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Pharm Dev Technol ; 24(3): 283-292, 2019 Mar.
Artículo en Inglés | MEDLINE | ID: mdl-29723078

RESUMEN

This study aimed at evaluating the shake-flask use as a universal method to evaluate drug solubility in a biowaiver context as proposed by FDA, EMA and ANVISA. The solubility of losartan was determined in three buffers using the shake-flask method, intrinsic dissolution (ID) and Quantum Chemistry. Moreover, the evaluation of a losartan dissolution profile from coated tablets was conducted. The losartan low solubility in pH 1.2 and high solubility in pH 6.8 were observed using the shake-flask method. However, the solubility results using ID demonstrated its high solubility in pH 1.2 and 6.8. It was not possible to find conclusive results regarding the solubility of the drug in pH 4.5. The studies conducted by Quantum Chemistry provide molecular and electronic data that helped understand the losartan solvation in different pH values. Our experimental results defined that losartan can be classified as a low-solubility drug. In addition, this work shows that shake-flask cannot be a universal method of solubility studies in biowaiver context. Individual analysis will be necessary. The intrinsic dissolution should be considered as a complementary method.


Asunto(s)
Bloqueadores del Receptor Tipo 1 de Angiotensina II/química , Química Farmacéutica/métodos , Losartán/química , Disponibilidad Biológica , Liberación de Fármacos , Concentración de Iones de Hidrógeno , Teoría Cuántica , Solubilidad , Comprimidos , Equivalencia Terapéutica
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