Pharmacokinetics, tissue distribution, plasma protein binding rate and excretion of sinoacutine following intravenous administration in female and male Sprague-Dawley rats

被引：4

作者：

Zhu, Liyuan ^{[1
]}

Mei, Jiahua ^{[2
,3
]}

Peng, Chaorui ^{[1
]}

Zhao, Yuancui ^{[2
]}

Liu, Yunkuan ^{[2
]}

Cui, Lili ^{[4
]}

Zhang, Kun ^{[2
]}

Ma, Yunshu ^{[2
,5
,6
]}

机构：

[1] Yunnan Xinxing Occupat Inst, Kunming, Yunnan, Peoples R China

[2] Yunnan Univ Chinese Med, Sch Chinese Mat Med, Kunming 650500, Yunnan, Peoples R China

[3] Yunnan Key Lab Dai & Yi Med, Kunming, Yunnan, Peoples R China

[4] Nanjing Univ Chinese Med, Sch Pharm, Nanjing, Peoples R China

[5] Key Lab External Drug Delivery Syst & Preparat Te, Kunming, Yunnan, Peoples R China

[6] Yunnan Key Lab Southern Med Resource, Kunming, Yunnan, Peoples R China

来源：

XENOBIOTICA | 2022年 / 52卷 / 01期

基金：

中国国家自然科学基金;

关键词：

Sinoacutine; pharmacokinetics; tissue distribution; plasma protein binding rate; excretion; gender difference; SINOMENINE; STRESS; INJURY;

D O I：

10.1080/00498254.2022.2036390

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Sinoacutine is a natural isoquinoline alkaloid isolated from traditional Chinese medicine Stephanina yunnanensis H. S. Lo. Our aim was to study the pharmacokinetic characteristics of sinoacutine, which is essential during the development of new drugs. In this study, an accurate, sensitive, and efficient liquid chromatography (HPLC) method was developed and applied to evaluate the pharmacokinetics, tissue distribution, plasma protein binding rate, and excretion after intravenous injection of sinoacutine in rats. The pharmacokinetic parameters of sinoacutine were accorded with a two-compartment model in rats, and the AUC(0-)(t) in female was greater than that in male. Sinoacutine could be detected in heart, liver, spleen, lung, kidney, and brain, and the content in liver and kidney was relatively high. Meanwhile, it had a high plasma protein binding rate of 79.16%. Excretion of sinoacutine through faeces and urine was low, and the average excretion rate was 9.96%. There were gender differences in blood drug concentration, tissue distribution, and excretion significantly (p < 0.05). In summary, this study lays a foundation for elucidating the pharmacokinetic rule of sinoacutine and the data can provide a reliable scientific resource for further research.

引用

页码：91 / 98

页数：8

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