【摘要】 采用双氧水法对23-羟基白桦酸进行131I标记;以硅胶纸为支持介质,V二氯甲烷:V甲醇=9:1为展开剂,测定标记率及标记物放化纯;ICR小鼠和荷肝癌HepA肿瘤鼠尾静脉注射131I-23-羟基白桦酸(0.74MBq/只)后考察标记物的药代动力学性质及荷瘤鼠体内分布。结果显示,131I-23-羟基白桦酸标记率达98%,其放化纯在1、4、8d分别为98.5%、97.3%、95.8%。131I-23-羟基白桦酸在正常小鼠体内血液清除较快,其药代动力学模型符合二室模型。注射后0.5h荷肝癌HepA肿瘤鼠肝摄取最高(9.14%ID·g-1组织),其次为肾、血、脾、肠、肺、肿瘤,脑中分布最少,仅为0.28%ID·g-1组织;肿瘤/肌肉比值>3。表明碘标23-羟基白桦酸标记率高,标记物稳定;碘标记物在荷肝癌HepA肿瘤鼠中的肿瘤靶向摄取提高2倍,可能是一新型增效的核素靶向治疗药物。更多还原

【Abstract】 In this work, preparation of 131I-labeled 23-hydroxybetulinic acid (131I-23-HBA) and its pharmacokinetics in mice were studied. 23-HBA was labeled with 131I using the hydrogen peroxide method. Purity and stability of the 131I-23-HBA were evaluated by silicon TLC, in which the substratum of Vdichoromethane: Vmethanol =9:1 was used as the developing agent. The dynamic distribution in ICR mice and liver cancer HepA tumor-bearing mice were studied. The results showed that the labeling yield of 131I-23-HBA was 98% and the radiochemical purities were 98.5%, 97.3%, and 95.8% after 1, 4 and 8 days, respectively. In ICR mice, the blood clearance was quick and the profile of the blood concentration-time was fitted with two compartment model. In tumor-bearing mice 0.5 h after intravenous injection, the liver uptake was the highest (9.14% ID·g-1). The radioisotope was concentrated in kidney, blood, spleen, intestine, lung and tumor, too. The brain uptake was the lowest as 0.28% ID/g at pi. 0.5 h. The tumor-to-muscle ratio was over 3. The labeling yield and purity of 131I-23-HBA are high and 131I-23-HBA is stable. The tumor uptake of 131I-23-HBA is higher than 23-HBA. 131I-23-HBA is a potent cancer treatment drug.更多还原