5-氟尿嘧啶在大鼠血液和肝脏中浓度分布的实验研究.docVIP

精品论文 参考文献 5-氟尿嘧啶在大鼠血液和肝脏中浓度分布的实验研究 胡夏荣1 郑惊雷1 王在国1 梁力健2 钟慕仪1 林志强1 俞武生1 邓润枢1 （1广东省东莞市人民医院肿瘤防治中心 523018）（2中山大学第一附属医院肝胆外科 510080） 【摘要】目的 研究静脉注射5-氟尿嘧啶(Fluorouracil,5-FU)在大鼠血液和肝脏组织中的浓度分布和消除过程，为临床肝脏肿瘤化疗提供参考和理论依据。方法 将Wistar大鼠随机分为两组，分别在不同时间采集血液和肝脏组织样本，用高效液相色谱法（HPLC）分别测定血浆和肝脏组织中的5-FU浓度，并计算穿透比率和药动学数据。结果 静脉注射5-FU后，药物在血浆和肝脏组织中的最高浓度（Cmax）分别为（36.85plusmn;5.96）mu;g/mL和（13.79plusmn;4.56）mu;g/g, 药时曲线下面积(AUC)分别为（842.00plusmn;158.00）micro;g.min/ml和（342.20plusmn;108.20）micro;g.min/g。肝脏组织药物浓度随血药浓度降低而下降。肝脏血液穿透比率（PR）为0.35～0.49。肝脏血液穿透指数（PI）为40.64%。结论 5-FU在血液中可达到较高浓度，其对肝脏的穿透力较强。 【关键词】 5-氟尿嘧啶 肝脏肿瘤 化学治疗 药物浓度 【中图分类号】R730.5【文献标识码】A【文章编号】2095-1752（2012）29-0102-03 Distribution of 5-FU in rat plasma and liver tissue. HU Xiarong 1,ZHENG Jinglei1，WANG Zaiguo1,LIANG Lijian2,ZHONG Muyi1,LIN Zhiqiang1，YU Wusheng1,DENG Runshu1，YE Zhenwei1,LIANG Zijun1 (1. Department of Oncology Surgery, Dongguan Peoplersquo;s Hospital, Dongguan 523018, P.R.China；2.Department of Hepatobiliary Surgery，the First Affiliated Hospital，Sun Yat-Sen University，Guangzhou 510080，China) 【Abstract】 Objective To study the distribution of 5-FU in rat plasma and liver tissue though systemic route. Methods To fufil the systemic venous bolus injection, Wistar ratsrsquo; jugular vein was catheterized. The dose was 20mg/kg and high performance liquid chromatography was adopted to measure the content of 5-FU in plasma and liver tissue. Thus the pharmacokinetics parameters, penetration rate of 5-FU were calculated. Result The peak concention（Cmax）and time-quality area under curve（AUC）of liver tissue were as followed: （13.79plusmn;4.56）micro;g/g，（342.20plusmn;108.20）micro;g.min/g；and the plasma Cmax and AUC were （36.85plusmn;5.96）micro;g/ml，（842.00plusmn;158.00）micro;g.min/ml. The concentration of liver tissue decreased with that of plasma. The liver-plasma penetration rate raged from 0.35 to 0.49 and the penetration index was 40.64%. Conclusion 5-FU could reach high concentration in plasma, and its penetration po