Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion

Autores
Soraci, Alejandro Luis; Tapia, Maria Ofelia; Garcia, Jorge
Año de publicación
2005
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
Flurbirpofen (FBP), a member of the 2-aryl propionate nonsteroidal anti-inflammatory drug class, has potent anti-inflammatory and analgesic properties. The commercial preparation is a racemic mixture of the R(−) and S(+) enantiomers of FBP. In this study, R(−) and S(+) FBP were used to investigate the metabolic chiral inversion. Each enantiomer was administered separately (0.25 mg/kg) and in a racemic mixture (0.5 mg/kg) intravenously to horses. Plasma and synovial concentration of each enantiomer was determined and the disposition of each was analyzed. After intravenous administration of R(−) FBP and S(+) FBP to horses no chiral inversion was detected. After the administration of the FBP racemate and individual enantiomers no differences were observed between pharmacokinetic parameters [t1/2â (h), Cl (L/h·kg), AUC (ìg·h/mL), Vss (L/kg) and MRT (h)] for R(−) and S(+) FBF. Synovial fluid concentrations of both FBP enantiomers were lower than plasma concentrations and no stereoselective differences were detected. These data indicate that the disposition of FBF in horses is not enantioselective and demonstrate a difference in the pharmacokinetic behavior of the enantiomers as compared with other 2-aryl-propionic acids, such as carprofen, ketoprofen and vedaprofen in the horse.
Fil: Soraci, Alejandro Luis. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; Argentina
Fil: Tapia, Maria Ofelia. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Garcia, Jorge. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; Argentina
Materia
FLURBIPROFEN
HORSES
ENANTIOMERS
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:11336/106014
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/106014
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversionSoraci, Alejandro LuisTapia, Maria OfeliaGarcia, JorgeFLURBIPROFENHORSESENANTIOMERShttps://purl.org/becyt/ford/4.3https://purl.org/becyt/ford/4Flurbirpofen (FBP), a member of the 2-aryl propionate nonsteroidal anti-inflammatory drug class, has potent anti-inflammatory and analgesic properties. The commercial preparation is a racemic mixture of the R(−) and S(+) enantiomers of FBP. In this study, R(−) and S(+) FBP were used to investigate the metabolic chiral inversion. Each enantiomer was administered separately (0.25 mg/kg) and in a racemic mixture (0.5 mg/kg) intravenously to horses. Plasma and synovial concentration of each enantiomer was determined and the disposition of each was analyzed. After intravenous administration of R(−) FBP and S(+) FBP to horses no chiral inversion was detected. After the administration of the FBP racemate and individual enantiomers no differences were observed between pharmacokinetic parameters [t1/2â (h), Cl (L/h·kg), AUC (ìg·h/mL), Vss (L/kg) and MRT (h)] for R(−) and S(+) FBF. Synovial fluid concentrations of both FBP enantiomers were lower than plasma concentrations and no stereoselective differences were detected. These data indicate that the disposition of FBF in horses is not enantioselective and demonstrate a difference in the pharmacokinetic behavior of the enantiomers as compared with other 2-aryl-propionic acids, such as carprofen, ketoprofen and vedaprofen in the horse.Fil: Soraci, Alejandro Luis. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; ArgentinaFil: Tapia, Maria Ofelia. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; ArgentinaFil: Garcia, Jorge. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; ArgentinaWiley Blackwell Publishing, Inc2005-02info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/106014Soraci, Alejandro Luis; Tapia, Maria Ofelia; Garcia, Jorge; Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion; Wiley Blackwell Publishing, Inc; Journal of Veterinary Pharmacology and Therapeutics; 28; 1; 2-2005; 65-700140-77831365-2885CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/doi/10.1111/j.1365-2885.2004.00627.xinfo:eu-repo/semantics/altIdentifier/url/https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1365-2885.2004.00627.xinfo:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-10T13:16:27Zoai:ri.conicet.gov.ar:11336/106014instacron: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:34982025-09-10 13:16:27.947CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
title Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
spellingShingle Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
Soraci, Alejandro Luis
FLURBIPROFEN
HORSES
ENANTIOMERS
title_short Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
title_full Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
title_fullStr Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
title_full_unstemmed Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
