Solubilization by cosolvents: Establishing useful constants for the log-linear model

Jeffrey W. Millard, F. A. Alvarez-Núñez, S. H. Yalkowsky

Research output: Contribution to journalArticlepeer-review

201 Scopus citations

Abstract

The purpose of this study was to develop constants for the log-linear cosolvent model, thereby allowing accurate prediction of solubilization in the most common pharmaceutical cosolvents: propylene glycol, ethanol, polyethylene glycol 400, and glycerin. The solubilization power (σ) of each cosolvent was determined for a large number of organic compounds from the slope of their log-solubility vs. cosolvent volume fraction plots. The solubilization data at room temperature were either experimentally determined or obtained from the literature. The slopes of the nearly linear relationship between solubilization power and solute hydrophobicity (logKow) were obtained by linear regression analysis for each considered cosolvent. Thus, knowing or calculating a compound's partition coefficient is all that is needed to predict solubilization.

Original languageEnglish (US)
Pages (from-to)153-166
Number of pages14
JournalInternational Journal of Pharmaceutics
Volume245
Issue number1-2
DOIs
StatePublished - Oct 1 2002

Keywords

  • Cosolvent
  • Modeling
  • Partition coefficient
  • Solubility
  • Solubility enhancement
  • Solution

ASJC Scopus subject areas

  • Pharmaceutical Science

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