三七总皂苷油水分分配系数及大鼠在体肠吸收动力学研究  

O/W partition coefficient of PNS and absorption kinetics of it in rat intestine

作　　者：翟永松[1] 杜守颖[1] 徐冰[1] 陆洋[1] 高瑛[1] 

机构地区：[1]北京中医药大学中药学院,北京100102

出　　处：《中国中药杂志》2010年第8期984-988,共5页China Journal of Chinese Materia Medica

基　　金：国家"十一五"科技支撑计划项目(2006BA106A17);科技部"重大新药创制"科技重大专项(2009ZX09502-008)

摘　　要：目的:测定三七总皂苷(PNS)3种主要有效成分三七皂苷R1、人参皂苷Rg1和Rb1的油水分配系数及其肠吸收情况。方法:采用经典摇瓶法测定3种主要有效成分的油水分配系数;采用大鼠在体肠吸收模型研究3种主要有效成分的肠吸收情况,考察其在小肠各段的吸收情况及药物浓度对吸收的影响。结果:三七皂苷R1(R1)、人参皂苷Rg1(Rg1)和Rb1(Rb1)的油水分配系数P分别为1.081 4,6.310 4,0.2743;logP分别为0.034 0,0.800 1,-0.561 8;PNS质量浓度0.2 g.L-1组R1,Rg1和Rb1的吸收速率常数(Ka)分别为(0.135±0.006),(0.144±0.015),(0.238±0.013)h-1;0.5 g.L-1组R1,Rg1和Rb1的Ka分别为(0.110±0.002),(0.110±0.006),(0.140±0.008)h-1,1 g.L-1组R1,Rg1和Rb1的Ka分别为(0.095±0.016),(0.099±0.011),(0.137±0.012)h-1,统计结果显示,0.2 g.L-1组Ka与0.5,1 g.L-1组有显著性差异(P<0.01),0.5 g.L-1与1 g.L-1Ka无显著差异;Rb1Ka与R1,Rg1有显著性差异(P<0.01);在十二指肠、空肠、回肠中,R1的Ka分别为(0.030±0.006),(0.033±0.004),(0.033±0.007)h-1,Rg1的Ka分别为(0.032±0.006),(0.044±0.012),(0.044±0.011)h-1,Rb1的Ka分别为(0.042±0.007),(0.065±0.007),(0.044±0.014)h-1,统计结果显示,不同肠段Ka无显著性差异。结论:根据经典理论,R1,Rg1和Rb1均不易吸收;PNS中3种成分Ka随浓度的增加而逐渐减小,0.2 g.L-1组Ka高于0.5,1 g.L-1组,Rb1的Ka高于R1和Rg1,PNS吸收除被动扩散外,可能还存在其他吸收机制;PNS在大鼠小肠各个肠段均有吸收。Objective： To determine the O/W partition coefficient of panax pseudo-ginseng saponin（PNS） and investigate the absortion kinetics of it in whole small intestine and different intestinal segments of rats.Method： The shake-flask method was employed to determine the O/W partition co-efficient of geniposide,and an in situ intestinal perfusion model was employed to investigate the absorptive kinetics of geniposide.Result： The partition coefficient（P） of R1,Rg1 and Rb1 of PNS were 1.081 4,6.310 4 and 0.274 3,respectively,and their logP were 0.034 0,0.800 1,-0.561 8,the absorptive rate constants（Ka） of R1,Rg1 and Rb1 of PNS at the concentration of 0.2,0.5,1.0 g·L-1 were（0.135±0.006）,（0.110±0.002）,（0.095±0.016）,（0.144±0.015）,（0.110±0.006）,（0.099±0.011）,（0.238±0.013）,（0.140±0.008）,（0.137±0.012）h-1,respectively.The Ka of R1,Rg1 and Rb1 of PNS were（0.030±0.006）,（0.033±0.004）,（0.033±0.007）,（0.032±0.006）,（0.044±0.012）,（0.044±0.011）,（0.042±0.007）,（0.065±0.007）,（0.044±0.014）h-1 at duodenum,jejunum,ileum,respectively.The absorption rate of Rb1 was higher than R1 and Rg1.Conclusion： According to the P and the logP,it can be conjectured that the absorption of R1 and Rg1 are better than Rb1.The absorption rate is decreased with the increase of the PNS concentration.Their absorption is the passive diffusion mechanism and other transport may also take part in the transport process.PNS is absorbed at all small-intestinal segments of rats,there are no significant differences between the three sections.

关 键 词：三七总皂苷 油水分配系数 三七皂苷R1 人参皂苷Rg1 人参皂苷RB1 肠吸收 

分 类 号：R284.1[医药卫生—中药学] R285.5[医药卫生—中医学]