陆光伟, 邹元杰, 莫启忠. 3H-天麻素在大鼠体内的吸收、分布、代谢和排泄J. 药学学报, 1985, 20(3): 167-172.
引用本文: 陆光伟, 邹元杰, 莫启忠. 3H-天麻素在大鼠体内的吸收、分布、代谢和排泄J. 药学学报, 1985, 20(3): 167-172.
LU Guang-Wei, ZOU Yuan-Jie , MO Qi-Zhong, . KINETIC ASPECTS OF ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF 3H-GASTRODIN IN RATSJ. Acta Pharmaceutica Sinica, 1985, 20(3): 167-172.
Citation: LU Guang-Wei, ZOU Yuan-Jie , MO Qi-Zhong, . KINETIC ASPECTS OF ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF 3H-GASTRODIN IN RATSJ. Acta Pharmaceutica Sinica, 1985, 20(3): 167-172.

3H-天麻素在大鼠体内的吸收、分布、代谢和排泄

KINETIC ASPECTS OF ABSORPTION, DISTRIBUTION, METABOLISM AND EXCRETION OF 3H-GASTRODIN IN RATS

  • 摘要: 大鼠口服3H-天麻素后,胃肠道放射性消失很快,8h仅剩给药后即刻放射性的1.1%。口服后5min血中放射性已有较高水平,50min左右达高峰。静注或口服后,组织放射性均以肾最高。肝、肺、子宫其次。脑中放射性较低,但变化不同于其他组织,2h达高峰。天麻素血浆蛋白结合率为4.3%,其甙元(对羟基苯甲醇)为69.3%。天麻素在体内主要代谢物是甙元。口服后放射性主要从尿排泄。口服后24h内从尿、粪和胆汁排出的总放射性分别为剂量的66.1,0.63和3.06%.

     

    Abstract: The physiological disposition of 3H-gastrodin in female Sprague-Dawley rats was studied. The decline of radioactivity from gastrointestinal tract (GIT) was rapid following oral administration of 3H-gastrodin, and only 1.1% of the dose was recovered from the GIT after 8 hours. Rats were given intragastrically 3H-gastrodin, the radioactivity in blood was on a moderate level at 5 min and reached its peak at 50 min. Radioactivity was found to be highest in the kidney, moderate in liver, lung and womb, lower in the brain and reached maximum at 2 hours in the brain. The radioactivity excreted in urine, feces and bile within 24 hours was 66.1%, 0.63% and 3.06% respectively of the dose per os. The drug-plasma protein binding of 3H-gastrodin was found to be 4.3%, and that of its genin was 69.3%. The main metabolite detected by TLC was the genin (p-hydroxybenzyl alcohol).

     

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