5-氟尿嘧啶不同容量腹腔化疗的药代动力学及活性炭应用对其的影响

目的　探讨不同药物浓度及缓释剂应用对 5 氟尿嘧啶 (5 Fu)药代动力学的影响。方法　以家兔为模型 ,用高效液相色谱法 ,检测相同 5 Fu剂量下 (10 0mg/kg) ,大容量腹腔化疗、小容量腹腔化疗、小容量缓释腹腔化疗 (加入活性炭 )在不同时间点的药物浓度 ,计算药代动力学参数。结果　大容量腹腔化疗峰浓度 69.75 3mg/L ,半衰期 0 .80 1h。小容量腹腔化疗峰浓度略低大容量腹腔化疗 60 .3 65mg/L ,半衰期 1.10 8h ,作用时间较长。小容量缓释腹腔化疗 ,虽然浓度较小2 0 .693mg/L ,但半衰期 19.10 2h ,作用时间最长。 结论　从药代动力学的角度 ,小容量腹腔化疗是一种较为理想的化疗方式。加入活性炭以后可以更进一步增加药物的作用时间。

Pharmacokinetic comparison of intraperitoneal chemotherapy with 5-Fu in different bulk fluid volumes and the effect of activated carbon particles

Objective To study the pharmacokinetic differences of intraperitoneal infusion with 5-Fu in large bulk fluid (50 ml/kg,first method),small bulk fluid (10 ml/kg,second method) and small bulk fluid plus activated carbon particles (third method).Methods In the rat model,the concentration of 5-Fu was measured in the 3 methods of intraperitoneal chemotherapy by high performance liquid chromatography (HPLC) at a series of given time points.Results The pharmacokinetic parameters,such as Cmax,Tpeak,T_ 1/2(ke) and AUC,were significantly different in statistical analysis.The Cmax of the first method was highest,but the T_ 1/2(ke) was shortest.The Cmax of the second method was slightly lower than the first one,but the T_ 1/2(ke) was longer.Though the Cmax was lowest in the third method,the T_ 1/2(ke) was longest.Conclusion Pharmacokinetic analysis revealed that the intraperitoneal infusion with 5-Fu in small bulk fluid was a better chemotherapy.If activated carbon particles administrated,the intraperitoneal administration can maintain longer.