HPLC determination of the equilibrium solubility and apparent oil/water partition coefficient of cantharidin
YUAN Li
ZHONG Si-yu
ZHOU Rong
ZHOU Wei
TANG Ying-nan
PENG Ying
ZHOU Li-li
XIA Xin-hua
Abstract：Objective:To determine the physical and chemical properties of cantharidin so as to provide a basis for investigating its dynamic properties and new dosage form design.Methods:The high performance liquid chromatography (HPLC) method was used to detect the equilibrium solubility of cantharidin in various solutions.The apparent partition coefficients of drugs in the octanol-water and octanol-buffer solution systems were measured by shaking-flask method.The stability of cantharidin in acid,alkali,oxidant and reducing solutions was determined.Results:The equilibrium solubility was 40.5 μg· mL-1 in water at 25 ℃,the largest in acetonitrile (36 927.6 μg· mL-1),and smaller in basic buffer solutions.After adding the surfactants,solubility of cantharidin was increased,in which the solubilization hydrogenated soybean lecithin was the strongest.The apparent oil/water partition coefficient of cantharidin was 2.541 2 (lgP =0.405 0).Cantharidin was unstable in the acids,alkali,oxidant and reducing solutions.Conclusion:The shake flask method established in this study is simple and feasible.Cantharidin has poor water solubility,and the equilibrium solubility as well as apparent oil/water partition coefficient of cantharidin is greatly influenced by the pH value of media.Cantharidin is a drug with low solubility,permeability and bioavailability.
Keywords：cantharidinHPLCequilibrium solubilityapparent oil/water partition coefficientstability test
Publication Date：2017-01-01
Online Publishing Date：2026-08-14(First online date of this platform, not the publication date of the document)
Pages：4( 1185-1188 )