Relationship between polysorbate 80 solubilization descriptors and octanol-water partition coefficients of drugs.
The molar solubilization capacities (kappa) and the molar micelle-water partition coefficients (K(M)(N)) in Polysorbate 80 of several drugs (including barbiturates, steroids, and benzoic acid derivatives) are related to their log octanol-water partition coefficients (logP). Both kappa and K(M)(N) values were calculated from solubility versus Polysorbate 80 concentration profiles, which were either experimentally determined or obtained from the literature. There is a linear relationship between logP of the tested compounds and the logarithm of the molar micelle-water partition coefficient (logK(M)(N)). On the other hand molar solubilization capacities are nearly independent of logP. It is shown that the ability of Polysorbate 80 to solubilize a drug can be predicted from its logP value.
Alvarez-Núñez
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Formulation R & D, Pharmaceutical Delivery Systems, Parke-Davis R&D, 07950, Morris Plains, NJ 07950, USA.
Yalkowsky
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D000442:Octanols / Q000737:chemistry; D004364:Pharmaceutical Preparations / Q000737:chemistry; D011136:Polysorbates / Q000737:chemistry*; D012995:Solubility; D014867:Water / Q000737:chemistry
D000442:Octanols; D004364:Pharmaceutical Preparations; D011136:Polysorbates; D014867:Water