Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina
Autor(a) principal: | |
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Data de Publicação: | 2019 |
Tipo de documento: | Dissertação |
Idioma: | por |
Título da fonte: | Manancial - Repositório Digital da UFSM |
dARK ID: | ark:/26339/0013000014trj |
Texto Completo: | http://repositorio.ufsm.br/handle/1/21716 |
Resumo: | Piperine is an alkaloid extracted from plants of the Piper genus, among which is the Piper nigrum species, the black pepper, widely employed in Indian cooking and traditional medicine. Moreover, piperine exhibits important pharmacological activities, as antioxidant, antitumoral and neuroprotector, as well as improving other drugs bioavailability when associated to it. However, when orally administered, presents as an inconveniency an irritation of the gastrointestinal tract and it’s insoluble in aqueous media. Microencapsulation using ethylcellulose is an alternative to overcome this issues, since this polymer is capable of masking unpleasant tastes and control the release of the microencapsulated active ingredientes. Thus, in this study, microparticulated systems containing piperine were prepared with the ethylcellulose polymer employing emulsification-evaporation of solvent O/W method. To quantify piperine, an analytical methodology by spectroscopy in UV region was validated. The developed microparticles were characterized regarding process yield, mean particle size and particle size distribution, piperine content, encapsulation efficiency, morphology, bulk and tapped densities, evaluation of flow properties and in vitro release of the active. After, to enable microparticles administration, they were converted into tablets, with the addition of polacrilin potassium and Pullulan®, and prepared by direct compression. The microparticulated tablets were characterized regarding weight, hardness, thickness, piperine content, uniformity of content, morphology and piperine in vitro release. The microparticles obtaining process presented 97.6 ± 0.3% yield and were spherical, with 190 ± 13 μm size and Span of 1.698 ± 0.180. Encapsulation efficiency was 90.0 ± 0.9%, a piperine content of 298.3 ± 2.9 mg/g. The in vitro release demonstrated a controlled release of piperine from the microparticulated systems: in 24 h, 34.8 ± 1.6% of piperine were release, while 80.9 ± 1.5% of bulk piperine was dissolved. Bulk and tapped density, Carr’s index and Hausner ratio revealed the microparticles have excellent flow properties. Thus, to prepare the microparticulated tablets, the excipients employed were only a dissolution promotor (Kyron® T-314) and the diluent (Pullulan®). The tablets presented 99.1 ± 0.9 mg weight; thickness of 3.38 ± 0.03 mm; hardness of 3.0 ± 0.2 kgf and friability 0.4%. Piperine content was 19.7 ± 0.4 mg, close to the theoretical value. The active release from the tablets was controlled, presenting 49.4 ± 2.4 % release in 24 h and the release profile was similar to the profile release of piperine from the microparticles. With this result and the scanning electron spectroscopy, it can be seen that the microparticles remained intact after the compression. Therefore, in this study microparticles and microparticulated tablets containing piperine were developed, which presented adequate physical-chemical characteristics and release profiles in order to overcome the issues presented by piperine in its oral administration and, so, the microparticulated tablets are a promising dosage unit for this purpose. |
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Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperinaDevelopment of microparticles and microparticulated tablets containing piperineBioativoEtilceluloseEmulsificação-evaporação do solventeCompressãoPiper nigrumBioactiveEthylcelluloseEmulsification-evaporation of solventCompressionCNPQ::CIENCIAS DA SAUDE::FARMACIAPiperine is an alkaloid extracted from plants of the Piper genus, among which is the Piper nigrum species, the black pepper, widely employed in Indian cooking and traditional medicine. Moreover, piperine exhibits important pharmacological activities, as antioxidant, antitumoral and neuroprotector, as well as improving other drugs bioavailability when associated to it. However, when orally administered, presents as an inconveniency an irritation of the gastrointestinal tract and it’s insoluble in aqueous media. Microencapsulation using ethylcellulose is an alternative