JOURNAL OF ISOTOPES

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The Acute Toxicity and Pharmacokinetics of the BSH

LI Feng-lin;LUO Zhi-fu;FAN Cai-yun;LIU Zi-hua;DENG Xin-rong   

  1. the Department of Isotopes, China Institute of Atomic Energy, Beijing 102413, China
  • Online:2016-08-20 Published:2016-08-10

巯基十二硼烷二钠盐的急性毒性与药代动力学研究

李凤林;罗志福;樊彩云;刘子华;邓新荣   

  1. 中国原子能科学研究院 同位素研究所,北京102413

Abstract:

In this study, the acute toxicity of BSH was studied at doses of 210, 300, 430, 614 mg/kg, and the LD50 was calculated at 381.94 mg/kg. A three-compartment model system was used to evaluate the pharmacokinetics of the BSH, and the pharmacokinetic parameters, such as t1/2,Vd, AUC, CL of BSH were calculated: t1/2α=3.6 min, t1/2β=55.8 min, t1/2γ=6.26 h, Vd=3 523.58 mL/kg, AUC= 247.55 hr*μg/mL,  CL=3572.45 mL/hr/kg. The biodistribution of the BSH was studied in normal mice, from which the characteristics of biodistribution of BSH was analyzed.

Key words: BNCT, BSH, acute toxicity, pharmacokinetics, biodistribution

摘要:

本研究采用210、300、430、614 mg/kg四个剂量对巯基十二硼烷二钠盐(BSH)进行了急性毒性实验,得到其半数致死量(LD50)为381.94 mg/kg,LD50的95%置信区间为[334.97 mg/kg,435.51 mg/kg]。进行BSH的药代动力学初步研究,根据给药后得到的药时曲线,选用三房室模型拟合得到BSH的半衰期分别为t1/2α=3.6 min、t1/2β=55.8 min、t1/2γ=6.26 h;表观分布容积Vd为3 523.58 mL/kg、药时曲线面积AUC为247.55 hr*μg/mL、清除率CL为3 572.45 mL/hr/kg。在小鼠体内的生物分布结果表明,BSH在血液中清除较快,各器官在注射后30 min达到最大摄取,其在体内主要通过肾脏排泄。以上研究结果可为BSH在国内临床应用的安全性提供实验基础。

关键词: BNCT, BSH, 急性毒性, 药代动力学, 生物分布