TY - JOUR
T1 - Solubilization by cosolvents
T2 - Establishing useful constants for the log-linear model
AU - Millard, Jeffrey W.
AU - Alvarez-Núñez, F. A.
AU - Yalkowsky, S. H.
PY - 2002/10/1
Y1 - 2002/10/1
N2 - 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.
AB - 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.
KW - Cosolvent
KW - Modeling
KW - Partition coefficient
KW - Solubility
KW - Solubility enhancement
KW - Solution
UR - http://www.scopus.com/inward/record.url?scp=0036805534&partnerID=8YFLogxK
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U2 - 10.1016/S0378-5173(02)00334-4
DO - 10.1016/S0378-5173(02)00334-4
M3 - Article
C2 - 12270252
AN - SCOPUS:0036805534
SN - 0378-5173
VL - 245
SP - 153
EP - 166
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -