Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas

Detalhes bibliográficos
Autor(a) principal: Silva, Elviscley de Oliveira
Data de Publicação: 2015
Tipo de documento: Dissertação
Idioma: por
Título da fonte: Repositório Institucional da UFG
dARK ID: ark:/38995/001300000bfc0
Texto Completo: http://repositorio.bc.ufg.br/tede/handle/tede/4909
Resumo: Artemisia annua is originally from China, where it is used over two thousand years in the treatment of various diseases, especially malaria. The chemical compound of main therapeutic importance is artemisinin, a sesquiterpene lactone with an endoperoxide ring, responsible for potent antimalarial activity of the plant. Only one study about the production of pharmaceutical forms to A. annua extract was found in the literature. The main objective of this work was to obtain a concentrated extract of aerial parts of A. annua and using this for production of phytomedicines. The vegetal drug showed adequate physicochemical properties and artemisinin content of 1.15 ± 0.05 %. All assays of the analytical method validation were in specifications with LOD and LOQ of 1.3 mg/ml and 4.0 mg/ml of artemisinin, respectively. The partial validations for analyze of tablets, capsules and pellets were within the specifications in selectivity, linearity and repeatability testing. The vegetable drug was percolated and obtained 80% yield artemisinin extraction. Four kilograms of vegetable drugs yielded 2.5 liters of concentrated extract with 1.47% (w/v) of artemisinin and 30.78% (w/w) of dry residue. This was used to produce pellets, tablets and capsules, which contained 8.1 mg, 9.6 mg and 10.0 mg of artemisinin, respectively. All showed determination weight and content uniformity within specifications, demonstrating that the manufacture from the concentrated extract was effective in relation to the desired dosage artemisinin. The tablets showed immediate dissolution at pH 6.8 only. At pH 1.2 disintegrated in 60 minutes, releasing 85.2% of artemisinin against 99.8% of the capsules at 20 min, and 103.3% of pellets at 30 minutes. The dissolution profile of the capsules and pellets showed a very fast immediate dissolution at pH 1.2 and 6.8. Therefore, the dissolution efficiency (DE) of the tablets was lower than that of the capsules and pellets, for both pH values. The value F2 indicated a difference between the profiles of the tablets at different pH values, with the smallest dissolution in pH 1.2. The formulations prepared in this study demonstrated how the concentrate extract of A. annua can be used to manufacture phytomedicines content artemisinin near the expected and other appropriate physico-chemical properties.
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spelling Bara, Maria Teresa Freitashttp://lattes.cnpq.br/3914164125498267Conceição, Edemilson Cardoso daBara, Maria Teresa FfreitasMarreto, Ricardo NevesRezende, Kênnia Rochahttp://lattes.cnpq.br/5320043494719184Silva, Elviscley de Oliveira2015-11-17T19:02:30Z2015-02-26SILVA, E. O. Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas. 2015. 89 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2015.http://repositorio.bc.ufg.br/tede/handle/tede/4909ark:/38995/001300000bfc0Artemisia annua is originally from China, where it is used over two thousand years in the treatment of various diseases, especially malaria. The chemical compound of main therapeutic importance is artemisinin, a sesquiterpene lactone with an endoperoxide ring, responsible for potent antimalarial activity of the plant. Only one study about the production of pharmaceutical forms to A. annua extract was found in the literature. The main objective of this work was to obtain a concentrated extract of aerial parts of A. annua and using this for production of phytomedicines. The vegetal drug showed adequate physicochemical properties and artemisinin content of 1.15 ± 0.05 %. All assays of the analytical method validation were in specifications with LOD and LOQ of 1.3 mg/ml and 4.0 mg/ml of artemisinin, respectively. The partial validations for analyze of tablets, capsules and pellets were within the specifications in selectivity, linearity and repeatability testing. The vegetable drug was percolated and obtained 80% yield artemisinin extraction. Four kilograms of vegetable drugs yielded 2.5 liters of concentrated extract with 1.47% (w/v) of artemisinin and 30.78% (w/w) of dry residue. This was used to produce pellets, tablets and capsules, which contained 8.1 mg, 9.6 mg and 10.0 mg of artemisinin, respectively. All showed determination weight and content uniformity within specifications, demonstrating that the manufacture from the concentrated extract was effective in relation to the desired dosage