Biopharmaceutics classification evaluation for paris saponin VII.
10.1016/S1875-5364(20)60010-3
- Author:
Xin ZHANG
1
;
Yang SUN
2
;
Ying CHENG
1
;
Wei-Liang YE
1
;
Bang-Le ZHANG
1
;
Qi-Bing MEI
2
;
Si-Yuan ZHOU
3
,
4
Author Information
1. Department of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi'an 710032, China.
2. Key Laboratory of Gastrointestinal Pharmacology of Chinese Materia Medica of the State Administration of Traditional Chinese Medicine, Fourth Military Medical University, Xi'an 710032, China.
3. Department of Pharmaceutics, School of Pharmacy, Fourth Military Medical University, Xi'an 710032, China
4. Key Laboratory of Gastrointestinal Pharmacology of Chinese Materia Medica of the State Administration of Traditional Chinese Medicine, Fourth Military Medical University, Xi'an 710032, China. Electronic address: zhousy@fmmu.edu.cn.
- Publication Type:Journal Article
- Keywords:
Biopharmaceutical classification system;
Caco-2 cells;
Oil-water partition coefficient;
Paris saponin VII;
Permeability;
Solubility
- From:
Chinese Journal of Natural Medicines (English Ed.)
2020;18(9):714-720
- CountryChina
- Language:English
-
Abstract:
To study the biopharmaceutics characteristics of paris saponin VII (PSVII). The solubility of PSVII was evaluated by measurement of the equilibrium solubility in different solvents and media. The permeability of PSVII was evaluated by measuring the oil/water partition coefficient (lgP) and determining the apparent permeability coefficient (PC) on a mono-layer Caco-2 cell model. The effects of p-glycoprotein and multidrug resistance related protein 2 on PSVII transport in mono-layer Caco-2 cell model were further investigated. Finally, the small intestinal absorption of PSVII was investigated in rat. In solvents of different pH, the equilibrium solubility of PSVII was quite low, and the dose number of PSVII was larger than 1. The lgP of PSVII was less than 0. The apparent permeability coefficient [PC] of PSVII in mono-layer Caco-2 cell model was less than 14.96 × 10 cm·s, and the efflux ratio of PSVII in mono-layer Caco-2 cell model was less than 1. The transport rate of PSVII in mono-layer Caco-2 cell model was not affected by the inhibitors of p-glycoprotein and multidrug resistance related protein 2. After oral administration, PSVII could be detected in rat intestinal contents, but could not be detected in the small intestinal mucosa. PSVII showed low solubility and permeability, which would result in low oral bioavailability in clinic. PSVII belonged to Class IV compound in biopharmaceutics classification system.
