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小鼠灌胃3H-β,β-二甲基丙烯酰紫草素后放射活性的组织分布与排泄研究

Tissue distribution and excretion of radioactivity in mice after intragastric administration of 3H-beta, beta-dimethylacrylshikonin

    摘要
  • 摘要: 摘要：采用氧化燃烧炉技术处理小鼠灌胃给予3H-β,β-二甲基丙烯酰紫草素后的组织、粪样（尿样直接加闪烁液测定），用液闪计数仪测定其放射性水平，并采用HPLC 技术分析生物样品，以研究其放射性在小鼠体内的组织分布与排泄情况。研究结果显示，胃肠道放射性浓度最高，肝脏、肺脏、肾脏、心脏等组织内放射性浓度次之，骨骼肌、脊髓、脑中分布较少；小鼠灌服 3H-β,β-二甲基丙烯酰紫草素（84mg/kg，22.3MBq/kg）后336h从粪中收集到给药总放射剂量的（72.879.92）%，尿液中回收到（6.810.18）%，粪尿合计（79.68±0.18）%；小鼠粪便中以原形药物为主，血浆、尿样中均未检测到原形药物。上述结果提示，3H-β,β-二甲基丙烯酰紫草素在小鼠体内分布广，排泄较完全，经粪便排泄为主，经肾排泄为辅。

     

    Abstract: Abstract: Tissue distribution and excretion of radioactivity in mice after intragastric administration of 3H-beta, beta-dimethylacrylshikonin were investigated. Tissues and feces were combusted by sample Oxidizer, the subsequent radioactivity measurements were carried out after addition of scintillator to the combusted samples and urine. The results showed that the radioactivity in gastrointestinal system was higher than that in the liver, lung, kidney and heart, while that in skeletal muscle, spinal cord, brain was low. After single intragastric administration (chemical dose 84mg/kg，radioactive dose 22.3MBq/kg) of beta, beta-dimethylacrylshikonin to mice, the cumulative radioactivity rate of urine and feces were（6.810.18）% and（72.879.92）% respectively within 336h, the total excretion rate was（79.68±0.18）%. The plasma, feces and urine were analyzed by HPLC, the results showed that parent drug mainly existed in feces, no parent drug was detected in plasma and urine. The results showed that 3H-beta, beta-dimethylacrylshikonin was distributed widely in mice, and was excreted mainly by fecal route and secondarily via urine.

     

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