Case Studies: Rational Development of Self-Emulsifying Formulations for Improving the Oral Bioavailability of Poorly Soluble, Lipophilic Drugs

Ping Gao Small Molecule Pharmaceutics, Amgen, Inc., Thousand Oaks, California, U.S.A.

Walter Morozowich Prodrug/Formulation Consultant, Kalamazoo, Michigan, U.S.A.

INTRODUCTION

Oral administration of highly lipophilic, poorly water-soluble drugs often results in poor and highly variable bioavailability due to poor dissolution in vivo. One approach for improving the absorption of these drugs involves the use of self-emulsifying drug delivery systems (SEDDS) (1-6) which rapidly disperse following oral administration yielding an o/w emulsion or microemulsion containing the solubilized drug.