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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 oil-water partition coefficients and gut absorption of notoginsenoside R1, ginsenoside Rg1 and Rb1, which are the three active constituents of Panax notoginseng saponins (PNS). Methods: The oil-water partition coefficients of three main active ingredients were determined by classical shake-flask method. The intestine absorption model of rats was used to study the intestinal absorption of the three main active ingredients, and the absorption of each of the three components Absorption effects. Results: The oil-water partition coefficients P of notoginsenoside R1 (R1), ginsenoside Rg1 (Rg1) and Rb1 (Rb1) were 1.081 4, 6.310 4 and 0.2743, respectively. The log P values were 0.034 0, 0.800 1 and -0.561 8, respectively. The absorption rate constants (R1) of R1, Rg1 and Rb1 in 0.2 gL-1 group were (0.135 ± 0.006), (0.144 ± 0.015) and (0.238 ± 0.013) h- The Ka of Rb1 and Rb1 were (0.010 ± 0.002), (0.110 ± 0.006) and (0.140 ± 0.008) h- 0.011), (0.137 ± 0.012) h-1. The statistical results showed that there was a significant difference between 0.5 gL-1 and 0.5 gL-1 K in 0.2 gL-1 Ka group (P <0.01) (0.030 ± 0.006), (0.033 ± 0.004), (0.033 ± 0.007), respectively, in the duodenum, jejunum and ileum (0.042 ± 0.006), (0.044 ± 0.012) and (0.044 ± 0.011) h-1 for Rg1 and Ka for Rb1 were (0.042 ± 0.007) and ± 0.014) h-1, the statistical results showed that there was no significant difference in different bowel segments Ka. CONCLUSION: According to the classical theory, R1, Rg1 and Rb1 are not easily absorbed. The three components Ka of PNS gradually decrease with the increasing of concentration, Ka of 0.2 gL-1 group is higher than that of 0.5 and 1 gL-1 group, In R1 and Rg1, PNS absorption in addition to passive diffusion, there may be other absorption mechanisms; PNS intestinal segments in the intestine of rats are absorbed.