to overcome this issues, since this polymer is capable of masking unpleasant tastes and control the release of the microencapsulated active ingredientes. Thus, in this study, microparticulated systems containing piperine were prepared with the ethylcellulose polymer employing emulsification-evaporation of solvent O/W method. To quantify piperine, an analytical methodology by spectroscopy in UV region was validated. The developed microparticles were characterized regarding process yield, mean particle size and particle size distribution, piperine content, encapsulation efficiency, morphology, bulk and tapped densities, evaluation of flow properties and in vitro release of the active. After, to enable microparticles administration, they were converted into tablets, with the addition of polacrilin potassium and Pullulan®, and prepared by direct compression. The microparticulated tablets were characterized regarding weight, hardness, thickness, piperine content, uniformity of content, morphology and piperine in vitro release. The microparticles obtaining process presented 97.6 ± 0.3% yield and were spherical, with 190 ± 13 μm size and Span of 1.698 ± 0.180. Encapsulation efficiency was 90.0 ± 0.9%, a piperine content of 298.3 ± 2.9 mg/g. The in vitro release demonstrated a controlled release of piperine from the microparticulated systems: in 24 h, 34.8 ± 1.6% of piperine were release, while 80.9 ± 1.5% of bulk piperine was dissolved. Bulk and tapped density, Carr’s index and Hausner ratio revealed the microparticles have excellent flow properties. Thus, to prepare the microparticulated tablets, the excipients employed were only a dissolution promotor (Kyron® T-314) and the diluent (Pullulan®). The tablets presented 99.1 ± 0.9 mg weight; thickness of 3.38 ± 0.03 mm; hardness of 3.0 ± 0.2 kgf and friability 0.4%. Piperine content was 19.7 ± 0.4 mg, close to the theoretical value. The active release from the tablets was controlled, presenting 49.4 ± 2.4 % release in 24 h and the release profile was similar to the profile release of piperine from the microparticles. With this result and the scanning electron spectroscopy, it can be seen that the microparticles remained intact after the compression. Therefore, in this study microparticles and microparticulated tablets containing piperine were developed, which presented adequate physical-chemical characteristics and release profiles in order to overcome the issues presented by piperine in its oral administration and, so, the microparticulated tablets are a promising dosage unit for this purpose.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior - CAPESA piperina é um alcaloide extraído de plantas do gênero Piper, entre as quais a espécie Piper nigrum, a pimenta do reino, muito empregada na culinária e na medicina tradicional indiana. Além disso, a piperina apresenta atividades farmacológicas importantes, como antioxidante, antitumoral e neuroprotetora, além de promover aumento na biodisponibilidade de outros fármacos quando a ela associados. Porém, quando administrada por via oral, apresenta como inconveniente a irritação do trato gastrintestinal, além de ser insolúvel em meio aquoso. A microencapsulação empregando a etilcelulose é uma alternativa para contornar estas características, uma vez que este polímero é capaz de mascarar sabores desagradáveis, além de promover o controle da liberação de substâncias ativas microencapsuladas. Portanto, neste trabalho, sistemas microparticulados a partir do polímero etilcelulose contendo piperina foram preparados pela técnica de emulsificação-evaporação do solvente O/A. As micropartículas desenvolvidas foram caracterizadas quanto ao rendimento do processo, tamanho médio e distribuição do tamanho de partículas, teor de piperina, eficiência de encapsulamento, morfologia, densidade bruta e de compactação, avaliação das propriedades de fluxo e liberação in vitro do bioativo. Posteriormente, para viabilizar a administração das micropartículas, estas foram convertidas em comprimidos, acrescidas de polacrilina potássica e Pullulan®, e preparados por compressão direta. Os comprimidos microparticulados foram caracterizados de acordo com o peso médio, dureza, espessura, teor de piperina, uniformidade de conteúdo, morfologia e liberação da piperina. O processo de obtenção das micropartículas apresentou rendimento de 97,6 ± 0,3 % e estas mostraram-se esféricas, com tamanho de 190 ± 13 μm e Span de 1,698 ± 0,180. A eficiência de