蟾酥中3种蟾毒配基组合物的表观溶解度和表观油水分配系数的测定

目的：测定蟾酥中3种蟾毒配基组合物的表观溶解度和表观油水分配系数。方法：采用高效液相色谱法测定了蟾酥中3种蟾毒配基组合物中RBG，CBG，BL的表观溶解度，采用摇瓶法测定了RBG，CBG，BL的表观油水分配系数。结果：37 ℃，pH 7.0时，蟾酥中3种蟾毒配基组合物中RBG，CBG，BL的表观溶解度均为最大值，分别是76.29，51.85，32.76 μg·mL^-1，总溶解度为160.9 μg·mL^-1。在偏酸和偏碱性条件下，三者均有不同程度的降解。RBG，CBG，BL在不同pH条件下各自log P值差别不大，pH对RBG，CBG，BL的油水分配系数影响不显著，三者的油水分配系数均较大，为典型的疏水性产物，三者的疏水性大小顺序为RBG>BL>CBG。结论：蟾酥中3种蟾毒配基组合物中RBG，CBG，BL的水溶性差，疏水性极强，应考虑加入表面活性剂增溶，以利于注射制剂的成型。

LIU Dan, FENG Jian-fang

OBJECTIVE: To investigate apparent aqueous solubility and apparent oil-water partition coefficients of three bufadienolides composition. METHOD: A high performance liquid chromatography method was established to determine apparent aqueous solubility of three bufadienolides composition; apparent oil-water partition coefficients of three bufadienolides composition was determined by shaking flask method. RESULT: The solubility of three bufadienolides composition reached the top value, 76.29 microg x mL(-1) (RBG), 51.85 microg x mL(-1) (CBG), 32.76 microg x mL(-1) (BL) respectively and a total of 160.9 microg x mL(-1) in the condition of 37 degrees C and pH 7.0, therefore three bufadienolides composition can be defined as insoluble products. The solubility of the three decreased in weak acid or base environment to some extent. RBG, CBG, BL are liposoluble components and the sequence of log P is RBG > BL > CBG. CONCLUSION: RBG, CBG, BL is water-insoluble and hydrophobic. Surfactants can be applied to increase the solubility of three bufadienolides composition.