Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods

Detalhes bibliográficos
Autor(a) principal: Mandal, Sanchita
Data de Publicação: 2010
Outros Autores: Kumar, S. Senthil, Krishnamoorthy, Balakrishnam, Basu, Sanat Kumar
Tipo de documento: Artigo
Idioma: eng
Título da fonte: Brazilian Journal of Pharmaceutical Sciences
Texto Completo: https://www.revistas.usp.br/bjps/article/view/10836
Resumo: The objective of this study was to develop a sustained release dosage form of Trimetazidine dihydrochloride (TMZ) using a natural polymeric carrier prepared in a completely aqueous environment. TMZ was entrapped in calcium alginate beads prepared with sodium alginate by the ionotropic gelation method using calcium chloride as a crosslinking agent. The drug was incorporated either into preformed calcium alginate gel beads (sequential method) or incorporated simultaneously during the gelation stage (simultaneous method). The beads were evaluated for particle size and surface morphology using optical microscopy and SEM, respectively. Beads produced by the sequential method had higher drug entrapment. Drug entrapment in the sequential method was higher with increased CaCl2 and polymer concentration but lower with increased drug concentration. In the simultaneous method, drug entrapment was higher when polymer and drug concentration were increased and also rose to a certain extent with increase in CaCl2 concentration, where further increase resulted in lower drug loading. FTIR studies revealed that there is no interaction between drug and CaCl2. XRD studies showed that the crystalline drug changed to an amorphous state after formulation. Release characteristics of the TMZ loaded calcium alginate beads were studied in enzyme-free simulated gastric and intestinal fluid.
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spelling Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods Alginato de sódioBeads de alginato de cálcioDicloridrato de trimetazidinaGelatinização ionotrópicaSodium alginateCalcium alginate beadsTrimetazidine dihydrochlorideIonotropic gelation The objective of this study was to develop a sustained release dosage form of Trimetazidine dihydrochloride (TMZ) using a natural polymeric carrier prepared in a completely aqueous environment. TMZ was entrapped in calcium alginate beads prepared with sodium alginate by the ionotropic gelation method using calcium chloride as a crosslinking agent. The drug was incorporated either into preformed calcium alginate gel beads (sequential method) or incorporated simultaneously during the gelation stage (simultaneous method). The beads were evaluated for particle size and surface morphology using optical microscopy and SEM, respectively. Beads produced by the sequential method had higher drug entrapment. Drug entrapment in the sequential method was higher with increased CaCl2 and polymer concentration but lower with increased drug concentration. In the simultaneous method, drug entrapment was higher when polymer and drug concentration were increased and also rose to a certain extent with increase in CaCl2 concentration, where further increase resulted in lower drug loading. FTIR studies revealed that there is no interaction between drug and CaCl2. XRD studies showed that the crystalline drug changed to an amorphous state after formulation. Release characteristics of the TMZ loaded calcium alginate beads were studied in enzyme-free simulated gastric and intestinal fluid. O objetivo deste estudo foi desenvolver forma de liberação controlada de dicloridrato de trimetazidina (TMZ) utilizando transportador plomérico natural em ambiente completamente aquoso. A TMZ foi presa em pérolas de alginato de cálcio preparadas com alginato de sódio pelo método de gelatinização ionotrópica, usando cloreto de cálcio como agente de formação de ligações cruzadas. O fármaco foi incorporado nas pérolas de gel de alginato de cálcio (método sequencial) ou incorporado, simultaneamente, durante o estágio de gelificação (método simultâneo). As pérolas foram avaliadas quanto ao tamanho das partículas e morfologia da superfície utilizando microscopia óptica de SEM, respectivamente. As pérolas produzidas pelo método sequencial apresentaram maior capacidade de inclusão. No método sequencial, a inclusão de fármaco foi maior com o aumento de CaCl2 e da concentração do plímero, mas menor com o aumento da concentração de fármaco. No método simultâneo, a inclusão de fármaco foi mais alta quando as concentrações de fármaco e plímero foram aumentadas e, também, atingiram certa extensão com aumento na concentração de CaCl2, cujo aumento posterior resultou em carga menor de fármaco. Estudos de FTIR revelaram que não há interação entre fármaco e CaCl2. Estudos de XRD mostraram que o fármaco mudou do estado cristalino para o amorfo após a formulação. As características de liberação de TMZ das pérolas carregadas com alginato de cálcio foram estudadas em fluidos simulados, gástrico e intestinal, livres de enzima. Universidade de São Paulo. Faculdade de Ciências Farmacêuticas2010-12-01info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionapplication/pdfhttps://www.revistas.usp.br/bjps/article/view/1083610.1590/S1984-82502010000400021Brazilian Journal of Pharmaceutical Sciences; Vol. 46 No. 4 (2010); 785-793 Brazilian Journal of Pharmaceutical Sciences; v. 46 n. 4 (2010); 785-793 Brazilian Journal of Pharmaceutical Sciences; Vol. 46 Núm. 4 (2010); 785-793 2175-97901984-8250reponame:Brazilian Journal of Pharmaceutical Sciencesinstname:Universidade de São Paulo (USP)instacron:USPenghttps://www.revistas.usp.br/bjps/article/view/10836/12604Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)info:eu-repo/semantics/openAccessMandal, SanchitaKumar, S. SenthilKrishnamoorthy, BalakrishnamBasu, Sanat Kumar2012-05-12T16:08:59Zoai:revistas.usp.br:article/10836Revistahttps://www.revistas.usp.br/bjps/indexPUBhttps://old.scielo.br/oai/scielo-oai.phpbjps@usp.br||elizabeth.igne@gmail.com2175-97901984-8250opendoar:2012-05-12T16:08:59Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)false
