Amorphous drugs and dosage forms

Holger Grohganz, K. Löbmann, P. Priemel, Katrine Birgitte Tarp Jensen, K. Graeser, C. Strachan, T. Rades

    36 Citations (Scopus)

    Abstract

    The transformation to an amorphous form is one of the most promising approaches to address the low solubility of drug compounds, the latter being an increasing challenge in the development of new drug candidates. However, amorphous forms are high energy solids and tend to recry stallize. New formulation principles are needed to ensure the stability of amorphous drug forms. The formation of solid dispersions is still the most investigated approach, but additional approaches are desirable to overcome the shortcomings of solid dispersions. Spatial separation by either coating or the use of micro-containers has shown potential to prevent or delay recrystallization. Another recent approach is the formation of co-amorphous mixtures between either two drugs or one drug and one low molecular weight excipient. Molecular interactions between the two molecules provide an energy barrier that has to be overcome before single molecules are available for the formation of crystal nuclei, thus stabilizing the amorphous form.
    Original languageEnglish
    JournalJournal of Drug Delivery Science and Technology
    Volume23
    Issue number4
    Pages (from-to)403-408
    Number of pages6
    ISSN1773-2247
    Publication statusPublished - 1 Jul 2013

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