[Biopharmaceuticals classification system(BCS) of nuciferin in Nelumbinis Folium].

Nuciferin is the main active ingredients in Nelumbinis Folium， which was proved to have good hypolipidemic， antioxidative and anti-inflammatory bioactivities. Currently， in vivo pharmacokinetic studies of nuciferin showed different results based on different animal models. In vitro evaluation experiments were low-cost， stable and controllable. Biopharmaceutical classification system(BCS) was an effective and reliable in vitro 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 vitro . 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， in vitro 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 in vitro method to evaluate and screen out the druggability of TCM ingredients.