生理药动学模型预测国产左羟丙哌嗪胶囊体外溶出特性及对体内药动学影响  

Dissolution characteristics of domestic levodropropizine capsules in vitro and their influence on pharmacokinetics in vivo by physiolog based pharmacokinetic model

作　　者：石笑弋 刘轶 兰文 李昌亮 李琦 刘雁鸣 李帅 陈涛 SHI Xiao-yi;LIU Yi;LAN Wen;LI Chang-liang;LI Qi;LIU Yan-ming;LI Shuai;CHEN Tao(Hunan Institute for Drug Control,Changsha 410001;NMPA Key Laboratory for Pharmaceutical Excipients Engineering Technology,Changsha 410001;Hunan Engineering&Technology Research Center for Pharmaceutical Quality Evaluation,Changsha 410001;PharmoGo Co.,Ltd.,Shanghai 200127)

机构地区：[1]湖南省药品检验检测研究院,长沙410001 [2]国家药品监督管理局药用辅料工程技术研究重点试验室,长沙410001 [3]湖南省药品质量评价工程技术研究中心,长沙410001 [4]上海凡默谷信息技术有限公司,上海200127

出　　处：《中南药学》2023年第7期1733-1737,共5页Central South Pharmacy

基　　金：2022年国家药品抽验计划(No.国药监药管[2022]1号)。

摘　　要：目的预测国产左羟丙哌嗪胶囊体外溶出特性及对体内药动学的影响。方法根据不同厂家产品的体外溶出结果拟合体内溶出释放曲线;采用Gastroplus软件建立生理药动学模型;虚拟群体模拟预测制剂体外溶出特性以及对体内药动学的影响。结果国产左羟丙哌嗪胶囊在40 min内溶出量(Q)达85%以上(T85%=40 min),达峰浓度(C_(max))、曲线下面积(AUC_(0→∞))等主要药动学参数在偏差范围内;不同厂家胶囊的体外溶出差异未影响体内药动学特征。结论国产左羟丙哌嗪胶囊体外呈快速溶出的特性,有利于其在体内迅速吸收,是发挥药效的有利因素。Objective To predict the dissolution characteristics of domestic levodropropizine capsules in vitro and their effects on pharmacokinetics in vivo.Methods The release rate curve in vivo was fit according to the dissolution of products from different manufacturers in vitro.Physiology based pharmacokinetic model was established by Gastroplus software,the dissolution characteristics of preparations in vitro and the effects on pharmacokinetics in vivo were predicted by virtual population simulation.Results The dissolution rate(Q)of domestic levodropropizine capsules within 40 min was over 85%(T85%=40 min),with the main pharmacokinetic parameters(C_(max),AUC_(0→∞)and so on)within the deviation range.The difference in dissolution in vitro did not affect the pharmacokinetic characteristics in vivo.Conclusion Domestic levodropropizine capsules dissolve rapidly in vitro,which is beneficial for its rapid absorption in vivo and the efficacy of drugs.

关 键 词：生理药动学模型 左羟丙哌嗪胶囊 体外溶出 药动学 

分 类 号：R94[医药卫生—药剂学] R96[医药卫生—药学]