Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas

Detalhes bibliográficos
Ano de defesa: 2012
Autor(a) principal: Pires, Sumaia Araújo lattes
Orientador(a): Trevisan, Marcello Garcia lattes
Banca de defesa: Torres, Cláudia, Schiavon, Marco Antônio
Tipo de documento: Dissertação
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Universidade Federal de Alfenas
Programa de Pós-Graduação: Programa de Pós-Graduação em Química
Departamento: Instituto de Química
País: Brasil
Palavras-chave em Português:
Área do conhecimento CNPq:
Link de acesso: https://repositorio.unifal-mg.edu.br/handle/123456789/384
Resumo: This study aimed to apply thermal analysis techniques in the study of drug-excipient compatibility losartano potassium (LST) - an antihypertensive, class of antagonists of angiotensin II, used to treat hypertension. Differential Scanning Calorimetry (DSC), thermogravimetry (TG), X-ray diffraction powder Absorption Spectrometry in the Infrared Region East and scanning electron microscopy were used to characterize the losartano potassium. For the purpose of evaluating possible interactions between the components of each binary mixture 1:1 losartano-carriers, excipients and each mixture were evaluated by X-ray diffraction powder, TG, DSC and Raman spectroscopy. The excipients were studied starch, lactose monohydrate (LAC), magnesium stearate (EM), hydroxypropylcellulose (HPC), croscarmellose sodium (CS), polyvinylpyrrolidone (PVP), talc, microcrystalline cellulose (MC), talc, hydroxyethylcellulose (HEC) , carboxymethylcellulose (CMC) and povidone (PD). The results of DSC and TG suggested that the excipients HEC, LAC, CS, HPC, EM, PVP show possible interactions with LST was confirmed by the disappearance of the event or shift transition of crystalline drug. The compatibility study using X-ray diffraction powder indicated that LST remained in the same polymorphic form I in the presence of excipients analyzed, except when mixed with the talc. The analysis by Raman spectroscopy showed chemical incompatibility with excipients EM, CMC, LAC e HEC. Tablets were prepared containing the form I and II which exhibited significantly different dissolution profile. Furthermore, it can be shown, with the construction of a calibration curve, the DSC is a useful technique for quantifying also polymorphic.
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spelling Pires, Sumaia Araújohttp://lattes.cnpq.br/6509414402989975Garcia, Jerusa SimoneTorres, CláudiaSchiavon, Marco AntônioTrevisan, Marcello Garciahttp://lattes.cnpq.br/81413550253192032015-06-13T00:32:35Z2012-08-09PIRES, Sumaia Araújo. Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas. 2012.107 f. Dissertação (Mestrado em Química) - Universidade Federal de Alfenas, Alfenas, MG, 2012.https://repositorio.unifal-mg.edu.br/handle/123456789/384This study aimed to apply thermal analysis techniques in the study of drug-excipient compatibility losartano potassium (LST) - an antihypertensive, class of antagonists of angiotensin II, used to treat hypertension. Differential Scanning Calorimetry (DSC), thermogravimetry (TG), X-ray diffraction powder Absorption Spectrometry in the Infrared Region East and scanning electron microscopy were used to characterize the losartano potassium. For the purpose of evaluating possible interactions between the components of each binary mixture 1:1 losartano-carriers, excipients and each mixture were evaluated by X-ray diffraction powder, TG, DSC and Raman spectroscopy. The excipients were studied starch, lactose monohydrate (LAC), magnesium stearate (EM), hydroxypropylcellulose (HPC), croscarmellose sodium (CS), polyvinylpyrrolidone (PVP), talc, microcrystalline cellulose (MC), talc, hydroxyethylcellulose (HEC) , carboxymethylcellulose (CMC) and povidone (PD). The results of DSC and TG suggested that the excipients HEC, LAC, CS, HPC, EM, PVP show possible interactions with LST was confirmed by the disappearance of the event or shift transition of crystalline drug. The compatibility study using X-ray diffraction powder indicated that LST remained in the same polymorphic form I in the presence of excipients analyzed, except when mixed with the talc. The analysis by Raman spectroscopy showed chemical incompatibility with excipients EM, CMC, LAC e HEC. Tablets were prepared containing the form I and II which exhibited significantly different dissolution profile. Furthermore, it can be shown, with the construction of a calibration curve, the DSC is a useful technique for quantifying also polymorphic.Este trabalho teve como objetivo aplicar técnicas de análise térmica no estudo de compatibilidade fármaco-excipiente de losartano potássico (LST) - um antihipertensivo, da classe dos antagonistas dos receptores de angiotensina II, empregado no tratamento da hipertensão. Calorimetria Exploratória Diferencial (DSC), Termogravimetria (TG), Difração de raios X em pó, Espectrometria de Absorção na Região do Infravermelho Médio e Microscopia Eletrônica de Varredura foram empregadas na caracterização de losartano potássico. Com a finalidade de avaliar possíveis interações existentes entre os componentes de cada mistura binária 1:1 losartano-excipiente, os excipientes e cada mistura foram avaliados por Difração de raios X em pó, TG, DSC e Espectroscopia Raman. Os excipientes estudados foram o amido, lactose monohidratada (LAC), estearato de magnésio (EM), hidroxipropilcelulose (HPC), croscarmelose sódica (CS), polivinilpirrolidona (PVP), talco, celulose microcristalina (CM), talco, hidroxietilcelulose (HEC), carboximetilcelulose (CMC) e povidona (PD). Os resultados de DSC e TG sugeriram que os excipientes HEC, LAC, CS, HPC, EM, PVP apresentam possíveis interações com LST que foi confirmado através do desaparecimento ou do deslocamento do evento de transição cristalina do fármaco. O estudo de compatibilidade empregando Difração de raios X em pó indicou que LST se manteve na forma polimórfica I mesmo na presença dos excipientes analisados, exceto quando mistura ao talco. As análises por Espectroscopia Raman evidenciaram incompatibilidade química com os excipientes EM, CMC, LAC e HEC. Foram preparados comprimidos contendo a forma I e II que apresentaram perfil de dissolução significativamente diferente. Além disso, pode-se demonstrar, com a construção de uma curva analítica, que o DSC é uma técnica útil também na quantificação polimórfica.