Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno
Autor(a) principal: | |
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Data de Publicação: | 2014 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Repositório Institucional da UFG |
Texto Completo: | http://repositorio.bc.ufg.br/tede/handle/tede/4020 |
Resumo: | Ketoprofen is a nonsteroidal anti-inflammatory drug used for the treatment of mild to moderate pain in chronic inflammatory conditions. Due to its superior potency ketoprofen can be used in the treatment of inflammatory bowel disease (IBD). The treatment of IBD becomes safer and more effective when the drug is incorporated into colon-specific drug delivery systems. Pellets are multiparticulate solid dosage forms extensively investigated as colon-specific drug delivery systems. Pellets can be introduced into capsules or compressed into tablets. The industrial production of tablets containing pellets has several advantages when compared to the production of capsules. However, the compression of the pellets should not affect the release of the drug and the tablets should quickly disintegrate following administration. Therefore, the aim of this study was to develop tablets containing ketoprofen coated pellets for colon-specific drug release. For this, pellets were produced by extrusion and spheronization technique containing 40% (w / w) ketoprofen. Ketoprofen pellets obtained were coated with two different pH - dependent polymers derived from methacrylic acid (Opadry ® k 94 or Eudragit ® FS 30D) with weight gains of 10 or 20% (w / w). The coated pellets were then compressed under different pellets’ amounts and different compression forces. An extra- granular mixture of lactose and microcrystalline cellulose was used as compression aid. The in vitro release of ketoprofen from the systems obtained was evaluated in Bio Dis ® apparatus. The morphological and physical properties of pellets and tablets were assessed. The Eudragit ® FS 30 D coated pellets with weight gains of 10 or 20% showed higher efficiency of colon-specific delivery (94 %), however, the drug was released slowly and incompletely in conditions mimicking the pH of the colonic region. After compression of the pellets, the efficiency of colon – specific drug delivery was lowered after compression (between 20% and 61%, depending on the formulation). The lowest decrease of colon specific efficiency was observed in formulations containing lower amount of pellets, which also produced disintegrating matrices with potential for use in the topical treatment of IBD. |
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Marreto, Ricardo Neveshttp://lattes.cnpq.br/6127043775208484Marreto, Ricardo NevesAraújo, Adriano Antunes de SouzaTaveira, Stephânia Fleuryhttp://lattes.cnpq.br/8958489303277830Alencar, Rodrigo Gomes de2015-01-30T12:58:45Z2014-04-25ALENCAR, Rodrigo Gomes de. Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno. 2014. 75 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2014.http://repositorio.bc.ufg.br/tede/handle/tede/4020ark:/38995/001300000c2sjKetoprofen is a nonsteroidal anti-inflammatory drug used for the treatment of mild to moderate pain in chronic inflammatory conditions. Due to its superior potency ketoprofen can be used in the treatment of inflammatory bowel disease (IBD). The treatment of IBD becomes safer and more effective when the drug is incorporated into colon-specific drug delivery systems. Pellets are multiparticulate solid dosage forms extensively investigated as colon-specific drug delivery systems. Pellets can be introduced into capsules or compressed into tablets. The industrial production of tablets containing pellets has several advantages when compared to the production of capsules. However, the compression of the pellets should not affect the release of the drug and the tablets should quickly disintegrate following administration. Therefore, the aim of this study was to develop tablets containing ketoprofen coated pellets for colon-specific drug release. For this, pellets were produced by extrusion and spheronization technique containing 40% (w / w) ketoprofen. Ketoprofen pellets obtained were coated with two different pH - dependent polymers derived from methacrylic acid (Opadry ® k 94 or Eudragit ® FS 30D) with weight gains of 10 or 20% (w / w). The coated pellets were then compressed under different pellets’ amounts and different compression forces. An extra- granular mixture of lactose and microcrystalline cellulose