Abstract

Ginsenoside Rg1 is a major bioactive component of ginseng. Limited information is available regarding Rg1 concentrations in the central neural system and the corresponding relationship of plasma/intracerebral concentrations, and intracerebral effects of Rg1. Awake Aβ model rats received a single subcutaneous administration of Rg1. Concentrations of unbound Rg1 and acetylcholine in the brain extracellular fluid and Rg1 in plasma were then determined. An E_max-two compartment pharmacokinetic/pharmacodynamics (PK/PD) model without effect compartment was finally obtained by evaluating three mechanism-based models. The corresponding relationship between the plasma PK and PD of Rg1 can be described as E = 119.05•C/(73.42 + C).

摘要

人参皂苷Rg1是人参的主要生物活性成分。关于中枢神经系统中Rg1的浓度以及血浆/脑内浓度的相应关系以及Rg1的脑内作用的信息有限。清醒的Aβ模型大鼠接受皮下注射Rg1。然后确定脑细胞外液中未结合的Rg1和乙酰胆碱的浓度以及血浆中Rg1的浓度。通过评估三个基于机理的模型，最终获得了没有效应区室的E _max-两个区室的药代动力学/药效学（PK / PD）模型。血浆PK与Rg1的PD之间的对应关系可以描述为E = 119.05•C /（73.42 + C）。