Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates.
Blagden, Nicholas de Matas, Marcel Gavan, Pauline T. York, Peter
Blagden, Nicholas
de Matas, Marcel
Gavan, Pauline T.
York, Peter
Publication Date
30/07/2007
End of Embargo
Supervisor
Rights
Peer-Reviewed
Yes
Open Access status
closedAccess
Accepted for publication
Institution
Department
Awarded
Embargo end date
Collections
Additional title
Abstract
The increasing prevalence of poorly soluble drugs in development provides notable risk of new products demonstrating low and erratic
bioavailabilty with consequences for safety and efficacy, particularly for drugs delivered by the oral route of administration. Although numerous
strategies exist for enhancing the bioavailability of drugs with low aqueous solubility, the success of these approaches is not yet able to be
guaranteed and is greatly dependent on the physical and chemical nature of the molecules being developed. Crystal engineering offers a number of
routes to improved solubility and dissolution rate, which can be adopted through an in-depth knowledge of crystallisation processes and the
molecular properties of active pharmaceutical ingredients. This article covers the concept and theory of crystal engineering and discusses the
potential benefits, disadvantages and methods of preparation of co-crystals, metastable polymorphs, high-energy amorphous forms and ultrafine
particles. Also considered within this review is the influence of crystallisation conditions on crystal habit and particle morphology with potential
implications for dissolution and oral absorption.
Version
No full-text in the repository
Citation
Blagden, N., De Matas, M., Gavan, P. T. and York, P. (2007). Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates. Advanced drug delivery reviews. Vol. 59, No. 7, pp. 617-630.
Link to publisher’s version
Link to published version
Link to Version of Record
Type
Article