Hydroxypropyl methylcellulose acetate succinate-based spray-dried dispersions: an overview

Mol Pharm. 2008 Nov-Dec;5(6):1003-19. doi: 10.1021/mp8000793.

Abstract

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.

Publication types

  • Review

MeSH terms

  • Absorption
  • Administration, Oral
  • Aerosols
  • Animals
  • Capsules
  • Chemical Phenomena
  • Colloids
  • Freeze Drying
  • Glass / chemistry
  • Humans
  • Methylcellulose / analogs & derivatives*
  • Methylcellulose / chemistry
  • Methylcellulose / pharmacokinetics
  • Micelles
  • Polymers / chemistry*
  • Temperature

Substances

  • Aerosols
  • Capsules
  • Colloids
  • Micelles
  • Polymers
  • hydroxypropylmethylcellulose acetate succinate
  • Methylcellulose