摘要
采用氧化燃烧炉技术处理小鼠给予3H-β，β-二甲基丙烯酰紫草素灌胃后的组织样品和粪样（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法分析生物样品，以研究放射性药物在小鼠体内的组织分布与排泄情况。研究结果显示：小鼠的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（84．0mg／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（8．43±0．26）％，粪尿回收合计（81．30±9．79）％；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。以上结果提示，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。
Tissue distribution and excretion of radioactivity in mice after intragastric administration of 3H-β,β-dimethylacrylshikonin were investigated. Tissues and feces were eombusted by sample Oxidizer, the subsequent radioactivity measurements were carried out af-ter 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 lower. After single intragastric administration （chemical dose 84.0 mg/kg,radioactive dose 22.3 MBq/kg） of β,β-dimethy- lacrylshikonin to mice, the cumulative radioactivity excretion rate of urine and feces were （8.43±0.26）% and （72.87±9.92）% respectively within 336 h , the total excretion rate was（81. 30± 9. 79）%. The samples of plasma, feces and urine were also analyzed by HPLC. The rsult is that parent drug mainly existed in feces, not in plasma or urine. This study showed that 3H-β,β-dimethylacrylshikonin was distributed widely in mice, and excreted mostly through fecal route and secondarily via urine.
出处
《同位素》
CAS
北大核心
2008年第4期209-214,共6页
Journal of Isotopes
