Kinetic solubility and lipophilicity evaluation connecting formulation technology strategy perspective

Lipophilicity and solubility are important physicochemical properties of pharmaceutical compounds, especially orally administration drugs. In this study, we developed a chromatographic distribution coefficient (LogD) determination method as lipophilicity evaluation and a kinetic solubility procedure with rapid quantitation by HPLC-UV. Both methods are simple and applicable for use of conventional equipment in early stage of drug discovery and development. Actually both data of model drugs were collected and discussed to improve the physicochemical properties using formulation technologies such as solubilization and enteric coating. The parallel measurement and consideration of both sets of data enables not only detail evaluation of the physicochemical properties but also the perspective of the relevant formulation strategies of drugs. Such rational evaluation will facilitate the development of high quality and effective drugs.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide