Chemistry Reference
In-Depth Information
12
SCIENTIFIC AND REGULATORY
CONSIDERATIONS IN PRODUCT
DEVELOPMENT
∗
Abhay Gupta, Ziyaur Rahman, and Mansoor A. Khan
Division of Product Quality Research, Of
ce of Pharmaceutical Science,
U.S. Food and Drug Administration, Silver Spring, MD, USA
12.1 INTRODUCTION
Ease of administration makes the oral route the most preferred route of drug delivery.
Orally administered drugs must dissolve in the gastrointestinal tract to get absorbed and
become bioavailable. Hence, the aqueous solubility of the drug substances becomes
important. With a large number of new drug substances showing very low aqueous
solubility, their development into commercially successful drug products is severely
hampered by their limited bioavailability, unless appropriate pharmaceutical and for-
mulation approaches are employed. Amorphous solid dispersions offer a practical and
viable approach to enhance the oral bioavailability of these compounds, without the
limitations of some other commonly used approaches such as particle size reduction, salt
formation, and/or use of cosolvent systems. This chapter focuses on the scienti
c and
regulatory considerations for developing amorphous solid dispersions of small-molecule
drugs with poor aqueous solubility for oral administration.
∗
The findings and conclusions in this chapter have not been formally disseminated by the Food and Drug
Administration and should not be construed to represent any Agency determination or policy.
