94@aliyun.com
[作者简介]刘亚丽，讲师，博士，主要从事中药药物代谢和新药开发研究，Tel：18007092727，E-mail：582685133@qq.comIntestinal absorption of pulchinenosides from Pulsatilla chinensis in rats
, 百拇医药
LIU Ya-li1， SONG Yong-gui1， GUAN Zhi-yu1， ZHANG Ling1， YANG Shi-lin1， WANG Meng1， CHEN Zhen-hua2， SU Dan1*
(1. Jiangxi University of Chinese Traditional Medicine， Nanchang 330025， China;
2. Pharmacy Department， Jiangxi Science and Technology Normal University， Nanchang 330013， China)
[Abstract]HPLC-ELSD was applied to explore the absorption mechanism of pulchinenosides(B3， BD， B7， B10， B11) in rats. The experimental results showed that the absorption rate constant， Ka value (B3， BD) and Permeability coefficient， Peff value (B3， B7) displayed significant difference(P<0.05) in various intestinal segments，The Ka value and Peff value of PRS was different from each other with the highest absorption in duodenum(duodenum>jejunum>colon>ileum); The PRS displayed excessive satuation as the concentration increased over 0.05-2.5 g·L-1. There were no obvious linear correlations between Peff values and concentrations in duodenum (0.600 7≤R2≤0.772 7);Ka and Peff value declined when the PRS was perfused with P-glycoprotein promoter digoxin， on the other hand， inclined when perfused with P-glycoprotein inhibitor verapamil with significant difference among PRS B3， BD， B7， B11 (P<0.05). All the above results demonstrated that B3， BD， B7 were greatly influenced by absorption sites， duodenum was the main absorption site; PRS didn′t entirely transported in a concentration dependent manner， and the transporter-protein involved the transportation， so the intestinal absorption of the five pulchinenosides was not entirely passive diffusion; and PRS might be the substrates of P-glycoprotein., 百拇医药(刘亚丽 宋永贵 关志宇 张凌 杨世林 王萌 陈振华 苏丹)