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Solid dispersion of efavirenz in PVP K-30 by conventional solvent and kneading methods

2014; Elsevier BV; Volume: 104; Linguagem: Inglês

10.1016/j.carbpol.2014.01.027

1879-1344

Lariza Darlene Santos Alves, Mônica Felts de La Roca Soares, Camila Tavares de Albuquerque, E.R. Silva, Alexandre C.C. Vieira, Danilo Augusto Ferreira Fontes, Camila Bezerra Melo Figueirêdo, José Lamartine Soares‐Sobrinho, Pedró José Rolim Neto,

Crystallization and Solubility Studies

Efavirenz (EFV) used as a part of the treatment of first choice in antiretroviral therapy for AIDS has low aqueous solubility and presents problems of absorption. We thus initially present a phase solubility diagram with carriers of different classes. With a view to obtaining a solid dispersion (SD) with suitable consistency to that of a solid formulation, we chose to use PVP K-30, since polymers present some of the best results. The kneading (KN) and solvent evaporation (EV) methods were thus used at different rates. These were characterized by the way of DSC, FT-IR, SEM, DR-X and dissolution. SD EV proved unsatisfactory, resulting in a decreased dissolution rate, despite the amorphous state of the samples, while the SD KN 4:1 (EFV:polymer) and physical mixtures (PM) had a higher rate of dissolution. SD KN and PM 4:1 were also evaluated for stability after storage, with benefits being observed in relation to EFV.