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  • Hydroxypropyl Methylcellulo...
    Friesen, Dwayne T; Shanker, Ravi; Crew, Marshall; Smithey, Daniel T; Curatolo, W. J; Nightingale, J. A. S

    Molecular pharmaceutics, 12/2008, Letnik: 5, Številka: 6
    Journal Article

    Spray-dried dispersions (SDDs) of low-solubility drugs have been prepared using the polymer hydroxypropyl methylcellulose acetate succinate (HPMCAS). For a variety of drug structures, these SDDs provide supersaturation in in vitro dissolution determinations and large bioavailability increases in vivo. In bile-salt/lecithin in vitro solutions, these SDDs provide amorphous drug/polymer colloids and an increased concentration of free drug and drug in micelles relative to crystalline or amorphous drug. As dry powders, the SDDs are a single amorphous phase in which the drug remains amorphous and dispersed and does not crystallize over storage times relevant for practical drug products. A melting temperature (T m)/glass-transition temperature (T g) (K/K) versus log P map for 139 compounds formulated as SDDs provides a perspective on an appropriate formulation strategy for low-solubility drugs with various physical properties.