10-羟基癸烯酸在动物体内吸收、分布、代谢和排泄

10-癸基癸烯酸(即10-HDA,定位标记为³H-10HDA),经小鼠和大鼠口服后,胃肠道吸收快,峰时均在1h,全身分布迅速广泛,与组织亲和力强,肝中放射性为最高,依次为肾、胰、脂肪、脑、脾、心和肺。平均Vd为9.71/kg。Ig和iv的T1/2β在12.6～22.7h。体内消除较缓慢,31 d内,尿粪中放射性累计排泄分别为给药量的85.4%和13.5%,提取尿和胆汁经分析结果主要以原形药物排出。血浆蛋白结合率为63%。血中放射—性时间曲线符合开放二室模型。

THE PHYSIOLOGICAL DISPOSITIONS OF 10-HYDROXY-△2-DECENOIC ACID (10-HDA) IN RATS AND MICE

10-Hydroxy-△²-decenoic acid (10-HDA) is the main fatty acid extracted from the royal jelly of the honey bee. ³H-10HDA given intragastrically to mice and rats was rapidly absorbed. The plasma radioactivity reached maximum level in about 1 h.Radioactivity was rapidly taken up by various organs and has a strong affinity for tissues. The highest radioactivity leval was found in the liver(6 times as much as in plasma), followed by kidney, pancreas, fat, brain, spleen, heart and lung. At all time intervals, the radioactivity in various organs was higher than the plasma level. Peak radioactivity level in organs appeared 1 d after intragastric administration. The radioactivity was shown to pass the blood-cerebral barrier and those in organs disappeared slowly.In 31 d, the cumulative excretion of radioactivity was 85.4% of the total dose in urine and 13.5% in feces. The radioactivity excreted in bile in 24 h was 2.6%.The radioactivity in urine and bile measured by TLC autoradiography and liquid scintillation counting indicated that ³H-10HDA excreted in the urine and bile was mainly in unchanged form and nearly no metabolite was found in the urine and bile.After intragastric and intravenous administration of ³H-10HDA to rats and mice, the declie of radioactivity in the plasma was shown to be biphasie (a distribution phase and a elimination phase). The ³H-10HDA in plasma was found to be 63% bound to plasma protein. The main pharmacokinetic parameters calculated from the plasma radioactivity-time data are shown in table 1.