An Examination of Water Vapor Sorption by Multicomponent Crystalline and Amorphous Solids and Its Effects on Their Solid-State Properties
| Autor: | Ann Newman, George Zografi |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Materials science
Chemistry Pharmaceutical Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy Cocrystal Dissociation (chemistry) law.invention 03 medical and health sciences 0302 clinical medicine Drug Stability law Solubility Crystallization Dissolution chemistry.chemical_classification Water Humidity Sorption 021001 nanoscience & nanotechnology Amorphous solid Drug Liberation Steam Absorption Physicochemical Pharmaceutical Preparations chemistry Chemical engineering Counterion 0210 nano-technology |
| Zdroj: | Journal of Pharmaceutical Sciences. 108:1061-1080 |
| ISSN: | 0022-3549 |
| DOI: | 10.1016/j.xphs.2018.10.038 |
| Popis: | This commentary critically evaluated the unique effects of water vapor sorption by multicomponent solid forms of active pharmaceutical ingredients (APIs), and its effects on their physical and chemical properties. Such multicomponent forms include the following: (1) crystalline salts and cocrystals, and (2) amorphous salts, coamorphous mixtures, and amorphous solid dispersions (ASDs). These solid forms are commonly used to increase the solubility, dissolution, and bioavailability of poorly soluble APIs. To achieve this increase, selected counterions or coformers exhibit much greater polarity, and have a tendency to enhance water vapor sorption, leading to possible instabilities. Such instabilities include salt disproportionation, cocrystal dissociation, and phase separation and crystallization from amorphous forms. Regarding crystalline multicomponent systems, significant instabilities arise on account of deliquescence or crystal hydrate formation. Such behavior often follows water-induced salt disproportionation or cocrystal dissociation. Regarding amorphous salts, coamorphous mixtures, and ASDs, we see the importance of absorbed water as a disrupter of API-coformer interactions and as a plasticizer in bringing about subsequent phase separation and crystallization. In preparing multicomponent solid forms, it is important to measure the water vapor sorption isotherm of the counterion or coformer to better understand the mode by which water is sorbed, and to anticipate and correct possible instabilities. |
| Databáze: | OpenAIRE |
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