title_sort Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion
dc.creator.none.fl_str_mv Soraci, Alejandro Luis
Tapia, Maria Ofelia
Garcia, Jorge
author Soraci, Alejandro Luis
author_facet Soraci, Alejandro Luis
Tapia, Maria Ofelia
Garcia, Jorge
author_role author
author2 Tapia, Maria Ofelia
Garcia, Jorge
author2_role author
author
dc.subject.none.fl_str_mv FLURBIPROFEN
HORSES
ENANTIOMERS
topic FLURBIPROFEN
HORSES
ENANTIOMERS
purl_subject.fl_str_mv https://purl.org/becyt/ford/4.3
https://purl.org/becyt/ford/4
dc.description.none.fl_txt_mv Flurbirpofen (FBP), a member of the 2-aryl propionate nonsteroidal anti-inflammatory drug class, has potent anti-inflammatory and analgesic properties. The commercial preparation is a racemic mixture of the R(−) and S(+) enantiomers of FBP. In this study, R(−) and S(+) FBP were used to investigate the metabolic chiral inversion. Each enantiomer was administered separately (0.25 mg/kg) and in a racemic mixture (0.5 mg/kg) intravenously to horses. Plasma and synovial concentration of each enantiomer was determined and the disposition of each was analyzed. After intravenous administration of R(−) FBP and S(+) FBP to horses no chiral inversion was detected. After the administration of the FBP racemate and individual enantiomers no differences were observed between pharmacokinetic parameters [t1/2â (h), Cl (L/h·kg), AUC (ìg·h/mL), Vss (L/kg) and MRT (h)] for R(−) and S(+) FBF. Synovial fluid concentrations of both FBP enantiomers were lower than plasma concentrations and no stereoselective differences were detected. These data indicate that the disposition of FBF in horses is not enantioselective and demonstrate a difference in the pharmacokinetic behavior of the enantiomers as compared with other 2-aryl-propionic acids, such as carprofen, ketoprofen and vedaprofen in the horse.
Fil: Soraci, Alejandro Luis. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; Argentina
Fil: Tapia, Maria Ofelia. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas; Argentina
Fil: Garcia, Jorge. Universidad Nacional del Centro de la Provincia de Buenos Aires. Facultad de Ciencia Veterinarias. Departamento de Fisiopatología. Laboratorio de Toxicología; Argentina
description Flurbirpofen (FBP), a member of the 2-aryl propionate nonsteroidal anti-inflammatory drug class, has potent anti-inflammatory and analgesic properties. The commercial preparation is a racemic mixture of the R(−) and S(+) enantiomers of FBP. In this study, R(−) and S(+) FBP were used to investigate the metabolic chiral inversion. Each enantiomer was administered separately (0.25 mg/kg) and in a racemic mixture (0.5 mg/kg) intravenously to horses. Plasma and synovial concentration of each enantiomer was determined and the disposition of each was analyzed. After intravenous administration of R(−) FBP and S(+) FBP to horses no chiral inversion was detected. After the administration of the FBP racemate and individual enantiomers no differences were observed between pharmacokinetic parameters [t1/2â (h), Cl (L/h·kg), AUC (ìg·h/mL), Vss (L/kg) and MRT (h)] for R(−) and S(+) FBF. Synovial fluid concentrations of both FBP enantiomers were lower than plasma concentrations and no stereoselective differences were detected. These data indicate that the disposition of FBF in horses is not enantioselective and demonstrate a difference in the pharmacokinetic behavior of the enantiomers as compared with other 2-aryl-propionic acids, such as carprofen, ketoprofen and vedaprofen in the horse.
publishDate 2005
dc.date.none.fl_str_mv 2005-02
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/11336/106014
Soraci, Alejandro Luis; Tapia, Maria Ofelia; Garcia, Jorge; Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion; Wiley Blackwell Publishing, Inc; Journal of Veterinary Pharmacology and Therapeutics; 28; 1; 2-2005; 65-70
0140-7783
1365-2885
CONICET Digital
CONICET
url http://hdl.handle.net/11336/106014
identifier_str_mv Soraci, Alejandro Luis; Tapia, Maria Ofelia; Garcia, Jorge; Pharmacokinetics and synovial fluid concentrations of flurbiprofen enantiomers in horses: chiral inversion; Wiley Blackwell Publishing, Inc; Journal of Veterinary Pharmacology and Therapeutics; 28; 1; 2-2005; 65-70
0140-7783
1365-2885
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/doi/10.1111/j.1365-2885.2004.00627.x
info:eu-repo/semantics/altIdentifier/url/https://onlinelibrary.wiley.com/doi/abs/10.1111/j.1365-2885.2004.00627.x
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
eu_rights_str_mv openAccess
rights_invalid_str_mv https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Wiley Blackwell Publishing, Inc
publisher.none.fl_str_mv Wiley Blackwell Publishing, Inc
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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score 12.993085

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