Disposition of the hypolipidaemic agent, 2,3-dihydrophthalazine-1,4-dione, in Sprague Dawley rats.
Disposition of the hypolipidaemic agent, 2,3-dihydrophthalazine-1,4-dione, in Sprague Dawley rats.
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降血脂剂 2,3-二氢酞嗪-1,4-二酮在 Sprague Dawley 大鼠中的处置。
DOI：
10.1111/j.2042-7158.1989.tb06484.x
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发表时间：
1989
期刊：
影响因子：
--
通讯作者：
Shrewsbury,RP
中科院分区：
文献类型：
--
作者：
Hall,IH;Oswald,CB;Wyrick,SD;Maguire,JH;Shrewsbury,RP
已测定静脉和口服给药后[1,4 C] 2，3-二氢酞嗪-1，4-二酮（一种强效降血脂剂）的处置。两种给药途径均提供了多指数分布，估计t1/2约为75 h。口服给药后，观察到药物从肠道迅速吸收，并迅速分布到身体的所有组织。在皮肤和尸体中发现了大量的14 C放射性。经口给药后，约35%的给药放射性经尿液排泄，11%经粪便排泄。经尿液排泄的放射性中约66%为母体药物。有证据表明存在额外的代谢物，占尿放射性排泄的28%。母体药物几乎没有血清蛋白结合，是高度水溶性的，并且可能通过被动扩散被细胞吸收。
The disposition of [14C]2,3-dihydrophthalazine-1,4-dione, a potent hypolipidaemic agent, has been determined after both intravenous and oral administration. Both the routes of administration afforded multi-exponential disposition with an estimated t 1/2 of approximately 75 h. After oral administration, the drug was observed to be absorbed rapidly from the intestine and distributed quickly to all tissues of the body. A large quantity of the14C-radioactivity was found in the skin and carcass. Approximately 35% of the administered radioactivity was excreted in urine after oral administration and 11% in the faeces. Approximately 66% of the radioactivity excreted in urine was the parent drug. There was evidence of an additional metabolite which accounted for 28% of the urinary radioactive excretion. The parent drug has little serum protein binding, is highly water soluble, and is probably taken up by cells by passive diffusion.