药代动力学
生物利用度
排泄
分布(数学)
口服
组织分布
药理学
化学
体内
内分泌学
内科学
生物
医学
数学
数学分析
生物技术
作者
Xiao Qing Wu,Jianguo Sun,Ying Peng,Yan Liang,Hui Chen,Jizhou Wu,Peng Zhang
出处
期刊:Molecules
[MDPI AG]
日期:2014-12-10
卷期号:19 (12): 20613-20626
被引量:7
标识
DOI:10.3390/molecules191220613
摘要
Verticinone, the main active component in F. hupehensis, exhibits potent antitussive and expectorant effects. Here, a LC-MS method was developed and applied to study the pharmacokinetics, tissue distribution and excretion of verticinone in rats, and its plasma protein binding in vitro. A significant gender difference in the pharmacokinetics of verticinone in rats was observed, as its absolute oral bioavailability in male and female rats was 45.8% and 2.74%, respectively. The relative bioavailability of verticinone was significantly lower in female rats as compared to male, following intragastrical (i.g.) and intravenous (i.v.) administration. After successive i.g. administration of verticinone, accumulation was observed in female rats but not in the male ones. The tissue distribution study showed that verticinone had a good tissue penetrability and a high tissue affinity in most studied tissues, except brain. After a 2 mg/kg oral dose, less than 4% of the dose was excreted as unchanged parent compound in male rats, and less than 1% in female rats, which indicated that verticinone was metabolized more extensively in female rats than in male rats.
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