A long-lasting oral preformulation of the angiotensin II AT1 receptor antagonist losartan

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dc.creatorWashington Xavier de Paula
dc.creatorÂngelo Márcio Leite Denadai
dc.creatorAline Nardoni Gonçalves Braga
dc.creatorVenkatram Prasad Shastri
dc.creatorSérgio Veloso Brant Pinheiro
dc.creatorFrédéric Jean Georges Frézard
dc.creatorRobson Augusto Souza dos Santos
dc.creatorRubén Dario Sinisterra Millán
dc.date.accessioned2023-11-21T19:28:54Z
dc.date.accessioned2025-09-09T01:23:49Z
dc.date.available2023-11-21T19:28:54Z
dc.date.issued2018
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Gerais
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.description.sponsorshipFINEP - Financiadora de Estudos e Projetos, Financiadora de Estudos e Projetos
dc.description.sponsorshipINCT – Instituto nacional de ciência e tecnologia (Antigo Instituto do Milênio)
dc.description.sponsorshipOutra Agência
dc.identifier.doihttps://doi.org/10.1080/03639045.2018.1467923
dc.identifier.issn1520-5762
dc.identifier.urihttps://hdl.handle.net/1843/61199
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofDrug Development and Industrial Pharmacy
dc.rightsAcesso Restrito
dc.subjectAgentes hipotensores
dc.subjectTecnologia de liberação controlada
dc.subjectFarmacocinética
dc.subjectAbsorção (Fisiologia)
dc.subjectBiodisponibilidade
dc.subjectCiclodextrinas
dc.subject.otherInclusion compound
dc.subject.otherControlled release
dc.subject.otherPharmacokinetics
dc.subject.otherAbsorption
dc.subject.otherReceptors
dc.titleA long-lasting oral preformulation of the angiotensin II AT1 receptor antagonist losartan
dc.typeArtigo de periódico
local.citation.epage1505
local.citation.issue9
local.citation.spage1498
local.citation.volume44
local.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.
local.identifier.orcidhttps://orcid.org/0000-0001-8259-6933
local.identifier.orcidhttps://orcid.org/0000-0001-5125-9678
local.identifier.orcidhttps://orcid.org/0000-0003-3783-5717
local.identifier.orcidhttps://orcid.org/0000-0001-7656-1849
local.publisher.countryBrasil
local.publisher.departmentICB - DEPARTAMENTO DE FISIOLOGIA E BIOFÍSICA
local.publisher.departmentICX - DEPARTAMENTO DE QUÍMICA
local.publisher.departmentMED - DEPARTAMENTO DE PEDIATRIA
local.publisher.initialsUFMG
local.url.externahttps://www.tandfonline.com/doi/full/10.1080/03639045.2018.1467923

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