Zhang Ying, Lin Li, Liu Guang-Yu, Liu Jian-Xun, Li Tao
Zhongguo Zhong Yao Za Zhi. 2014 Jan;39(2):316-21.
Sailuotong (SLT) is a compound preparation composed of ginseng, ginkgo and saffron for the treatment of vascular dementia In order to identify its material foundation and provide evidence for therapeutic regimen, the pharmacokinetics and brain distribution of ginsenosides were investigated after intragastric administration of SLT. An LC-MS/MS method was developed for the determination of 7 ginsenosides in rat plasma simultaneously. Statistical analysis of obtained data demonstrated that the method has achieved the desired linearity, precision, accuracy and sensitivity. After administration of SLT at 60 mg x kg(-1) dose, 7 ginsengosides were all absorbed into systematic circulation. The quantitative and statistical analysis of gensenosides in plasma showed that protopanaxdiol saponins exhibited higher concentration and longer half life than protopanaxatriol saponins. The mean value of half life of ginsenosides Rg1, Re, Rb1, Rb2/b3, Rc and Rd were 15.26, 2.46, 18.41, 27.70, 21.86 and 61.58 h respectively. The peak concentration of them were 7.15, 2.83, 55.32, 30.22, 21.42, 8.81 microg x L(-1) respectively. The determination of brain distribution at different time after dosing revealed ginsenosides entered into brain promptly but the concentration declined along with time rapidly. The ginsenosides with higher concentration in brain were Rg1, Re, Rb1 and Rc. These findings demonstrated ginsenosides could be absorbed in blood and penetrated into brain rapidly. Some ginsenosides, especially Rg1 and Re, might be the main components directly effecting neurocyte in brain taking advantage of their better brain distribution. While ginsenosides of mostly protopanaxdiol saponins might protect brain mainly depending on peripheral efficacy in virtue of their long residence in blood, by which higher concentration could be reached after multiple dosing.
参络通(SLT)是一种由人参、银杏和藏红花组成的复方制剂,用于治疗血管性痴呆。为了确定其物质基础并为治疗方案提供依据,在灌胃给予参络通后,对人参皂苷的药代动力学和脑分布进行了研究。建立了一种LC-MS/MS方法,用于同时测定大鼠血浆中的7种人参皂苷。对所得数据的统计分析表明,该方法达到了所需的线性、精密度、准确度和灵敏度。以60mg·kg⁻¹的剂量给予参络通后,7种人参皂苷均被吸收进入体循环。血浆中人参皂苷的定量和统计分析表明,原人参二醇型皂苷的浓度较高,半衰期比原人参三醇型皂苷长。人参皂苷Rg1、Re、Rb1、Rb2/b3、Rc和Rd的半衰期平均值分别为15.26、2.46、18.41、27.70、21.86和61.58小时。它们的峰浓度分别为7.15、2.83、55.32、30.22、21.42、8.81μg·L⁻¹。给药后不同时间的脑分布测定显示,人参皂苷迅速进入脑内,但浓度随时间迅速下降。脑内浓度较高的人参皂苷为Rg1、Re、Rb1和Rc。这些结果表明,人参皂苷可被血液吸收并迅速穿透进入脑内。一些人参皂苷,尤其是Rg1和Re,可能因其在脑内的良好分布而成为直接影响脑内神经细胞的主要成分。而大多原人参二醇型皂苷的人参皂苷可能主要通过其在血液中的长时间驻留而依赖外周效应来保护脑,多次给药后可达到更高的浓度。