补肾温肺微乳中淫羊藿苷的大鼠在体肠吸收特征研究  

In situ Rat Intestinal Absorption of Icariin in Bushenwenfei Microemulsion

作　　者：冯传平[1] 李福元[1] 丁海霞[2] 

机构地区：[1]湖南中医药高等专科学校,湖南株洲412012 [2]湖南中医药高等专科学校附属第一医院

出　　处：《中国药师》2015年第9期1456-1459,1522,共5页China Pharmacist

基　　金：湖南省教育厅科学研究项目(编号:12C1187);株洲市科学技术局科研项目(编号:33)

摘　　要：目的：研究补肾温肺微乳中淫羊藿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法测定淫羊藿苷的含量,分别研究肠段不同吸收部位、不同淫羊藿苷浓度、Pgp抑制药维拉帕米对淫羊藿苷单体及其在补肾温肺微乳中吸收的影响。结果：淫羊藿苷单体在各肠段的吸收速率常数（Ka）和表观吸收系数（Papp）差异显著（P〈0.01）;在0.10～0.40 ml·min-1流速内和0.1～1.0 mg·ml-1质量浓度内,十二指肠吸收速率常数和表观吸收系数无显著差异;补肾温肺微乳中淫羊藿苷的肠灌流试验结果与淫羊藿苷单体相比略小,但无显著差异;P-gp抑制药对淫羊藿苷的肠吸收有影响,加入0.1 mmol·L-1盐酸维拉帕米后,Ka和Papp分别为（2.13±0.66）×10-2h·cm-1和（0.23±0.051）×10-6cm·s-1,与不加P-gp抑制药组相比较差异显著（P〈0.01）。结论：淫羊藿苷属于难吸收化合物,淫羊藿苷和补肾温肺微乳中淫羊藿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受P-gp外排转运影响。因此,推测淫羊藿苷可能是P-gp的底物。Objective：To research the absorption characteristics of icariin in Bushenwenfei microemulsion at different intestinal sections in rats and study the impact of P-glycoprotein （P-gp） on the icariin absorption. Methods：One-way in vivo intestinal perfusion was used to reveal the absorption characteristics of icariin. HPLC was used to determine the content of icariin in the intestinal perfusate. The＇absorption rate constant（ Ka ） and the apparent absorption coefficient（ Papp ） in each intestinal section were calculated. The impact of P-gp inhibitor （ verapamil hydrochloride） on the Ka and Papp of icariin was studied. Results： By the testing of statistics, the Ka and the Papp values for duodenum, jejunum, ileum and colon had significant differences（ P 〈 0.01 ）. The flow rate of perfusion solution from 0. 1043.40 ml · min-1 and the concentration from 0.1-1.0 mg· ml-1 had no distinctive effect on the Ka and Papp of duodenum. Al- though some differences were shown, the differences between icariin and icariin in Bushenwenfei microemulsion were not statistically significant. Each value was changed significantly after the addition of the P-gp inhibitor（ verapamil hydrochloride） [ Ka was （ 2.13 ± 0. 66）×10-2h · cm- 1 and Papp was （0.23±0.051 ）×10-6 cm · s- 1, P 〈0.01 ]. Conclusion： Icariin is hardly absorbed in rats and the ab- sorption characteristics of icariin and icariin in Bushenwenfei microemulsion at different intestinal sections in rats are almost the same. The absorption action of icariin is affected by the P-gp inhibitor（ verapamil hydrochloride） ,thus icariin might be the substrate of P-gp.

关 键 词：淫羊藿苷 补肾温肺微乳 吸收动力学 在体肠灌流模型 

分 类 号：R945[医药卫生—微生物与生化药学]