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Drug Dev Ind Pharm ; 41(9): 1479-87, 2015.
Artículo en Inglés | MEDLINE | ID: mdl-25224341

RESUMEN

The recrystallization of an amorphous drug in a solid dispersion system could lead to a loss in the drug solubility and bioavailability. The primary objective of the current research was to use an improved kinetic model to evaluate the recrystallization kinetics of amorphous structures and to further understand the factors influencing the physical stability of amorphous solid dispersions. Amorphous solid dispersions of fenofibrate with different molecular weights of hydroxypropylcellulose, HPC (Klucel™ LF, EF, ELF) were prepared utilizing hot-melt extrusion technology. Differential scanning calorimetry was utilized to quantitatively analyze the extent of recrystallization in the samples stored at different temperatures and relative humidity (RH) conditions. The experimental data were fitted into the improved kinetics model of a modified Avrami equation to calculate the recrystallization rate constants. Klucel LF, the largest molecular weight among the HPCs used, demonstrated the greatest inhibition of fenofibrate recrystallization. Additionally, the recrystallization rate (k) decreased with increasing polymer content, however exponentially increased with higher temperature. Also k increased linearly rather than exponentially over the range of RH studied.


Asunto(s)
Celulosa/análogos & derivados , Fenofibrato/administración & dosificación , Modelos Químicos , Polímeros/química , Rastreo Diferencial de Calorimetría , Celulosa/química , Química Farmacéutica/métodos , Cristalización , Composición de Medicamentos , Estabilidad de Medicamentos , Fenofibrato/química , Calor , Humedad , Cinética , Peso Molecular , Solubilidad , Temperatura
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