Biopharmaceuticals classification system (BCS) of periplocin, periplocymarin and periplogenin / 中草药

Objective To investigate the biopharmaceutical classification of periplocin, periplocymarin and periplogenin by biopharmaceuticals classification system (BCS). Methods The solubility and permeability of periplocin, periplocymarin and periplogenin were studied by using experimental and computer prediction software Pipeline Pilot 8.5 and ChemDraw. These three substances were sorted based on experimental and predicted values by BCS classification method. Results According to the test results, periplocin, periplocymarin and periplogenin were classified as BCS III, which are different from the classification results predicted by different software. The permeability results based on ClgP was consistent with the experimental results; The solubility based on lgCs and the permeability based on AlgP and lgD were opposite to the experimental results. Conclusion The periplocin, periplocymarin and periplogenin are BCS III drugs, the solubility is decreased in turn, but they are still highly soluble components. The permeability is the key factor affecting its absorption. The predicted value of biopharmaceutical properties of active ingredients of A-type cardiac glycosides based on the chemical structure are significant different with the test results, for the BCS study and the in vitro and in vivo correlation evaluation of oral absorption of traditional Chinese medicine preparations containing such ingredients, it is recommended to use a variety of methods to correct the data and increase the reliability of the results.

Biopharmaceuticals classification system(BCS) of nuciferin in Nelumbinis Folium / 中国中药杂志

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.