5氟尿嘧啶在大鼠血液和肝脏中浓度分布的实验研究.doc

5-氟尿嘧啶在大鼠血液和肝脏中浓度分布的实验研宄 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) 】目的研究静脉注射5-氟尿嘧啶(Fluorouracil,5-FU疵大鼠血液和肝脏 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，分别在不同时间釆集血液和肝脏组织样木，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 】R730.5 】A 】2095-1752 ( 2012) 29-0102-03 Distribution of 5-FU in rat plasma and liver tissue. HU Xiarong 1,ZHENG Jingleil, WANG Zaiguol,LIANG Lijian2,ZHONG Muyil,UN Zhiqiangl, YU WushenglDENG Runshul, YE Zhenweil,LIANG Zijunl (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 power to liver is strong. Key words