甲磺酸雷沙吉兰油水分配系数的测定

Determination of oil /water partition coefficient of rasagiline mesylate

目的:测定甲磺酸雷沙吉兰在正辛醇-不同pH值缓冲液体系中的油水分配系数。方法:采用HPLC法测定甲磺酸雷沙吉兰的浓度,采用改进的摇瓶法测定其表观油水分配系数。结果:甲磺酸雷沙吉兰的油水分配系数在一定范围内随着缓冲液pH值的增加而增加,当pH值大于6.5时,95%以上的甲磺酸雷沙吉兰进入正辛醇层。结论:甲磺酸雷沙吉兰在酸性体系中亲脂性差,在偏碱性的体系中亲脂性强。

Objective： To determine the oil/water partition coefficient of rasagiline mesylate in the nctanol-buffer solution system at different pH values. Methods： The concentration of rasagiline mesylate was determined by HPLC, and the oil/water partition coefficient was determined by an improved shaking flask method. Results： The oil/water partition coefficient of rasagitine mesylate increased with an increase in the buffer solution pH value within a certain range. More than 95% of rasagiline mesylate was in n-octanol when the buffer solution pH value was above 6.5. Conclusion ： The lipophilicity of rasagiline mesylate is high in acid system while is low in alkaline system.