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Merck
  • Ravuconazole self-emulsifying delivery system: in vitro activity against

Ravuconazole self-emulsifying delivery system: in vitro activity against

International journal of nanomedicine (2017-05-30)
Pollyanna Álvaro Spósito, Ana Lia Mazzeti, Caroline de Oliveira Faria, Julio A Urbina, Gwenaelle Pound-Lana, Maria Terezinha Bahia, Vanessa Furtado Mosqueira
摘要

Self-emulsifying drug delivery systems (SEDDSs) are lipid-based anhydrous formulations composed of an isotropic mixture of oil, surfactant, and cosurfactants usually presented in gelatin capsules. Ravuconazole (Biopharmaceutics Classification System [BCS] Class II) is a poorly water-soluble drug, and a SEDDS type IIIA was designed to deliver it in a predissolved state, improving dissolution in gastrointestinal fluids. After emulsification, the droplets had mean hydrodynamic diameters <250 nm, zeta potential values in the range of -45 mV to -57 mV, and showed no signs of ravuconazole precipitation. Asymmetric flow field-flow fractionation with dynamic and multiangle laser light scattering was used to characterize these formulations in terms of size distribution and homogeneity. The fractograms obtained at 37°C showed a polydisperse profile for all blank and ravuconazole-SEDDS formulations but no large aggregates. SEDDS increased ravuconazole in vitro dissolution extent and rate (20%) compared to free drug (3%) in 6 h. The in vivo toxicity of blank SEDDS comprising Labrasol

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雷夫康唑, ≥97% (NMR)