Study of Pharmacokinetic Properties for <sup>99m</sup>Tc-MAG<sub>3</sub>-ASON

HUANG Jiajun; et al

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Study of Pharmacokinetic Properties for ^99mTc-MAG₃-ASON

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- Study of Pharmacokinetic Properties for ^99mTc-MAG₃-ASON
- Journal of Chongqing Medical University Issue 3, Pages: 366-368(2006)
- 作者机构：
  
  1. 重庆医科大学基础医学院药理学教研室
  2. 重庆医科大学核医学教研室
  3. 贵州省人民医院
  5. ,贵阳,550001
- 作者简介：
- 基金信息：
- DOI：
  CLC： R96
- Published：2006，
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[1]黄家君,董孟杰,谢娟,李少林.~(99m)Tc-MAG_3-ASON药代动力学研究[J].重庆医科大学学报,2006(03):366-368.

HUANG Jiajun, et al. Study of Pharmacokinetic Properties for ^99mTc-MAG₃-ASON. [J]. Journal of Chongqing Medical University (3):366-368(2006)
[1]黄家君,董孟杰,谢娟,李少林.~(99m)Tc-MAG_3-ASON药代动力学研究[J].重庆医科大学学报,2006(03):366-368. DOI：

HUANG Jiajun, et al. Study of Pharmacokinetic Properties for ^99mTc-MAG₃-ASON. [J]. Journal of Chongqing Medical University (3):366-368(2006) DOI：

摘要

目的:研究99mTc标记的MAG3-ASON螯合物的药代动力学特征。方法:制备99mTc-MAG3-ASON螯合物;随后用放射性计数法测定其半衰期

用3P97软件求出其分布半衰期、消除半衰期、中央室分布容积、总表观分布容积、总清除率;最后用三氯醋酸法测定其血浆蛋白结合率。结果:99mTc-MAG3-ASON的分布半衰期是2.11min;消除半衰期是95.19min;中央室分布容积是114.9ml;总表观分布容积是2430.8ml;总清除率是17.7ml/min。与人血浆孵育1.5h后

血浆蛋白结合率为11.82%。结论:99mTc-MAG3-ASON螯合物在体内的转运过程符合二室模型

其良好的药代动力学特征

可望用于肿瘤的显像诊断和治疗。

Abstract

Objective: To study the pharmacokinetic properties of 99mTc-labeled chelic polymer of MAG3-ASON.Methods: Chelic polymer of 99mTc-MAG3-ASON was prepared according to former methods.Subsequently

this chelic polymer change of concentration was determined by radioactivity counts per minute(CPM)

and its half-life of distribution(T1/2α)

the half-life of elimination(T1/2β)

the central compartment volume of distribution(Vc)

the total apparent volume of distribution(Vd) and the total rate of clearance(CL) were calculated by means of 3P97 software.Finally

its rate of binding to serum protein was measured by trichloroacetic acid precipitation.Results: The T1/2α

the T1/2β

the Vc

the Vd and the CL were 2.11min

95.19min

114.9ml

2430.8ml and 17.7ml/min

respectively.After being incubated with fresh human serum for 1.5h

its rate of binding to serum protein was 11.82%.Conclusion: The process of transportation for chelic polymer of 99mTc-MAG3-ASON in vivo is consistent with two-compartment model and it has desirable pharmacokinetic properties.Therefore

it may be used for diagnostic imaging and therapy of cancer.

关键词

药代动力学半衰期反义寡核苷酸（ASON）巯基乙酰三甘氨酸（MAG3）99mTc-MAG3-ASON

Keywords

pharmacokineticsHalf-lifeAntisense oligonucleotide(ASON)Mercaptoacetylglycylglycylglycine(MAG3)99mTc-MAG3-ASON

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Study of Pharmacokinetic Properties for 99mTc-MAG3-ASON

DOI：

摘要

Abstract

关键词

Keywords

references

Study of Pharmacokinetic Properties for ^99mTc-MAG₃-ASON