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Int J Pharm ; 478(1): 348-360, 2015 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-25450477

RESUMO

The Pharmaceutical industry is increasingly utilizing amorphous technologies to overcome solubility challenges. A common approach is the use of drug in polymer dispersions to prevent recrystallization of the amorphous drug. Understanding the factors affecting chemical and physical degradation of the drug within these complex systems, e.g., temperature and relative humidity, is an important step in the selection of a lead formulation, and development of appropriate packaging/storage control strategies. The Arrhenius equation has been used as the basis of a number of models to predict the chemical stability of formulated product. In this work, we investigate the increase in chemical degradation seen for one particular spray dried dispersion formulation using hydroxypropyl methylcellulose acetate succinate (HPMC-AS). Samples, prepared using polymers with different substitution levels, were placed on storage for 6 months under a range of different temperature and relative humidity conditions and the degradant level monitored using high-performance liquid chromatography (HPLC). While the data clearly illustrates the impact of temperature and relative humidity on the degradant levels detected, it also highlighted that these terms do not account for all the variability in the data. An extension of the Arrhenius equation to include a term for the polymer chemistry, specifically the degree of succinoyl substitution on the polymer backbone, was shown to improve the fit of the model to the data.


Assuntos
Estabilidade de Medicamentos , Excipientes/química , Metilcelulose/análogos & derivados , Modelos Teóricos , Algoritmos , Dessecação , Composição de Medicamentos , Umidade , Metilcelulose/química , Oxidiazóis/química , Ácido Succínico/química , Sulfonamidas/química , Temperatura
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