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dc.contributor.authorWyttenbach, Nicole
dc.contributor.authorKuentz, Martin
dc.date.accessioned2018-01-09T12:31:56Z
dc.date.available2018-01-09T12:31:56Z
dc.date.issued2017-03
dc.identifier.doi10.1016/j.ejpb.2016.11.031
dc.identifier.urihttp://hdl.handle.net/11654/25763
dc.description.abstractThis note is about the glass-forming ability (GFA) of drugs marketed as amorphous solid dispersions or as pure amorphous compounds. A thermoanalytical method was complemented with an in silico study, which made use of molecular properties that were identified earlier as being relevant for GFA. Thus, molar volume together with effective numbers of torsional bonds and hydrogen bonding were used to map drugs that are as amorphous products on the market either as solid dispersion of without co-processed carrier as amorphous drug in a solid dosage form. Differential scanning calorimetry experiments showed that most compounds were stable glass formers (GFs) (class III) followed by so-called unstable GFs (class II) and finally, only vemurafenib was found in class I with increased crystallization propensity. The in silico results, however showed that all drugs were either clearly in the chemical space expected for GFs or they were borderline to the region that holds for high crystallization tendency. Interestingly, the pure amorphous compounds scattered in a very confined region of the molecular predictors. These findings can guide amorphous product development of future drug candidates. Based on the compound location in the given chemical space, amorphous formulation opportunities can be balanced against the risks of physical instability upon storage.
dc.description.urihttps://ac.els-cdn.com/S0939641116305495/1-s2.0-S0939641116305495-main.pdf?_tid=c650d060-f538-11e7-80f0-00000aab0f01&acdnat=1515501165_4873e69f68205f103a6cbd60a1829381
dc.language.isoen_US
dc.relation.ispartofEuropean Journal of Pharmaceutics and Biopharmaceutics
dc.accessRightsAnonymous
dc.subjectAmorphous drug
dc.subjectSolid dispersion
dc.subjectGlass-forming ability
dc.subjectMolecular prediction
dc.titleGlass-forming ability of compounds in marketed amorphous drug products
dc.type01 - Zeitschriftenartikel, Journalartikel oder Magazin
dc.volume112
dc.audienceScience
fhnw.publicationStatePublished
fhnw.ReviewTypeAnonymous ex ante peer review of a complete publication
fhnw.InventedHereYes
fhnw.PublishedSwitzerlandYes
fhnw.pagination204-208
fhnw.IsStudentsWorkno
fhnw.publicationOnlineJa


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