artemisinin. The tablets showed immediate dissolution at pH 6.8 only. At pH 1.2 disintegrated in 60 minutes, releasing 85.2% of artemisinin against 99.8% of the capsules at 20 min, and 103.3% of pellets at 30 minutes. The dissolution profile of the capsules and pellets showed a very fast immediate dissolution at pH 1.2 and 6.8. Therefore, the dissolution efficiency (DE) of the tablets was lower than that of the capsules and pellets, for both pH values. The value F2 indicated a difference between the profiles of the tablets at different pH values, with the smallest dissolution in pH 1.2. The formulations prepared in this study demonstrated how the concentrate extract of A. annua can be used to manufacture phytomedicines content artemisinin near the expected and other appropriate physico-chemical properties.A Artemisia annua é originária da China, onde é utilizada há mais de dois mil anos no tratamento de diversas patologias, principalmente malária. O composto químico de principal importância terapêutica é a artemisinina, uma lactona sesquiterpênica que contém um anel endoperóxido, responsável pela potente atividade antimalárica da planta. Apenas um estudo sobre a produção de formas farmacêuticas com extrato de A. annua foi encontrado na literatura e não foram encontrados no mercado fitoterápicos contendo este. Desta forma, o objetivo principal deste trabalho foi a obtenção de extrato concentrado de partes aéreas de A. annua e utilização deste para produção de formas farmacêuticas sólidas. A droga vegetal apresentou teor de artemisinina de 1,15 ± 0,05 %. Todos os ensaios da validação do método analítico ficaram dentro das especificações, com LD e LQ de 1,3 μg/mL e 4,0 μg/mL de artemisinina, respectivamente. As validações parciais para análise dos comprimidos, cápsulas e péletes também ficaram dentro das especificações nos ensaios realizados. A droga vegetal foi percolada e obteve-se rendimento de 80 % na extração de artemisinina. Quatro quilos de droga vegetal deram origem a 2,5 litros de extrato concentrado, com 1,47 % (m/v) de artemisinina e 30,78 % (m/m) de resíduo seco. Este foi utilizado para produzir péletes, cápsulas e comprimidos, que contiveram 8,1 mg, 9,6 mg e 10,0 mg de artemisinina, respectivamente. Todas apresentaram determinação de peso e uniformidade de conteúdo dentro das especificações, demonstrando que sua produção foi eficiente em relação à dosagem de artemisinina almejada. Os comprimidos apresentaram dissolução imediata somente em pH 6,8. Em pH 1,2 desintegraram em 60 min, com liberação de 85,2 % de artemisinina, contra 99,8 % das cápsulas, em 20 min, e 103,3 % e dos péletes, em 30 min. O perfil de dissolução das cápsulas e dos péletes revelou uma dissolução imediata muito rápido em pH 1,2 e 6,8. Logo, a eficiência de dissolução (ED) dos comprimidos foi menor que das cápsulas e dos péletes, em ambos os pH. O valor de F2 indicou diferença entre os perfis dos comprimidos nos diferentes valores de pH, sendo a menor dissolução em pH 1,2. As formulações preparadas neste trabalho demonstraram como o extrato concentrado de A. annua pode ser utilizado na fabricação de fitoterápicos com teor de artemisinina próximo do esperado e demais propriedades físico-químicas adequadas.Submitted by Erika Demachki (erikademachki@gmail.com) on 2015-11-17T19:00:34Z No. of bitstreams: 2 Dissertação - Elviscley de Oliveira Silva - 2015.pdf: 1699560 bytes, checksum: 1d3e86c573e3ea74ff0239f2b7255be1 (MD5) license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5)Approved for entry into archive by Erika Demachki (erikademachki@gmail.com) on 2015-11-17T19:02:30Z (GMT) No. of bitstreams: 2 Dissertação - Elviscley de Oliveira Silva - 2015.pdf: 1699560 bytes, checksum: 1d3e86c573e3ea74ff0239f2b7255be1 (MD5) license_rdf: 23148 bytes, checksum: 9da0b6dfac957114c6a7714714b86306 (MD5)Made available in DSpace on 2015-11-17T19:02:30Z (GMT). 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dc.title.por.fl_str_mv Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
title Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
spellingShingle Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
Silva, Elviscley de Oliveira
Extrato vegetal
Fitoterápicos
Perfil de dissolução
Validação analítica
Vegetal extract
Phytomedicines
Dissolution profile
Analytical validation
CIENCIAS DA SAUDE::FARMACIA
title_short Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
title_full Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
title_fullStr Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
title_full_unstemmed Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
title_sort Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas
author Silva, Elviscley de Oliveira
author_facet Silva, Elviscley de Oliveira
