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目的建立~(153)Sm 标记聚氨基葡糖的方法,观察其通过尾静脉及肝间质内注射给药后在小鼠体内的生物分布,为进一步用于肿瘤治疗奠定基础。方法将~(153)Sm_2O_3与盐酸在适当的条件下制备成~(153)SmCl_3,然后与聚氨基葡糖螯合生成~(153)Sm-CHICO(~(153)Sm-聚氨基葡糖复合物)。昆明种小鼠90只随机分为3组。1、2组小鼠分别经肝间质注射等活度的~(153)Sm-CHICO 和~(153)SmCl_3,3组小鼠经尾静脉注射~(153)Sm-CHICO,剂量为6.1 MBq/0.05 ml,分别于给药后0.5、1、2、6、24及48 h 各组处死5只,取血及主要脏器测定放射性计数率值,计算每克组织的百分注射剂量率(%ID/g),每组各时间点取1只小鼠行 SPECT 显像。结果~(153)Sm-CHICO 的标记率为(95.6±2.7)%,48 h 放化纯为(89.6±1.9)%。1组小鼠肝间质注射~(153)Sm-CHICO 放射性核素主要浓聚于穿刺点,仅有少量分布于注射点外肝脏、肾脏、脾脏、骨等组织器官。1组小鼠肝间质注射点区(直径5 mm)在48 h 百分注射剂量率均值为27.16%ID/g,为2组注射点的139倍,为3组肝组织百分注射剂量率值的131倍。2组和3组小鼠血2 h 的放射性活度为1组130倍以上,且血中放射性计数在较短时间内快速下降。结论~(153)Sm-CHICO 标记方法简单、可行,具有较高的标记率及较好的稳定性。肝间质注射的~(153)Sm-CHICO 较长时间滞留在注射部位局部较小范围,在注射点以外组织和器官分布较少,血液清除快,~(153)Sm-CHICO 可能成为肿瘤核素内照射治疗的一种新药。
Objective To establish a method of ~ (153) Sm labeled chitosan and observe its biodistribution in mice after injection through the tail vein and intrahepatic interstitial injection, which will lay the foundation for the further treatment of cancer. Methods ~ (153) Sm-CHICO (~ (153) Sm-chitosan was chelated with ~ (153) SmCl_3 by ~ (153) Sm_2O_3 and hydrochloric acid under suitable conditions. Thing). Ninety Kunming mice were randomly divided into three groups. Groups (~ (153) Sm-CHICO and ~ (153) SmCl_3,3) were injected via the tail vein with a dose of 6.1 MBq /0.05 ml, 5, 5, 1, 2, 6, 24 and 48 h after the administration were sacrificed in each group 5, the blood and major organs were measured radioactivity count value, calculated per gram of tissue dose rate % ID / g), each group at each time point to take a SPECT SPECT imaging. Results The labeling rate of ~ (153) Sm-CHICO was (95.6 ± 2.7)% and the radiochemical purity was (89.6 ± 1.9)% after 48 h. In group 1, interstitial injection of ~ (153) Sm-CHICO radionuclides mainly concentrated on the puncture site, with only a small amount distributed in liver, kidney, spleen, bone and other tissues and organs outside the injection site. The average injection dose rate at 1 hour after injection was 27.16% ID / g, which was 139 times of that of the 2 injection groups, which was the dose-per-injection rate of liver in 3 groups 131 times the value. Radioactivity of mice in groups 2 and 3 was 130-fold higher than that in group 1 at 2 h, and the radioactivity in the blood decreased rapidly in a short period of time. Conclusion The ~ (153) Sm-CHICO labeling method is simple and feasible with high labeling efficiency and good stability. The (153) Sm-CHICO injected into the liver interstitially occured for a long time in a small part of the injection site, with less distribution of tissues and organs outside the injection site and faster blood clearance. The (153) Sm-CHICO may become the tumor nucleus A new drug for internal radiation therapy.