Tolerability and pharmacokinetics of ginsenosides Rb1, Rb2, Rc, Rd, and compound K after single or multiple administration of red ginseng extract in human beings
Tolerability and pharmacokinetics of ginsenosides Rb1, Rb2, Rc, Rd, and compound K after single or multiple administration of red ginseng extract in human beings
复制标题
DOI：
10.1016/j.jgr.2018.10.006
复制
发表时间：
2020-03-01
影响因子：
6.3
通讯作者：
Song, Im-Sook
中科院分区：
文献类型：
--
作者：
Choi, Min-Koo;Jin, Sojeong;Song, Im-Sook
工作背景：我们研究了人体单次或多次服用红参提取物后各种人参皂苷（包括Rb 1、Rb 2、Rc、Rd和化合物K）的耐受性和药代动力学特性。方法：对15名健康韩国人一次重复服用红参提取物（干参> 60%），持续15天。单次和重复给予红参提取物后，采集血样，测量血压和体温，并进行常规实验室检查，超过48小时的测试periods.Results：重复给予大剂量红参15天耐受性良好，并没有产生显着的变化，体温或血压。重复给药15天后，Rb 1、Rb 2和Rc的血浆浓度稳定，且血浆浓度-时间曲线下面积（AUC）值相似。与单次给药AUC相比，重复给予红参提取物15天后的AUC值累积了4.5至6.7倍。然而，Rd和化合物K的血浆浓度显示出较大的个体间差异，但Rd和化合物K的AUC之间具有良好的相关性。结论：Rd和化合物K的AUC值之间具有良好的相关性，这可能是由于Rb 1、Rb 2和Rc在肠道内生物转化为Rd，然后再转化为化合物K的结果，而不是由于这些皂苷在肠道内的渗透性。增加生物转化或降低代谢受试者间变异性的策略可能会增加Rd和化合物K的血浆浓度。(C)2018韩国人参协会，由Elsevier Korea LLC出版。
Background: We investigated the tolerability and pharmacokinetic properties of various ginsenosides, including Rb1, Rb2, Rc, Rd, and compound K, after single or multiple administrations of red ginseng extract in human beings.Methods: Red ginseng extract (dried ginseng > 60%) was administered once and repeatedly for 15 days to 15 healthy Korean people. After single and repeated administration of red ginsengextract, blood sample collection, measurement of blood pressure and body temperature, and routine laboratory test were conducted over 48-h test periods.Results: Repeated administration of high-dose red ginseng for 15 days was well tolerated and did not produce significant changes in body temperature or blood pressure. The plasma concentrations of Rb1, Rb2, and Rc were stable and showed similar area under the plasma concentration-time curve (AUC) values after 15 days of repeated administration. Their AUC values after repeated administration of red ginseng extract for 15 days accumulated 4.5- to 6.7-fold compared with single-dose AUC. However, the plasma concentrations of Rd and compound K showed large interindividual variations but correlated well between AUC of Rd and compound K. Compound K did not accumulate after 15 days of repeated administration of red ginseng extract.Conclusion: A good correlation between the AUC values of Rd and compound K might be the result of intestinal biotransformation of Rb1, Rb2, and Rc to Rd and subsequently to compound K, rather than the intestinal permeability of these ginsenosides. A strategy to increase biotransformation or reduce metabolic intersubject variability may increase the plasma concentrations of Rd and compound K. (C) 2018 The Korean Society of Ginseng, Published by Elsevier Korea LLC.