天麻素是天麻主要活性成分之一,具有镇静、安眠和镇痛等中枢神经抑制作用。临床用于治疗神经衰弱、神衰综合征及血管神经性头痛等疾病。本实验报告~3H-天麻素在小鼠体内的吸收,分布和消除。 ~3H-天麻素用化学还原法标记,比放射性4.57Ci/mM,放化纯度>95%。给药时加入未标记天麻素,剂量为50mg/kg。给小鼠灌服~3-天麻素后,放射性从胃肠道消失很快。2小时胃肠道放射性仅存剂量的5.2%。血中放射性上升很快,t_(1/2a)。仅6分钟。血中放射性在1小时前后维持较高水平,与小鼠镇静作用时间一致。消除半衰期静注为4.44小时,口服为7.47小时。放射性在体内分布以肾最高,其次为肝、肺、心、脾及脑。放射性能透过血脑屏障,但在脑中变化与血不一致。放射性主要从尿中排出。灌胃后24小时从尿、粪及胆汁排出的总放射性为给药剂量的76.8%,其中尿排出97%。尿中放射性排出主要在前2小时。胆汁和粪排 Gastrodin is one of the main active ingredients of Gastrodia elata, which has central nervous inhibitory effects such as sedation, hypnosis and analgesia. Clinical treatment of neurasthenia, Shen Su syndrome and vascular neuropathic headache and other diseases. The experiment reported 3H-gastrodin absorption, distribution and elimination in mice. ~ 3H-gastrodin labeled with chemical reduction method, specific radioactivity 4.57Ci / mM, radiochemical purity> 95%. Unpublished gastrodin was added at the time of administration at a dose of 50 mg / kg. Giving mice 3 ~ gastrodin, radioactive disappeared rapidly from the gastrointestinal tract. 2 hours The only remaining dose of gastrointestinal radioactivity 5.2%. Radioactive blood rose rapidly, t_ (1 / 2a). Only 6 minutes. Blood radioactivity in the 1 hour before and after maintaining a high level, consistent with the time of sedation in mice. The elimination half-life was 4.44 hours for intravenous injection and 7.47 hours for oral administration. Radiation distribution in the body to the highest kidney, followed by liver, lung, heart, spleen and brain. Radiation penetrates the blood-brain barrier, but changes in the brain are not consistent with blood. Radioactivity is mainly excreted from the urine. Total radioactivity discharged from urine, feces and bile at 24 hours after gavage was 76.8% of the dose administered, with 97% of urine excreted. Urinary radioactive discharge mainly in the first 2 hours. Bile and excrement