Theoretical Considerations in Developing Amorphous Solid Dispersions

TY - CHAP

T1 - Theoretical Considerations in Developing Amorphous Solid Dispersions

AU - Laitinen, Riikka

AU - Priemel, Petra Alexandra

AU - Surwase, Sachin

AU - Graeser, Kirsten

AU - Strachan, Clare J.

AU - Grohganz, Holger

AU - Rades, Thomas

PY - 2014

Y1 - 2014

N2 - Before pursuing the laborious route of amorphous solid dispersion formulation and development, which is the topic of many of the subsequent chapters in this book, the formulation scientist would benefit from a priori knowledge whether the amorphous route is a viable one for a given drug and how much solubility improvement, and hence increase in bioavailability, can be expected, and what forms of solid dispersion have been developed in the past. In this chapter, we therefore initially define the various forms of solid dispersions, and then go on to discuss properties of pure drugs with respect to their glass-forming ability and glass stability. In the main parts of this chapter, we review theoretical approaches to determine amorphous drug polymer miscibility and crystalline drug polymer solubility, as a prerequisite to develop amorphous solid dispersions (glass solutions).

AB - Before pursuing the laborious route of amorphous solid dispersion formulation and development, which is the topic of many of the subsequent chapters in this book, the formulation scientist would benefit from a priori knowledge whether the amorphous route is a viable one for a given drug and how much solubility improvement, and hence increase in bioavailability, can be expected, and what forms of solid dispersion have been developed in the past. In this chapter, we therefore initially define the various forms of solid dispersions, and then go on to discuss properties of pure drugs with respect to their glass-forming ability and glass stability. In the main parts of this chapter, we review theoretical approaches to determine amorphous drug polymer miscibility and crystalline drug polymer solubility, as a prerequisite to develop amorphous solid dispersions (glass solutions).

U2 - 10.1007/978-1-4939-1598-9_2

DO - 10.1007/978-1-4939-1598-9_2

M3 - Book chapter

SN - 978-1-4939-1597-2

SP - 35

EP - 90

BT - Amorphous Solid Dispersions - Theory and Practice

A2 - Shah, Navnit

A2 - Sandhu, Harpreet

A2 - Choi, Duk Soon

A2 - Chokshi, Hitesh

A2 - Malick, A. Waseem

PB - Springer Science+Business Media

CY - New York

ER -