【作者】 吕大鹏； 牟阿平； 徐光炜； 张梅颖；

【Author】 Lu Dapeng, Xu Guangwei, Zhang Meiying et al. Beijing Institute for Cancer Reserach, 100036

【机构】 北京铁路总医院； 北京肿瘤医院；

【摘要】 本研究把传统的外周静脉给药、门静脉给药与腹腔给药的药代动力学进行比较研究,证实腹腔内应用导向药物治疗胃肠癌的合理性。方法家兔12只,经门静脉和腹腔置管后分为3组, 即耳静脉、门静脉和腹腔注射组,注射¹³¹I—3H11 120μci／kg体重。分别于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;腹腔液内药物浓度仅为血液内的35.5％;（2）门静脉给药后,即刻门静脉血内药物浓度明显高于外周围静脉内药物浓度,30分钟后,门静脉与外周静脉血没有明显差别,腹腔液内药物浓度为血液内的34.1％;（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5.36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24小时仍达1.8倍;外周静脉血内药物浓度从始至终保持在较低水平,至 24小时,仅为腹腔液内的1／3。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,这些药代学特性保持了腹腔、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。更多还原

【Abstract】 In order to identify the rationality of RIT by I. P., we compare the pharma cokinetics of ¹³¹I—3H11 after intraperitoneal, intraportal and intraveinal administrations. Meth otis Twelve rabbits were operated to place plastic vessels in portal vein and abdominal cavity. Then they were divided into 3 groups and injected ¹³¹I—3H11 120μci/kg by ear vein, portal vein and peritoneal cavity respectively. In regular times, the blood was acquired from ear vein, portal vein and peritoneal cavity and was tested for the ¹³¹I—3H11 content. Results （1） The ¹³¹I— 3H11 content in ear and portal veins was same in ear vein injection group. The ¹³¹I—3H11 con tent in peritoneal cavity was 35.5％ of those in the ear and portal veins. （2） At zero time, the ¹³¹ I—3H11 content in portal vein was higher than in ear vein in portal injection group. Thirty min utes later, the ¹³¹I—3H11 content in ear and portal veins was same. The ¹³¹I—3H11 content in peritoneal cavity was the same as that of the ear vein injection group. （3） In peritoneal cavity in jection group, at zero time the ¹³¹I—3H11 content in peritoneal cavity was higher than ear and portal veins （37.2 and 5.4 times respectively）. Twenty—four hours later, it was still i. 7 and 3. 0 times respectively. The ¹³¹I—3H11 content in portal vein was 6.9 times as it was in ear vein; 24 hours later, it was 1.8 times. Conclusion The results indicated that there are high concen trations of ¹³¹I—3H11 in the abdominal cavity, portal vein and liver, but less enter the systemic circulation after ¹³¹I—SH11 I.P. administration. It shows that there is a significant pharma cokinetic advantage for I.P. over I.V. and intra—portal vein administrations.更多还原