In vivo dissolution of poorly water-soluble drugs:Proof of concept based on fluorescence bioimaging

作     者：Yinqian Yang Yongjiu Lv Chengying Shen Tingting Shi Haisheng He Jianping Qi Xiaochun Dong Weili Zhao Yi Lu Wei Wu Yinqian Yang;Yongjiu Lv;Chengying Shen;Tingting Shi;Haisheng He;Jianping Qi;Xiaochun Dong;Weili Zhao;Yi Lu;Wei Wu

作者机构：Key Laboratory of Smart Drug Delivery of MOESchool of PharmacyFudan UniversityShanghai 201203China Center for Medical Research and InnovationShanghai Pudong HospitalFudan University Pudong Medical CenterShanghai 201399China 

出 版 物：《Acta Pharmaceutica Sinica B》 (药学学报（英文版）)

年 卷 期：2021年第11卷第4期

页      面：1056-1068页

核心收录：

学科分类：100702[医学-药剂学] 1007[医学-药学(可授医学、理学学位)] 1006[医学-中西医结合] 1004[医学-公共卫生与预防医学(可授医学、理学学位)] 1001[医学-基础医学(可授医学、理学学位)] 100602[医学-中西医结合临床] 10[医学] 

基　　金：supported by the National Natural Science Foundation of China(Nos.81973247,81872815,81872826 and 81690263) Science and Technology Commission of Shanghai Municipality(19XD1400300,China) 

主　　题：In vivo dissolution Fenofibrate Fluorescence Aggregation-caused quenching Bioimaging IVIVC 

摘      要：In vitro-in vivo correlation(IVIVC)of solid dosage forms should be established basically between in vitro and in vivo dissolution of active pharmaceutical ***,in vivo dissolution profles have never been accurately *** current practice of IVIVC has to resort to in vivo absorption fractions(Fa).In this proof-of-concept study,in vivo dissolution of a model poorly watersoluble drug fenofbrate(FNB)was investigated by fuorescence *** crystals were frst labeled by near-infrared fuorophores with aggregation-caused quenching *** dyes illuminated FNB crystals but quenched immediately and absolutely once been released into aqueous media,enabling accurate monitoring of residual drug *** linearity established between fuorescence and crystal concentration justifed reliable quantifcation of FNB *** vitro dissolution was frst measured following pharmacopoeia monograph protocols with well-documented *** synchronicity between fuorescence and in vitro dissolution of FNB supported using fuorescence as a measure for determination of *** vitro dissolution correlated well with in vivo dissolution,acquired by either live or ex vivo *** newly established IVIVC was further validated by correlating both in vitro and in vivo dissolution with Faobtained from pharmacokinetic data.