Antisolvent Recrystallization Strategy to Screen Appropriate Carriers to Stabilize Filgotinib Amorphous Solid Dispersions

作者：Ren, Fuzheng^*; Sun, Hanjing; Cui, Lin; Si, Yike; Chen, Ning; Ren, Guobin; Jing, Qiufang

来源：Journal of Pharmaceutical Sciences, 2018, 107(6): 1624-1632.

DOI：10.1016/j.xphs.2018.02.008

• filgotinib
• polymers
• screening method
• amorphous solid dispersions
• interaction

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.

• 出版日期2018-6
• 单位华东理工大学