ABSTRACT

Navnit H. Shah, Wantanee Phuapradit, Yu-E Zhang, Hashim Ahmed, and A. Waseem Malick

Pharmaceutical and Analytical Research and Development, Roche, Nutley, New Jersey, U.S.A.

INTRODUCTION

The advent of combinatorial chemistry and high throughput screening as the primary technologies for drug discovery has resulted in the generation of a preponderance of potential drug candidates, which do not possess favorable “drug-like” biopharmaceutical properties. Specifically, these candidate compounds are highly lipophilic (Log P 5) and possess very poor solubility (10 mg/mL) in physiological fluids, resulting in poor and highly variable absorption, after oral administration, that is often strongly influenced by the presence of food in the gastrointestinal (GI) tract (1). In many instances, the GI absorption of these challenging compounds can be significantly improved through the use of lipid-based formulations (2,3).