title: Solid dispersion of efavirenz in PVP K-30 by conventional solvent and kneading methods.
abstract: 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.
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: Lariza Darlene Santos
authors.initials: LD
authors.lastname: Alves
authors.affiliation: Core of Medicines and Corelated Quality Control - NCQMC, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: Mônica Felts
authors.initials: MF
authors.lastname: de La Roca Soares
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: Camila Tavares
authors.initials: CT
authors.lastname: de Albuquerque
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: Elica Rodrigues
authors.initials: ER
authors.lastname: da Silva
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: Alexandre Couto Carneiro
authors.initials: AC
authors.lastname: Vieira
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: Danilo Augusto Ferreira
authors.initials: DA
authors.lastname: Fontes
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: Camila Bezerra Melo
authors.initials: CB
authors.lastname: Figueirêdo
authors.affiliation: Core of Medicines and Corelated Quality Control - NCQMC, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil.
authors.forename: José Lamartine
authors.initials: JL
authors.lastname: Soares Sobrinho
authors.affiliation: Laboratory of Medicines Technology - LTM, Department of Pharmaceutical Sciences - Federal University of Pernambuco, Arthur de Sá, s/n, 50740-521 Recife, PE, Brazil. Electronic address: rolim.pedro@gmail.com.
authors.forename: Pedro José
authors.initials: PJ
authors.lastname: Rolim Neto
mesh_terms: D000480:Alkynes; D048588:Benzoxazines / Q000737:chemistry*; D003521:Cyclopropanes; D014677:Pharmaceutical Vehicles / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry*; D018894:Reverse Transcriptase Inhibitors / Q000737:chemistry*; D012995:Solubility
chemical_list: D000480:Alkynes; D048588:Benzoxazines; D003521:Cyclopropanes; D014677:Pharmaceutical Vehicles; D018894:Reverse Transcriptase Inhibitors; D011205:Povidone; C098320:efavirenz
keywords: Dissolution; Drug delivery; Polymers; Solubility; Stability