Solid-state characterization of novel active pharmaceutical ingredients: Cocrystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salt.

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dc.contributor.author Paluch, Krzysztof J.
dc.contributor.author Tajber, Lidia
dc.contributor.author Elcoate, Curtis J.
dc.contributor.author Corrigan, Owen I.
dc.contributor.author Lawrence, Simon E.
dc.contributor.author Healy, Anne Marie
dc.date.accessioned 2014-02-27T11:56:49Z
dc.date.available 2014-02-27T11:56:49Z
dc.date.issued 2011-04
dc.identifier.citation Paluch,Krzysztof J.,Tajber,Lidia,Elcoate,Curtis J.,Corrigan,Owen I.,Lawrence,Simon E.,Healy,Anne Marie. (2011) 'Solid-state characterization of novel active pharmaceutical ingredients: Cocrystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salt'. Journal of Pharmaceutical Sciences, 100 (8):3268-3283. en
dc.identifier.volume 100 en
dc.identifier.issued 8 en
dc.identifier.startpage 3268 en
dc.identifier.endpage 3283 en
dc.identifier.issn 1520-6017
dc.identifier.uri http://hdl.handle.net/10468/1419
dc.identifier.doi 10.1002/jps.22569
dc.description.abstract The 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, (Pī), 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 ± 2 mg/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. en
dc.description.sponsorship Science Foundation Ireland (07/SRC/B1158) en
dc.format.mimetype application/pdf en
dc.language.iso en en
dc.publisher Wiley-Liss, Inc. en
dc.rights © 2011 Wiley-Liss, Inc. and the American Pharmacists Association. This is the pre-peer reviewed version of the following article: PALUCH, K. J., TAJBER, L., ELCOATE, C. J., CORRIGAN, O. I., LAWRENCE, S. E. & HEALY, A. M. 2011. Solid-state characterization of novel active pharmaceutical ingredients: Cocrystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salt. Journal of Pharmaceutical Sciences, 100, 3268-3283., which has been published in final form at http://dx.doi.org/10.1002/jps.22569. en
dc.subject Cocrystals en
dc.subject Crystal structure en
dc.subject Desolvation en
dc.subject Dissolution rate en
dc.subject Solubility en
dc.subject Solvate en
dc.subject Thermal analysis en
dc.subject Water sorption en
dc.subject X-ray powder diffraction en
dc.title Solid-state characterization of novel active pharmaceutical ingredients: Cocrystal of a salbutamol hemiadipate salt with adipic acid (2:1:1) and salbutamol hemisuccinate salt. en
dc.type Article (peer-reviewed) en
dc.internal.authorcontactother Simon Lawrence, Chemistry, University College Cork, Cork, Ireland. +353-21-490-3000 Email: simon.lawrence@ucc.ie en
dc.internal.availability Full text available en
dc.date.updated 2013-01-08T11:30:46Z
dc.description.version Accepted Version en
dc.internal.rssid 117321855
dc.contributor.funder Irish Research Council for Science Engineering and Technology en
dc.contributor.funder Science Foundation Ireland en
dc.description.status Peer reviewed en
dc.identifier.journaltitle Journal of Pharmaceutical Sciences en
dc.internal.copyrightchecked No Journal of Pharmaceutical Science was not on the spreadsheet, i notice it is a Wiley journal, so have submitted the accepted version. !!CORA!! Wiley permit selfarchiving with set statement en
dc.internal.licenseacceptance Yes en
dc.internal.IRISemailaddress simon.lawrence@ucc.ie en


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