Antisolvent Recrystallization Strategy to Screen Appropriate Carriers to Stabilize Filgotinib Amorphous Solid Dispersions
| Autor: | Ning Chen, Hanjing Sun, Lin Cui, Guobin Ren, Fuzheng Ren, Yike Si, Qiufang Jing |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Materials science
Polymers Pyridines Pharmaceutical Science Infrared spectroscopy 02 engineering and technology Flory–Huggins solution theory behavioral disciplines and activities 030226 pharmacology & pharmacy Excipients 03 medical and health sciences symbols.namesake 0302 clinical medicine Hypromellose Derivatives Drug Stability mental disorders Binary system Dissolution Protein Kinase Inhibitors chemistry.chemical_classification Drug Carriers Recrystallization (metallurgy) Povidone Polymer Janus Kinase 1 Triazoles 021001 nanoscience & nanotechnology Amorphous solid chemistry Chemical engineering Solubility symbols 0210 nano-technology Crystallization Raman scattering |
| Zdroj: | Journal of pharmaceutical sciences. 107(6) |
| ISSN: | 1520-6017 |
| Popis: | 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. Fourier-transform infrared spectroscopy, Raman scattering, and nuclear magnetic resonance revealed hydrogen-bonding formation in the drug-polymer binary system, which was critical for ASDs stabilization. A Flory-Huggins 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|