Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis

Detalhes bibliográficos
Ano de defesa: 2016
Autor(a) principal: Magalh?es, Viviane de Souza lattes
Orientador(a): Scott, Fabio Barbour
Banca de defesa: Castro, Bruno Gomes de, Martins, Jo?o Ricardo de Souza, Martins, Isabella Vilhena Freire
Tipo de documento: Tese
Tipo de acesso: Acesso aberto
Idioma: por
Instituição de defesa: Universidade Federal Rural do Rio de Janeiro
Programa de Pós-Graduação: Programa de P?s-Gradua??o em Ci?ncia, Tecnologia e Inova??o em Agropecu?ria
Departamento: Pr?-Reitoria de Pesquisa e P?s-Gradua??o
País: Brasil
Palavras-chave em Português:
Palavras-chave em Inglês:
Área do conhecimento CNPq:
Link de acesso: https://tede.ufrrj.br/jspui/handle/jspui/5328
Resumo: Brazil is the country belonging to MERCOSUL with the largest cattle herd. It is the first in number of slaughter and meat production, therefore occupies a prominent place on the international scene. To maintain productivity is needed investments in management, genetics and sanities operations. When talk about sanities the parasitosis play a role of importance and may determine serious damage to health of animals. In the last three decades have not been a new development of molecules with fungicidal action only the introduce, in the veterinary market Brazilian products, innovations in associations, presentations, formulations, routes and forms of administration. The aim of this study is development an injectable formulation of fipronil and evaluate its bioavailability and efficacy to control Haematobia irritans e Dermatobia hominis. Thirteen formulations were developed (F1 to F13). It was performed accelerated stability test where after six months five formulations were stable (F3, F4, F5, F10 e F11). It studied the plasma profile of stable higher dosage formulations (F10 and F11) and compared with the topical commercial formulation. For the development of analytical methods, two sample preparation techniques were tested, both using HPLC-UV techniques. The use of RAM column was not efficient and the SPE technique was validated with a linear range of 5 to 500 ng / mL for fipronil and 10 a 500 ng / mL for fipronil sulfone. The precisions were 13.7 e 10.9 to fipronil and fipronil sulfone respectively and accuracy of 7.2 and 5.5% to fipronil and fipronil sulfone respectively. With this methodology it was possible to evaluate the plasma profile of the formulations F10, F11 and topical commercial formulation finding the higher bioavailability at injectable formulation with fewer N-metilpirrolidone (F10). The metabolism product, fipronil sulfone, was quantitated after approximately 15 days in all formulations and the half-life time of fipronil was 37 hours for injectable formulations (F10 e F11) and 100 hours for topical commercial formulation. To evaluate the influence of the formulations in the interruption of the life cycle of H.irritans was performed a efficacy test during 21 days. For this test was collected feces of treated animals. Faeces samples were incubated for evaluate of hatching eggs. The results show that F10 and F11 were able to inhibit the hatching eggs of H.irritans. To evaluate the efficacy to control D.hominis larvae was performed a efficacy test with 10 cattle during 28 days finding 54, 65 and 72% efficacy for commercial topical formulation, F10 and F11 respectively, 7 days after treatment. Twenty-one days after treatment, the efficacy increased to 97, 99 and 98% for F10, F11 and commercial topical formulation respectively demonstrating that the formulations were effective in controlling D.hominis in cattle. These results clearly demonstrate that subcutaneously fipronil action as a ectoparasiticide to control of these parasites in cattle and may be a new treatment alternative.
