Institute of Medicinal Plant Development (IMPLAD), Chinese Academy of Medical Sciences & Peking Union Medical College, Haidian District, Beijing, PR China.
J Ethnopharmacol. 2010 Sep 15;131(2):313-20. doi: 10.1016/j.jep.2010.06.034. Epub 2010 Jun 30.
To investigate the effect of Acorus gramineus (AG), a supposed 'delivering servant' according to traditional Chinese medicine principles governing multi-herb formula preparation and formulation, on facilitating the uptake of ginsenosides Rg1, Re and Rb1 to the brain after oral administration of Kai-Xin-San (KXS) preparations.
Ginseng extracts or KXS with or without AG were administered to rats for pharmacokinetic study and mice for behaviour tests at a dose of 3 g ginseng per kg. The concentrations of ginsenosides in plasma and brain were determined by an LC-MS/MS method, whilst the effects of preparations on spatial learning were evaluated using the Morris water maze test.
KXS in the presence of AG tended to significantly reverse the learning impairment induced by scopolamine. The presence of AG in the KXS formula led to increases in the initial absorption rate and extent of Rg1 and Re in terms of Cmax1 and AUC(0-3h) compared to KXS without AG. Although KXS were found to increase the bioavailabilities and brain concentrations of ginsenosides relative to ginseng extract, the brain-to-plasma AUC(0-12h) ratios appeared not to be affected.
The results suggested that the presence of AG in the KXS formula promoted the initial absorption of ginsenosides Rg1 and Re in the gastrointestinal tract, but unlikely affected the brain-to-plasma AUC ratios.
考察菖蒲（AG）作为一种根据传统中药多草药配方制备和配方原则的“使药”，对口服安神复方（KXS）制剂后人参皂苷 Rg1、Re 和 Rb1 向大脑转运的影响。
将人参提取物或 KXS 与或不与 AG 以 3 克/公斤人参的剂量给予大鼠进行药代动力学研究和小鼠进行行为测试。采用 LC-MS/MS 法测定血浆和脑组织中人参皂苷的浓度，采用 Morris 水迷宫试验评价制剂对空间学习的影响。
KXS 加 AG 可显著逆转东莨菪碱引起的学习障碍。与不含 AG 的 KXS 配方相比，AG 存在于 KXS 配方中会导致 Rg1 和 Re 的 Cmax1 和 AUC（0-3h）的初始吸收速率和程度增加。虽然 KXS 被发现相对于人参提取物增加了人参皂苷的生物利用度和脑浓度，但脑-血浆 AUC（0-12h）比值似乎不受影响。
结果表明，KXS 配方中 AG 的存在促进了胃肠道中人参皂苷 Rg1 和 Re 的初始吸收，但不太可能影响脑-血浆 AUC 比值。