encapsulação foi 90,0 ± 0,9 %, um teor de piperina de 298,3 ± 2,9 mg/g. O ensaio de liberação in vitro demonstrou o controle da liberação da piperina a partir dos sistemas microparticulados: em 24 h, foram liberados 34,8 ± 1,6 %, enquanto que 80,9 ± 1,5% da piperina pura foi dissolvida. A avaliação da densidade bruta e de compactação e a determinação do índice de Carr e do fator de Hausner revelaram que as micropartículas possuem um excelente fluxo. Desta forma, para preparar os comprimidos microparticulados foram utilizados como excipientes apenas um promotor de dissolução, Kyron® T-314, e o diluente, Pullulan®. Os comprimidos apresentaram um peso médio de 99,1 ± 0,9 mg; espessura de 3,38 ± 0,03 mm; dureza de 3,0 ± 0,2 kgf e friabilidade de 0,4%. O teor de piperina foi de 19,7 ± 0,4 mg, próximo ao teórico. A liberação do bioativo a partir dos comprimidos foi controlada, liberando 49,4 ± 2,4 % em 24 h, e o perfil de liberação se mostrou semelhante ao perfil de liberação da piperina a partir das micropartículas. Com este resultado e a microscopia eletrônica de varredura, pode-se afirmar que as micropartículas se mantiveram intactas após a compressão. Sendo assim, neste trabalho foram desenvolvidos micropartículas e comprimidos microparticulados contendo piperina, os quais apresentaram características físico-químicas e perfis de liberação adequados para contornar os obstáculos apresentados pela piperina para sua administração por via oral e, portanto, os comprimidos microparticulados são uma promissora forma farmacêutica para tal fim.Universidade Federal de Santa MariaBrasilAnálises Clínicas e ToxicológicasUFSMPrograma de Pós-Graduação em Ciências FarmacêuticasCentro de Ciências da SaúdeSilva, Cristiane de Bona dahttp://lattes.cnpq.br/6029111646602279Cruz, LetíciaBeck, Ruy Carlos RuverSchaffazick, Scheila RezendeSchneider, Aline Colling2021-08-04T00:40:27Z2021-08-04T00:40:27Z2019-08-30info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/masterThesisapplication/pdfhttp://repositorio.ufsm.br/handle/1/21716ark:/26339/0013000014trjporAttribution-NonCommercial-NoDerivatives 4.0 Internationalhttp://creativecommons.org/licenses/by-nc-nd/4.0/info:eu-repo/semantics/openAccessreponame:Manancial - Repositório Digital da UFSMinstname:Universidade Federal de Santa Maria (UFSM)instacron:UFSM2022-03-04T10:28:44Zoai:repositorio.ufsm.br:1/21716Biblioteca Digital de Teses e Dissertaçõeshttps://repositorio.ufsm.br/ONGhttps://repositorio.ufsm.br/oai/requestatendimento.sib@ufsm.br||tedebc@gmail.comopendoar:2022-03-04T10:28:44Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM)false |
dc.title.none.fl_str_mv |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina Development of microparticles and microparticulated tablets containing piperine |
title |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina |
spellingShingle |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina Schneider, Aline Colling Bioativo Etilcelulose Emulsificação-evaporação do solvente Compressão Piper nigrum Bioactive Ethylcellulose Emulsification-evaporation of solvent Compression CNPQ::CIENCIAS DA SAUDE::FARMACIA |
title_short |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina |
title_full |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina |
title_fullStr |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina |
title_full_unstemmed |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina |
title_sort |
Desenvolvimento de micropartículas e comprimidos microparticulados contendo piperina |
author |
Schneider, Aline Colling |
author_facet |
Schneider, Aline Colling |
author_role |
author |
dc.contributor.none.fl_str_mv |
Silva, Cristiane de Bona da http://lattes.cnpq.br/6029111646602279 Cruz, Letícia Beck, Ruy Carlos Ruver Schaffazick, Scheila Rezende |
dc.contributor.author.fl_str_mv |
Schneider, Aline Colling |
dc.subject.por.fl_str_mv |
Bioativo Etilcelulose Emulsificação-evaporação do solvente Compressão Piper nigrum Bioactive Ethylcellulose Emulsification-evaporation of solvent Compression CNPQ::CIENCIAS DA SAUDE::FARMACIA |
topic |
Bioativo Etilcelulose Emulsificação-evaporação do solvente Compressão Piper nigrum Bioactive Ethylcellulose Emulsification-evaporation of solvent Compression CNPQ::CIENCIAS DA SAUDE::FARMACIA |
description |
