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目的研究131I-3H11不同给药途径的药代动力学。方法将家兔分为3组,即耳静脉、门静脉和腹腔注射组,按4.44MBq/kg体重注射131I-3H11。给药后固定时刻抽取耳静脉血、门静脉血及腹腔液并检测其放射性药物的含量。结果(1)耳静脉给药后,门静脉与外周静脉血内药物浓度没有明显差别;(2)门静脉给药30min后,门静脉与外周静脉血没有明显差别;(3)腹腔给药后,腹腔液中的药物浓度始终保持最高,其峰值浓度分别是外周静脉和门静脉血的37.2倍和5.4倍;门静脉血药物浓度次之,峰值浓度是外周静脉血的6.9倍,至24h仍达1.8倍。结论131I-3H11腹腔给药具有高选择性区域导向治疗的药代动力学特点。腹腔液中高浓度的导向药物主要经门静脉吸收进入肝脏,保持了腹腔、门静脉和肝脏内持久恒定高浓度的导向治疗药物,有利于预防和治疗胃肠癌术后腹腔内复发和肝转移。
Objective To study the pharmacokinetics of 131I-3H11 in different routes of administration. Methods Rabbits were divided into 3 groups, namely, ear vein, portal vein and intraperitoneal injection group, and 131I-3H11 was injected according to 4.44MBq / kg body weight. After administration, ear vein, portal vein blood and peritoneal fluid were extracted at a fixed time and the contents of radiopharmaceuticals were measured. Results (1) There was no significant difference in drug concentration between portal vein and peripheral venous blood after intravenous administration; (2) There was no significant difference between portal vein and peripheral venous blood after 30min portal vein administration; (3) After intraperitoneal administration, The peak concentration was 37.2 times and 5.4 times higher than the peripheral venous and portal venous blood, followed by the portal venous blood drug concentration, the peak concentration was 6.9 times that of peripheral venous blood and reached 1.8 times of 24h. Conclusion The 131I-3H11 intraperitoneal administration has the pharmacokinetic characteristics of high selective area-directed therapy. Peritoneal fluid in the high concentration of lead-based drugs mainly through the portal vein into the liver, to maintain the peritoneal, portal vein and liver long-lasting high concentration of targeted therapy is conducive to the prevention and treatment of gastrointestinal cancer after intraperitoneal recurrence and liver metastases.