Effect of Moisture Sorption on Free Volume and Relaxation of Spray Dried Dispersions: Relation to Drug Recrystallization
| Autor: | Jinjiang Li, Swathi Pinnamaneni, Ramesh K. Ramakrishnan, Junshu Zhao, Mario Hubert, Sergei Nazarenko, Li Tao, Shasad Sharif |
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| Rok vydání: | 2020 |
| Předmět: |
Recrystallization (geology)
Materials science Diffusion Pharmaceutical Science 02 engineering and technology 030226 pharmacology & pharmacy law.invention 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Drug Stability X-Ray Diffraction law Vinyl acetate medicine Crystallization Polyvinylpyrrolidone Hydroxypropyl cellulose Relaxation (NMR) Sorption 021001 nanoscience & nanotechnology Ketoconazole Solubility chemistry Chemical engineering Powders 0210 nano-technology medicine.drug |
| Zdroj: | Journal of Pharmaceutical Sciences. 109:1050-1058 |
| ISSN: | 0022-3549 |
| Popis: | The effect of vapor sorption on the free volume of drug-polymer spray-dried dispersions (SDDs) was investigated, along with the crystallization propensity of drug molecules in SDDs after exposure to humidity. Subsequently, the correlation of free volume change and relaxation time with drug recrystallization was examined. Four polymers, including polyvinylpyrrolidone, polyvinylpyrrolidone vinyl acetate copolymer, hydroxypropyl cellulose, and hydroxypropyl methylcellulose acetate succinate, and 2 drugs (indomethacin and ketoconazole) were selected for preparing SDDs. Free volume data of the exposed SDDs were obtained with positron annihilation lifetime spectroscopy, while the relaxation time was measured using a TA rheometer. Additionally, the crystallization propensity of active pharmaceutical ingredients (APIs) in the exposed SDDs was assessed using both polarized light microscopy and powder X-ray diffraction, followed by relating API crystallization inclination with expansion of holes and relaxation time. Finally, Cohen and Turnbull molecular transport model, along with its extensions by Vrentas and Duda, was qualitatively utilized for interpreting the recrystallization propensity of API molecules. In conclusion, API recrystallization is closely related to free volume change upon moisture sorption and relaxation time, but system dependent; overall, drug-hydroxypropyl methylcellulose acetate succinate SDDs appear physically stable against recrystallization due to less increase in free volume. |
| Databáze: | OpenAIRE |
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