山楂叶总黄酮的在体肠吸收研究  

In situ rat intestinal absorption of hawthorn leaves flavonoids

作　　者：许英爱[1] 范国荣[1] 高申[1] 洪战英[1] 

机构地区：[1]第二军医大学药学院,上海200433

出　　处：《中成药》2007年第12期1745-1748,共4页Chinese Traditional Patent Medicine

基　　金：上海市科委科研计划项目课题(编号03JC14005)

摘　　要：目的:研究山楂叶总黄酮中牡荆素鼠李糖苷的肠吸收机制。方法:运用大鼠在体肠单向灌流模型并采用高效液相色谱法测定灌流液中山楂叶总黄酮中的牡荆素鼠李糖苷浓度,计算其有效渗透系数。结果:牡荆素鼠李糖苷在大鼠十二指肠、空肠、回肠和结肠的有效渗透系数没有显著性差异(P>0.05);山楂叶总黄酮的浓度为0.05～0.5mg/mL时,牡荆素鼠李糖苷的有效渗透系数均大于0.2×10-4cm/s,并且均无显著性差异(P>0.05),而加入P-糖蛋白抑制剂维拉帕米和地高辛后,都能显著提高牡荆素鼠李糖苷的有效渗透系数。结论:山楂叶总黄酮中的牡荆素鼠李糖苷属于高渗透性药物,其在大鼠小肠的转运机制为被动扩散,无特殊的吸收窗,P-糖蛋白介导了牡荆素鼠李糖苷的小肠吸收。AIM： To study the tion mechanism of rhamnosylvitexin in hawthorn leaves flavonoids （HLF） The in situ rat single-pass intestinal perfusion model was used. The concentration of the index component of HLF, rhamnosylvitexin in the perfusate, was determined by HPLC, and the effective permeability coefficients （Peff） were calculated. RFSULTS ： There were no significant differences in the Peff values of rhamnosylvitexin in HLF in the four segments of the rat intestine, duodenum, jejunum, ileum and colon （P 〉 0. 05 ）. The Poff values for rhamnosylvitexin in the rat jejunal perfusion at the concentration ranging from 0.05 mg/ mL to 0.5 mg/mL were all over 0.2 × 10^ -4 cm/s, and there were no significant differences in the effective permeability coeffients of rhamnosylvitexin in HLF at different concentrations of HLF （P 〉 0.05 ）. But the Peff values were significantly increased in the presence of P-glycoportein （P-gp） inhibitor, verapamil or digoxin. CONCLUSION ： Rhamnosylvitexin can be classified into high penetrating drug. Passive diffusion dominates the absorptive transport behavior of rhamnosylvitexin in HLF. There is not a preferential absorption zone in the intestine for rhamnosylvitexin. The absorption and secretion of rhamnosylvitexin in HLF are mediated by the efflux transport system, P-gp.

关 键 词：山楂叶总黄酮 牡荆素鼠李糖苷 肠吸收 在体单向肠灌流模型 P-糖蛋白 

分 类 号：R969.1[医药卫生—药理学]