【摘要】 目的:观察研究5-氟尿嘧啶腹腔、静脉和灌胃三种给药途径化疗的优劣。方法:采用高效液相色谱法比较研究了家兔5-氟尿嘧啶腹腔、静脉和灌胃化疗三种给药途径的药代动力学。结果:大剂量腹腔给药能在腹腔、门静脉及肝脏提供高浓度药物,且维持时间较长,腹腔液和门静脉的消除半衰期(T_1/2β)分别为3.81±0.14 h 和1.28±0.09 h,而周围血药浓度极低,腹腔液及门静脉药峰浓度分别为股静脉的206倍和6.7倍。静脉给药周围血药浓度及门静脉血药浓度均较高,但有效血药浓度维持时间短,T_1/2β分别为0.71±0.02 h 和0.67±0.04 h。灌胃给药后,腹腔液药浓度极低,门静脉血药浓度虽然高于周围血,但吸收极不规则,个体差异较大。组织中药浓度测定发现,腹腔给药后,肝脏中的药浓度最高,肾脏浓度最低,而静脉给药则肾脏浓度最高。结论:这些药代动力学特点提示,对胃肠道恶性肿瘤术后腹腔内复发和肝转移的防治,腹腔化疗将远较传统的静脉化疗和口服给药为优。是一种较为理想的术后辅助化疗措施,可作为一种常规措施用于胃肠道肿瘤术后化疗。更多还原

【Abstract】 Objective:The aim of this experiment was to observe the effects of intraperitoneal（ip）, intraveinous（iv）and intragastric（ig）administration.Methods:Pharmacokinetic comparison of 5-fluo- rouracil（5-Fu）administerd ip,iv and ig was made in rabbits by HPLC method.Results:ip administra- tion of 5-Fu could maintain high,stable and sustained concetrantion in the peritoneal cavity,portal vein and liver while sparing the systemic blood.T_1/2β was 3.81±0.14 h and 1.28±0.09 h respectively.Af- ter iv administration of 5-Fu,drug concentration in systemic blood and portal vein was very high.Sustain- men of concentration was relatively of short duration.T_1/2β was 0.71±0.02 h and 0.67±0.04 h re- spectively.After iv administration the concentration of 5-Fu in portal vein was higher than that in ststemic blood.But absorption of 5-Fu was irregular.There was a high difference in the individuals.Conclusion: ip chemotherapy has a significant pharmacokinetic advantage over the convention iv and ig routes after surgery for gastrointestinal malignancies.更多还原