Chemistry Reference
In-Depth Information
11
FORMULATION DEVELOPMENT
OF AMORPHOUS DISPERSIONS
Tapan Sanghvi,
1
Jeff Katstra,
2
Brian Patrick Quinn,
3
Hayden Thomas,
1
and Patricia Hurter
4
1
Formulation Development, Vertex Pharmaceuticals Incorporated,
Boston, MA, USA
2
Formulation Development, Vertex Pharmaceuticals Incorporated,
Cambridge, MA, USA
3
Parthenon - Ernst & Young, New York, NY, USA
4
Global Pharmaceutical Development and Regulatory Affairs, Vertex
Pharmaceuticals Incorporated, Boston, MA, USA
11.1 PREPARING DISPERSIONS FOR DRUG PRODUCTS
11.1.1 Introduction
A pharmaceutical development group may decide to move forward with an amorphous
dispersion for a number of reasons [1]. One of these reasons is solubility [2
-
4]. For a
promising compound with a high af
nity for its target that nonetheless has poor aqueous
solubility, creating an amorphous dispersion is onemeans for keeping themolecule in play.
Simply asking the medicinal chemistry group for more scaffolds may not always be an
option; for some protein targets, most effective ligands are likely to have the same or similar
characteristics. For example, as our colleagues discussed in Chapter 7, competitive
inhibitors of proteases, which generally have to bind tightly to an apolar active site, are
