Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos

Detalhes bibliográficos
Ano de defesa: 2020
Autor(a) principal: Carvalho, Murilo Ferreira de lattes
Orientador(a): Gil, Eric de Souza lattes
Banca de defesa: Garcia, Luane Ferreira, Leite, Karla Carneiro de Siqueira, Alecrim, Morgana Fernandes, Marreto, Ricardo Neves, Oliveira, Thiago Levi Silva
Tipo de documento: Tese
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Universidade Federal de Goiás
Programa de Pós-Graduação: Programa de Pós-graduação em Ciências Farmacêuticas (FF)
Departamento: Faculdade de Farmácia - FF (RG)
País: Brasil
Palavras-chave em Português:
Palavras-chave em Inglês:
Área do conhecimento CNPq:
Link de acesso: http://repositorio.bc.ufg.br/tede/handle/tede/10852
Resumo: Introduction: The pharmaceutical industry faces a major challenge to improve the solubility of some active ingredients. Carvedilol (CRV) is the drug of therapeutic choice in cardiovascular diseases. CRV presents low water solubility and low bioavaliability. Several researches were performed in order to increase the oral bioavailability, where selfemulsifying appeared as viable alternatives. Objective: The objective of this work was to evaluate interactions between CRV and its excipients, detecting the oxidative potential of these substances, thus, providing predictive data for the oxidation that may affect the stability and bioavailability of the drug system. Methodology: In the carbon pastes preparation were used 70 mg (graphite) and 30 mg (oil). Six excipients, oleic acid, canola, capmul, safflower, sesame and Plurol isoestearique. The following proportions were used in the making of the paste: 30:0, 20:10, 15:15, 10:20 and 0:30 of liquid excipient (sample): mineral oil (mg:mg) and 1.5:68.5, 3:67 and 7:63 of solid excipient (sample): graphite (mg:mg). CRV was incorporated in the oil moiety for solubilization and after used in solidstate analysis in the carbon paste. The techniques used were cyclic voltammetry, differential pulse voltammetry and electrochemical impedance spectroscopy. Results and Discussions: The Isostearique Plurol® was found to be electro-active in the studied potential, however, this oil oxidizes in different potentials from CRV. The results show that Isostearique Plurol®, liquid excipient, isoestearique acid and the solid excipient presented the greatest variations of anodic potential and were considered the best excipients for the CRV formulation. CRV presented higher stability at room temperature (25 ºC), whereas, it presented higher stability at 50 ºC when mixed with 7% estearique acid. Conclusions: Evidences of incompatibility were not found, relative to the increase of oxidation vulnerability, when in the presence of these excipients. The employment of electroanalysis for CRV compatibility studies show promising viability.
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spelling Gil, Eric de Souzahttp://lattes.cnpq.br/3218622824233303Garcia, Luane Ferreirahttp://lattes.cnpq.br/6624146379323596Garcia, Luane FerreiraLeite, Karla Carneiro de SiqueiraAlecrim, Morgana FernandesMarreto, Ricardo NevesOliveira, Thiago Levi Silvahttp://lattes.cnpq.br/2242548114202074Carvalho, Murilo Ferreira de2020-10-09T13:10:52Z2020-10-09T13:10:52Z2020-08-31Carvalho, M. F. Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos. 2020. 43 f. Tese (Doutorado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2020.http://repositorio.bc.ufg.br/tede/handle/tede/10852Introduction: The pharmaceutical industry faces a major challenge to improve the solubility of some active ingredients. Carvedilol (CRV) is the drug of therapeutic choice in cardiovascular diseases. CRV presents low water solubility and low bioavaliability. Several researches were performed in order to increase the oral bioavailability, where selfemulsifying appeared as viable alternatives. Objective: The objective of this work was to evaluate interactions between CRV and its excipients, detecting the oxidative