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猫单剂量研究中地高辛和二氢地高辛药代动力学的比较。

Comparison of the pharmacokinetics of digoxin and dihydrodigoxin in cats in single-dose studies.

作者信息

Heinz N, Flasch H

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1978 Jun;303(2):181-7. doi: 10.1007/BF00508066.

Abstract

Pharmacokinetics of 3H-dihydrodigoxin and 3H-digoxin after single intravenous and intraduodenal administration in cats are compared. Data could be described by an open two compartment body model. The beta half-life in plasma of dihydrodigoxin after initial rapid distribution is 4.6h compared to 10.4 h after digoxin administration. The volume of tissue distribution of dihydrodigoxin is 7 times smaller than that of digoxin (0.311 versus 2.051). The "specific uptake" of dihydrodigoxin into myocardium and some other tissues is very low. Over 5.5h the cumulative biliary and urinary elimination of dihydrodigoxin is definitely higher (45.7% versus 14.4%). An unexpected peak in TLC plates after dihydrodigoxin administration in blood, bile and urine was identified to be the sodium salt of the opened lactone structure: dihydrodigoxin acid.

摘要

比较了猫单次静脉注射和十二指肠给药后3H-二氢地高辛和3H-地高辛的药代动力学。数据可用开放二室模型描述。二氢地高辛初始快速分布后血浆中的β半衰期为4.6小时,而地高辛给药后为10.4小时。二氢地高辛的组织分布容积比地高辛小7倍(分别为0.311和2.051)。二氢地高辛进入心肌和其他一些组织的“特异性摄取”非常低。在5.5小时内,二氢地高辛经胆汁和尿液的累积消除量明显更高(分别为45.7%和14.4%)。在血液、胆汁和尿液中给予二氢地高辛后,薄层色谱板上出现一个意外峰,鉴定为开环内酯结构的钠盐:二氢地高辛酸。

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