药代动力学
化学
分布(数学)
高效液相色谱法
药理学
组织分布
色谱法
内科学
医学
数学分析
数学
作者
Xiaotong Zhao,Leilei Fang,Tan Yang,Yanqing Zhang,Junbo Xie
出处
期刊:Current Drug Metabolism
[Bentham Science]
日期:2023-09-01
卷期号:24 (9): 656-666
标识
DOI:10.2174/0113892002263771230920092659
摘要
Isovitexin-2"-O-D-glucopyranoside (IVG) has been known to exhibit sedative and hypnotic effects. However, there is little understanding of the in vivo pharmacokinetics and tissue distribution of IVG.This study aimed to investigate the pharmacokinetics and tissue distribution of IVG.The study employed an HPLC-ESI-MS/MS method to analyze the pharmacokinetics and tissue distribution of IVG.Under mass spectrometry, IVG and internal standard (IS) showed strong negative ionization signals. MRM analysis chose ion transitions m/z 593.3 → 293.0 (IVG) and m/z 579.8 → 271.4 (IS). Method validation indicated high precision, accuracy, and reliability with a quantitation limit under 20 ng/mL. After intravenously administering 5.0 mg/kg of IVG, rapid clearance from rat plasma was observed, with a half-life (t1/2) of 3.49 ± 0.99 h and a clearance rate of 54.53 ± 11.90 mL/kg/h. The area under the curve (AUC0-12h) of 37.79 ± 7.65 μg·h/mL indicated a brisk metabolic rate. Evaluating the tissue distribution, the highest accumulation was seen in the liver (30.32 ± 3.06 μg/g), followed by the kidney (20.58 ± 2.12 μg/g) and intestine (6.69 ± 0.93 μg/g), suggesting a propensity for IVG to concentrate in these tissues. Importantly, the presence of IVG in the brain underlines its potential to traverse the blood-brain barrier. These findings revealed that following intravenous administration, IVG was swiftly and broadly distributed throughout various rat tissues.This study provides valuable information on the pharmacokinetics and tissue distribution of IVG, implicating its potential as a novel and effective drug candidate for sedative and anxiolytic treatment.
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