Brain Concentration of Ginsenosides and Pharmacokinetics after Oral Administration of Mountain‐cultivated Ginseng

Abstract

Mountain‐cultivated ginseng (MCG) can be considered a mimic of wild ginseng, whose seeds are sowed artificially, cultivated in the natural environment, and returned to the wild state before being used clinically. Cultivated ginseng (CG) and MCG are mainly used as the commercial material for clinical applications. However, MCG is much more expensive but effective than CG. The aim of this study is to explore the differences in the pharmacokinetics and brain concentration of Rg1, Re, Rb1, and Rd after oral administration of MCG, CG, and pure ginsenosides. An ultra‐performance liquid chromatography‐tandem mass spectrometry method was developed and validated to determine the concentration of the four ginsenosides in rat plasma and brain tissue. Compared with the pure group, the area under the curve (AUC) of all the four ginsenosides for CG and MCG increased. The mean brain concentrations of the four ginsenosides were found to be 10‐ to 15‐fold lower than the corresponding contents in the plasma, and the poor permeability of ginsenosides into blood–brain barrier was indicated by the low concentrations of the four ginsenosides.