CPSA Shanghai 2011
Changing Paradigm in Drug Discovery & Development:
East Meets West
April 13 - 16, 2011
Renaissance Shanghai Pudong Hotel
Shanghai, China
Abstract
Wednesday AM - Parallel Session II
Enhancing Oral Bioavailability through Enabled Formulation
Qun Lu, Ph.D.
Fellow, Pharmaceutical Sciences and Clinical Supplies
Merck
Oral dosage forms are the most popular and convenient methods of drug delivery. The solubility/dissolution behavior of drug is one important factor affecting the drug release from oral dosage forms in the gastrointestinal fluids and the subsequent absorption into the systemic circulation. It is estimated that poorly water-soluble drugs account for more than 40% of marketed products and almost 90% of compounds in development. Therefore achieving the desired bioavailability of poorly water-soluble drugs becomes one of the most challenging aspects in design and development of an oral dosage form.
Several solubilization technologies to improve the oral bioavailability of poorly water-soluble drugs will be reviewed. A case study will also be given to address the challenges encountered during the formulation development of a poorly water-soluble compound. Significant enhancement in bioavailability, reduction in inter-subject variability, and minimization of food effect were achieved by incorporating the appropriate solubilization technology and functional excipients.