5-氟尿嘧啶白及微球家兔肾动脉栓塞后体内药代动力学研究

Pharmacokinetics of 5-Fu Bletilla Microspheres Following Renal Arterial Embolization in Rabbits

以常规 5 -氟尿嘧啶 ( 5 - Fu)注射液为对照品 ,研究了 5 - Fu白及微球家兔肾动脉栓塞后体内药代动力学过程。血药 5 - Fu浓度采用反相高效液相色谱法 ,所得血药浓度数据用 3 P87药代动力学程序处理。实验结果 :5 - Fu白及微球体内过程符合二室模型 ,t1 /2 a ( 6.2 7± 6.10 ) min,t1 /2β ( 2 0 3 .6± 97.5 ) m in,Cm ax( 4 .8± 1.9) μg/ml。t1 /2 a,t1 /2β均比注射剂明显延长 ( P<0 .0 1)。表明微球剂型具有靶向制剂长效、高效、低毒的特点。

A pharmacokinetic study on 5-Fu Bletilla Microspheres was carried out following renal arterial embolization in 7 rabbits, with 5-Fu injection as controls. The concentration of 5-Fu in serum was determined by reversed phase HPLC and the data were treated with 3P87 programme. The results showed that both the microspheres and the injection met two-compartment model in vivo, the t 1/2a , t 1/2β and Cmax of 5-Fu microspheres were (6 27±6 10) min, (203 6±97 5) min and (4 8±1 9) μg/ml respectively. t 1/2a and t 1/2β of 5-Fu microspheres were prolonged obviously as compared with control group (P<0 01), suggesting microspheres were characterized by long-term and high efficacy and low toxicity.