Determination of drug permeability and biopharmaceutical classification of liquiritigenin in vivo by unidirectional intestinal perfusion model
Objective To determine the permeability of liquiritigenin at different concentrations,explore the absorption mechanism of liquiritigenin in different intestinal segments of rat,and predict the biopharmaceutical classification properties of liquiritigenin.Methods With reference to the definition of medium solubility in the 2020 Edition of Chinese Pharmacopoeia,the solubility of liquiritigenin was evaluated with the equilibrium solubility of buffer solution and water at pH 1.2,4.0,6.8,and 7.4.The permeability of liquiritigenin to duodenum,colon,jejunum and ileum of rats at 25,50,and 75 μg·mL-1 was determined by in vivo unidirectional intestinal perfusion model.The biopharmaceutical classification of liquiritigenin was inferred by combining the solubility and permeability results.Results The equilibrium solubility of liquiritigenin was lower than 100 μg·mL-1 at different pH values and in water,the solubility was low or almost insoluble,and lipophilicity was poor.The permeability of liquiritigenin in different intestinal segments of rats was greater than 1.2×10-3 cm·min-1,indicating easy absorption.Conclusion Liquiritigenin has self-absorption inhibition and saturation absorption characteristics in the intestinal of rats,which may involve the transport mechanism such as active transport or diffusion.Liquiritigenin is predicted to be a biopharmaceutical classⅡdrug with low solubility and high permeability.
万方数据
维普
