Pharmacokinetics of <sup>125</sup>I-TAP-SSL5 in normal rabbits

房兆飞; 龚丽莎; 胡厚源; 李前伟; 曲小龙; 程彦; 宋治远; 张静

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Pharmacokinetics of ¹²⁵I-TAP-SSL5 in normal rabbits

更新时间：2026-01-09

- Pharmacokinetics of ¹²⁵I-TAP-SSL5 in normal rabbits
- Journal of Army Medical University Vol. 34, Issue 21, Pages: 2145-2148(2012)
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  CLC： R817.4;R969.1;R977.6
- Published：2012
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房兆飞,龚丽莎,胡厚源,李前伟,曲小龙,程彦,宋治远,张静.125I标记融合蛋白TAP-SSL5在健康大耳兔体内的药代动力学研究[J].陆军军医大学学报(原第三军医大学学报),2012,34(21):2145-2148.

　Fang Zhaofei,Gong Lisha,Hu Houyuan,Li Qianwei,Qu Xiaolong,Cheng Yan,Song Zhiyuan,Zhang Jing.Pharmacokinetics of 125I-TAP-SSL5 in normal rabbits[J].J Amry Med Univ (J Third Mil Med Univ),2012,34(21):2145-2148.
房兆飞,龚丽莎,胡厚源,李前伟,曲小龙,程彦,宋治远,张静.125I标记融合蛋白TAP-SSL5在健康大耳兔体内的药代动力学研究[J].陆军军医大学学报(原第三军医大学学报),2012,34(21):2145-2148. DOI：

　Fang Zhaofei,Gong Lisha,Hu Houyuan,Li Qianwei,Qu Xiaolong,Cheng Yan,Song Zhiyuan,Zhang Jing.Pharmacokinetics of 125I-TAP-SSL5 in normal rabbits[J].J Amry Med Univ (J Third Mil Med Univ),2012,34(21):2145-2148. DOI：

摘要

目的研究

125

I标记的抗炎抗凝双效融合蛋白TAP-SSL5单次静脉注射后在健康日本大耳兔体内的药代动力学过程。方法采用固相氧化法（Iodogen法）将Na

125

I直接标记于TAP-SSL5，由耳缘静脉给每只大耳兔注射18.5×10

kBq的

125

I-TAP-SSL5，分别于注射后1.5、3、5、10、30、60、120、240、480 min采血，称量并测定放射性计数（Counts per minute

cpm），换算为血液放射性浓度，经DAS软件分析得出最佳房室模型及相关药代动力学参数。结果纸层析法测得

125

I-TAP-SSL5的标记率为（67.32±9.91）%，放射化学纯度为（91.62±3.22）%，比活度为（30.2±4.4）TBq/μmol；TAP-SSL5在大耳兔体内的药代动力学过程符合权重为1的二室模型，分布相半衰期（t

1/2α

）及消除相半衰期（t

1/2β

）分别为（0.08±0.04） h 和（4.97±0.75）h，清除率（Clearance

CL）为（0.015±0.011）ml/h，一室向二室转运常数（K

）为（6.651±3.642）/h ，二室向一室转运常数（K

）为（4.072±1.737）/h。结论

125

I-TAP-SSL5在健康大耳兔体内的药代动力学过程符合权重系数为1的二室模型，自体清除率缓慢，可保证与组织有更多的结合几率。

Abstract

Objective To investigate the pharmacokinetics of

125

I- tick anticoagulant peptide (TAP)-staphylococcal superantigen like protein-5 (SSL5) in normal rabbits. Methods TAP-SSL5 was labeled directly with Na

125

I using the idogen method. The best compartment model and its pharmacokinetic parameters were determined in rabbits （n=6） by

measuring the blood radioactive concentrations at 1.5

120

240 and 480 min after bolus injection of 18.5 MBq

125

I-TAP-SSL5. Results The labeling rate and radiochemical purity of

125

I-TAP-SSL5 was (67.32±9.91)% and (91.62±3.22)% respectively. The specific activity was (30.2±4.4) TBq/μmol. TAP-SSL5 showed two compartment model in rabbit

the main parameters of pharmacokinetics were as follows: t

1/2α

=（0.08±0.04） h

1/2β

=（4.97±0.75） h

clearance （CL）=0.015±0.011 ml/h

=(6.651±3.642)/h

and K

=(4.072±1.737)/h. Conclusion The pharmacokinetic of

125

I-TAP-SSL5 fits the two compartment model (weight coefficient =1) in normal rabbits. Its clearance is low

which ensures more chance to combine with tissues．

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Pharmacokinetics of 125I-TAP-SSL5 in normal rabbits

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Pharmacokinetics of ¹²⁵I-TAP-SSL5 in normal rabbits