摘要
目的:以反相高效液相色谱法测定5-氟尿嘧啶(5-Fu)磁性微球及小鼠各组织中5-Fu的含量,并评价5-Fu磁性微球在小鼠体内的靶向性。方法:15只小鼠尾静脉注射5-Fu及其磁性微球,采用0.5%胃蛋白酶消解磁性微球后经乙酸乙酯2次萃取后以反相高效液相色谱法测定心、肝、肾、脾、肺、脑和肌肉等组织匀浆中5-Fu含量。结果:组织匀浆中5-Fu检测浓度在0.1～25mg·L-1范围内线性关系良好,最低检测浓度为0.1mg·L-1。与注射单一5-Fu对照品比较,小鼠静脉注射5-Fu磁性微球后在肝脏分布明显增加(P<0.05),加入磁性支架和体表磁场的肌肉组织中可见5-Fu分布。结论:本方法适用于测定磁性微球及小鼠各组织中5-Fu的含量;5-Fu磁性微球具有肝靶向性和磁靶向性。
OBJECTIVE： To establish a RP - HPLC method for the determination of 5- fluorouracil（5- Fu） in magnetic micropheres （MMS）, and to evaluate the target ability of 5- Fu magnetic microspheres in mice. METHODS： 5- Fu- MMS was digested with 0.5% pepsin, and then free 5 Fu was extracted from tissue with ethyl acetate, and detected by a validated RP -HPLC method. RESULTS： The calibration curve was linear over the range of 0.1--25mg·L^-1 and the limit of quan- t ization was 0. 1mg ·L^-1. The tissue distribution of 5 Fu-MMS in the liver was significantly increased as compared to control（P〈0.05）; Furthermore, 5- Fu- MMS was detected in muscle by using an internal magnetic holder and externally applied magnetic field in muscle section. CONCLUSION .The established HPLC method is suitable for the study of 5- Fu content in magnetic - microspheres and tissues, and for the evaluation of the target ability of 5- Fu MMS in mice; 5- Fu - MMS has remarkable hepatic targeting and good magnetic targeting.
出处
《中国药房》
CAS
CSCD
北大核心
2007年第7期497-499,共3页
China Pharmacy
基金
国家科技部863课题(2002AA214061)
