125I-MIL50在大鼠体内的药代动力学及生物分布

doi:10.7538/tws.2016.29.02.0065

摘要/Abstract

摘要：

为探究¹²⁵I标记重组抗蓖麻毒素（Ricin）人源化单克隆抗体（¹²⁵I-MIL50）在大鼠体内的药代动力学、生物分布及排泄特点，采用Iodogen法对MIL50进行¹²⁵I标记，结合TCA法测定不同时间¹²⁵I-MIL50在大鼠血清、组织、体液和排泄物中的含量。结果表明：Ricin染毒组和直接给药组血药浓度在14 d内没有差异，14 d后染毒组¹²⁵I-MIL50消除快于未染毒组；血清中¹²⁵I-MIL50浓度高于其他组织和体液，肾、膀胱组织中浓度较高，脑、脊髓、脂肪等脂性组织中浓度一直较低；¹²⁵I-MIL50给药后27d内经尿累积排泄率约为62.6%，经粪便的排泄率为15.5%。研究结果为临床实验和给药方案提供参考依据。

关键词: 蓖麻毒素, ¹²⁵I-MIL50, 药代动力学, 生物分布, 排泄

Abstract:

In order to study the impact of Ricin on the pharmacokinetics of ¹²⁵I-MIL50 and to investigate the tissue distribution and excretion of ¹²⁵I-MIL50 in Wistar rats, MIL50 was labeled with ¹²⁵I using the Iodogen method. Then, the concentration of ¹²⁵I-MIL50 in serum、tissues、body fluids and excretions was measured by TCA method at different time. The results showed that ¹²⁵I-MIL50 was eliminated faster after 14 days in the Ricin administrated group. The concentration of ¹²⁵I-MIL50 in serum was always higher than that in other tissues. The level in kidney and bladder were high and in brain, spine and fat were low. The cumulative excretion rate of ¹²⁵I-MIL50 was 62.6% in urine, and 15.5% in feces within 27 days. Ricin could fasten the elimination of ¹²⁵I-MIL50 when the concentration of ¹²⁵I-MIL50 was low in Wistar rats. It might because of the interaction between antigen and antibody. ¹²⁵I-MIL50 had no specific combination with tissues and it could hardly entered into lipophilic tissues. Urinary excretion represented the major pathway of elimination of ¹²⁵I-MIL50. The results of the study provide a reference for clinical trials and drug administration program.

Key words: Ricin, ¹²⁵I-MIL50, pharmacokinetics, biodistribution, excretion

雷晓;朱晓霞;王德才;孟志云;甘慧;顾若兰;吴卓娜;郑颖;李俭;吕明;窦桂芳. ¹²⁵I-MIL50在大鼠体内的药代动力学及生物分布[J]. 同位素, 2016, 29(2): 65-70.

LEI Xiao;ZHU Xiao-xia;WANG De-cai;MENG Zhi-yun;GAN Hui;GU Ruo-lan;WU Zhuo-na;ZHENG Ying;LI Jian;Lv Ming;DOU Gui-fang. Pharmacokinetics and Biodistribution of ¹²⁵I-MIL50 in Wistar Rats[J]. Journal of Isotopes, 2016, 29(2): 65-70.

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¹²⁵I-MIL50在大鼠体内的药代动力学及生物分布

Pharmacokinetics and Biodistribution of ¹²⁵I-MIL50 in Wistar Rats

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