Park Jong Dae
R&D Center, REBIO Co., Ltd., Seoul, Republic of Korea.
J Ginseng Res. 2024 May;48(3):253-265. doi: 10.1016/j.jgr.2024.02.003. Epub 2024 Mar 4.
Orally administered ginsenosides, the major active components of ginseng, have been shown to be biotransformed into a number of metabolites by gastric juice, digestive and bacterial enzymes in the gastrointestinal tract and also in the liver. Attention is brought to pharmacokinetic studies of ginseng that need further clarification to better understand the safety and possible active mechanism for clinical application. Experimental results demonstrated that ginsenoside metabolites play an important role in the pharmacokinetic properties such as drug metabolizing enzymes and drug transporters, thereby can be applied as a metabolic modulator. Very few are known on the possibility of the consistency of detected ginsenosides with real active metabolites if taken the recommended dose of ginseng, but they have been found to act on the pharmacokinetic key factors in any clinical trial, affecting oral bioavailability. Since ginseng is increasingly being taken in a manner more often associated with prescription medicines, ginseng and drug interactions have been also reviewed. Considering the extensive oral administration of ginseng, the aim of this review is to provide a comprehensive overview and perspectives of recent studies on the pharmacokinetic properties of ginsenosides such as deglycosylation, absorption, metabolizing enzymes and transporters, together with ginsenoside and drug interactions.
口服人参皂苷是人参的主要活性成分，已被证明会在胃肠道以及肝脏中被胃液、消化酶和细菌酶生物转化为多种代谢产物。人参的药代动力学研究需要进一步阐明，以便更好地理解其临床应用的安全性和可能的作用机制，这一点已受到关注。实验结果表明，人参皂苷代谢产物在药物代谢酶和药物转运体等药代动力学特性中发挥重要作用，因此可作为代谢调节剂应用。如果按照推荐剂量服用人参，关于所检测到的人参皂苷与真正的活性代谢产物一致性的可能性，目前所知甚少，但在任何临床试验中都已发现它们会作用于药代动力学关键因素，影响口服生物利用度。由于人参越来越多地以与处方药相关的方式服用，人参与药物相互作用也已得到综述。考虑到人参的广泛口服使用，本综述的目的是全面概述和展望近期关于人参皂苷药代动力学特性的研究，如去糖基化、吸收、代谢酶和转运体，以及人参皂苷与药物的相互作用。
