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dc.contributor.authorHEALY, ANNE MARIE
dc.contributor.authorCORRIGAN, OWEN
dc.contributor.authorTAJBER, LIDIA
dc.contributor.authorPALUCH, KRZYSZTOF
dc.date.accessioned2011-07-07T13:36:22Z
dc.date.available2011-07-07T13:36:22Z
dc.date.issued2011
dc.date.submitted2011en
dc.identifier.citationPaluch, K., Tajber, L., Elcoate, C.J., Corrigan, O.I., Lawrence, S.E., Healy A.M., Solid state characterisation of novel active pharmaceutical ingredients: co-crystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salt, Journal of Pharmaceutical Sciences, 100, 8, 2011, 3268 - 3283en
dc.identifier.otherY
dc.identifier.urihttp://hdl.handle.net/2262/57492
dc.descriptionPUBLISHEDen
dc.description.abstractThe production of salt or cocrystalline forms is a common approach to alter the physicochemical properties of pharmaceutical compounds. The goal of this work was to evaluate the impact of anion choice (succinate, adipate, and sulfate) on the physicochemical characteristics of salbutamol forms. Novel crystals of salbutamol were produced by solvent evaporation: a cocrystal of salbutamol hemiadipate with adipic acid (salbutamol adipate, SA), salbutamol hemisuccinate tetramethanolate (SSU.MeOH), and its desolvated form (SSU). The crystalline materials obtained were characterized using thermal, X-ray, nuclear magnetic resonance, Fourier transform infrared spectroscopy, dynamic vapor sorption (DVS), and elemental analysis. The crystal forms of SA and SSU.MeOH were determined to be triclinic, (P?i), and monoclinic, (P21/n), respectively. DVS analysis confirmed that SSU and SA do not undergo hydration under increased relative humidity. Both thermal and elemental analyses confirmed the stoichiometry of the salt forms. The aqueous solubilities of SA and SSU were measured to be 82? 2mg/mL (pH 4.5? 0.1) and 334? 13 mg/mL (pH 6.6? 0.1), respectively. Measured values corresponded well with the calculated pH solubility profiles. The intrinsic dissolution rate of cocrystallized SA was approximately four times lower than that of SSU, suggesting its use as an alternative to more rapidly dissolving salbutamol sulfate. ? 2011 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 100:3268?3283, 2011en
dc.description.sponsorshipThe authors wish to acknowledge the funding for this research from the Irish Research Council for Science and Engineering Technology and the Solid State Pharmaceutical Cluster, supported by Science Foundation Ireland under grant number [07/SRC/B1158].en
dc.format.extent3268en
dc.format.extent3283en
dc.language.isoenen
dc.publisherWileyen
dc.relation.ispartofseriesJournal of Pharmaceutical Sciences;
dc.relation.ispartofseries100;
dc.relation.ispartofseries8;
dc.rightsYen
dc.subjectPhysical chemistryen
dc.subjectcocrystalsen
dc.subjectcrystal structureen
dc.subjectdesolvationen
dc.titleSolid state characterisation of novel active pharmaceutical ingredients: co-crystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salten
dc.typeJournal Articleen
dc.contributor.sponsorIrish Research Council for Science Engineering and Technologyen
dc.contributor.sponsorScience Foundation Irelanden
dc.type.supercollectionscholarly_publicationsen
dc.type.supercollectionrefereed_publicationsen
dc.identifier.peoplefinderurlhttp://people.tcd.ie/paluchk
dc.identifier.peoplefinderurlhttp://people.tcd.ie/healyam
dc.identifier.peoplefinderurlhttp://people.tcd.ie/ocorrign
dc.identifier.peoplefinderurlhttp://people.tcd.ie/ltajber
dc.identifier.peoplefinderurlhttp://people.tcd.ie/paluchk
dc.identifier.rssinternalid73941
dc.contributor.sponsorGrantNumber07/SRC/B1158en
dc.identifier.rssurihttp://dx.doi.org/10.1002/jps.22569en


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