potential of these substances, thus, providing predictive data for the oxidation that may affect the stability and bioavailability of the drug system. Methodology: In the carbon pastes preparation were used 70 mg (graphite) and 30 mg (oil). Six excipients, oleic acid, canola, capmul, safflower, sesame and Plurol isoestearique. The following proportions were used in the making of the paste: 30:0, 20:10, 15:15, 10:20 and 0:30 of liquid excipient (sample): mineral oil (mg:mg) and 1.5:68.5, 3:67 and 7:63 of solid excipient (sample): graphite (mg:mg). CRV was incorporated in the oil moiety for solubilization and after used in solidstate analysis in the carbon paste. The techniques used were cyclic voltammetry, differential pulse voltammetry and electrochemical impedance spectroscopy. Results and Discussions: The Isostearique Plurol® was found to be electro-active in the studied potential, however, this oil oxidizes in different potentials from CRV. The results show that Isostearique Plurol®, liquid excipient, isoestearique acid and the solid excipient presented the greatest variations of anodic potential and were considered the best excipients for the CRV formulation. CRV presented higher stability at room temperature (25 ºC), whereas, it presented higher stability at 50 ºC when mixed with 7% estearique acid. Conclusions: Evidences of incompatibility were not found, relative to the increase of oxidation vulnerability, when in the presence of these excipients. The employment of electroanalysis for CRV compatibility studies show promising viability.Introdução: A indústria farmacêutica enfrenta um grande desafio no sentido de melhorar a solubilidade de alguns insumos ativos. O Carvedilol (CRV) é um dos fármacos de escolha para o tratamento das doenças cardiovasculares, que apresenta baixa solubilidade em água e baixa biodisponibilidade, motivando a realização de pesquisas para melhorar a biodisponibilidade por via oral, sendo os sistemas auto-emulsificantes uma alternativa promissora. Objetivo: O objetivo deste trabalho foi avaliar as interações entre o CRV e os excipientes, detectando o potencial oxidante dessas substâncias e fornecendo dados preditivos da estabilidade do sistema e biodisponibilidade do fármaco. Metodologia: No preparo das pastas foram utilizados 70 mg (grafite) e 30 mg (óleo). Os excipientes, ácido oleico, canola, capmul, cártamo, gergelim e plurol isostearique, foram utilizados no preparo das pastas, na proporção de 30:0, 20:10, 15:15, 10:20 e 0:30 deexcipiente líquido (amostra): óleo mineral (mg:mg) ou 1,5:68,5, 3:67 e 7:63 de excipiente sólido (amostra): grafite (mg:mg). O CRV foi incorporado na porção oleosa para solubilização e após o preparo da pasta de carbono foi utilizado nas análises em estado sólido. As técnicas utilizadas no estudo foram voltametria cíclica, de pulso diferencial e espectroscopia de impedância eletroquímica. Resultados e discussões: O Plurol® isostearique foi eletroativo na faixa de potencial estudada, porém, esse óleo se oxida em potenciais diferentes do CRV, não inviabilizando a análise. Os resultados mostraram que o Plurol® isostearique, excipiente líquido, e ácido esteárico, excipiente sólido, apresentaram as maiores variações de potencial de pico anódico e foram considerados os melhores excipientes para a formulação de CRV. O fármaco analisado apresentou maior estabilidade à temperatura ambiente e a 50 °C quando misturada com ácido esteárico a 7%. Conclusões: Nos ensaios realizados não se observou evidências de incompatibilidade, relativa ao aumento da vulnerabilidade à oxidação, quando na presença de todos estes excipientes. Estudos em longo prazo são uma possibilidade real para avaliar o emprego da eletroanálise em estudos de compatibilidade do CRV no desenvolvimento de formulações.Submitted by Valéria Martins (valeriamartins@ufg.br) on 2020-10-08T14:04:52Z No. of bitstreams: 2 license_rdf: 805 bytes, checksum: 4460e5956bc1d1639be9ae6146a50347 (MD5) Tese - Murilo Ferreira de Carvalho - 2020.pdf: 10209755 bytes, checksum: ea03260bad2b8e2f085a56aa1bc1bdb9 (MD5)Rejected by Luciana Ferreira (lucgeral@gmail.com), reason: Observe como digitou as palavras-chave (A primeira letra da primeira palavra deve ser sempre maiúscula, caso seja uma expressão, também, somente a primeira letra da primeira palavra fica em maiúsculo, a não ser que seja nome próprio): ERRADO Espectroscopia de Impedância Eletroquímica Bloqueador de Receptores Adrenérgicos Tecnologia Farmacêutica Electrochemical Impedance Spectroscopy Adrenergic Receptor Blocker Pharmaceutical Technology CERTO Espectroscopia de impedância eletroquímica Bloqueador de receptores adrenérgicos Tecnologia farmacêutica Electrochemical impedance spectroscopy Adrenergic receptor blocker Pharmaceutical technology on 2020-10-08T15:12:33Z (GMT)Submitted by Valéria Martins (valeriamartins@ufg.br) on 2020-10-09T11:36:25Z No. of bitstreams: 2 license_rdf: 805 bytes, checksum: 4460e5956bc1d1639be9ae6146a50347 (MD5) Tese - Murilo Ferreira de Carvalho - 2020.pdf: 10209755 bytes, checksum: ea03260bad2b8e2f085a56aa1bc1bdb9 (MD5)Approved for entry into archive by Luciana Ferreira (lucgeral@gmail.com) on 2020-10-09T13:10:52Z (GMT) No. of bitstreams: 2 license_rdf: 805 bytes, checksum: 4460e5956bc1d1639be9ae6146a50347 (MD5) Tese - Murilo Ferreira de Carvalho - 2020.pdf: 10209755 bytes, checksum: ea03260bad2b8e2f085a56aa1bc1bdb9 (MD5)Made available in DSpace on 2020-10-09T13:10:52Z (GMT). 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dc.title.pt_BR.fl_str_mv Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
dc.title.alternative.eng.fl_str_mv Electroanalysis applied to compatibility and stability assays of medicines
title Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
spellingShingle Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
Carvalho, Murilo Ferreira de
Voltametria
Espectroscopia de impedância eletroquímica
Bloqueador de receptores adrenérgicos
Tecnologia farmacêutica
Formulação
Excipientes
Voltammetry
Electrochemical impedance spectroscopy
Adrenergic receptor blocker
Pharmaceutical technology
Formulation
Excipients
CIENCIAS BIOLOGICAS::FARMACOLOGIA::FARMACOLOGIA GERAL
title_short Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
title_full Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
title_fullStr Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
title_full_unstemmed Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
title_sort Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos
author Carvalho, Murilo Ferreira de
author_facet Carvalho, Murilo Ferreira de
author_role author
dc.contributor.advisor1.fl_str_mv Gil, Eric de Souza
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/3218622824233303
dc.contributor.advisor-co1.fl_str_mv Garcia, Luane Ferreira
dc.contributor.advisor-co1Lattes.fl_str_mv http://lattes.cnpq.br/6624146379323596
dc.contributor.referee1.fl_str_mv Garcia, Luane Ferreira
dc.contributor.referee2.fl_str_mv Leite, Karla Carneiro de Siqueira
dc.contributor.referee3.fl_str_mv Alecrim, Morgana Fernandes
dc.contributor.referee4.fl_str_mv Marreto, Ricardo Neves
dc.contributor.referee5.fl_str_mv Oliveira, Thiago Levi Silva
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/2242548114202074
dc.contributor.author.fl_str_mv Carvalho, Murilo Ferreira de
contributor_str_mv Gil, Eric de Souza
Garcia, Luane Ferreira
Garcia, Luane Ferreira
Leite, Karla Carneiro de Siqueira
Alecrim, Morgana Fernandes
Marreto, Ricardo Neves
Oliveira, Thiago Levi Silva
dc.subject.por.fl_str_mv Voltametria
Espectroscopia de impedância eletroquímica
Bloqueador de receptores adrenérgicos
Tecnologia farmacêutica
Formulação
Excipientes
topic Voltametria
Espectroscopia de impedância eletroquímica
Bloqueador de receptores adrenérgicos
Tecnologia farmacêutica
Formulação
Excipientes
Voltammetry
Electrochemical impedance spectroscopy
Adrenergic receptor blocker
Pharmaceutical technology
Formulation
Excipients
CIENCIAS BIOLOGICAS::FARMACOLOGIA::FARMACOLOGIA GERAL