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spelling Scott, Fabio Barbour001.382.167-97Castro, Bruno Gomes deMartins, Jo?o Ricardo de SouzaMartins, Isabella Vilhena Freire057.185.477-00http://lattes.cnpq.br/1129995417777144Magalh?es, Viviane de Souza2022-01-24T08:07:47Z2016-03-21MAGALH?ES, Viviane de Souza. Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis. 2016. 93 f. Tese (Doutorado em Ci?ncia, Tecnologia e Inova??o em Agropecu?ria) - Pr?-Reitoria de Pesquisa e P?s-Gradua??o, Universidade Federal Rural do Rio de Janeiro, Serop?dica, 2016.https://tede.ufrrj.br/jspui/handle/jspui/5328Brazil is the country belonging to MERCOSUL with the largest cattle herd. It is the first in number of slaughter and meat production, therefore occupies a prominent place on the international scene. To maintain productivity is needed investments in management, genetics and sanities operations. When talk about sanities the parasitosis play a role of importance and may determine serious damage to health of animals. In the last three decades have not been a new development of molecules with fungicidal action only the introduce, in the veterinary market Brazilian products, innovations in associations, presentations, formulations, routes and forms of administration. The aim of this study is development an injectable formulation of fipronil and evaluate its bioavailability and efficacy to control Haematobia irritans e Dermatobia hominis. Thirteen formulations were developed (F1 to F13). It was performed accelerated stability test where after six months five formulations were stable (F3, F4, F5, F10 e F11). It studied the plasma profile of stable higher dosage formulations (F10 and F11) and compared with the topical commercial formulation. For the development of analytical methods, two sample preparation techniques were tested, both using HPLC-UV techniques. The use of RAM column was not efficient and the SPE technique was validated with a linear range of 5 to 500 ng / mL for fipronil and 10 a 500 ng / mL for fipronil sulfone. The precisions were 13.7 e 10.9 to fipronil and fipronil sulfone respectively and accuracy of 7.2 and 5.5% to fipronil and fipronil sulfone respectively. With this methodology it was possible to evaluate the plasma profile of the formulations F10, F11 and topical commercial formulation finding the higher bioavailability at injectable formulation with fewer N-metilpirrolidone (F10). The metabolism product, fipronil sulfone, was quantitated after approximately 15 days in all formulations and the half-life time of fipronil was 37 hours for injectable formulations (F10 e F11) and 100 hours for topical commercial formulation. To evaluate the influence of the formulations in the interruption of the life cycle of H.irritans was performed a efficacy test during 21 days. For this test was collected feces of treated animals. Faeces samples were incubated for evaluate of hatching eggs. The results show that F10 and F11 were able to inhibit the hatching eggs of H.irritans. To evaluate the efficacy to control D.hominis larvae was performed a efficacy test with 10 cattle during 28 days finding 54, 65 and 72% efficacy for commercial topical formulation, F10 and F11 respectively, 7 days after treatment. Twenty-one days after treatment, the efficacy increased to 97, 99 and 98% for F10, F11 and commercial topical formulation respectively demonstrating that the formulations were effective in controlling D.hominis in cattle. These results clearly demonstrate that subcutaneously fipronil action as a ectoparasiticide to control of these parasites in cattle and may be a new treatment alternative.O Brasil ? o pa?s pertencente ao MERCOSUL com o maior rebanho bovino, sendo tamb?m o primeiro lugar em n?mero de abates e produ??o de carnes, por este motivo ocupa lugar de destaque no cen?rio internacional. Para manter esta produtividade se faz necess?rio investimentos em manejo, gen?tica e sanidades. Quanto a sanidade as parasitoses desempenham um papel de relev?ncia podendo determinar s?rios preju?zos a sa?de dos animais. Nas ?ltimas tr?s d?cadas n?o t?m ocorrido o desenvolvimento pronunciado de novas mol?culas com a??o parasiticidas. O que se observa ? o lan?amento no mercado veterin?rio brasileiro de produtos que apresentam inova??es em associa??es, apresenta??es, formula??es, vias e formas de administra??o. Este estudo tem como