Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations

Autores
Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Ballent, Mariana; Sallovitz, Juan Manuel; Imperiale, Fernanda Andrea; Pis, Alejandra; Lanusse, Carlos Edmundo
Año de publicación
2007
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Ivermectin (IVM) is a broad-spectrum antiparasitic drug extensively used in veterinary medicine. The composition of the pharmaceutical preparation affects IVM absorption and its systemic availability. After the introduction of the first approved IVM formulation (propylene glycol/glycerol formal 60:40) used at 200 µg/kg, different pharmaceutical modifications have been assayed to extend IVM persistent endectocide activity. Recently, IVM 3.15% long-acting (IVM-LA) preparations to be administered at 630 µg/kg to cattle were introduced into the veterinary pharmaceutical market. The work reported here was designed to evaluate the comparative IVM absorption pattern and plasma concentration profiles obtained after subcutaneous administration of the classic pioneer IVM formulation (1%) and two different commercially available IVM-LA preparations (3.15 %) to cattle. Twenty-eight (28) Holstein heifers were divided in 4 experimental groups (n=7) and treated subcutaneously as follows: Group A: IVM 1% given at 200 µg/kg, Group B: IVM 1% administered at 630 µg/kg, Group C: IVM-LA (A) injected at 630 µg/kg and Group D: IVM-LA (B) given at 630 µg/kg. Blood samples were taken between 0.5 and 90 days post-treatment and IVM plasma concentrations were determined by HPLC with fluorescence detection. There were no differences in the persistence of IVM plasma concentrations after the administration of IVM 1 % formulation at the two used dose levels (200 and 630 µg/kg). Higher peak plasma concentration (Cmax) and shorter mean residence time (MRT) were obtained for IVM 1 % given at 630 µg/kg (Group B) compared to the treatments with both IVM-LA preparations. The IVM-LA (A) formulation showed a more extended absorption process than IVM-LA (B) preparation, which accounted for a longer persistence of detectable IVM plasma concentrations. The parasitological implications of the observed differences in peak plasma concentrations (Cmax values) and in the IVM concentration levels measured from day 20, and afterwards until day 90 post-treatment, between the different preparations assayed need to be elucidated. The characterization of the absorption patterns and kinetic behaviour obtained after injection of these novel long-acting formulations used at three times the therapeutic dose recommended for the classic IVM preparation in cattle is a further contribution to the field.
Fil: Lifschitz, Adrian Luis. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Virkel, Guillermo Leon. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Ballent, Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Sallovitz, Juan Manuel. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Imperiale, Fernanda Andrea. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Pis, Alejandra. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Materia
IVERMECTIN
PHARMACOKINETICS
LONG ACTING PREPARATIONS
CATTLE
Nivel de accesibilidad
acceso abierto
Condiciones de uso
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
Repositorio
CONICET Digital (CONICET)
Institución
Consejo Nacional de Investigaciones Científicas y Técnicas
OAI Identificador
oai:ri.conicet.gov.ar:11336/103807
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/103807
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repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerationsLifschitz, Adrian LuisVirkel, Guillermo LeonBallent, MarianaSallovitz, Juan ManuelImperiale, Fernanda AndreaPis, AlejandraLanusse, Carlos EdmundoIVERMECTINPHARMACOKINETICSLONG ACTING PREPARATIONSCATTLEhttps://purl.org/becyt/ford/4.3https://purl.org/becyt/ford/4Ivermectin (IVM) is a broad-spectrum antiparasitic drug extensively used in veterinary medicine. The composition of the pharmaceutical preparation affects IVM absorption and its systemic availability. After the introduction of the first approved IVM formulation (propylene glycol/glycerol formal 60:40) used at 200 µg/kg, different pharmaceutical modifications have been assayed to extend IVM persistent endectocide activity. Recently, IVM 3.15% long-acting (IVM-LA) preparations to be administered at 630 µg/kg to cattle were introduced into the veterinary pharmaceutical market. The work reported here was designed to evaluate the comparative IVM absorption pattern and plasma concentration profiles obtained after subcutaneous administration of the classic pioneer IVM formulation (1%) and two different commercially available IVM-LA preparations (3.15 %) to cattle. Twenty-eight (28) Holstein heifers were divided in 4 experimental groups (n=7) and treated subcutaneously as follows: Group A: IVM 1% given at 200 µg/kg, Group B: IVM 1% administered at 630 µg/kg, Group C: IVM-LA (A) injected at 630 µg/kg and Group D: IVM-LA (B) given at 630 µg/kg. Blood samples were taken between 0.5 and 90 days post-treatment and IVM plasma concentrations were determined by HPLC with fluorescence detection. There were no differences in the persistence of IVM plasma concentrations after the administration of IVM 1 % formulation at the two used dose levels (200 and 630 µg/kg). Higher peak plasma concentration (Cmax) and shorter mean residence time (MRT) were obtained for IVM 1 % given at 630 µg/kg (Group B) compared to the treatments with both IVM-LA preparations. The IVM-LA (A) formulation showed a more extended absorption process than IVM-LA (B) preparation, which accounted for a longer persistence of detectable IVM plasma concentrations. The parasitological implications of the observed differences in peak plasma concentrations (Cmax values) and in the IVM concentration levels measured from day 20, and afterwards until day 90 post-treatment, between the different preparations assayed need to be elucidated. The characterization of the absorption patterns and kinetic behaviour obtained after injection of these novel long-acting formulations used at three times the therapeutic dose recommended for the classic IVM preparation in cattle is a further contribution to the field.Fil: Lifschitz, Adrian Luis. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; ArgentinaFil: Virkel, Guillermo Leon. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Ballent, Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; ArgentinaFil: Sallovitz, Juan Manuel. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; ArgentinaFil: Imperiale, Fernanda Andrea. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; ArgentinaFil: Pis, Alejandra. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; ArgentinaFil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; ArgentinaElsevier Science2007-07info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/103807Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Ballent, Mariana; Sallovitz, Juan Manuel; Imperiale, Fernanda Andrea; et al.; Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations; Elsevier Science; Veterinary Parasitology; 147; 3-4; 7-2007; 303-3100304-4017CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1016/j.vetpar.2007.04.009info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0304401707002300info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T10:00:07Zoai:ri.conicet.gov.ar:11336/103807instacron:CONICETInstitucionalhttp://ri.conicet.gov.ar/Organismo científico-tecnológicoNo correspondehttp://ri.conicet.gov.ar/oai/requestdasensio@conicet.gov.ar; lcarlino@conicet.gov.arArgentinaNo correspondeNo correspondeNo correspondeopendoar:34982025-09-03 10:00:07.311CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
title Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
spellingShingle Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
Lifschitz, Adrian Luis
IVERMECTIN
PHARMACOKINETICS
LONG ACTING PREPARATIONS
CATTLE
title_short Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
title_full Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
title_fullStr Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
title_full_unstemmed Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
title_sort Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations
dc.creator.none.fl_str_mv Lifschitz, Adrian Luis
Virkel, Guillermo Leon
Ballent, Mariana
Sallovitz, Juan Manuel
Imperiale, Fernanda Andrea
Pis, Alejandra
Lanusse, Carlos Edmundo
author Lifschitz, Adrian Luis
author_facet Lifschitz, Adrian Luis
Virkel, Guillermo Leon
Ballent, Mariana
Sallovitz, Juan Manuel
Imperiale, Fernanda Andrea
Pis, Alejandra
Lanusse, Carlos Edmundo
author_role author
author2 Virkel, Guillermo Leon
Ballent, Mariana
Sallovitz, Juan Manuel
Imperiale, Fernanda Andrea
Pis, Alejandra
Lanusse, Carlos Edmundo
author2_role author
author
author
author
author
author
dc.subject.none.fl_str_mv IVERMECTIN
PHARMACOKINETICS
LONG ACTING PREPARATIONS
CATTLE
topic IVERMECTIN
PHARMACOKINETICS
LONG ACTING PREPARATIONS
CATTLE
purl_subject.fl_str_mv https://purl.org/becyt/ford/4.3
https://purl.org/becyt/ford/4
dc.description.none.fl_txt_mv Ivermectin (IVM) is a broad-spectrum antiparasitic drug extensively used in veterinary medicine. The composition of the pharmaceutical preparation affects IVM absorption and its systemic availability. After the introduction of the first approved IVM formulation (propylene glycol/glycerol formal 60:40) used at 200 µg/kg, different pharmaceutical modifications have been assayed to extend IVM persistent endectocide activity. Recently, IVM 3.15% long-acting (IVM-LA) preparations to be administered at 630 µg/kg to cattle were introduced into the veterinary pharmaceutical market. The work reported here was designed to evaluate the comparative IVM absorption pattern and plasma concentration profiles obtained after subcutaneous administration of the classic pioneer IVM formulation (1%) and two different commercially available IVM-LA preparations (3.15 %) to cattle. Twenty-eight (28) Holstein heifers were divided in 4 experimental groups (n=7) and treated subcutaneously as follows: Group A: IVM 1% given at 200 µg/kg, Group B: IVM 1% administered at 630 µg/kg, Group C: IVM-LA (A) injected at 630 µg/kg and Group D: IVM-LA (B) given at 630 µg/kg. Blood samples were taken between 0.5 and 90 days post-treatment and IVM plasma concentrations were determined by HPLC with fluorescence detection. There were no differences in the persistence of IVM plasma concentrations after the administration of IVM 1 % formulation at the two used dose levels (200 and 630 µg/kg). Higher peak plasma concentration (Cmax) and shorter mean residence time (MRT) were obtained for IVM 1 % given at 630 µg/kg (Group B) compared to the treatments with both IVM-LA preparations. The IVM-LA (A) formulation showed a more extended absorption process than IVM-LA (B) preparation, which accounted for a longer persistence of detectable IVM plasma concentrations. The parasitological implications of the observed differences in peak plasma concentrations (Cmax values) and in the IVM concentration levels measured from day 20, and afterwards until day 90 post-treatment, between the different preparations assayed need to be elucidated. The characterization of the absorption patterns and kinetic behaviour obtained after injection of these novel long-acting formulations used at three times the therapeutic dose recommended for the classic IVM preparation in cattle is a further contribution to the field.
