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Development and physicochemical characterization of saquinavir mesylate solid dispersions using Gelucire 44/14 or PEG 4000 as carrier

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Abstract

Solid dispersions of saquinavir mesylate containing either Gelucire® 44/14 or poly(ethylene glycol) (PEG) 4000, or mixtures of each carrier with Tween 80 or polyvinyl pyrrolidone (PVP) K30 were prepared in order to enhance the drug dissolution rate. These systems were prepared by the melting method and characterized by X-ray powder diffraction, microscopical techniques, and Raman spectroscopy aiming to establish a relationship between physicochemical and dissolution properties under different cooling conditions. Modifications in degree of crystalline order/disorder over time were observed in preparations with both carriers. Overall, formulations cooled and stored at −20 °C showed less variation in dissolution rates than those at 25 °C. Although Tween 80 has enhanced the known self-emulsifying properties of Gelucire® 44/14, its combination with PEG 4000 displayed miscibility problems. The addition of PVP K30 was not the most effective approach in enhancing the dissolution in early steps; however, the drug dissolution was stable after 7 days of storage at 25 °C. The combination of PEG 4000 and PVP K30 maintained the dissolution properties for 60 and 90 days at 25 °C/95 % relative humidity and 40 °C/75 % (f 2 values >50), respectively.

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Acknowledgments

We would like to acknowledge FAPESC/CNPq/MS/SES-SC (Grant Number 15.949/2009-2) for financial support. We also thank CAPES/MEC (Nanobiotechnology Network, Grant Number 759/2009) and CNPq/MCT for the authors fellowships. All the XRPD and SEM measurements were performed in multiuser facilities provided by the Federal University of Santa Catarina: Central Laboratory of Electron Microscopy (LCME) and X-ray Diffraction Laboratory (LDRX), respectively. Silvia L. Cuffini thanks to CAPES/PVE program.

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Authors and Affiliations

  1. Laboratório de Virologia Aplicada, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil

    Thiago Caon, Ricardo Augusto Konig, Ariadne Cristiane Cabral da Cruz & Cláudia Maria Oliveira Simões

  2. Laboratório de Controle de Qualidade, Departamento de Ciências Farmacêuticas, Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil

    Simone Gonçalves Cardoso & Silvia Lucia Cuffini

  3. Laboratório de Difração de Raios-X, Departamento de Física, Universidade Federal de Santa Catarina, Campus Universitário, Trindade, Florianópolis, SC, 88040-900, Brazil

    Carlos Eduardo Maduro Campos

  4. Laboratório de Desenvolvimento Galênico, Departamento de Produção e Controle de Medicamentos, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Santana, Porto Alegre, RS, 90610-000, Brazil

    Letícia Scherer Koester

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  1. Thiago Caon
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  7. Letícia Scherer Koester
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  8. Cláudia Maria Oliveira Simões
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Correspondence to Cláudia Maria Oliveira Simões.

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Caon, T., Konig, R.A., da Cruz, A.C.C. et al. Development and physicochemical characterization of saquinavir mesylate solid dispersions using Gelucire 44/14 or PEG 4000 as carrier. Arch. Pharm. Res. 36, 1113–1125 (2013). https://doi.org/10.1007/s12272-013-0142-2

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