Piperine is an alkaloid extracted from plants of the Piper genus, among which is the Piper nigrum species, the black pepper, widely employed in Indian cooking and traditional medicine. Moreover, piperine exhibits important pharmacological activities, as antioxidant, antitumoral and neuroprotector, as well as improving other drugs bioavailability when associated to it. However, when orally administered, presents as an inconveniency an irritation of the gastrointestinal tract and it’s insoluble in aqueous media. Microencapsulation using ethylcellulose is an alternative to overcome this issues, since this polymer is capable of masking unpleasant tastes and control the release of the microencapsulated active ingredientes. Thus, in this study, microparticulated systems containing piperine were prepared with the ethylcellulose polymer employing emulsification-evaporation of solvent O/W method. To quantify piperine, an analytical methodology by spectroscopy in UV region was validated. The developed microparticles were characterized regarding process yield, mean particle size and particle size distribution, piperine content, encapsulation efficiency, morphology, bulk and tapped densities, evaluation of flow properties and in vitro release of the active. After, to enable microparticles administration, they were converted into tablets, with the addition of polacrilin potassium and Pullulan®, and prepared by direct compression. The microparticulated tablets were characterized regarding weight, hardness, thickness, piperine content, uniformity of content, morphology and piperine in vitro release. The microparticles obtaining process presented 97.6 ± 0.3% yield and were spherical, with 190 ± 13 μm size and Span of 1.698 ± 0.180. Encapsulation efficiency was 90.0 ± 0.9%, a piperine content of 298.3 ± 2.9 mg/g. The in vitro release demonstrated a controlled release of piperine from the microparticulated systems: in 24 h, 34.8 ± 1.6% of piperine were release, while 80.9 ± 1.5% of bulk piperine was dissolved. Bulk and tapped density, Carr’s index and Hausner ratio revealed the microparticles have excellent flow properties. Thus, to prepare the microparticulated tablets, the excipients employed were only a dissolution promotor (Kyron® T-314) and the diluent (Pullulan®). The tablets presented 99.1 ± 0.9 mg weight; thickness of 3.38 ± 0.03 mm; hardness of 3.0 ± 0.2 kgf and friability 0.4%. Piperine content was 19.7 ± 0.4 mg, close to the theoretical value. The active release from the tablets was controlled, presenting 49.4 ± 2.4 % release in 24 h and the release profile was similar to the profile release of piperine from the microparticles. With this result and the scanning electron spectroscopy, it can be seen that the microparticles remained intact after the compression. Therefore, in this study microparticles and microparticulated tablets containing piperine were developed, which presented adequate physical-chemical characteristics and release profiles in order to overcome the issues presented by piperine in its oral administration and, so, the microparticulated tablets are a promising dosage unit for this purpose. |
publishDate |
2019 |
dc.date.none.fl_str_mv |
2019-08-30 2021-08-04T00:40:27Z 2021-08-04T00:40:27Z |
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.uri.fl_str_mv |
http://repositorio.ufsm.br/handle/1/21716 |
dc.identifier.dark.fl_str_mv |
ark:/26339/0013000014trj |
url |
http://repositorio.ufsm.br/handle/1/21716 |
identifier_str_mv |
ark:/26339/0013000014trj |
dc.language.iso.fl_str_mv |
por |
language |
por |
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.format.none.fl_str_mv |
application/pdf |
dc.publisher.none.fl_str_mv |
Universidade Federal de Santa Maria Brasil Análises Clínicas e Toxicológicas UFSM Programa de Pós-Graduação em Ciências Farmacêuticas Centro de Ciências da Saúde |
publisher.none.fl_str_mv |
Universidade Federal de Santa Maria Brasil Análises Clínicas e Toxicológicas UFSM Programa de Pós-Graduação em Ciências Farmacêuticas Centro de Ciências da Saúde |
dc.source.none.fl_str_mv |
reponame:Manancial - Repositório Digital da UFSM instname:Universidade Federal de Santa Maria (UFSM) instacron:UFSM |
instname_str |
Universidade Federal de Santa Maria (UFSM) |
instacron_str |
UFSM |
institution |
UFSM |
reponame_str |
Manancial - Repositório Digital da UFSM |
collection |
Manancial - Repositório Digital da UFSM |
repository.name.fl_str_mv |
Manancial - Repositório Digital da UFSM - Universidade Federal de Santa Maria (UFSM) |
repository.mail.fl_str_mv |
atendimento.sib@ufsm.br||tedebc@gmail.com |
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1815172449521631232 |