objetivo desenvolver uma formula??o injet?vel de fipronil e avaliar a sua biodisponibilidade e efic?cia contra Haematobia irritans e Dermatobia hominis. Para isto, foram desenvolvidas 13 formula??es (F1 a 13) e submetidas ao teste de estabilidade acelerada onde ao fim de 6 meses 5 eram est?veis (F3, F4, F5, F10 e F11). Foi constru?do o perfil plasm?tico das formula??es est?veis de maior dosagem (F10 e F11) e comparadas a formula??o t?pica comercial. Para o desenvolvimento de m?todos de an?lise, duas t?cnicas de prepara??o de amostras foram testadas. Ambas com an?lise por CLAE-UV. A t?cnica com utiliza??o de coluna MAR n?o foi eficiente sendo validade a t?cnica com EFS com intervalo de 5 a 500 ng / mL para fipronil e de 10 a 500 ng / mL para fipronil-sulfona. Os valores de precis?o m?dia encontrados foram de 13,7 e 10, 9 de fipronil e fipronil sulfona, respectivamente, e a exatid?o m?dia de 7,2 e 5,5% para o fipronil e fipronil sulfona, respectivamente. Com esta metodologia foi poss?vel avaliar o perfil plasm?tico das formula??es F10, F11 e comercial encontrando maiores biodisponibilidade na formula??o injet?vel com menor quantidade de N-metilpirrolidona (F10). A presen?a do produto de metaboliza??o fipronil sulfona s? pode ser quantificada ap?s aproximadamente 15 dias em todas as formula??es e um tempo de meia-vida do fipronil de 37 horas para as formula??es injet?veis (F10 e F11) e 100 horas para a formula??o t?pica comercial foi encontrado. A fim de testar a influ?ncia das formula??es na interrup??o do ciclo evolutivo de H.irritans de ovo a adulto foi realizado um teste de efic?cia durante 21 dias. Neste teste foi coletada fezes de animais tratados. As amostras de fezes foram incubadas para avalia??o da eclos?o de ovos. Os resultados mostraram que as F10 e F11 foram formula??es capazes de inibir a eclos?o de ovos de H.irritans inibindo o ciclo de crescimento deste parasita. Para testar a efic?cia contra larvas de D.hominis foi realizado um teste de efic?cia com 10 bovinos durante 28 dias encontrando efic?cias de 54, 65 e 72% para a formula??o t?pica comercial, F10 e F11 respectivamente ap?s 7 dias de tratamento. Ap?s 21 dias de tratamento, as efic?cias aumentaram para 97, 99 e 98% para F10, F11 e formula??o t?pica comercial respectivamente, demonstrando que as formula??es foram eficazes no controle D.hominis em bovinos. Com os dados obtidos neste trabalho fica demonstrado claramente que o fipronil possui a??o ectoparisiticida por via subcut?nea para o controle destes parasitas em bovinos. Podendo ser uma nova alternativa de tratamento.Submitted by Jorge Silva (jorgelmsilva@ufrrj.br) on 2022-01-24T08:07:47Z No. of bitstreams: 1 2016 - Viviane de Souza Magalh?es.pdf: 1557364 bytes, checksum: c38b7032ca5ab5d3949f02597c2fe38f (MD5)Made available in DSpace on 2022-01-24T08:07:47Z (GMT). No. of bitstreams: 1 2016 - Viviane de Souza Magalh?es.pdf: 1557364 bytes, checksum: c38b7032ca5ab5d3949f02597c2fe38f (MD5) Previous issue date: 2016-03-21CAPES - Coordena??o de Aperfei?oamento de Pessoal de N?vel Superiorapplication/pdfhttps://tede.ufrrj.br/retrieve/67932/2016%20-%20Viviane%20de%20Souza%20Magalh%c3%a3es.pdf.jpgporUniversidade Federal Rural do Rio de JaneiroPrograma de P?s-Gradua??o em Ci?ncia, Tecnologia e Inova??o em Agropecu?riaUFRRJBrasilPr?-Reitoria de Pesquisa e P?s-Gradua??oAAJOUD, A.; RAVANEL, P.; TISSUT, M. Fipronil Metabolism and Dissipation in a Simplified Aquatic Ecosystem. Journal of Agricultural and Food Chemistry, v. 51, n. 5, p. 1347?1352, 26 fev. 2003. AHMED, I. Pharmaceutical challenges in veterinary product development. Advanced Drug Delivery Reviews, v. 54, n. 6, p. 871?882, 4 out. 2002. ALVIM, A. M.; MORAES, S. L. Os investimentos estrangeiros diretos no agroneg?cio brasileiro. Indicadores Econ?micos, v. 40, n. 3, p. 105?120, 2013. ANDRADE, S. 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dc.title.por.fl_str_mv Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
dc.title.alternative.eng.fl_str_mv Fipronil injection for cattle: pharmacokinetics and effectiveness to control Haematobia irritans and Dermatobia hominis
title Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
spellingShingle Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
Magalh?es, Viviane de Souza
Fenilpirazol
Ectoparasito
Farmacot?cnica
Fipronil
Ectoparasites
Pharmaceutical Technology
Medicina Veterin?ria
