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125I示踪法检测西夫韦肽在生物体内的代谢过程

Determination of Sifuvirtide Concentration by 125I Tracer Labeling Method

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【作者】 刘德胜宋敏窦桂芳栾海云王垣芳张树平李庆忠

【Author】 LIU De-sheng~1,SONG Min~1,DOU Gui-fang~2,LUAN Hai-yun~1,WANG Yuan-fang~1,ZHANG Shu-ping~1,LI Qing-zhong~1(1.Department of Pharmacology of Binzhou Medical College,Binzhou 264003,China;2.Institute of Transfusion Medicine,Beijing 100850,China)

【机构】 滨州医学院药理教研室军事医学科学院野战输血研究所滨州医学院药理教研室 山东滨州256603山东滨州256603北京100850

【摘要】 采用Iodogen法标记了西夫韦肽(Sifuvirtide),并用S-100 HR凝胶柱分离纯化标记物1。25I-sifuvirtide放化纯度>99.0%,比活度为3.9 GBq.g-1;标记后的蛋白仍具有一定的生物活性。三氯醋酸(TCA)沉淀法测定125I-sifuvirtide在生物样品中含量:血浆中125I-sifuvirtide的放射性活度为286.5~26 125.5 Bq.mL-1时,125I-sifuvirtide的放射性计数和沉淀放射性计数的线性相关系数为0.999 8±0.000 5,回收率为72.3%±6.9%。猕猴静脉和皮下推注125I-sifuvirtide后,血浆TCA酸沉放射性浓度时间曲线符合二房室模型;皮下给药后平均消除半衰期为95.83 h,达峰时间平均为3.35 h,平均绝对生物利用度为85.2%。

【Abstract】 125I-sifuvirtide is prepared by Iodogen method,the radiochemical purity of 125I-sifuvirtide is over 99.0%,and the specific activity of 125I-sifuvirtide is 3.9 GBq·g-1.The labeled product still maintain some biological activity.The radioactivity in plasma is determined by trichloroacetic acid precipitation method.The pharmacokinetics of 125I-sifuvirtide is successfully modeled using two-compartmental after subcutaneous(SC) or intravenous(IV) administration in rhesus monkeys according to the curve of radioactivity of TCA precipitable vs time.The mean half-life(t1/2) value is 95.83 h,the mean time to maximum concentration is 3.35 h,and the mean bioavailability is 85.2% after SC administration.

  • 【分类号】R96
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