dc.title.none.fl_str_mv Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
title Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
spellingShingle Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
Mandal, Sanchita
Alginato de sódio
Beads de alginato de cálcio
Dicloridrato de trimetazidina
Gelatinização ionotrópica
Sodium alginate
Calcium alginate beads
Trimetazidine dihydrochloride
Ionotropic gelation
title_short Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
title_full Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
title_fullStr Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
title_full_unstemmed Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
title_sort Development and evaluation of calcium alginate beads prepared by sequential and simultaneous methods
author Mandal, Sanchita
author_facet Mandal, Sanchita
Kumar, S. Senthil
Krishnamoorthy, Balakrishnam
Basu, Sanat Kumar
author_role author
author2 Kumar, S. Senthil
Krishnamoorthy, Balakrishnam
Basu, Sanat Kumar
author2_role author
author
author
dc.contributor.author.fl_str_mv Mandal, Sanchita
Kumar, S. Senthil
Krishnamoorthy, Balakrishnam
Basu, Sanat Kumar
dc.subject.por.fl_str_mv Alginato de sódio
Beads de alginato de cálcio
Dicloridrato de trimetazidina
Gelatinização ionotrópica
Sodium alginate
Calcium alginate beads
Trimetazidine dihydrochloride
Ionotropic gelation
topic Alginato de sódio
Beads de alginato de cálcio
Dicloridrato de trimetazidina
Gelatinização ionotrópica
Sodium alginate
Calcium alginate beads
Trimetazidine dihydrochloride
Ionotropic gelation
description The objective of this study was to develop a sustained release dosage form of Trimetazidine dihydrochloride (TMZ) using a natural polymeric carrier prepared in a completely aqueous environment. TMZ was entrapped in calcium alginate beads prepared with sodium alginate by the ionotropic gelation method using calcium chloride as a crosslinking agent. The drug was incorporated either into preformed calcium alginate gel beads (sequential method) or incorporated simultaneously during the gelation stage (simultaneous method). The beads were evaluated for particle size and surface morphology using optical microscopy and SEM, respectively. Beads produced by the sequential method had higher drug entrapment. Drug entrapment in the sequential method was higher with increased CaCl2 and polymer concentration but lower with increased drug concentration. In the simultaneous method, drug entrapment was higher when polymer and drug concentration were increased and also rose to a certain extent with increase in CaCl2 concentration, where further increase resulted in lower drug loading. FTIR studies revealed that there is no interaction between drug and CaCl2. XRD studies showed that the crystalline drug changed to an amorphous state after formulation. Release characteristics of the TMZ loaded calcium alginate beads were studied in enzyme-free simulated gastric and intestinal fluid.
publishDate 2010
dc.date.none.fl_str_mv 2010-12-01
dc.type.driver.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
format article
status_str publishedVersion
dc.identifier.uri.fl_str_mv https://www.revistas.usp.br/bjps/article/view/10836
10.1590/S1984-82502010000400021
url https://www.revistas.usp.br/bjps/article/view/10836
identifier_str_mv 10.1590/S1984-82502010000400021
dc.language.iso.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv https://www.revistas.usp.br/bjps/article/view/10836/12604
dc.rights.driver.fl_str_mv Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)
info:eu-repo/semantics/openAccess
rights_invalid_str_mv Copyright (c) 2018 Brazilian Journal of Pharmaceutical Sciences (Impresso)
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
dc.publisher.none.fl_str_mv Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
publisher.none.fl_str_mv Universidade de São Paulo. Faculdade de Ciências Farmacêuticas
dc.source.none.fl_str_mv Brazilian Journal of Pharmaceutical Sciences; Vol. 46 No. 4 (2010); 785-793
Brazilian Journal of Pharmaceutical Sciences; v. 46 n. 4 (2010); 785-793
Brazilian Journal of Pharmaceutical Sciences; Vol. 46 Núm. 4 (2010); 785-793
2175-9790
1984-8250
reponame:Brazilian Journal of Pharmaceutical Sciences
instname:Universidade de São Paulo (USP)
instacron:USP
instname_str Universidade de São Paulo (USP)
instacron_str USP
institution USP
reponame_str Brazilian Journal of Pharmaceutical Sciences
collection Brazilian Journal of Pharmaceutical Sciences
repository.name.fl_str_mv Brazilian Journal of Pharmaceutical Sciences - Universidade de São Paulo (USP)
repository.mail.fl_str_mv bjps@usp.br||elizabeth.igne@gmail.com
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