title_short Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
title_full Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
title_fullStr Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
title_full_unstemmed Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
title_sort Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis
author Magalh?es, Viviane de Souza
author_facet Magalh?es, Viviane de Souza
author_role author
dc.contributor.advisor1.fl_str_mv Scott, Fabio Barbour
dc.contributor.advisor1ID.fl_str_mv 001.382.167-97
dc.contributor.referee1.fl_str_mv Castro, Bruno Gomes de
dc.contributor.referee2.fl_str_mv Martins, Jo?o Ricardo de Souza
dc.contributor.referee3.fl_str_mv Martins, Isabella Vilhena Freire
dc.contributor.authorID.fl_str_mv 057.185.477-00
dc.contributor.authorLattes.fl_str_mv http://lattes.cnpq.br/1129995417777144
dc.contributor.author.fl_str_mv Magalh?es, Viviane de Souza
contributor_str_mv Scott, Fabio Barbour
Castro, Bruno Gomes de
Martins, Jo?o Ricardo de Souza
Martins, Isabella Vilhena Freire
dc.subject.por.fl_str_mv Fenilpirazol
Ectoparasito
Farmacot?cnica
topic Fenilpirazol
Ectoparasito
Farmacot?cnica
Fipronil
Ectoparasites
Pharmaceutical Technology
Medicina Veterin?ria
dc.subject.eng.fl_str_mv Fipronil
Ectoparasites
Pharmaceutical Technology
dc.subject.cnpq.fl_str_mv Medicina Veterin?ria
description Brazil is the country belonging to MERCOSUL with the largest cattle herd. It is the first in number of slaughter and meat production, therefore occupies a prominent place on the international scene. To maintain productivity is needed investments in management, genetics and sanities operations. When talk about sanities the parasitosis play a role of importance and may determine serious damage to health of animals. In the last three decades have not been a new development of molecules with fungicidal action only the introduce, in the veterinary market Brazilian products, innovations in associations, presentations, formulations, routes and forms of administration. The aim of this study is development an injectable formulation of fipronil and evaluate its bioavailability and efficacy to control Haematobia irritans e Dermatobia hominis. Thirteen formulations were developed (F1 to F13). It was performed accelerated stability test where after six months five formulations were stable (F3, F4, F5, F10 e F11). It studied the plasma profile of stable higher dosage formulations (F10 and F11) and compared with the topical commercial formulation. For the development of analytical methods, two sample preparation techniques were tested, both using HPLC-UV techniques. The use of RAM column was not efficient and the SPE technique was validated with a linear range of 5 to 500 ng / mL for fipronil and 10 a 500 ng / mL for fipronil sulfone. The precisions were 13.7 e 10.9 to fipronil and fipronil sulfone respectively and accuracy of 7.2 and 5.5% to fipronil and fipronil sulfone respectively. With this methodology it was possible to evaluate the plasma profile of the formulations F10, F11 and topical commercial formulation finding the higher bioavailability at injectable formulation with fewer N-metilpirrolidone (F10). The metabolism product, fipronil sulfone, was quantitated after approximately 15 days in all formulations and the half-life time of fipronil was 37 hours for injectable formulations (F10 e F11) and 100 hours for topical commercial formulation. To evaluate the influence of the formulations in the interruption of the life cycle of H.irritans was performed a efficacy test during 21 days. For this test was collected feces of treated animals. Faeces samples were incubated for evaluate of hatching eggs. The results show that F10 and F11 were able to inhibit the hatching eggs of H.irritans. To evaluate the efficacy to control D.hominis larvae was performed a efficacy test with 10 cattle during 28 days finding 54, 65 and 72% efficacy for commercial topical formulation, F10 and F11 respectively, 7 days after treatment. Twenty-one days after treatment, the efficacy increased to 97, 99 and 98% for F10, F11 and commercial topical formulation respectively demonstrating that the formulations were effective in controlling D.hominis in cattle. These results clearly demonstrate that subcutaneously fipronil action as a ectoparasiticide to control of these parasites in cattle and may be a new treatment alternative.