author_role author
dc.contributor.advisor1.fl_str_mv Bara, Maria Teresa Freitas
dc.contributor.advisor1Lattes.fl_str_mv http://lattes.cnpq.br/3914164125498267
dc.contributor.advisor-co1.fl_str_mv Conceição, Edemilson Cardoso da
dc.contributor.referee1.fl_str_mv Bara, Maria Teresa Ffreitas
dc.contributor.referee2.fl_str_mv Marreto, Ricardo Neves
dc.contributor.referee3.fl_str_mv Rezende, Kênnia Rocha
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/5320043494719184
dc.contributor.author.fl_str_mv Silva, Elviscley de Oliveira
contributor_str_mv Bara, Maria Teresa Freitas
Conceição, Edemilson Cardoso da
Bara, Maria Teresa Ffreitas
Marreto, Ricardo Neves
Rezende, Kênnia Rocha
dc.subject.por.fl_str_mv Extrato vegetal
Fitoterápicos
Perfil de dissolução
Validação analítica
topic Extrato vegetal
Fitoterápicos
Perfil de dissolução
Validação analítica
Vegetal extract
Phytomedicines
Dissolution profile
Analytical validation
CIENCIAS DA SAUDE::FARMACIA
dc.subject.eng.fl_str_mv Vegetal extract
Phytomedicines
Dissolution profile
Analytical validation
dc.subject.cnpq.fl_str_mv CIENCIAS DA SAUDE::FARMACIA
description Artemisia annua is originally from China, where it is used over two thousand years in the treatment of various diseases, especially malaria. The chemical compound of main therapeutic importance is artemisinin, a sesquiterpene lactone with an endoperoxide ring, responsible for potent antimalarial activity of the plant. Only one study about the production of pharmaceutical forms to A. annua extract was found in the literature. The main objective of this work was to obtain a concentrated extract of aerial parts of A. annua and using this for production of phytomedicines. The vegetal drug showed adequate physicochemical properties and artemisinin content of 1.15 ± 0.05 %. All assays of the analytical method validation were in specifications with LOD and LOQ of 1.3 mg/ml and 4.0 mg/ml of artemisinin, respectively. The partial validations for analyze of tablets, capsules and pellets were within the specifications in selectivity, linearity and repeatability testing. The vegetable drug was percolated and obtained 80% yield artemisinin extraction. Four kilograms of vegetable drugs yielded 2.5 liters of concentrated extract with 1.47% (w/v) of artemisinin and 30.78% (w/w) of dry residue. This was used to produce pellets, tablets and capsules, which contained 8.1 mg, 9.6 mg and 10.0 mg of artemisinin, respectively. All showed determination weight and content uniformity within specifications, demonstrating that the manufacture from the concentrated extract was effective in relation to the desired dosage artemisinin. The tablets showed immediate dissolution at pH 6.8 only. At pH 1.2 disintegrated in 60 minutes, releasing 85.2% of artemisinin against 99.8% of the capsules at 20 min, and 103.3% of pellets at 30 minutes. The dissolution profile of the capsules and pellets showed a very fast immediate dissolution at pH 1.2 and 6.8. Therefore, the dissolution efficiency (DE) of the tablets was lower than that of the capsules and pellets, for both pH values. The value F2 indicated a difference between the profiles of the tablets at different pH values, with the smallest dissolution in pH 1.2. The formulations prepared in this study demonstrated how the concentrate extract of A. annua can be used to manufacture phytomedicines content artemisinin near the expected and other appropriate physico-chemical properties.
publishDate 2015
dc.date.accessioned.fl_str_mv 2015-11-17T19:02:30Z
dc.date.issued.fl_str_mv 2015-02-26
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
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dc.identifier.citation.fl_str_mv SILVA, E. O. Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas. 2015. 89 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2015.
dc.identifier.uri.fl_str_mv http://repositorio.bc.ufg.br/tede/handle/tede/4909
dc.identifier.dark.fl_str_mv ark:/38995/001300000bfc0
identifier_str_mv SILVA, E. O. Produção de extrato de Artemisia annua L. asteraceae e o uso deste na obtenção de formas farmacêuticas sólidas. 2015. 89 f. Dissertação (Mestrado em Ciências Farmacêuticas) - Universidade Federal de Goiás, Goiânia, 2015.
ark:/38995/001300000bfc0
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dc.publisher.none.fl_str_mv Universidade Federal de Goiás
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publisher.none.fl_str_mv Universidade Federal de Goiás
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repository.name.fl_str_mv Repositório Institucional da UFG - Universidade Federal de Goiás (UFG)
repository.mail.fl_str_mv tasesdissertacoes.bc@ufg.br
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