HPLC测定3′-氟尿苷-4-[3-(3,5-二叔丁基-4-甲氧基苯基)-3-氧代-1-丙烯基]苯甲酸酯的稳定性  

Study on stability of 3'-FUDR-BOBA by RP-HPLC

作　　者：陈建刚[1] 靳菊情[1] 张三奇[2] 张继业[2] 刘宇凡[2] 

机构地区：[1]西安交通大学理学院,西安710061 [2]西安交通大学医学院,西安710061

出　　处：《药物分析杂志》2008年第12期2132-2134,共3页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:建立检测3′-氟尿苷-4-[3-(3,5-二叔丁基-4-甲氧基苯基)-3-氧代-1-丙烯基]苯甲酸酯(3′-FUDR-BOBA 酯)的 HPLC 法,并对其稳定性进行研究。方法:用 Diamonsil C_(18)色谱柱(150 mm×4.6 mm,5μm),甲醇-水(85:15)为流动相,流速1 mL·min^(-1),检测波长270 nm 等条件下分析测定3′-FUDR-BOBA 酯在不同 pH 的缓冲溶液中及小鼠脏器匀浆中的降解情况,研究其稳定性。结果:在0.1～100μg·mL^(-1)范围内线性关系良好,回归方程为 A=2.039×10~4C+2.259×10~3(r=0.9998)。在血清、肝脏、肾脏和肺组织匀浆中,药物的半衰期(t_(1/2))分别为:12.6,0.99,1.64,4.48 h。结论:3′-FUDR-BOBA 酯在酸性及中性溶液中较稳定,在碱性溶液中水解较快;不同生物组织匀浆中稳定性考察结果显示,药物在肝脏和肾脏中衰减较快。Objective ： To establish an RP - HPLC method to determine 3＇ - FUDR - 4 - （ 3 - （ 3,5 - di - tert - butyl - 4 - methoxyphenyl） - 3 - oxoprop - 1 - enyl） benzoate （ 3＇ - FUDR - BOBA） and its stability in different pH buffer solution and biological media. Method：The samples were determined on a Diamonsil C18 column （150 mm ×4.6 mm,5 μm） ,with the mobile phase of methanol -water （85： 15）. The flow rate was 1 mL ·min-1 ,and the UV detection was set at 270 nm. The degradation of 3＇ - FUDR - BOBA in different pH buffer solution and in homogenate of mice were determined. Results： The linearity range was 0. 1 - 100μg · mL- 1, regression equation was A = 2. 039 × 10^4 C ＋ 2. 259 ×10^3 （r = 0. 9998 ）. The half life （t1/2 ） in homogenate of serum, liver, kidney and lung were 12.6,0.99,1.64 and 4. 48 h,respectively. Conclusion：3＇- FUDR- BOBA is stable in acidic and neu- tral solution, and easily hydrolyzed in alkaline solution;it is easily hydrolyzed in homogenate of liver and kidney of mice.

关 键 词：3’-氟尿苷酯 高效液相色谱 稳定性 水解常数 半衰期 

分 类 号：R917[医药卫生—药物分析学]