Thermodynamics Research Center / ThermoML | Fluid Phase Equilibria

Determination and correlation of solubilities of famotidine in water + co-solvent mixed solvents

Matsuda, H.[Hiroyuki], Matsumoto, S.[Sho], Kaguragi, K.[Kenta], Kurihara, K.[Kiyofumi], Tochigi, K.[Katsumi], Tomono, K.[Kazuo]
Fluid Phase Equilib. 2011, 302, 1-2, 115-122
ABSTRACT
This study aims to measure the solubilities of poorly water-soluble drugs and to enhance their solubilities by adding co-solvents. The solubilities were measured using high-performance liquid chromatography (HPLC). We selected famotidine, a histamine H2-receptor antagonist, as the pharmaceutical compound. We measured the solubilities of famotidine at 298.15 K in five water/co-solvent mixed solvents, that is, two water + liquid co-solvent mixtures: water + ethanol, and water + polyethylene glycol (PEG) 400; and three water + solid co-solvent mixtures: water + a-cyclodextrin (a-CD), water + PEG 1000, and water + lauryl sulfate (SLS). In the two water + liquid co-solvent mixed solvents, the solubilities were measured over the entire co-solvent mole fraction range. In the three water + solid co-solvent mixtures, the solubility was determined up to the co-solvent saturation point. In addition, for the three solid co-solvents, i.e. a-CD, PEG 1000, and SLS, the solubilization power of each co-solvent solute system was evaluated using a log-linear model. The experimental solubility data for the two water + liquid co-solvent mixtures were correlated using three local composition models: modified Wilson, NRTL 1, and UNIQUAC. For the three water + solid co-solvent mixtures, a modified Chrastil model was used to correlate the experimental solubility data.
Compounds
# Formula Name
1 C8H15N7O2S3 famotidine
2 H2O water
3 C2H6O ethanol
Datasets
The table above is generated from the ThermoML associated json file (link above). POMD and RXND refer to PureOrMixture and Reaction Datasets. The compound numbers are included in properties, variables, and phases, if specificied; the numbers refer to the table of compounds on the left.
Type Compound-# Property Variable Constraint Phase Method #Points
  • POMD
  • 3
  • 2
  • 1
  • Mole fraction - 1 ; Liquid
  • Solvent: Mole fraction - 3; Liquid
  • Temperature, K; Liquid
  • Pressure, kPa; Liquid
  • Liquid
  • Crystal - 1
  • Chromatography
  • 13