publishDate 2016
dc.date.issued.fl_str_mv 2016-03-21
dc.date.accessioned.fl_str_mv 2022-01-24T08:07:47Z
dc.type.status.fl_str_mv info:eu-repo/semantics/publishedVersion
dc.type.driver.fl_str_mv info:eu-repo/semantics/doctoralThesis
format doctoralThesis
status_str publishedVersion
dc.identifier.citation.fl_str_mv MAGALH?ES, Viviane de Souza. Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis. 2016. 93 f. Tese (Doutorado em Ci?ncia, Tecnologia e Inova??o em Agropecu?ria) - Pr?-Reitoria de Pesquisa e P?s-Gradua??o, Universidade Federal Rural do Rio de Janeiro, Serop?dica, 2016.
dc.identifier.uri.fl_str_mv https://tede.ufrrj.br/jspui/handle/jspui/5328
identifier_str_mv MAGALH?ES, Viviane de Souza. Fipronil injet?vel para bovinos: farmacocin?tica e efic?cia no controle de Haematobia irritans e Dermatobia hominis. 2016. 93 f. Tese (Doutorado em Ci?ncia, Tecnologia e Inova??o em Agropecu?ria) - Pr?-Reitoria de Pesquisa e P?s-Gradua??o, Universidade Federal Rural do Rio de Janeiro, Serop?dica, 2016.
url https://tede.ufrrj.br/jspui/handle/jspui/5328
dc.language.iso.fl_str_mv por
language por
dc.relation.references.por.fl_str_mv AAJOUD, A.; RAVANEL, P.; TISSUT, M. Fipronil Metabolism and Dissipation in a Simplified Aquatic Ecosystem. Journal of Agricultural and Food Chemistry, v. 51, n. 5, p. 1347?1352, 26 fev. 2003. AHMED, I. Pharmaceutical challenges in veterinary product development. Advanced Drug Delivery Reviews, v. 54, n. 6, p. 871?882, 4 out. 2002. ALVIM, A. M.; MORAES, S. L. Os investimentos estrangeiros diretos no agroneg?cio brasileiro. Indicadores Econ?micos, v. 40, n. 3, p. 105?120, 2013. ANDRADE, S. F.; SANTAREM, V. A. Endoparaditicidas e ectoparasiticidas. In: Manual de Terap?utica Veterin?ria. 2. ed. S?o Paulo: Roca, 2002. p. 437?468. ANZIANI, O. S.; FLORES, S. G.; GUGLIELMONE, A. A. Activity of Injectable Doramectin Against Haematobia Irritans in Cattle. Revista Brasileira de Parasitologia Veterin?ria, v. 9, n. 2, p. 115?118, 2000. AULTON, M. E. Delineamento de formas farmac?utica. 2. ed. Porto Alegre: Artmed, 2005. BARBOSA, Catarina In?s Oliveira Gama Nunes. Novas Formas Farmac?uticas Para Uso Veterin?rio. 2010. 62 f. TCC (Gradua??o) - Curso de Licenciatura em Ci?ncias Farmac?uticas, Universidade Fernando Pessoa, Porto, 2010. BARROS, A. T. M.; SHUMAKER, T. T. S.; KOLLER, W. W.; KLAFKE, G. M.; ALBUQUERQUE, T. A.; GONZALEZ, R.. Mechanisms of pyrethroid resistance in Haematobia irritans ( Muscidae ) from Mato Grosso do Sul state , Brazil. Revista Brasileira de Parasitologia Veterin?ria, v. 22, n. 1, p. 136?142, 2013. BIANCHIN, I.; ALVES, R. G. O. Mosca-dos-chifres , Haematobia irritans : comportamento e danos em vacas e bezerros Nelore antes da desmama 1. Pesquisa Veterinaria Brasileira, v. 22, n. 3, p. 109?113, 2002. BIANCHIN, I.; KOLLER, W. W.; DETMANN, E. Sazonalidade de Haematobia irritans no Brasil Central. Pesquisa Veterin?ria Brasileira, v. 26, n. 2, p. 79?86, jun. 2006. BICHON, E.; RICHARD, C. A.; BIZEC, B. LE. 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