Plasma and intracerebral pharmacokinetics and pharmacodynamics modeling for the acetylcholine releasing effect of ginsenoside Rg1 in mPFC of Aβ model rats

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).

Graphical Abstract

Keywords:

• Ginsenoside Rg1
• pharmacokinetics
• acetylcholine
• microdialysis
• PK/PD model

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was financially supported by the National Natural Science Foundation of China [grant number 81303250] and the Ministry of Science and Technology of China [No. 2017ZX09304026014].