Studies on Pharmacokinetics and Liver Microsome Metabolism of Nuciferine in Different Species of Animals

Q4 Biochemistry, Genetics and Molecular Biology
Dong Xiao-chen, Liu Ming-qi, L. Jun, Guan Feng, Xue Ai-chun, Zhao Jin, Ge Jian
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引用次数: 0

Abstract

Corresponding Author: Ge Jian College of Life Sciences, China JiLiang University, Hangzhou, Zhejiang, 310018, China E-mail: gejian16888@163.com Abstract: This study aimed to compare the characteristics of pharmacokinetics and liver microsome metabolism among different species of animals including rabbit, rat and mouse and healthy New Zealand white rabbits, SPF Sprague Dawley (SD) rats and ICR mice were given intraperitoneal injection of nuciferine at a dose of 50 mg per kg body weight. Blood samples were collected via caudal vein after administration and nuciferine concentrations in different points were determined by the method of HPLC-UV. Then the plasma concentration-time curves were drawn and the pharmacokinetics parameters were calculated by DAS 3.0 software. Besides, liver microsome from rabbit, rats and mice were prepared to study the metabolism of nuciferine in vitro. These results showed that nuciferine fitted two-compartment model in rabbits and rats and one-compartment model in mice. The calculated results of pharmacokinetics parameters showed that the fast absorption of nuciferine exhibited in rabbits, rats and mice, while the elimination was relatively slow. Compared with rabbits and rats, the nuciferine elimination was fastest in mice. The Km value of nuciferine metabolism in vitro was least in mice liver microsome, which suggested that the fastest metabolism of nuciferine existed in mice liver. Therefore, the pharmacokinetics characteristics of nuciferine in different species were significantly different, the elimination of nuciferine is the fastest in mice and the slowest in rabbits, which was in line with the in vitro metabolism trends by liver microsome from different species.
荷叶碱在不同动物体内的药代动力学及肝微粒体代谢研究
摘要:本研究旨在比较兔、大鼠、小鼠和健康新西兰大白兔、SPF级SD大鼠、ICR小鼠腹腔注射50 mg / kg剂量的nucifine的药代动力学和肝微体代谢特征。给药后经尾静脉采血,采用高效液相色谱-紫外分光光度法测定不同部位的哌嗪浓度。绘制血药浓度-时间曲线,利用DAS 3.0软件计算药动学参数。制备兔、大鼠和小鼠肝微粒体,研究荷叶碱的体外代谢。结果表明,荷叶碱适用于家兔和大鼠的双室模型和小鼠的单室模型。药代动力学参数计算结果表明,荷叶碱在家兔、大鼠和小鼠体内吸收较快,消除较慢。与家兔和大鼠相比,小鼠的荷叶碱消除速度最快。荷叶碱体外代谢Km值在小鼠肝微粒体中最低,说明荷叶碱在小鼠肝脏中代谢最快。因此,不同物种荷叶碱的药代动力学特征有显著差异,荷叶碱在小鼠体内的消除速度最快,在家兔体内的消除速度最慢,这符合不同物种肝微粒体体外代谢的趋势。
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来源期刊
American Journal of Biochemistry and Biotechnology
American Journal of Biochemistry and Biotechnology Biochemistry, Genetics and Molecular Biology-Biotechnology
CiteScore
0.70
自引率
0.00%
发文量
27
期刊介绍: :: General biochemistry :: Patho-biochemistry :: Evolutionary biotechnology :: Structural biology :: Molecular and cellular biology :: Molecular medicine :: Cancer research :: Virology :: Immunology :: Plant molecular biology and biochemistry :: Experimental methodologies
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