摘要
目的:研究补肾温肺微乳中黄芪甲苷的大鼠不同肠段的吸收特性,并考察P-糖蛋白(P-gp)对其肠吸收的影响。方法:采用大鼠在体单向肠灌流实验,采用HPLC法测定黄芪甲苷的含量,分别研究肠段不同吸收部位、黄芪甲苷浓度、P-糖蛋白抑制剂盐酸维拉帕米对黄芪甲苷单体及其在补肾温肺微乳中吸收的影响。结果:黄芪甲苷单体在各肠段的吸收速率常数(Ka)和表观吸收系数(Papp)有显著性差异(P〈0.05);流速在0.10~0.40ml·min。内和质量浓度在0.1~1.0mg·ml-1范围内,十二指肠吸收速率常数和表观吸收系数无显著性差异;补肾温肺微乳中黄芪甲苷的肠灌流试验结果与黄芪甲苷单体相比略小,但无显著性差异;P-糖蛋白抑制剂对黄芪甲苷的肠吸收影响很小。结论:黄芪甲苷和补肾温肺微乳中黄芪甲苷在大鼠不同肠段的吸收具有相似的吸收特性;其在大鼠肠内的吸收不受P-糖蛋白影响。因此,推测黄芪甲苷不是P—gP的底物。
OBJECTIVE To research absorption characteristics of astragaloside IV of Bushenwenfei microemulsion in different intestinal sections and to study impact of P-glycoprotein (P-gp) on astragaloside IV absorption. METHODS One-way in vivo intestinal perfusion was used to reveal absorption characteristics of astragaloside IV. High performance liquid chromatography was used to determine contents of astragaloside IV and astragaloside IV in Bushenwenfei microemulsion in intestinal perfusate. Apparent absorption coefficient (Papp) and the absorption rate constant (Ka) were respectively calculated in each intestinal section. RESULTS KAand Papp values of the duodenum, jejunum, ileum and colon had significant differences (P〈0. 05). Flow rates of perfusion solutions from 0. 10 - 0. 40 ml. rain-1 and concentration from 0. 1 - 1.0 mg-ml-1 had no distinctive effects on KA and Papp of duodenum. Although differences were observed, astragaloside IV and astragaloside IV in Bushenwen-fei microemulsion showed no statistically significance. Each value was not changed significantly after adding P-gp inhibitor. CONCLUSION Absorption characteristics of astragaloside IV and astragaloside IV in Bushenwenfei microemulsion in different intestinal sections are almost the same. Absorption action of astragaloside IV is not affected by P-gp inhibitor, so astragaloside IV might not be the substrate of P-gp.
出处
《中国医院药学杂志》
CAS
CSCD
北大核心
2015年第19期1732-1736,共5页
Chinese Journal of Hospital Pharmacy
基金
湖南省教育厅科学研究项目(12C1187)
2012年株洲市科学技术局科研项目(33)
关键词
黄芪甲苷
补肾温肺微乳
吸收动力学
在体肠灌流模型
astragaloside IV
Bushenwenfei microemulsion
absorption kinetic
in situ perfused rat intestinal mode