[1]房兆飞,龚丽莎,胡厚源,等.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].第三军医大学学报,2012,34(21):2145-2148.
 Fang Zhaofei,Gong Lisha,Hu Houyuan,et al.Pharmacokinetics of 125I-TAP-SSL5 in normal rabbits[J].J Third Mil Med Univ,2012,34(21):2145-2148.
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《第三军医大学学报》[ISSN:1000-5404/CN:51-1095/R]

卷:
34卷
期数:
2012年第21期
页码:
2145-2148
栏目:
论著
出版日期:
2012-11-15

文章信息/Info

Title:
Pharmacokinetics of 125I-TAP-SSL5 in normal rabbits
作者:
房兆飞龚丽莎胡厚源李前伟曲小龙程彦宋治远张静
第三军医大学西南医院:心血管内科,重庆市介入心脏病学研究所,核医学科
Author(s):
Fang Zhaofei Gong Lisha Hu Houyuan Li Qianwei Qu Xiaolong Cheng Yan Song Zhiyuan Zhang Jing
Department of Cardiology, Department of Nuclear Medicine, Southwest Hospital, Third Military Medical University, Chongqing, 400038, China
关键词:
金黄色葡萄球菌超抗原样蛋白-5蜱抗凝血肽融合蛋白药代动力学放射性核素标记
Keywords:
staphylococcal superantigen like protein-5tick anticoagulant peptidefusion proteinpharmacokinetics radionuclide labeling
分类号:
R817.4; R969.1; R977.6
文献标志码:
A
摘要:
目的      研究125I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Na125I直接标记于TAP-SSL5,由耳缘静脉给每只大耳兔注射18.5×103 kBq的125I-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125I-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(t1/2α)及消除相半衰期(t1/2β) 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(K12)为(6.651±3.642)/h ,二室向一室转运常数(K21)为(4.072±1.737)/h。       结论      125I-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 125I- tick anticoagulant peptide (TAP)-staphylococcal superantigen like protein-5 (SSL5) in normal rabbits.       Methods       TAP-SSL5 was labeled directly with Na125I 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, 3, 5, 10, 30, 60, 120, 240 and 480 min after bolus injection of 18.5 MBq 125I-TAP-SSL5.       Results      The labeling rate and radiochemical purity of 125I-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: t1/2α=(0.08±0.04) h, t1/2β=(4.97±0.75) h, clearance (CL)=0.015±0.011 ml/h, K12=(6.651±3.642)/h, and K21=(4.072±1.737)/h.       Conclusion        The pharmacokinetic of 125I-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.

参考文献/References:

房兆飞, 龚丽莎, 胡厚源, 等. 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]. 第三军医大学学报,2012,34(21):2145-2148.

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更新日期/Last Update: 2012-11-06