Fil: Lifschitz, Adrian Luis. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Virkel, Guillermo Leon. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Ballent, Mariana. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Sallovitz, Juan Manuel. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Imperiale, Fernanda Andrea. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Pis, Alejandra. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
Fil: Lanusse, Carlos Edmundo. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencias Veterinarias. Departamento de Fisiopatología. Laboratorio de Farmacología; Argentina
description Ivermectin (IVM) is a broad-spectrum antiparasitic drug extensively used in veterinary medicine. The composition of the pharmaceutical preparation affects IVM absorption and its systemic availability. After the introduction of the first approved IVM formulation (propylene glycol/glycerol formal 60:40) used at 200 µg/kg, different pharmaceutical modifications have been assayed to extend IVM persistent endectocide activity. Recently, IVM 3.15% long-acting (IVM-LA) preparations to be administered at 630 µg/kg to cattle were introduced into the veterinary pharmaceutical market. The work reported here was designed to evaluate the comparative IVM absorption pattern and plasma concentration profiles obtained after subcutaneous administration of the classic pioneer IVM formulation (1%) and two different commercially available IVM-LA preparations (3.15 %) to cattle. Twenty-eight (28) Holstein heifers were divided in 4 experimental groups (n=7) and treated subcutaneously as follows: Group A: IVM 1% given at 200 µg/kg, Group B: IVM 1% administered at 630 µg/kg, Group C: IVM-LA (A) injected at 630 µg/kg and Group D: IVM-LA (B) given at 630 µg/kg. Blood samples were taken between 0.5 and 90 days post-treatment and IVM plasma concentrations were determined by HPLC with fluorescence detection. There were no differences in the persistence of IVM plasma concentrations after the administration of IVM 1 % formulation at the two used dose levels (200 and 630 µg/kg). Higher peak plasma concentration (Cmax) and shorter mean residence time (MRT) were obtained for IVM 1 % given at 630 µg/kg (Group B) compared to the treatments with both IVM-LA preparations. The IVM-LA (A) formulation showed a more extended absorption process than IVM-LA (B) preparation, which accounted for a longer persistence of detectable IVM plasma concentrations. The parasitological implications of the observed differences in peak plasma concentrations (Cmax values) and in the IVM concentration levels measured from day 20, and afterwards until day 90 post-treatment, between the different preparations assayed need to be elucidated. The characterization of the absorption patterns and kinetic behaviour obtained after injection of these novel long-acting formulations used at three times the therapeutic dose recommended for the classic IVM preparation in cattle is a further contribution to the field.
publishDate 2007
dc.date.none.fl_str_mv 2007-07
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/publishedVersion
http://purl.org/coar/resource_type/c_6501
info:ar-repo/semantics/articulo
format article
status_str publishedVersion
dc.identifier.none.fl_str_mv http://hdl.handle.net/11336/103807
Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Ballent, Mariana; Sallovitz, Juan Manuel; Imperiale, Fernanda Andrea; et al.; Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations; Elsevier Science; Veterinary Parasitology; 147; 3-4; 7-2007; 303-310
0304-4017
CONICET Digital
CONICET
url http://hdl.handle.net/11336/103807
identifier_str_mv Lifschitz, Adrian Luis; Virkel, Guillermo Leon; Ballent, Mariana; Sallovitz, Juan Manuel; Imperiale, Fernanda Andrea; et al.; Ivermectin (3.15%) long-acting formulations in cattle: Absorption pattern and pharmacokinetic considerations; Elsevier Science; Veterinary Parasitology; 147; 3-4; 7-2007; 303-310
0304-4017
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1016/j.vetpar.2007.04.009
info:eu-repo/semantics/altIdentifier/url/https://www.sciencedirect.com/science/article/abs/pii/S0304401707002300
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
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eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
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dc.publisher.none.fl_str_mv Elsevier Science
publisher.none.fl_str_mv Elsevier Science
dc.source.none.fl_str_mv reponame:CONICET Digital (CONICET)
instname:Consejo Nacional de Investigaciones Científicas y Técnicas
reponame_str CONICET Digital (CONICET)
collection CONICET Digital (CONICET)
instname_str Consejo Nacional de Investigaciones Científicas y Técnicas
repository.name.fl_str_mv CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicas
repository.mail.fl_str_mv dasensio@conicet.gov.ar; lcarlino@conicet.gov.ar
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