巯基十二硼烷二钠盐的急性毒性与药代动力学研究  

The Acute Toxicity and Pharmacokinetics of the BSH

作　　者：李凤林[1] 罗志福[1] 樊彩云[1] 刘子华[1] 邓新荣[1] 

机构地区：[1]中国原子能科学研究院同位素研究所,北京102413

出　　处：《同位素》2016年第3期164-169,共6页Journal of Isotopes

摘　　要：本研究采用210、300、430、614mg/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381.94mg/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=3.6min、t1/2β=55.8min、t1/2γ=6.26h;表观分布容积Vd为3 523.58mL/kg、药时曲线面积AUC为247.55hr*μg/mL、清除率CL为3 572.45mL/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30min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。In this study,the acute toxicity of BSH was studied at doses of 210,300,430,614mg/kg,and the LD50 was calculated at 381.94mg/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=3.6min,t1/2β=55.8 min,t1/2γ=6.26 h,Vd=3 523.58 mL/kg,AUC= 247.55hr＊μg/mL,CL=3 572.45mL/hr/kg.The biodistribution of the BSH was studied in normal mice,from which the characteristics of biodistribution of BSH was analyzed.

关 键 词：BNCT BSH 急性毒性 药代动力学 生物分布 

分 类 号：R817[医药卫生—影像医学与核医学]