ABSTRACT
INTRODUCTION Over the past two decades, advances in drug discovery techniques have been significant in identifying new and novel therapeutics agents in the pharmaceutical industry. Receptor mapping and molecular modeling coupled with high-throughput screening have revealed plethora drug candidates for numerous disease states. Because of the nature and the location of many of these receptors in a lipophilic membrane, drug candidates having the best molecular configuration and fitting into these receptors may, by design, be poorly water soluble in nature. It is estimated that over 40% of the new chemical entities in drug development are characterized as poorly water soluble (1). Lipitor (atorvastatin calcium), the top selling drug in 2007, and Prevacid (lansoprazole), also in the top 10 in sales in 2007, are examples of drugs with significant therapeutic impact, which are classified as poorly water soluble. It is certain that more will follow. However, poorly water-soluble drugs present a challenge to formulators of pharmaceutical oral solid dosage forms to improve the drug’s bioavailability while maintaining product stability, both physically and chemically, and providing a robust commercial process.
