Biopharmaceuticals classification system(BCS) of nuciferin in Nelumbinis Folium.
10.19540/j.cnki.cjcmm.20171023.001
- Author:
Jun-Rui ZHAO
1
;
Xiao-Liang REN
2
;
Meng WANG
1
Author Information
1. Institute of Traditional Chinese Medicine， Tianjin University of Traditional Chinese Medicine， Tianjin 300193， China.
2. School of Traditional Chinese Medicine， Tianjin University of Traditional Chinese Medicine， Tianjin 300193， China.
- Publication Type:Journal Article
- Keywords:
biopharmaceuticals classification system;
in vitro;
nuciferine;
oil-water partition coefficient;
permeability;
solubility
- MeSH:
Animals;
Aporphines;
chemistry;
Biological Availability;
Biological Products;
classification;
Biopharmaceutics;
Caco-2 Cells;
Humans;
Intestinal Absorption;
Mice;
Nelumbo;
chemistry;
Permeability;
Plant Leaves;
chemistry;
Solubility
- From:
China Journal of Chinese Materia Medica
2018;43(3):511-519
- CountryChina
- Language:Chinese
-
Abstract:
Nuciferin is the main active ingredients in Nelumbinis Folium， which was proved to have good hypolipidemic， antioxidative and anti-inflammatory bioactivities. Currently， pharmacokinetic studies of nuciferin showed different results based on different animal models. evaluation experiments were low-cost， stable and controllable. Biopharmaceutical classification system(BCS) was an effective and reliable simulation method to evaluate the bioavailability of oral drugs. It was a scientific framework for classifying drugs or active pharmaceutical ingredients(API) according to their solubility and impermeability . In the study， BCS was applied in an active ingredient in traditional Chinese medicine(TCM)， which was consisted of numerous chemical components. To study the equilibrium solubility of nuciferine， ideal solution model， Ape blat model and polynomial model were adopted. The permeability was measured based on partition coefficient(logP) and distribution coefficient(logD). Besides， apparent permeabilities of Caco-2 cells and murine intestine tissues were evaluated. Nuciferine was classified as BCSⅠ， since it had a good solubility and permeability in all methods under acidic conditions. However， in neutral and alkaline environments， nuciferine was classified as BCSⅣ by using everted intestinal sac. It indicated that the species of experimental animals has a significant influence on the absorption of nuciferine. This experiment can provide data support to the prediction in a complex environment(medicinal materials and absorbed parts). The application of BCS on TCM ingredients provided a new method to evaluate and screen out the druggability of TCM ingredients.
