Pharmacokinetics and tissue distribution of ginsenoside Rh2 and Rg3 epimers after oral administration of BST204, a purified ginseng dry extract, in rats
Pharmacokinetics and tissue distribution of ginsenoside Rh2 and Rg3 epimers after oral administration of BST204, a purified ginseng dry extract, in rats
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DOI：
10.3109/00498254.2014.929192
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发表时间：
2014-12-01
期刊：
影响因子：
1.8
通讯作者：
Bae, Soo Kyung
中科院分区：
文献类型：
--
作者：
Bae, Soo Hyeon;Park, Jung Bae;Bae, Soo Kyung
1. BST 204是一种含有高浓度外消旋Rh 2和Rg 3混合物的纯化人参干提取物，正在韩国开发用于癌症患者的支持性护理。本研究探讨了BST 204在大鼠体内的药代动力学和组织分布.经口给予BST 204后，大鼠血浆中仅可测定S差向异构体S-Rh 2和S-Rg 3。R-差向异构体R-Rh 2和R-Rg 3的吸收差可能归因于较低的膜渗透性和广泛的肠氧合和/或去糖基化为代谢物。BST 204口服给药后S-Rh 2和S-Rg 3的AUC和C-max值与BST 204的给药剂量（400 mg/kg至2000 mg/kg）成正比，表明其具有线性药代动力学特性.与口服BST 204 1000 mg/kg相比，口服纯S-Rh 2（31.5 mg/kg）和S-Rg 3（68 mg/kg）后S-Rh 2和S-Rg 3的药代动力学无统计学显著差异。这表明BST 204提取物中其他组分的存在对S-Rh 2和S-Rg 3的药代动力学行为没有影响。大鼠口服BST 204后，S-Rh 2和S-Rg 3主要分布于肝脏和胃肠道.本研究有助于全面了解S-Rh 2、R-Rh 2、S-Rg 3和R-Rg 3的药代动力学特征，为BST 204的临床应用提供参考。
1. BST204, a purified ginseng dry extract containing a high concentration of racemic Rh2 and Rg3 mixtures, is being developed for supportive care use in cancer patients in Korea. This study investigates the pharmacokinetics and tissue distribution of BST204 in rats.2. After oral administration of BST204, only the S epimers, S-Rh2 and S-Rg3, could be determined in rat plasma. The poor absorption of the R-epimers, R-Rh2 and R-Rg3, may be attributed to lower membrane permeability and extensive intestinal oxygenation and/or deglycosylation into metabolites. The AUC and C-max values of both S-Rh2 and S-Rg3 after BST204 oral administration were proportional to the administered BST204 doses ranged from 400 mg/kg to 2000 mg/kg, which suggested linear pharmacokinetic properties.3. There were no statistically significant differences in the pharmacokinetics of S-Rh2 and S-Rg3 after oral administration of pure S-Rh2 (31.5 mg/kg) and S-Rg3 (68 mg/kg) compared with oral administration of BST204, 1000 mg/kg. These indicated that the presence of other components of BST204 extract did not influence the pharmacokinetic behavior of S-Rh2 and S-Rg3.4. After oral dosing of BST204, S-Rh2 and S-Rg3 were distributed mainly to the liver and gastrointestinal tract in rats.5. Our finding may help to understand pharmacokinetic characteristics of S-Rh2, R-Rh2, S-Rg3, and R-Rg3, comprehensively, and provide useful information in clinical application of BST204.