College of Pharmacy, Dankook University, Cheon-an 31116, Korea.
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Kyungpook National University, Daegu 41566, Korea.
Molecules. 2019 Jul 18;24(14):2618. doi: 10.3390/molecules24142618.
We aimed to develop a sensitive method for detecting 13 ginsenosides using liquid chromatography-tandem mass spectrometry and to apply this method to pharmacokinetic studies in human following repeated oral administration of red ginseng extract. The chromatograms of Rb1, Rb2, Rc, Rd, Re, Rf, Rg1, Rg3, Rh2, F1, compound K (CK), protopanaxadiol (PPD), and protopanaxatriol (PPT) in human plasma were well separated. The calibration curve range for 13 ginsenosides was 0.5-200 ng/mL and the lower limit of quantitation was 0.5 ng/mL for all ginsenosides. The inter- and intra-day accuracy, precision, and stability were less than 15%. Among the 13 ginsenosides tested, nine ginsenosides (Rb1, Rb2, Rc, Rd, Rg3, CK, Rh2, PPD, and PPT) were detected in the human plasma samples. The plasma concentrations of Rb1, Rb2, Rc, Rd, and Rg3 were correlated with the content in red ginseng extract; however, CK, Rh2, PPD, and PPT were detected although they are not present in red ginseng extract, suggesting the formation of these ginsenosides through the human metabolism. In conclusion, our analytical method could be effectively used to evaluate pharmacokinetic properties of ginsenosides, which would be useful for establishing the pharmacokinetic-pharmacodymic relationship of ginsenosides as well as ginsenoside metabolism in humans.
我们旨在开发一种灵敏的液相色谱-串联质谱法检测 13 种人参皂苷的方法，并将该方法应用于红参提取物重复口服给药后的人体药代动力学研究。在人血浆中，Rb1、Rb2、Rc、Rd、Re、Rf、Rg1、Rg3、Rh2、F1、化合物 K（CK）、原人参二醇（PPD）和原人参三醇（PPT）的色谱图得到了很好的分离。13 种人参皂苷的校准曲线范围为 0.5-200ng/mL，所有人参皂苷的定量下限均为 0.5ng/mL。日内和日间准确度、精密度和稳定性均小于 15%。在所测试的 13 种人参皂苷中，有 9 种（Rb1、Rb2、Rc、Rd、Rg3、CK、Rh2、PPD 和 PPT）在人血浆样品中被检测到。Rb1、Rb2、Rc、Rd 和 Rg3 的血浆浓度与红参提取物中的含量相关；然而，尽管 CK、Rh2、PPD 和 PPT 不在红参提取物中存在，但它们被检测到，这表明这些人参皂苷是通过人体代谢形成的。总之，我们的分析方法可有效地用于评估人参皂苷的药代动力学特性，这对于建立人参皂苷的药代动力学-药效学关系以及人参皂苷在人体内的代谢非常有用。