dc.subject.eng.fl_str_mv Voltammetry
Electrochemical impedance spectroscopy
Adrenergic receptor blocker
Pharmaceutical technology
Formulation
Excipients
dc.subject.cnpq.fl_str_mv CIENCIAS BIOLOGICAS::FARMACOLOGIA::FARMACOLOGIA GERAL
description Introduction: The pharmaceutical industry faces a major challenge to improve the solubility of some active ingredients. Carvedilol (CRV) is the drug of therapeutic choice in cardiovascular diseases. CRV presents low water solubility and low bioavaliability. Several researches were performed in order to increase the oral bioavailability, where selfemulsifying appeared as viable alternatives. Objective: The objective of this work was to evaluate interactions between CRV and its excipients, detecting the oxidative potential of these substances, thus, providing predictive data for the oxidation that may affect the stability and bioavailability of the drug system. Methodology: In the carbon pastes preparation were used 70 mg (graphite) and 30 mg (oil). Six excipients, oleic acid, canola, capmul, safflower, sesame and Plurol isoestearique. The following proportions were used in the making of the paste: 30:0, 20:10, 15:15, 10:20 and 0:30 of liquid excipient (sample): mineral oil (mg:mg) and 1.5:68.5, 3:67 and 7:63 of solid excipient (sample): graphite (mg:mg). CRV was incorporated in the oil moiety for solubilization and after used in solidstate analysis in the carbon paste. The techniques used were cyclic voltammetry, differential pulse voltammetry and electrochemical impedance spectroscopy. Results and Discussions: The Isostearique Plurol® was found to be electro-active in the studied potential, however, this oil oxidizes in different potentials from CRV. The results show that Isostearique Plurol®, liquid excipient, isoestearique acid and the solid excipient presented the greatest variations of anodic potential and were considered the best excipients for the CRV formulation. CRV presented higher stability at room temperature (25 ºC), whereas, it presented higher stability at 50 ºC when mixed with 7% estearique acid. Conclusions: Evidences of incompatibility were not found, relative to the increase of oxidation vulnerability, when in the presence of these excipients. The employment of electroanalysis for CRV compatibility studies show promising viability.
publishDate 2020
dc.date.accessioned.fl_str_mv 2020-10-09T13:10:52Z
dc.date.available.fl_str_mv 2020-10-09T13:10:52Z
dc.date.issued.fl_str_mv 2020-08-31
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/doctoralThesis
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dc.identifier.citation.fl_str_mv Carvalho, M. F. Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos. 2020. 43 f. Tese (Doutorado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2020.
dc.identifier.uri.fl_str_mv http://repositorio.bc.ufg.br/tede/handle/tede/10852
identifier_str_mv Carvalho, M. F. Eletroanálise aplicada a ensaios de compatibilidade e estabilidade de fármacos. 2020. 43 f. Tese (Doutorado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2020.
url http://repositorio.bc.ufg.br/tede/handle/tede/10852
dc.language.iso.fl_str_mv por
language por
dc.relation.program.fl_str_mv 26
dc.relation.confidence.fl_str_mv 500
500
500
dc.relation.department.fl_str_mv 22
dc.relation.cnpq.fl_str_mv 524
dc.rights.driver.fl_str_mv Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Attribution-NonCommercial-NoDerivatives 4.0 International
http://creativecommons.org/licenses/by-nc-nd/4.0/
eu_rights_str_mv openAccess
dc.publisher.none.fl_str_mv Universidade Federal de Goiás
dc.publisher.program.fl_str_mv Programa de Pós-graduação em Ciências Farmacêuticas (FF)
dc.publisher.initials.fl_str_mv UFG
dc.publisher.country.fl_str_mv Brasil
dc.publisher.department.fl_str_mv Faculdade de Farmácia - FF (RG)
publisher.none.fl_str_mv Universidade Federal de Goiás
dc.source.none.fl_str_mv reponame:Repositório Institucional da UFG
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