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dc.contributor.authorHealy, Anne-Marieen
dc.contributor.authorO'Connell, Peteren
dc.date.accessioned2019-08-01T17:36:15Z
dc.date.available2019-08-01T17:36:15Z
dc.date.issued2018en
dc.date.submitted2018en
dc.identifier.citationSerrano DR, Walsh D, O'Connell P, Mugheirbi NA, Work, ZA, Bolas-Fernandez F, Galiana C, Dea-Ayuela MA, Healy AM, Optimising the in vitro and in vivo performance of oral cocrystal formulations via spray coating, European Journal of Pharmaceutics and Biopharmaceutics, 124, 2018, 13-27en
dc.identifier.otherYen
dc.identifier.urihttp://hdl.handle.net/2262/89138
dc.descriptionPUBLISHEDen
dc.description.abstractEngineering of pharmaceutical cocrystals is an advantageous alternative to salt formation for improving the aqueous solubility of hydrophobic drugs. Although, spray drying is a well-established scale-up technique in the production of cocrystals, several issues can arise such as sublimation or stickiness due to low glass transition temperatures of some organic molecules, making the process very challenging. Even though, fluidised bed spray coating has been successfully employed in the production of amorphous drug-coated particles, to the best of our knowledge, it has never been employed in the production of cocrystals. The feasibility of this technique was proven using three model cocrystals: sulfadimidine (SDM)/4-aminosalicylic acid (4ASA), sulfadimidine/nicotinic acid (NA) and ibuprofen (IBU)/ nicotinamide (NAM). Design of experiments were performed to understand the critical formulation and process parameters that determine the formation of either cocrystal or coamorphous systems for SDM/4ASA. The amount and type of binder played a key role in the overall solid state and in vitro performance characteristics of the cocrystals. The optimal balance between high loading efficiencies and high degree of crystallinity was achieved only when a binder: cocrystal weight ratio of 5:95 or 10:90 was used. The cocrystal coated beads showed an improved in vitro-in vivo performance characterised by: (i) no tendency to aggregate in aqueous media compared to spray dried formulations, (ii) enhanced in vitro activity (1.8-fold greater) against S. aureus, (iii) larger oral absorption and bioavailability (2.2-fold higher Cmax), (iv) greater flow properties and (v) improved chemical stability than cocrystals produced by other methods derived from the morphology and solid nature of the starter cores.en
dc.format.extent13-27en
dc.language.isoenen
dc.relation.ispartofseriesEuropean Journal of Pharmaceutics and Biopharmaceuticsen
dc.relation.ispartofseries124en
dc.rightsYen
dc.subjectCocrystalen
dc.subjectFluidised beden
dc.subjectBeadsen
dc.subjectSpray coatingen
dc.subjectSulfadimidineen
dc.subjectPelletsen
dc.subjectASAPen
dc.subjectAmorphousen
dc.subjectControlled releaseen
dc.titleOptimising the in vitro and in vivo performance of oral cocrystal formulations via spray coatingen
dc.typeJournal Articleen
dc.type.supercollectionscholarly_publicationsen
dc.type.supercollectionrefereed_publicationsen
dc.identifier.peoplefinderurlhttp://people.tcd.ie/healyamen
dc.identifier.peoplefinderurlhttp://people.tcd.ie/peoconneen
dc.identifier.rssinternalid186810en
dc.identifier.doihttp://dx.doi.org/10.1016/j.ejpb.2017.11.015en
dc.rights.ecaccessrightsopenAccess
dc.identifier.orcid_id0000-0001-5093-9786en


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