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Please use this identifier to cite or link to this item: http://hdl.handle.net/1843/61199
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dc.creatorWashington Xavier de Paulapt_BR
dc.creatorÂngelo Márcio Leite Denadaipt_BR
dc.creatorAline Nardoni Gonçalves Bragapt_BR
dc.creatorVenkatram Prasad Shastript_BR
dc.creatorSérgio Veloso Brant Pinheiropt_BR
dc.creatorFrédéric Jean Georges Frézardpt_BR
dc.creatorRobson Augusto Souza dos Santospt_BR
dc.creatorRubén Dario Sinisterra Millánpt_BR
dc.date.accessioned2023-11-21T19:28:54Z-
dc.date.available2023-11-21T19:28:54Z-
dc.date.issued2018-
dc.citation.volume44pt_BR
dc.citation.issue9pt_BR
dc.citation.spage1498pt_BR
dc.citation.epage1505pt_BR
dc.identifier.doihttps://doi.org/10.1080/03639045.2018.1467923pt_BR
dc.identifier.issn1520-5762pt_BR
dc.identifier.urihttp://hdl.handle.net/1843/61199-
dc.description.resumoLosartan (Los), a non-peptidic orally active agent, reduces arterial pressure through specific and selective blockade of angiotensin II receptor AT1. However, this widely used AT1 antagonist presents low bioavailability and needs once or twice a day dosage. In order to improve its bioavailability, we used the host: guest strategy based on β-cyclodextrin (βCD). The results suggest that Los included in βCD showed a typical pulsatile release pattern after oral administration to rats, with increasing the levels of plasma of Los. In addition, the inclusion compound presented oral efficacy for 72 h, in contrast to Los alone, which shows antagonist effect for only 6 h. In transgenic (mREN2)L27 rats, the Los/βCD complex reduced blood pressure for about 6 d, whereas Los alone reduced blood pressure for only 2 d. More importantly, using this host: guest strategy, sustained release of Los for over a week via the oral route can be achieved without the need for encapsulation in a polymeric carrier. The proposed preformulation increased the efficacy reducing the dose or spacing between each dose intake.pt_BR
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológicopt_BR
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Geraispt_BR
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superiorpt_BR
dc.description.sponsorshipFINEP - Financiadora de Estudos e Projetos, Financiadora de Estudos e Projetospt_BR
dc.description.sponsorshipINCT – Instituto nacional de ciência e tecnologia (Antigo Instituto do Milênio)pt_BR
dc.description.sponsorshipOutra Agênciapt_BR
dc.languageengpt_BR
dc.publisherUniversidade Federal de Minas Geraispt_BR
dc.publisher.countryBrasilpt_BR
dc.publisher.departmentICB - DEPARTAMENTO DE FISIOLOGIA E BIOFÍSICApt_BR
dc.publisher.departmentICX - DEPARTAMENTO DE QUÍMICApt_BR
dc.publisher.departmentMED - DEPARTAMENTO DE PEDIATRIApt_BR
dc.publisher.initialsUFMGpt_BR
dc.relation.ispartofDrug Development and Industrial Pharmacypt_BR
dc.rightsAcesso Restritopt_BR
dc.subjectInclusion compoundpt_BR
dc.subjectControlled releasept_BR
dc.subjectPharmacokineticspt_BR
dc.subjectAbsorptionpt_BR
dc.subjectReceptorspt_BR
dc.subject.otherAgentes hipotensorespt_BR
dc.subject.otherTecnologia de liberação controladapt_BR
dc.subject.otherFarmacocinéticapt_BR
dc.subject.otherAbsorção (Fisiologia)pt_BR
dc.subject.otherBiodisponibilidadept_BR
dc.subject.otherCiclodextrinaspt_BR
dc.titleA long-lasting oral preformulation of the angiotensin II AT1 receptor antagonist losartanpt_BR
dc.typeArtigo de Periódicopt_BR
dc.url.externahttps://www.tandfonline.com/doi/full/10.1080/03639045.2018.1467923pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0001-8259-6933pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0001-5125-9678pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0003-3783-5717pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0001-7656-1849pt_BR
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