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Determination of 5-Fluorouracil in Human Plasma by High- Performance Liquid Chromatography (HPLC
引用本文:谷元,陆榕,司端运,刘昌孝.Determination of 5-Fluorouracil in Human Plasma by High- Performance Liquid Chromatography (HPLC[J].天津大学学报(英文版),2010,16(3):167-173.
作者姓名:谷元  陆榕  司端运  刘昌孝
作者单位:GU Yuan(School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;Tianjin State Key Laboratory of Pharmacokinetics and Pharmacodynamics,Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China);LU Rong,SI Duanyun,LIU Changxiao(Tianjin State Key Laboratory of Pharmacokinetics and Pharmacodynamics,Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China) 
基金项目:国家自然科学基金,Major State Basic Research Development Program of China ("97Y" Program) 
摘    要:5-Fluorouracil (5-FU) has a broad spectrum of anti-tumor activity, widely applied to the treatment of cancers. However, it is necessary to determine the plasma concentration of 5-FU in clinical practice due to its narrow therapeutic index. Therefore, a simple, economic and sensitive high-performance liquid chromatography (HPLC) method was developed and validated for the determination of 5-FU in human plasma. Ethyl acetate was chosen as extraction reagent. Chromatographic separation was performed on a Diamonsil C18 column (250 mm × 4.6 mm i.d., 5 μm) with the mobile phase consisting of methanol and 20 mmol/L ammonium formate using a linear gradient elution at a flow rate of 0.8 mL/min. 5-FU and 5-bromouracil (5-BU) were detected by UV detector at 265 nm. The calibration curve was linear over the concentration range of 5—500 ng/mL and the correlation coefficient was not less than 0.992 6 for all calibration curves. The intra- and inter-day precisions were less than 10.5% and 4.3%, respectively, and the accuracy was within ±3.7%. The recovery at all concentration levels was 80.1±8.6%. 5-FU was stable under possible conditions of storing and handling. This method is proved applicable to therapeutic drug monitoring and pharmacokinetic studies of 5-FU in human.

关 键 词:高效液相色谱法  氟尿嘧啶  HPLC  人血浆  紫外检测器  测定  线性梯度洗脱  校准曲线
收稿时间:12 June 2008

Determination of 5-fluorouracil in human plasma by high-performance liquid chromatography (HPLC)
GU Yuan,LU Rong,SI Duanyun,LIU Changxiao.Determination of 5-fluorouracil in human plasma by high-performance liquid chromatography (HPLC)[J].Transactions of Tianjin University,2010,16(3):167-173.
Authors:GU Yuan  LU Rong  SI Duanyun  LIU Changxiao
Institution:1. School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;Tianjin State Key Laboratory of Pharmacokinetics and Pharmacodynamics,Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
2. Tianjin State Key Laboratory of Pharmacokinetics and Pharmacodynamics,Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China
Abstract:5-Fluorouracil (5-FU) has a broad spectrum of anti-tumor activity, widely applied to the treatment of can-cers. However, it is necessary to determine the plasma concentration of 5-FU in clinical practice due to its narrow therapeutic index. Therefore, a simple, economic and sensitive high-performance liquid chromatography (HPLC)method was developed and validated for the determination of 5-FU in human plasma. Ethyl acetate was chosen as ex-traction reagent. Chromatographic separation was performed on a Diamonsil C18 column (250 mm x 4.6 mm I.d., 5μm) with the mobile phase consisting of methanol and 20 mmol/L ammonium formate using a linear gradient elution at a flow rate of 0.8 mL/min. 5-FU and 5-bromouracil (5-BU) were detected by UV detector at 265 nm. The calibra-tion curve was linear over the concentration range of 5-500 ng/mL and the correlation coefficient was not less than 0.992 6 for all calibration curves. The intra- and inter-day precisions were less than 10.5% and 4.3%, respectively, and the accuracy was within ±3.7%,. The recovery at all concentration levels was 80.1±8.6%. 5-FU was stable under possi-ble conditions of storing and handling. This method is proved applicable to therapeutic drug monitoring and pharma-cokinetic studies of 5-FU in human.
Keywords:5-fluorouracil (5-FU)  high-performance liquid chromatography (HPLC)  human plasma
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