| 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 |
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| 引用本文： | 翟永松,杜守颖,徐冰,陆洋,高瑛.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[J].中国中药杂志,2010,35(8):984-988. |
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| 作者姓名： | 翟永松 杜守颖 徐冰 陆洋 高瑛 |
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| 作者单位： | 北京中医药大学,中药学院,北京,100102 |
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| 基金项目： | 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) |
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| 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(P0.01),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(P0.01);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。
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| 关 键 词： | 三七总皂苷 油水分配系数 三七皂苷R_1 人参皂苷Rg_1 人参皂苷Rb_1 肠吸收 |
| 收稿时间： | 9/3/2009 12:00:00 AM |
O/W partition coefficient of PNS and absorption kinetics of it in rat intestine |
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| ZHAI Yongsong,DU Shouying,XU Bing,LU Yang and GAO Ying.O/W partition coefficient of PNS and absorption kinetics of it in rat intestine[J].China Journal of Chinese Materia Medica,2010,35(8):984-988. |
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| Authors: | ZHAI Yongsong DU Shouying XU Bing LU Yang and GAO Ying |
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| Institution: | School of Chinese Pharmacy, Beijing University of Traditional Chinese Medicine, Beijing 100102, China;School of Chinese Pharmacy, Beijing University of Traditional Chinese Medicine, Beijing 100102, China;School of Chinese Pharmacy, Beijing University of Traditional Chinese Medicine, Beijing 100102, China;School of Chinese Pharmacy, Beijing University of Traditional Chinese Medicine, Beijing 100102, China;School of Chinese Pharmacy, Beijing University of Traditional Chinese Medicine, Beijing 100102, China |
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| Abstract: | 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,resp... |
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| Keywords: | PNS in situ intestinal perfusion model notoginsenoside R1 ginsenoside Rg1 ginsenoside Rb1 O/W partition coefficient |
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