正电子计算机断层显像骨显像剂氟化钠的药动学和显像效果研究

郭飞虎, 陈雪祺, 刘萌, 徐晓敏, 冯婷婷, 黄宪男, 杜建冬, 姜华, 成伟华, 吴建爽, 王成龙, 李艳涛, 梁巍, 王荣福, 樊红强, 张春丽

中国药学杂志 ›› 2019, Vol. 54 ›› Issue (16) : 1317-1322.

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中国药学杂志
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中国药学杂志 ›› 2019, Vol. 54 ›› Issue (16) : 1317-1322. DOI: 10.11669/cpj.2019.16.007
论著

正电子计算机断层显像骨显像剂氟化钠的药动学和显像效果研究

  • 郭飞虎1, 陈雪祺2, 刘萌2, 徐晓敏1, 冯婷婷1, 黄宪男1, 杜建冬1, 姜华1, 成伟华1, 吴建爽1, 王成龙1, 李艳涛1, 梁巍1, 王荣福2,3, 樊红强1*, 张春丽2*
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Pharmacokinetics and Imaging Effect of PET Bone Imaging Agent Sodium Fluoride

  • GUO Fei-hu1,CHEN Xue-qi2, LIU Meng2, XU Xiao-min1, FENG Ting-ting1, HUANG Xian-nan1, DU Jian-dong1, JIANG Hua1, CHENG Wei-hua1, WU Jian-shuang1, WANG Cheng-long1, LI Yan-tao1, LIANG Wei1, WANG Rong-fu2,3, FAN Hong-qiang1*, ZHANG Chun-li2*
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摘要

目的 氟化钠是一种正电子计算机断层显像(PET)骨显像剂,主要用于诊断成骨活性有改变的病灶。本实验旨在考查氟化钠的药动学性质,并通过PET显像研究其诊断效果。方法 首先制备氟化钠注射液,并对其进行质量控制,然后研究其在新西兰兔体内的血液清除情况和血浆蛋白结合率,进行氟化钠PET和99Tcm-MDP SPECT显像的随机对照试验,并对显像效果进行比较。结果 制备了氟化钠注射液,检验结果均符合质控要求。氟化钠在血液中清除相半衰期为37 min,在体内的清除率(CL)为56 mL·min-1·kg-1,血浆蛋白结合率为0.57%。2种显像方式均可见全身骨骼,但氟化钠PET显像给药后30 min就可获得良好的显像效果,骨骼部位显示更为清晰,骨骼部位与肌肉的放射性摄取比明显高于99Tcm-MDP。结论 氟化钠PET骨显像性能优于99Tcm-MDP SPECT,本实验为氟化钠PET用于骨显像的临床应用提供了实验依据。

Abstract

OBJECTIVE Sodium fluoride is a radioactive diagnostic agent for positron emission tomography (PET) indicated for imaging of bone to define areas of altered osteogenic activity. To investigate the pharmacokinetic properties of sodium fluoride, and to study its diagnostic effects by PET imaging. METHODS This study was focused on the preparation and the quality control of sodium fluoride injection, the blood clearance and plasma protein binding rate of sodium fluoride in New Zealand rabbits, the randomized controlled trial of sodium fluoride PET and 99Tcm-MDP SPECT imaging, and comparing of the imaging results. RESULTS Sodium fluoride was prepared, the test results conformed to the requirements of the quality control. The half-life of blood clearance phase was 37 min, the clearance rate in the body was 56 mL·min-1·kg-1, and the plasma protein binding rate was 0.57%. From both sodium fluoride PET and 99Tcm-MDP SPECT imaging, the whole body skeleton were visible. However, it only took 30 min for sodium fluoride to present excellent imaging with clearer bone after administration. The radioactive uptake ratio (T/NT) of sodium fluoride between the bone and the muscle was significantly higher than the T/NT of 99Tcm-MDP.CONCLUSION Sodium fluoride PET is superior to 99Tcm-MDP SPECT for bone imaging. This study provides an experimental basis for the clinical application of sodium fluoride PET in the bone imaging.

关键词

正电子计算机断层显像 / 骨显像 / 氟化钠 / 药动学 / 药效学

Key words

positron emission tomography / bone imanging / sodium fluoride / pharmacokinetics / pharmacodynamics

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郭飞虎, 陈雪祺, 刘萌, 徐晓敏, 冯婷婷, 黄宪男, 杜建冬, 姜华, 成伟华, 吴建爽, 王成龙, 李艳涛, 梁巍, 王荣福, 樊红强, 张春丽. 正电子计算机断层显像骨显像剂氟化钠的药动学和显像效果研究[J]. 中国药学杂志, 2019, 54(16): 1317-1322 https://doi.org/10.11669/cpj.2019.16.007
GUO Fei-hu,CHEN Xue-qi, LIU Meng, XU Xiao-min, FENG Ting-ting, HUANG Xian-nan, DU Jian-dong, JIANG Hua, CHENG Wei-hua, WU Jian-shuang, WANG Cheng-long, LI Yan-tao, LIANG Wei, WANG Rong-fu, FAN Hong-qiang, ZHANG Chun-li. Pharmacokinetics and Imaging Effect of PET Bone Imaging Agent Sodium Fluoride[J]. Chinese Pharmaceutical Journal, 2019, 54(16): 1317-1322 https://doi.org/10.11669/cpj.2019.16.007
中图分类号： R969.1   

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