文献类型：期刊文献

英文题名：Antisolvent Recrystallization Strategy to Screen Appropriate Carriers to Stabilize Filgotinib Amorphous Solid Dispersions

作者：Ren, Fuzheng[1,2];Sun, Hanjing[1];Cui, Lin[1];Si, Yike[1];Chen, Ning[1];Ren, Guobin[1];Jing, Qiufang[1,2]

机构：[1]East China Univ Sci & Technol, Lab Pharmaceut Crystal Engn & Technol, Sch Pharm, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Shanghai Key Lab New Drug Design, Sch Pharm, Shanghai 200237, Peoples R China

年份：2018

卷号：107

期号：6

起止页码：1624

外文期刊名：JOURNAL OF PHARMACEUTICAL SCIENCES

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000441014200018)】；

基金：The authors are grateful for support from the Shanghai Committee of Science and Technology (grant no. 14DZ1930802) and the National Natural Science Foundation of China (grant no. 21576080).

语种：英文

外文关键词：filgotinib; polymers; screening method; amorphous solid dispersions; interaction

摘要：Drugs in amorphous solid dispersions (ASDs) are highly dispersed in hydrophilic polymeric carriers, which also help to restrain recrystallization and stabilize the ASDs. In this study, microscopic observation after antisolvent recrystallization was developed as a rapid screening method to select appropriate polymers for the initial design filgotinib (FTN) ASDs. Using solvent evaporation, FTN ASDs with the polymers were prepared, and accelerated experimentation validated this screening method. Fouriertransform infrared spectroscopy, Raman scattering, and nuclear magnetic resonance revealed hydrogenbonding formation in the drug-polymer binary system, which was critical for ASDs stabilization. A FloryHuggins interaction parameter and water sorption isotherms were applied to evaluate the strength of the interaction between FTN and the polymers. The dissolution rate was also significantly improved by ASDs formulation, and the presence of the polymers exerted solubilization effects. These results suggested the efficacy of this screening method as a preliminary tool for polymer selection in ASDs design. (C) 2018 American Pharmacists Association (R) . Published by Elsevier Inc. All rights reserved.