was used as compression aid. The in vitro release of ketoprofen from the systems obtained was evaluated in Bio Dis ® apparatus. The morphological and physical properties of pellets and tablets were assessed. The Eudragit ® FS 30 D coated pellets with weight gains of 10 or 20% showed higher efficiency of colon-specific delivery (94 %), however, the drug was released slowly and incompletely in conditions mimicking the pH of the colonic region. After compression of the pellets, the efficiency of colon – specific drug delivery was lowered after compression (between 20% and 61%, depending on the formulation). The lowest decrease of colon specific efficiency was observed in formulations containing lower amount of pellets, which also produced disintegrating matrices with potential for use in the topical treatment of IBD.O cetoprofeno é um antiinflamatório não esteroidal usado para o tratamento de dores leves a moderadas, em condições inflamatórias crônicas. Devido a sua elevada potência antiinflamatória, o cetoprofeno pode ser aproveitado no tratamento das doenças inflamatórias intestinais (DII). O tratamento das DII se torna mais seguro e eficaz quando o fármaco é incorporado em sistemas de liberação cólon-específica. Pellets são formas farmacêuticas multiparticuladas bastante investigadas como sistemas de liberação cólon-específica. Após sua produção, os pellets podem ser inseridos em cápsulas ou comprimidos. A produção industrial de comprimidos contendo pellets apresenta inúmeras vantagens quando comparada ao processo de enchimento de cápsulas. No entanto, a compressão dos pellets não deve afetar as características de liberação do fármaco e os comprimidos formados devem se desintegrar rapidamente. Dessa forma, o objetivo deste trabalho foi desenvolver comprimidos contendo pellets revestidos para liberação cólon-específica de cetoprofeno. Para tanto, foram produzidos pellets contendo 40% (p/p) de cetoprofeno e celulose microcristalina pela técnica de extrusão e esferonização. Os pellets de cetoprofeno obtidos foram revestidos com dois diferentes polímeros pH-dependentes, ambos derivados do ácido metacrílico (Opadry ® 94 k ou Eudragit ® FS 30) com ganhos de massa 10 ou 20% (p/p). Os pellets revestidos foram então comprimidos com diferentes cargas de pellets e submetidos a diferentes forças de compressão, utilizando como adjuvante extra-pellets uma mistura granulada de lactose e celulose microcristalina. A liberação in vitro do cetoprofeno a partir das formas farmacêuticas obtidas foi avaliada em dissolutor Bio Dis aparato III. As caracterizações morfológicas e físicas dos pellets e comprimidos foram conduzidas. Os pellets obtidos por revestimento com Eudragit ® FS 30 D, com ganhos de massa de 10 ou 20%, mostraram elevada eficiência de liberação cólon-específica in vitro (até 94%), no entanto, o fármaco foi liberado de forma lenta e incompleta em meio com pH similar ao encontrado na região colônica. Após a compressão dos pellets, os valores de eficiência de liberação cólon-específica sofreram reduções entre 20% e 61%. A menor diminuição da eficiência de liberação cólon-específica foi observada nas formulações contendo a menor carga de pellets, as quais deram origem à matrizes desintegráveis com potencial para utilização no tratamento tópico das DII.Submitted by Cássia Santos (cassia.bcufg@gmail.com) on 2015-01-30T10:47:22Z No. of bitstreams: 2 license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5) Dissertação - Rodrigo Gomes de Alencar - 2014.pdf: 13066901 bytes, checksum: 15e26e7a3dde863c6267ef54f83385be (MD5)Approved for entry into archive by Luciana Ferreira (lucgeral@gmail.com) on 2015-01-30T12:58:45Z (GMT) No. of bitstreams: 2 license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5) Dissertação - Rodrigo Gomes de Alencar - 2014.pdf: 13066901 bytes, checksum: 15e26e7a3dde863c6267ef54f83385be (MD5)Made available in DSpace on 2015-01-30T12:58:45Z (GMT). No. of bitstreams: 2 license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5) Dissertação - Rodrigo Gomes de Alencar - 2014.pdf: 13066901 bytes, checksum: 15e26e7a3dde863c6267ef54f83385be (MD5) Previous issue date: 2014-04-25Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESapplication/pdfhttp://repositorio.bc.ufg.br/tede/retrieve/15936/Disserta%c3%a7%c3%a3o%20-%20Rodrigo%20Gomes%20de%20Alencar%20-%202014.pdf.jpgporUniversidade Federal de GoiásPrograma de Pós-graduação em Ciências Farmacêuticas (FF)UFGBrasilFaculdade Farmácia - FF (RG)http://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessExtrusãoEsferonizaçãoCompressão de pellets revestidosCetoprofenoPolímeros acrílicosRevestimento de pelletsExtrusionSpheronizationCompression of coated pelletsKetoprofenAcrylic polymersCoating of pelletsSolid multiparticulate systemsFARMACOLOGIA::FARMACOLOGIA GERALDesenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofenoDevelopment of tablets contain coated pellets for colon specific release of ketoprofeninfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesis8249369881961524126006006006006010281161524209375-39594841539407582472075167498588264571reponame:Repositório Institucional da UFGinstname:Universidade Federal de Goiás (UFG)instacron:UFGORIGINALDissertação - Rodrigo Gomes de Alencar - 2014.pdfDissertação - Rodrigo Gomes de Alencar - 2014.pdfDissertação - Rodrigo Gomes de Alencar - 2014application/pdf13066901http://repositorio.bc.ufg.br/tede/bitstreams/19fdd5eb-32fb-4ab4-811f-1900ea4a47a9/download15e26e7a3dde863c6267ef54f83385beMD52LICENSElicense.txtlicense.txttext/plain; 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dc.title.eng.fl_str_mv |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno |
dc.title.alternative.eng.fl_str_mv |
Development of tablets contain coated pellets for colon specific release of ketoprofen |
title |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno |
spellingShingle |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno Alencar, Rodrigo Gomes de Extrusão Esferonização Compressão de pellets revestidos Cetoprofeno Polímeros acrílicos Revestimento de pellets Extrusion Spheronization Compression of coated pellets Ketoprofen Acrylic polymers Coating of pellets Solid multiparticulate systems FARMACOLOGIA::FARMACOLOGIA GERAL |
title_short |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno |
title_full |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno |
title_fullStr |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno |
title_full_unstemmed |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno |
title_sort |
Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno |
author |
Alencar, Rodrigo Gomes de |
author_facet |
Alencar, Rodrigo Gomes de |
author_role |
author |
dc.contributor.advisor1.fl_str_mv |
Marreto, Ricardo Neves |
dc.contributor.advisor1Lattes.fl_str_mv |
http://lattes.cnpq.br/6127043775208484 |
dc.contributor.referee1.fl_str_mv |
Marreto, Ricardo Neves |
dc.contributor.referee2.fl_str_mv |
Araújo, Adriano Antunes de Souza |
dc.contributor.referee3.fl_str_mv |
Taveira, Stephânia Fleury |
dc.contributor.authorLattes.fl_str_mv |
http://lattes.cnpq.br/8958489303277830 |
dc.contributor.author.fl_str_mv |
Alencar, Rodrigo Gomes de |
contributor_str_mv |
Marreto, Ricardo Neves Marreto, Ricardo Neves Araújo, Adriano Antunes de Souza Taveira, Stephânia Fleury |
dc.subject.por.fl_str_mv |
Extrusão Esferonização Compressão de pellets revestidos Cetoprofeno Polímeros acrílicos Revestimento de pellets |
topic |
Extrusão Esferonização Compressão de pellets revestidos Cetoprofeno Polímeros acrílicos Revestimento de pellets Extrusion Spheronization Compression of coated pellets Ketoprofen Acrylic polymers Coating of pellets Solid multiparticulate systems FARMACOLOGIA::FARMACOLOGIA GERAL |
dc.subject.eng.fl_str_mv |
Extrusion Spheronization Compression of coated pellets Ketoprofen Acrylic polymers Coating of pellets Solid multiparticulate systems |
dc.subject.cnpq.fl_str_mv |
FARMACOLOGIA::FARMACOLOGIA GERAL |
description |
Ketoprofen is a nonsteroidal anti-inflammatory drug used for the treatment of mild to moderate pain in chronic inflammatory conditions. Due to its superior potency ketoprofen can be used in the treatment of inflammatory bowel disease (IBD). The treatment of IBD becomes safer and more effective when the drug is incorporated into colon-specific drug delivery systems. Pellets are multiparticulate solid dosage forms extensively investigated as colon-specific drug delivery systems. Pellets can be introduced into capsules or compressed into tablets. The industrial production of tablets containing pellets has several advantages when compared to the production of capsules. However, the compression of the pellets should not affect the release of the drug and the tablets should quickly disintegrate following administration. Therefore, the aim of this study was to develop tablets containing ketoprofen coated pellets for colon-specific drug release. For this, pellets were produced by extrusion and spheronization technique