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Hydroxypropyl Methylcellulose Acetate Succinate-Based Spray-Dried Dispersions: An Overview

2008; American Chemical Society; Volume: 5; Issue: 6 Linguagem: Inglês

10.1021/mp8000793

1543-8392

Dwayne T. Friesen, Ravi Shanker, M. Crew, D. T. Smithey, William Curatolo, James Nightingale,

Analytical Methods in Pharmaceuticals

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 (Tm)/glass-transition temperature (Tg) (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.