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    Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates.

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    Publication date
    30/07/2007
    Author
    Blagden, Nicholas
    de Matas, Marcel
    Gavan, Pauline T.
    York, Peter
    Keyword
    Crystal engineering
    Crystallisation
    Supramolecular chemistry
    Polymorphism
    Co-crystal
    Solubility
    Dissolution rate
    Bioavailability
    Low aqueous solubility
    Peer-Reviewed
    Yes
    
    Metadata
    Show full item record
    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.
    URI
    http://hdl.handle.net/10454/4844
    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
    http://dx.doi.org/10.1016/j.addr.2007.05.011
    Type
    Article
    Collections
    Life Sciences Publications

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