Study on pharmacokinetics and tissue distribution of the isocorydine derivative (AICD) in rats by HPLC-DAD method

• 作者: Duolong Di Jinxia Liu Junxi Liu Mei Zhong Qian Yan Quanyi Zhao Yali Chen
• 来源期刊: 药学学报:英文版
• 学科: 医学
• 关键词: Alkaloids Pharmacokinetics Tissue distribution High-performance liquid chromatography with didode-array detection 8-Acetaminao-isocorydine
• 年，卷（期）: 2015,（3）
• 页码范围: 238-245
• 页数: 8页
• 分类号: R965
• 语种: 中文

摘要

A simple and effective high-performance liquid chromatography with diode-array detection method coupled with a liquid-liquid extraction pretreatment has been developed for determining the pharmacokinetics and tissue distribution of a novel structurally modified derivative(8-acetaminoisocorydine) of isocorydine.According to the in vivo experiments data calculations by DAS 2.0 software,a two-compartment metabolic model was suitable for describing the pharmacokinetic of 8-acetaminoisocorydine in rats.8-Acetamino-isocorydine was absorbed well after oral administration,and the absolute bioavailability was 76.5%.The half-life of 8-acetamino-isocorydine after intravenous and oral administration was 2.2 h and 2.0 h,respectively.In vivo,8-acetamino-isocorydine was highly distributed in the lungs,kidney and liver;however,relatively little entered the brain,suggesting that 8-acetaminoisocorydine could not easily pass through the blood brain barrier.Our work describes the first characterization of the pharmacokinetic parameters and tissue distribution of 8-acetamino-isocorydine.The acquired data will provide useful information for the in vivo pharmacology of 8-acetaminoisocorydine,and can be applied to new drug research.