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《Acta Pharmaceutica Sinica》 2008-01
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Tissue distribution and excretion of 5-fluorouracil from indomethacin 5-fluorouracil-1-ylmethylester in rats

WANG Guang-hou,WANG Jing,QI Wei,CHEN Yang,SUN Li-xin(School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)  
To study the tissue distribution and excretion of indomethacin 5-fluorouracil-1-ylmethyl ester(IFM) metabolite 5-fluorouracil in rats,an accurate and specific high performance liquid chromatography method for quantifying IFM in rat plasma and tissues was developed.Biological samples were prepared by liquid-liquid extraction and separated on a Diamonsil~(TM) C_(18) column(250 mm×4.6 mm ID,5 μm).The mobile phase for tissue samples,plasma samples and feces samples were composed of methanol-water-36% acetic acid(3∶96.9∶0.1,v/v) and the mobile phase for urine samples was a mixture of methanol-water-36% acetic acid(10∶89.9∶0.1,v/v).The eluate was monitored by UV absorbance at 260 nm.After a single ig dose of 100 mg·kg~(-1) IFM in rats,5-Fu was mainly distributed in stomach,small intestine,and liver.The concentrations of 5-fluorouracil in other tissues and plasma were low.The excretion of 5-Fu in urine and feces amounted to 0.006 5% and 0.063% of the dose,respectively.The method is shown to be accurate and specific,and suitable for preclinical pharmacokinetic studies of IFM.
【CateGory Index】: R96
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1 CHAI Yi-feng*,ZHU Zhen-yu and CHEN Xiao-fei(Department of Pharmaceutical Analysis,School of Pharmacy,Second Military Medical University,Shanghai 200433),Fenxi Shiyanshi,2010,29(9):78~122;Pharmaceutical analysis(I)[J];Chinese Journal of Analysis Laboratory;2010-09
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