^(131)I-3H11经不同途径给药的药代动力学比较研究

Comparative study on pharmacokinetics of ^(131)I-3H11 by different administration paths

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 explore the pharmacokinetics of 131I 3H11 by different administration paths.Methods Twelve rabbits were divided into 3 groups and received 131I 3H11 4 44 MBq/kg by ear vein, portal vein and peritoneal cavity respectively. In regular times, the blood was acquired from ear vein and portal vein, and the peritoneal fluid from peritoneal cavity. The samples were tested for the 131I 3H11 content.Results (1)131I 3H11 content of ear and portal veins was same in ear vein injection group. (2)In portal injection group, thirty minutes later,131I 3H11 content of ear and portal veins was same.(3)In peritoneal cavity injection group, at zero time,131I 3H11 content of peritoneal fluid was higher than that of ear and portal veins (37 2 and 5 4 times respectively). Twenty four hours later, it was still 1 7 and 3 0 times respectively.131I 3H11 content of portal vein was 6 9 times as that of ear vein; 24 hours later, it was still 1 8 times. Conclusions There are high concentrations of 131I 3H11 in the abdominal cavity, portal vein and liver, but low content in the systemic circulation after 131I 3H11 intraperitoneal administration. It was showeds that there is a significant pharmacokinetical advantage for intraperitoneal administrations over intravenous and intraportal veinous ones.