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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 investigate the relationship between the lipid-water partition coefficient of 5-fluorouracil and nasal absorption rate constant. Methods: The lipid-water partition coefficients of (4,6,7,8,10) 5-FU in n-octanol-water were determined under different pH values. The 5- FU nasal absorption rate constant, and the two kinds of results data regression. Results: With the increase of pH value, the lipid-water partition coefficient and nasal absorption rate constant of 5-FU increased, and both were positively correlated (r = 0.9838). Conclusion: There is a good linear relationship between drug nasal absorption rate constant and lipid-water partition coefficient.