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。
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 （T1/2 α ）, the half-life of elimination （T1/2 β）, 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 T1/2 α, the T1/2 β, the Vc, the Vd and the CL were 2.1 lmin, 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.
出处
《重庆医科大学学报》
CAS
CSCD
2006年第3期366-368,共3页
Journal of Chongqing Medical University
基金
国家自然科学基金资助课题(30070230)
