Impact of Azithromycin on Forsythiaside Pharmacokinetics in Rats:A Population Modeling Method  

作　　者：Jing-chen TIAN Xuan-ling ZHANG Jian-rong CUI Xin-gang LI 

机构地区：[1]Department of Pharmacy,Beijing Tiantan Hospital,Capital Medical University,Beijing 100070,China [2]School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 100102,China [3]Department of Pharmacy,Beijing Friendship Hospital,Capital Medical University,Beijing 100050,China [4]Department of Pharmacy,Chengdu Seventh People's Hospital,Chengdu 610000,China

出　　处：《Current Medical Science》2022年第4期863-870,共8页当代医学科学（英文）

基　　金：supported by the Natural Science Foundation of Beijing Municipality(No.7192060).

摘　　要：Objective:Lianhuaqingwen and Shuanghuanglian are drug treatment options for Corona Virus Disease 2019(COVID-19).In China,use of traditional Chinese medicine with Shuanghuanglian or Lianhuaqingwen(for them,forsythiaside is the active antiviral and antibacterial component)in combination with azithromycin is common for the treatment of pediatric pneumonia.It is important to understand the reason why the combination of these compounds is better than a single drug treatment.This study aimed to explore the pharmacokinetic interaction between forsythiaside and azithromycin.Methods:Twelve male Sprague-Dawley rats were randomly divided into an experimental group(Forsythia suspensa extract and azithromycin)and a control group(a single dose of Forsythia suspensa extract in 5%glucose solution).Plasma samples were collected at scheduled time points,and the high-performance liquid chromatography combined with ultraviolet method was used to determine the plasma forsythiaside concentration.Non-compartmental analysis and population pharmacokinetic methods were used to investigate the forsythiaside pharmacokinetic difference between the experimental and control group.Results:Compared with a single administration,the area under the curve and half-life of forsythiaside increased,and forsythiaside clearance decreased significantly after co-administration with azithromycin.The in vivo behavior of forsythiaside could be described by the one compartment model.The forsythiaside clearance decreased when combined with azithromycin.Visual evaluation and bootstrap results suggested that the final model was precise and stable.Conclusion:Co-administration of azithromycin can significantly decrease the forsythiaside clearance and increase drug exposure.A lower dose of azithromycin can obtain sufficient forsythiaside concentration to provide antiviral and antibacterial activity.

关 键 词：AZITHROMYCIN FORSYTHIASIDE PHARMACOKINETICS drug interaction traditional Chinese medicine Corona Virus Disease 2019 ANTIVIRALS 

分 类 号：R969.1[医药卫生—药理学]