The Development of a Thermodynamic Solubility Assay to Predict Possible Formulations of Low Aqueous Soluble Compounds
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In recent years, drug discovery and development has become less productive. In the early stages, a kinetic system has been adopted to screen out low-aqueous soluble compounds, which are associated with high developmental barriers. However, this method dismisses compounds based on a property that can be increased through the use of solvent and/or excipient systems. The experiment described in this paper is to develop a thermodynamic solubility assay that can be used as a predictor of formulations for low aqueous soluble compounds. In order to be most universal, the compounds analyzed in this experiment represent a range of pKa's, partition coefficients, molecular weights, and melting points. Compounds are analyzed in a panel of solvents that include buffers and surfactants followed by the predictions of formulations based off of the data. This method efficiently identifies formulations that could be used in first-in-animal testing and ultimately in clinical studies.
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