In situ solid-state NMR characterization of pharmaceutical materials: An example of drug-polymer thermal mixing
| Autor: | Hanxi Guan, Jinglin Yin, Yongchao Su, Zhenfeng Pang, Chengbin Huang, Xueqian Kong |
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| Rok vydání: | 2020 |
| Předmět: |
chemistry.chemical_classification
Antifungal Agents Magnetic Resonance Spectroscopy Molecular Structure 010405 organic chemistry Chemistry Pharmaceutical Polyacrylic acid Acrylic Resins Temperature General Chemistry Polymer 010402 general chemistry 01 natural sciences Miscibility 0104 chemical sciences Characterization (materials science) Amorphous solid chemistry.chemical_compound Ketoconazole chemistry Solid-state nuclear magnetic resonance Chemical engineering Magic angle spinning General Materials Science Dissolution |
| Zdroj: | Magnetic Resonance in Chemistry. |
| ISSN: | 0749-1581 |
| Popis: | Pharmaceutical amorphous solid dispersions, a multicomponent system prepared by dispersing drug substances into polymeric matrix via thermal and mechanical processes, represent a major platform to deliver the poorly water-soluble drug. Microscopic properties of drug-polymer contacts play mechanistic roles in manipulating long-term physical stability as well as dissolution profiles. Although solid-state nuclear magnetic resonance has been utilized as an indispensable tool to probe structural details, previous studies are limited to ex situ characterizations. Our work provides likely the first documented example to investigate comelting of ketoconazole and polyacrylic acid, as a model system, in an in situ manner. Their physical mixture is melted and mixed in the solid-state nuclear magnetic resonance rotor under magic angle spinning at up to approximately 400 K. Critical structural events of molecular miscibility and interaction have been successfully identified. These results design and evaluate the instrumental and experimental protocols for real-time characterizations of the comelting of pharmaceutical materials. |
| Databáze: | OpenAIRE |
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