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The role of ionic vs. non-ionic excipients in APIs-based eutectic systems

2021Journal article Open access
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dc.contributor.authorMartins, Mónia A.R.
dc.contributor.authorSilva, Liliana P.
dc.contributor.authorJorge, Patrícia S.
dc.contributor.authorAbranches, Dinis O.
dc.contributor.authorPinho, Simão
dc.contributor.authorCoutinho, João A.P.
dc.date.accessioned2018-02-19T10:00:00Z
dc.date.accessioned2021-11-22T15:11:47Z
dc.date.available2018-01-19T10:00:00Z
dc.date.available2021-11-22T15:11:47Z
dc.date.issued2021
dc.description.abstractAiming to contribute to drug pre-formulation, new eutectic mixtures were developed. Thymol, coumarin, or quaternary ammonium chlorides as excipients, were combined with the active pharmaceutical ingredients (APIs) acetylsalicylic acid, acetaminophen, ibuprofen, ketoprofen, or lidocaine. Their solid-liquid equilibrium (SLE) binary phase diagrams were measured to study eventual phase separation between the compounds, preventing manufacturing problems, and to study the molecular interactions between the APIs and ionic or non-ionic excipients. The Conductor-like Screening Model for Real Solvents (COSMO-RS) capability to predict the SLE of mixtures containing non-ionic excipients was further evaluated. COSMO-RS gives a good quantitative description of the experimental SLE being a tool with great potential in the screening of eutectic systems containing APIs and non-ionic excipients. While thymol presents strong interactions with the APIs, and consequently negative deviations to thermodynamic ideality, systems containing coumarin follow a quasi-ideal behavior. Regarding the ionic excipients, both choline chloride and the tetraalkylammonium chlorides are unable to establish relevant interactions with the APIs, and no significant negative deviations to ideality are observed. The liquefaction of the APIs here studied is favored by using non-ionic excipients, such as thymol, due to the strong interactions it can establish with the APIs.en_EN
dc.description.sponsorshipThis work was developed within the scope of the project CICECO Aveiro Institute of Materials, UIDB/50011/2020 & UIDP/50011/2020, and CIMO-Mountain Research Center, UIDB/00690/2020, both financed by national funds through the Portuguese Foundation for Science and Technology/MCTES. L.P.S. acknowledges FCT for her PhD grant (SFRH/BD/135976/2018).
dc.description.versioninfo:eu-repo/semantics/publishedVersionen_EN
dc.identifier.citationMartins, Mónia A.R.; Silva, Liliana P.; Jorge, Patrícia S.; Abranches, Dinis O.; Pinho, Simão P.; Coutinho, João A.P. (2021). The role of ionic vs. non-ionic excipients in APIs-based eutectic systems. European Journal of Pharmaceutical Sciences. ISSN 0928-0987. 156, p. 1-10en_EN
dc.identifier.doi10.1016/j.ejps.2020.105583en_EN
dc.identifier.issn0928-0987
dc.identifier.urihttp://hdl.handle.net/10198/24285
dc.language.isoeng
dc.peerreviewedyesen_EN
dc.relationPost-combustion gas capture/separation by gas-liquid membrane contactors using non-volatile solvents.
dc.relationCICECO-Aveiro Institute of Materials
dc.relationCICECO-Aveiro Institute of Materials
dc.subjectCOSMO-RSen_EN
dc.subjectDrug formulationen_EN
dc.subjectPhase diagramsen_EN
dc.subjectQuaternary ammonium chloridesen_EN
dc.subjectSolid-liquid equilibriumen_EN
dc.subjectThymolen_EN
dc.titleThe role of ionic vs. non-ionic excipients in APIs-based eutectic systemsen_EN
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitlePost-combustion gas capture/separation by gas-liquid membrane contactors using non-volatile solvents.
oaire.awardTitleCICECO-Aveiro Institute of Materials
oaire.awardTitleCICECO-Aveiro Institute of Materials
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/POR_CENTRO/SFRH%2FBD%2F135976%2F2018/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50011%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDP%2F50011%2F2020/PT
oaire.fundingStreamPOR_CENTRO
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream6817 - DCRRNI ID
person.familyNamePinho
person.givenNameSimão
person.identifier810882
person.identifier.ciencia-id481D-73AD-8D0F
person.identifier.orcid0000-0002-9211-857X
person.identifier.ridD-4148-2013
person.identifier.scopus-author-id7003570175
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccessen_EN
rcaap.typearticleen_EN
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relation.isAuthorOfPublication.latestForDiscovery8ef7789a-34f3-4915-a666-4efe26272a30
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