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESapplication/pdfporUniversidade Federal de AlfenasPrograma de Pós-Graduação em QuímicaUNIFAL-MGBrasilInstituto de Químicainfo:eu-repo/semantics/openAccesshttp://creativecommons.org/licenses/by-nc-nd/4.0/PolimorfismoLosartanCalorimetria Diferencial de VarreduraQUIMICA::QUIMICA ANALITICAEstudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicasinfo:eu-repo/semantics/masterThesisinfo:eu-repo/semantics/publishedVersion1328253078826782306600600600-86616021054614395492075167498588264571reponame:Repositório Institucional da Universidade Federal de Alfenas - RiUnifalinstname:Universidade Federal de Alfenas (UNIFAL)instacron:UNIFALPires, Sumaia AraújoLICENSElicense.txtlicense.txttext/plain; charset=utf-81987https://repositorio.unifal-mg.edu.br/bitstreams/b8c3022b-1380-4805-817c-76366e657876/download31555718c4fc75849dd08f27935d4f6bMD51CC-LICENSElicense_urllicense_urltext/plain; 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dc.title.pt-BR.fl_str_mv Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
title Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
spellingShingle Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
Pires, Sumaia Araújo
Polimorfismo
Losartan
Calorimetria Diferencial de Varredura
QUIMICA::QUIMICA ANALITICA
title_short Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
title_full Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
title_fullStr Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
title_full_unstemmed Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
title_sort Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas
author Pires, Sumaia Araújo
author_facet Pires, Sumaia Araújo
author_role author
dc.contributor.author.fl_str_mv Pires, Sumaia Araújo
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/6509414402989975
dc.contributor.advisor-co1.fl_str_mv Garcia, Jerusa Simone
dc.contributor.referee1.fl_str_mv Torres, Cláudia
dc.contributor.referee2.fl_str_mv Schiavon, Marco Antônio
dc.contributor.advisor1.fl_str_mv Trevisan, Marcello Garcia
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/8141355025319203
contributor_str_mv Garcia, Jerusa Simone
Torres, Cláudia
Schiavon, Marco Antônio
Trevisan, Marcello Garcia
dc.subject.por.fl_str_mv Polimorfismo
Losartan
Calorimetria Diferencial de Varredura
topic Polimorfismo
Losartan
Calorimetria Diferencial de Varredura
QUIMICA::QUIMICA ANALITICA
dc.subject.cnpq.fl_str_mv QUIMICA::QUIMICA ANALITICA
description This study aimed to apply thermal analysis techniques in the study of drug-excipient compatibility losartano potassium (LST) - an antihypertensive, class of antagonists of angiotensin II, used to treat hypertension. Differential Scanning Calorimetry (DSC), thermogravimetry (TG), X-ray diffraction powder Absorption Spectrometry in the Infrared Region East and scanning electron microscopy were used to characterize the losartano potassium. For the purpose of evaluating possible interactions between the components of each binary mixture 1:1 losartano-carriers, excipients and each mixture were evaluated by X-ray diffraction powder, TG, DSC and Raman spectroscopy. The excipients were studied starch, lactose monohydrate (LAC), magnesium stearate (EM), hydroxypropylcellulose (HPC), croscarmellose sodium (CS), polyvinylpyrrolidone (PVP), talc, microcrystalline cellulose (MC), talc, hydroxyethylcellulose (HEC) , carboxymethylcellulose (CMC) and povidone (PD). The results of DSC and TG suggested that the excipients HEC, LAC, CS, HPC, EM, PVP show possible interactions with LST was confirmed by the disappearance of the event or shift transition of crystalline drug. The compatibility study using X-ray diffraction powder indicated that LST remained in the same polymorphic form I in the presence of excipients analyzed, except when mixed with the talc. The analysis by Raman spectroscopy showed chemical incompatibility with excipients EM, CMC, LAC e HEC. Tablets were prepared containing the form I and II which exhibited significantly different dissolution profile. Furthermore, it can be shown, with the construction of a calibration curve, the DSC is a useful technique for quantifying also polymorphic.
publishDate 2012
dc.date.issued.fl_str_mv 2012-08-09
dc.date.accessioned.fl_str_mv 2015-06-13T00:32:35Z
dc.type.driver.fl_str_mv info:eu-repo/semantics/masterThesis
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dc.identifier.citation.fl_str_mv PIRES, Sumaia Araújo. Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas. 2012.107 f. Dissertação (Mestrado em Química) - Universidade Federal de Alfenas, Alfenas, MG, 2012.
dc.identifier.uri.fl_str_mv https://repositorio.unifal-mg.edu.br/handle/123456789/384
identifier_str_mv PIRES, Sumaia Araújo. Estudos de pré-formulação em losartano potássico através das técnicas de análise térmica e espectroscópicas. 2012.107 f. Dissertação (Mestrado em Química) - Universidade Federal de Alfenas, Alfenas, MG, 2012.
url https://repositorio.unifal-mg.edu.br/handle/123456789/384
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publisher.none.fl_str_mv Universidade Federal de Alfenas
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