Pharmacokinetics of ginsenoside Rb1 and its metabolite compound K after oral administration of Korean Red Ginseng extract.
Pharmacokinetics of ginsenoside Rb1 and its metabolite compound K after oral administration of Korean Red Ginseng extract.
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DOI：
10.5142/jgr.2013.37.451
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发表时间：
2013-10
影响因子：
6.3
通讯作者：
Kim HK
中科院分区：
文献类型：
--
作者：
Kim HK
化合物K是Rb1的主要代谢产物，在体内和体外具有多种药理活性。然而，以前的研究集中在单一代谢物或母体化合物的药代动力学，尚未描述两种化合物在人体中的药代动力学。为了研究Rb1和化合物K的药代动力学，我们使用韩国红参提取物进行了一项开放标签、单次口服剂量的药代动力学研究。我们在这项研究中招募了10名健康的韩国男性志愿者。在韩国红参提取物给药后36小时内收集系列血液样品，以测定血浆中的Rb1和化合物K浓度。化合物K的平均最大血药浓度为8.35 ± 3.19 ng/mL，显著高于化合物Rb 1的平均最大血药浓度（3.94 ± 1.97 ng/mL）。化合物K的半衰期比化合物Rb 1的半衰期短7倍。这些结果表明，化合物K的药代动力学，特别是吸收不受其母体化合物的药代动力学的影响，除了达到最大血药浓度的时间。化合物K的延迟吸收支持肠道菌群在Rb1转化为化合物K中起重要作用的证据。
Compound K is a major metabolite of ginsenoside Rb1, which has various pharmacological activities in vivo and in vitro. However, previous studies have focused on the pharmacokinetics of a single metabolite or the parent compound and have not described the pharmacokinetics of both compounds in humans. To investigate the pharmacokinetics of ginsenoside Rb1 and compound K, we performed an open-label, single-oral dose pharmacokinetic study using Korean Red Ginseng extract. We enrolled 10 healthy Korean male volunteers in this study. Serial blood samples were collected during 36 h after Korean Red Ginseng extract administration to determine plasma concentrations of ginsenoside Rb1 and compound K. The mean maximum plasma concentration of compound K was 8.35±3.19 ng/mL, which was significantly higher than that of ginsenoside Rb1 (3.94±1.97 ng/mL). The half-life of compound K was 7 times shorter than that of ginsenoside Rb1. These results suggest that the pharmacokinetics, especially absorption, of compound K are not influenced by the pharmacokinetics of its parent compound, except the time to reach the maximum plasma concentration The delayed absorption of compound K support the evidence that the intestinal microflora play an important role in the transformation of ginsenoside Rb1 to compound K.