N_(1)-山梨酰-5-氟脲嘧啶前体药物的体外降解动力学研究

STUDIES ON DEGRADATION KINETICS OF N_(1)-SORBYL-5-FLUOROURACIL IN VITRA

目的 :研究N1 山梨酰 5 氟脲嘧啶体外降解情况和稳定性。方法 :用HPLC测定N1 山梨酰 5 氟脲嘧啶在不同pH值的缓冲溶液、不同的组织匀浆和醇 /水两相中的浓度 ,然后进行拟合计算 ,数学拟合求取降解动力学方程和分配系数。结果 :N1 山梨酰 5 氟脲嘧啶在缓冲溶液和组织匀浆中的降解服从表观一级反应 ,分配系数logP =1.5 780。结论 :N1 山梨酰 5 氟脲嘧啶比 5 氟脲嘧啶的稳定性好。

OBJECTIVE:The degradation kinetics of N 1 sorbyl 5 Fu were studied to determine the stability in vitra . METHODS:The concentrations of N 1 sorbyl 5 Fu in various solutions were determined by HPLC,from which could deduce the functions and partition coefficients. RESULTS:The degradations of N 1 sorbyl 5 Fu were shown to display pseudo first order kinetics in buffer solutions and biological media. The partition coefficient of N 1 sorbyl 5 Fu is larger than parent 5 fluorouracil.CONCLUSION:Sorbyl 5 fluorouracil was chosen as potential prodrug.