containing 40% (w / w) ketoprofen. Ketoprofen pellets obtained were coated with two different pH - dependent polymers derived from methacrylic acid (Opadry ® k 94 or Eudragit ® FS 30D) with weight gains of 10 or 20% (w / w). The coated pellets were then compressed under different pellets’ amounts and different compression forces. An extra- granular mixture of lactose and microcrystalline cellulose was used as compression aid. The in vitro release of ketoprofen from the systems obtained was evaluated in Bio Dis ® apparatus. The morphological and physical properties of pellets and tablets were assessed. The Eudragit ® FS 30 D coated pellets with weight gains of 10 or 20% showed higher efficiency of colon-specific delivery (94 %), however, the drug was released slowly and incompletely in conditions mimicking the pH of the colonic region. After compression of the pellets, the efficiency of colon – specific drug delivery was lowered after compression (between 20% and 61%, depending on the formulation). The lowest decrease of colon specific efficiency was observed in formulations containing lower amount of pellets, which also produced disintegrating matrices with potential for use in the topical treatment of IBD. |
publishDate |
2014 |
dc.date.issued.fl_str_mv |
2014-04-25 |
dc.date.accessioned.fl_str_mv |
2015-01-30T12:58:45Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/masterThesis |
format |
masterThesis |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
ALENCAR, Rodrigo Gomes de. Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno. 2014. 75 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2014. |
dc.identifier.uri.fl_str_mv |
http://repositorio.bc.ufg.br/tede/handle/tede/4020 |
dc.identifier.dark.fl_str_mv |
ark:/38995/001300000c2sj |
identifier_str_mv |
ALENCAR, Rodrigo Gomes de. Desenvolvimento de comprimidos contendo pellets revestidos para liberação cólon específica de cetoprofeno. 2014. 75 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2014. ark:/38995/001300000c2sj |
url |
http://repositorio.bc.ufg.br/tede/handle/tede/4020 |
dc.language.iso.fl_str_mv |
por |
language |
por |
dc.relation.program.fl_str_mv |
824936988196152412 |
dc.relation.confidence.fl_str_mv |
600 600 600 600 |
dc.relation.department.fl_str_mv |
6010281161524209375 |
dc.relation.cnpq.fl_str_mv |
-3959484153940758247 |
dc.relation.sponsorship.fl_str_mv |
2075167498588264571 |
dc.rights.driver.fl_str_mv |
http://creativecommons.org/licenses/by-nc-nd/4.0/ info:eu-repo/semantics/openAccess |
rights_invalid_str_mv |
http://creativecommons.org/licenses/by-nc-nd/4.0/ |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
application/pdf |
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 Farmácia - FF (RG) |
publisher.none.fl_str_mv |
Universidade Federal de Goiás |
dc.source.none.fl_str_mv |
reponame:Repositório Institucional da UFG instname:Universidade Federal de Goiás (UFG) instacron:UFG |
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Universidade Federal de Goiás (UFG) |
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UFG |
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UFG |
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Repositório Institucional da UFG |
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Repositório Institucional da UFG |
bitstream.url.fl_str_mv |
http://repositorio.bc.ufg.br/tede/bitstreams/19fdd5eb-32fb-4ab4-811f-1900ea4a47a9/download http://repositorio.bc.ufg.br/tede/bitstreams/a908c709-0b9f-4315-b0e4-2c6331e35aba/download http://repositorio.bc.ufg.br/tede/bitstreams/4c410dc6-7e1d-4059-ac8f-c246cd743793/download http://repositorio.bc.ufg.br/tede/bitstreams/d907aa13-de1f-4336-93f0-bfd70fbee570/download http://repositorio.bc.ufg.br/tede/bitstreams/85d03850-a245-46e8-8a60-3b299518e8e9/download http://repositorio.bc.ufg.br/tede/bitstreams/b1c6fba9-359c-4c06-a5a4-56cba028138c/download http://repositorio.bc.ufg.br/tede/bitstreams/be27f7ee-70af-4cf7-b185-dddd9a825014/download |
bitstream.checksum.fl_str_mv |
15e26e7a3dde863c6267ef54f83385be bd3efa91386c1718a7f26a329fdcb468 4afdbb8c545fd630ea7db775da747b2f 29b9d5e95be03707f9d4a2e110421c11 9da0b6dfac957114c6a7714714b86306 4541df819b30f0022e2aa4c3bbe5ba2f 7ab780ac81c4745f377616b325e58e69 |
bitstream.checksumAlgorithm.fl_str_mv |
MD5 MD5 MD5 MD5 MD5 MD5 MD5 |
repository.name.fl_str_mv |
Repositório Institucional da UFG - Universidade Federal de Goiás (UFG) |
repository.mail.fl_str_mv |
tasesdissertacoes.bc@ufg.br |
_version_ |
1811721494305177600 |