23-羟基白桦酸的碘标记及其在荷肝癌HepA肿瘤鼠体内的分布

杨敏; 王广基; 徐宇平; 潘栋辉; 王颂佩; 李晓敏; 唐婕; 罗世能

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23-羟基白桦酸的碘标记及其在荷肝癌HepA肿瘤鼠体内的分布

核化学、放射性药物和核医学 | 更新时间：2021-03-12

- 23-羟基白桦酸的碘标记及其在荷肝癌HepA肿瘤鼠体内的分布
- Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice
- 核技术 2008年31卷第8期
- 作者机构：
  
  1. 江苏省原子医学研究所,卫生部核医学重点实验室
  2. 中国药科大学
- 作者简介：
- 基金信息：
  
  (No.ZX069);(No.ZX069);(No.ZX069)
- DOI：
  中图分类号： R735.7;R817.9
- 纸质出版日期：2008-08-01
- 稿件说明：
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[1]杨敏,王广基,徐宇平,潘栋辉,王颂佩,李晓敏,唐婕,罗世能.23-羟基白桦酸的碘标记及其在荷肝癌HepA肿瘤鼠体内的分布[J].核技术,2008,31(08):637-640.

YANG Min1 WANG Guangji2 XU Yuping1 PAN Donghui1 WANG Songpei1 LI Xiaomin1 TANG Jie1 LUO Shineng1 1. Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice[J]. Nuclear techniques, 2008, 31(8): 637-640.
[1]杨敏,王广基,徐宇平,潘栋辉,王颂佩,李晓敏,唐婕,罗世能.23-羟基白桦酸的碘标记及其在荷肝癌HepA肿瘤鼠体内的分布[J].核技术,2008,31(08):637-640. DOI：

YANG Min1 WANG Guangji2 XU Yuping1 PAN Donghui1 WANG Songpei1 LI Xiaomin1 TANG Jie1 LUO Shineng1 1. Preparation of ¹³¹I-23-hydroxybetulinic acid and in vivo evaluations in liver cancer HepA tumor-bearing mice[J]. Nuclear techniques, 2008, 31(8): 637-640. DOI：

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。

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.

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