Characterisation, solubility and intrinsic dissolution behaviour of benzamide: dibenzyl sulfoxide cocrystal

dc.contributor.authorGrossjohann, Christine
dc.contributor.authorEccles, Kevin S.
dc.contributor.authorMaguire, Anita R.
dc.contributor.authorLawrence, Simon E.
dc.contributor.authorTajber, Lidia
dc.contributor.authorCorrigan, Owen I.
dc.contributor.authorHealy, Anne Marie
dc.contributor.funderScience Foundation Irelanden
dc.date.accessioned2013-01-23T22:01:09Z
dc.date.available2013-01-23T22:01:09Z
dc.date.copyright2012
dc.date.issued2012-01
dc.date.updated2013-01-08T11:24:58Z
dc.description.abstractThis study examined the 1:1 cocrystal benzamide: dibenzyl sulfoxide, comprising the poorly water soluble dibenzyl sulfoxide (DBSO) and the more soluble benzamide (BA), to establish if this cocrystal shows advantages in terms of solubility and dissolution in comparison to its pure components and to a physical mixture. Solubility studies were performed by measuring DBSO solubility as a function of BA concentration, and a ternary phase diagram was constructed. Dissolution was examined through intrinsic dissolution studies. Solid-state characterisation was carried out by powder X-ray diffraction (PXRD), energy-dispersive X-ray diffraction (EDX), infra-red spectroscopy (ATR-FTIR) and thermal analysis. DBSO solubility was increased by means of complexation with BA. For the cocrystal, the solubility of both components was decreased in comparison to pure components. The cocrystal was identified as metastable and incongruently saturating. Dissolution studies revealed that dissolution of DBSO from the cocrystal was not enhanced in comparison to the pure compound or a physical mix, while BA release was retarded and followed square root of time kinetics. At the disk surface a layer of DBSO was found. The extent of complexation in solution can change the stability of the complex substantially. Incongruent solubility and dissolution behaviour of a cocrystal can result in no enhancement in the dissolution of the less soluble component and retardation of release of the more soluble component.en
dc.description.sponsorshipScience Foundation grant numbers 07/SRC/B1158 (Solid State Pharmaceutical Cluster) and 08/RFP/MTR1664.en
dc.description.statusPeer revieweden
dc.description.versionAccepted Versionen
dc.format.mimetypeapplication/pdfen
dc.identifier.citationGrossjohann, C., Eccles, K.S., Maguire, A.R., Lawrence, S.E.,Tajber, L., Corrigan, O.I., Healy, A.M. (2012) 'Characterisation, solubility and intrinsic dissolution behaviour of benzamide: dibenzyl sulfoxide cocrystal'. International Journal of Pharmaceutics, 422 :24-32. http://dx.doi.org/10.1016/j.ijpharm.2011.10.016en
dc.identifier.doi10.1016/j.ijpharm.2011.10.016
dc.identifier.endpage32en
dc.identifier.issn0378-5173
dc.identifier.issued17en
dc.identifier.journaltitleInternational Journal of Pharmaceuticsen
dc.identifier.startpage24en
dc.identifier.urihttps://hdl.handle.net/10468/921
dc.identifier.volume422en
dc.language.isoenen
dc.publisherElsevieren
dc.rightsCopyright © 2012, Elsevier. NOTICE: this is the author’s version of a work that was accepted for publication in International Journal of Pharmaceutics. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in International Journal of Pharmaceutics, [422, January 2012] http://dx.doi.org/10.1016/j.ijpharm.2011.10.016en
dc.subjectIntrinsic dissolutionen
dc.subjectSolubilityen
dc.subjectComplexationen
dc.subjectHPLCen
dc.subjectIndomethacin-saccharin cocrystalsen
dc.subjectPharmaceutical cocrystalsen
dc.subjectPhase-diagramsen
dc.subjectRotating disken
dc.subjectCocrystalen
dc.subjectAciden
dc.subjectBioavailabilityen
dc.subjectCompositesen
dc.subjectGabapentinen
dc.subjectApparatusen
dc.subject.lcshBenzamideen
dc.subject.lcshCrystalsen
dc.titleCharacterisation, solubility and intrinsic dissolution behaviour of benzamide: dibenzyl sulfoxide cocrystalen
dc.typeArticle (peer-reviewed)en
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