高效液相色谱法测定蝙蝠葛碱的平衡溶解度和油水分配系数

摘要

Objective:To determine the equilibrium solubility of dauricine at various pHs and its oil/water partition coefficient in the n-Octanol-buffer solution system. Methods: An HPLC method was established to determine the concentration of dauricine. A shake flask-HPLC method was applied and the value of oil/water partition coefficient was calculated by the concentration ratio of dauricine in n-octyl alcolhol and water phase. Results: At 37 ℃ both the equilibrium solubility and the oil/water partition coefficient increased with the increasing pH. Conclusions : Both equilibrium solubility and oil/water partition coefficient of dauricine are affected by pH;this method can be used to accurately determine the equilibrium solubility and oil/water partition coefficient of dauricine and help to predict its behavior in vivo.%目的:测定蝙蝠葛碱在不同pH条件下的平衡溶解度以及在正辛醇-缓冲液体系中的油水分配系数.方法:采用HPLC法测定蝙蝠葛碱的浓度,以饱和法测定平衡溶解度,采用摇瓶法-HPLC法测定蝙蝠葛碱在正辛醇和水相中浓度,从而计算油水分配系数.结果:37℃下蝙蝠葛碱的平衡溶解度随pH的升高而增大；油水分配系数随pH的升高而增大,在pH 6.8 ～8.0范围内(小肠的pH环境),蝙蝠葛碱的lgP约为0.5,说明其脂溶性较强.结论:蝙蝠葛碱平衡溶解度和油水分配系数都受pH的影响；本试验所建立的方法可准确测定蝙蝠葛碱的平衡溶解度和油水分配系数,并预测其体内过程.