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塞络通(SLT)是由人参、银杏叶、西红花组方,主治血管性痴呆的现代复方中药。为探讨SLT药效物质基础,并为给药方案提供依据,该文对治疗剂量SLT给与大鼠后,人参皂苷成分的血药浓度、药代特征、以及脑分布进行了研究。实验建立了同时检测生物样品中7种人参皂苷的高灵敏度LC-MS/MS分析方法,经过对线性、专属性、回收率、准确度、精密度的考察,所建立的分析方法符合临床前药代动力学研究要求。灌胃SLT 60 mg·kg-1后,7种目标成分均在大鼠血浆中检出,其中二醇型皂苷比三醇型的皂苷有更高的血药浓度和更长的消除半衰期。血浆中人参皂苷Rg1,Re,Rb1,Rb2/b3,Rc,Rd的平均消除半衰期分别为15.26,2.46,18.41,27.70,21.86,61.58 h;平均峰浓度分别为7.15,2.83,55.32,30.22,21.42,8.81μg·L-1。SLT给药后人参皂苷成分能够迅速进入脑组织,但是随时间下降很快。人参皂苷Rg1,Re,Rb1,Rc脑组织中含量较高的成分。研究结果显示服用SLT后,人参皂苷成分能够快速吸收入血并进入脑组织。人参皂苷,尤其是Rg1,Re可通过快速进入脑组织直接作用于神经细胞发挥作用;以二醇型为主的人参皂苷在血浆中长时间滞留,连续给药方式时会累计达到较高稳态血药浓度,它们可能是通过对外周的药理作用保护脑组织的主要成分。
Plug the network through (SLT) is a ginseng, ginkgo biloba, saffron prescription, treatment of vascular dementia modern compound Chinese medicine. In order to explore the substance basis of SLT and to provide the basis for the drug regimen, the concentration of ginsenoside, pharmacokinetics and brain distribution in rats treated with SLT were studied. A high-sensitivity LC-MS / MS method for the simultaneous determination of seven ginsenosides in biological samples was established. The linearity, specificity, recovery, accuracy and precision of the LC-MS / MS method were established. A generation of dynamic research requirements. After gavage with 60 mg · kg-1 of SLT, all seven target components were detected in rat plasma. Among them, diol type saponin had higher plasma concentration and longer elimination half-life than triol type saponin. The average elimination half-lives of ginsenosides Rg1, Re, Rb1, Rb2 / b3, Rc and Rd in plasma were 15.26, 2.46, 18.41, 27.70, 21.86 and 61.58 h, respectively; mean peak concentrations were 7.15, 2.83, 55.32, 30.22 and 21.42 , 8.81 μg · L-1. Ginsenoside components rapidly enter brain tissue after SLT administration, but decline rapidly over time. Ginsenosides Rg1, Re, Rb1, Rc content of brain tissue components. The results show that after taking SLT, ginsenosides can quickly absorb into the blood and into the brain. Ginsenosides, especially Rg1 and Re, can act directly on nerve cells by quickly entering the brain tissue. Ginsenosides mainly in the diol form remain in the plasma for a long time and accumulate to a higher steady state in continuous administration mode Blood concentration, they may be the main component of brain tissue through the pharmacological effects on the periphery.