氟尿嘧啶的脂水分配系数与鼻腔吸收速率常数的相关性研究

Study on Relationship of Oil/water Partition Coefficient with Nasal Absorption Constant of Fluorouracil

目的:考察氟尿嘧啶(5-FU)的脂水分配系数与鼻腔吸收速率常数的关系。方法:测定不同pH值条件下(4、6、7、8、10)5-FU在正辛醇-水中的脂水分配系数;采用大鼠鼻腔在体重循环方法测定不同pH值条件下5-FU鼻腔吸收速率常数,并将2种结果数据进行回归。结果:随着pH值的升高5-FU脂水分配系数及鼻腔吸收速率常数均增大,且二者呈正相关(r=0.9838)。结论:药物鼻腔吸收速度常数与脂水分配系数之间有良好的线性关系。

OBJECTIVE： To study the relationship of oil/water partition coefficient of fluorouracil （5-FU） with its nasal absorption.METHODS： The octanol /water partition coefficient of 5-FU in Octanol-water were determine at different pH condition （4,6,7,8,10）.In situ nasal recirculation method was used to estimate nasal absorption constant of 5-FU at different pH condition in rat.Regression analysis of obtained data was carried out.RESULTS： Oil/water partition coefficient and nasal absorption constant of 5-FU were increased as long as the value of pH with a positive correlation between them （r=0.983 8）.CONCLUSION： There is a good linear relationship between oil/water partition coefficient and nasal absorption constant.