A systematic evaluation of biopharmaceutics classification system of main efficacy and toxic ingredients in Polygoni Multiflori Radix Praeparata
10.7501/j.issn.0253-2670.2020.13.012
- VernacularTitle: 制何首乌中主要药效/毒效成分的生物药剂学分类系统评价研究
- Author:
Xue-Xiao CAO
1
Author Information
1. School of Chinese Materia Medica, Tianjin University of Traditional Chinese Medicine
- Publication Type:Journal Article
- Keywords:
Absorption in vivo;
Anthraquinone;
Bioavailability in vitro;
Biopharmaceutics classification system (BCS);
Correlation;
Emodin;
Emodin-8-O-β-D-glucoside;
Equilibrium solubility method;
Everted gut sacs method;
False positive;
Gallic acid;
Permeability;
Pesticide effect;
Physcion;
Polygoni Multiflori Radix Praeparata;
Security;
Solubility;
Stilbene glycoside;
Toxic effect
- From:
Chinese Traditional and Herbal Drugs
2020;51(13):3451-3456
- CountryChina
- Language:Chinese
-
Abstract:
Objective: Biopharmaceutics classification system (BCS) of five main pharmacological/toxic components (gallic acid, emodin, stilbene glycoside, physcion, and emodin-8-O-β-D-glucoside) of Polygoni Multiflori Radix Praeparata (PMRP) were carried out. Methods: The solubility and permeability of each representative component were studied by equilibrium solubility method and everted intestinal sac method, respectively. Using two softwares (Pipeline Pilot 7.5, ChemDraw 7.0) to predict the solubility and permeability parameters of each component. Classical BCS classification of measured and predicted values of representative components was conducted according to Food and Drug Administration (FDA) standards, and their correlation was evaluated. Results: The emodin, emodin-8-O-β-D-glucoside, and physcion in PMRP was preliminary determined as BCS IV drugs. THSG and gallic acid belong to BCS III drugs, and permeability was the main limiting factor in their absorption process. There was software which predicts false positives of anthraquinone in BCS classification studies. Conclusion: In this study, five main pharmacodynamic/toxic components of PMRP were classified by BCS method, which provided data support and technical reference for in vivo absorption prediction and in vitro safety evaluation of traditional Chinese medicine.
