In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats

Autores
Cárdenas, Paola Andrea; Kratz, Jadel Müller; Hernández, Aura; Costa, Geison Modesti; Ospina, Luis Fernando; Baena, Yolima; Simões, Cláudia Maria Oliveira; Jimenez Kairuz, Alvaro Federico; Aragón, Marcela
Año de publicación
2017
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
6-Methylcoumarin (6MC) is a semisynthetic coumarin with important in vitro and in vivo anti-inflammatory activity. In order to continue the pre-clinical characterization of this molecule, in vitro intestinal permeability, plasma profile and tissue distribution after oral administration in rats were studied. The permeability of 6MC was evaluated by the Caco-2 cellular model in both the apical-basal (A-B) and basal-apical (B-A) directions. The pharmacokinetics and biodistribution were evaluated in rats after oral and intraperitoneal administration at doses of 200 mg/kg. Transport experiments with Caco-2 cells showed that 6MC presented high permeability at all concentrations evaluated. This finding suggested that 6MC could be transported across the gut wall by passive diffusion. The plasma concentration-time curve showed that the maximum concentration (Cmax) was 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration, with elimination constant of (Ke) 0.0070 min-1 and a short life half time of (T1/2) lower that 120 min. The distribution study showed that 6MC has high accumulation in the liver, and widespread distribution in all the organs evaluated.
Fil: Cárdenas, Paola Andrea. Universidad Nacional de Colombia. Departamento de Farmacia. Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
Fil: Kratz, Jadel Müller. Universidade Federal de Santa Catarina. Departamento de Ciências Farmacêuticas. Grupo de Análise e Desenvolvimento de Fármacos de Origem Natural; Brasil
Fil: Hernández, Aura. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
Fil: Costa, Geison Modesti. Universidad Nacional de Colombia. Departamento de Química. Grupo de Estudio y Aprovechamiento de Productos Naturales Marinos y Frutas de Colombia ; Colombia
Fil: Ospina, Luis Fernando. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo de Principios Bioactivos de Plantas Medicinales; Colombia
Fil: Baena, Yolima. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
Fil: Simões, Cláudia Maria Oliveira. Universidade Federal de Santa Catarina. Departamento de Ciências Farmacêuticas. Grupo de Análise e Desenvolvimento de Fármacos de Origem Natural; Brasil
Fil: Jimenez Kairuz, Alvaro Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Ciencias Farmacéuticas; Argentina
Fil: Aragón, Marcela. Universidad Nacional de Colombia. Departamento de Farmacia. Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
Materia
6-METHYLCOUMARIN/DISTRIBUTION
6-METHYLCOUMARIN/PHARMACOKINETICS/RATS
INTESTINAL PERMEABILITY/STUDY
INTESTINAL PERMEABILITY/STUDY/IN VITRO
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:11336/65859
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/65859
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar ratsCárdenas, Paola AndreaKratz, Jadel MüllerHernández, AuraCosta, Geison ModestiOspina, Luis FernandoBaena, YolimaSimões, Cláudia Maria OliveiraJimenez Kairuz, Alvaro FedericoAragón, Marcela6-METHYLCOUMARIN/DISTRIBUTION6-METHYLCOUMARIN/PHARMACOKINETICS/RATSINTESTINAL PERMEABILITY/STUDYINTESTINAL PERMEABILITY/STUDY/IN VITROhttps://purl.org/becyt/ford/3.1https://purl.org/becyt/ford/36-Methylcoumarin (6MC) is a semisynthetic coumarin with important in vitro and in vivo anti-inflammatory activity. In order to continue the pre-clinical characterization of this molecule, in vitro intestinal permeability, plasma profile and tissue distribution after oral administration in rats were studied. The permeability of 6MC was evaluated by the Caco-2 cellular model in both the apical-basal (A-B) and basal-apical (B-A) directions. The pharmacokinetics and biodistribution were evaluated in rats after oral and intraperitoneal administration at doses of 200 mg/kg. Transport experiments with Caco-2 cells showed that 6MC presented high permeability at all concentrations evaluated. This finding suggested that 6MC could be transported across the gut wall by passive diffusion. The plasma concentration-time curve showed that the maximum concentration (Cmax) was 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration, with elimination constant of (Ke) 0.0070 min-1 and a short life half time of (T1/2) lower that 120 min. The distribution study showed that 6MC has high accumulation in the liver, and widespread distribution in all the organs evaluated.Fil: Cárdenas, Paola Andrea. Universidad Nacional de Colombia. Departamento de Farmacia. Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; ColombiaFil: Kratz, Jadel Müller. Universidade Federal de Santa Catarina. Departamento de Ciências Farmacêuticas. Grupo de Análise e Desenvolvimento de Fármacos de Origem Natural; BrasilFil: Hernández, Aura. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; ColombiaFil: Costa, Geison Modesti. Universidad Nacional de Colombia. Departamento de Química. Grupo de Estudio y Aprovechamiento de Productos Naturales Marinos y Frutas de Colombia ; ColombiaFil: Ospina, Luis Fernando. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo de Principios Bioactivos de Plantas Medicinales; ColombiaFil: Baena, Yolima. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; ColombiaFil: Simões, Cláudia Maria Oliveira. Universidade Federal de Santa Catarina. Departamento de Ciências Farmacêuticas. Grupo de Análise e Desenvolvimento de Fármacos de Origem Natural; BrasilFil: Jimenez Kairuz, Alvaro Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Ciencias Farmacéuticas; ArgentinaFil: Aragón, Marcela. Universidad Nacional de Colombia. Departamento de Farmacia. Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; ColombiaUniversidade de São Paulo2017-04-20info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/65859Cárdenas, Paola Andrea; Kratz, Jadel Müller; Hernández, Aura; Costa, Geison Modesti; Ospina, Luis Fernando; et al.; In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats; Universidade de São Paulo; Brazilian Journal Of Pharmaceutical Sciences; 53; 1; 20-4-20171984-82502175-9790CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100621&lng=en&nrm=iso&tlng=eninfo:eu-repo/semantics/altIdentifier/doi/10.1590/s2175-97902017000116081info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-09-03T09:48:42Zoai:ri.conicet.gov.ar:11336/65859instacron: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 09:48:42.991CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
title In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
spellingShingle In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
Cárdenas, Paola Andrea
6-METHYLCOUMARIN/DISTRIBUTION
6-METHYLCOUMARIN/PHARMACOKINETICS/RATS
INTESTINAL PERMEABILITY/STUDY
INTESTINAL PERMEABILITY/STUDY/IN VITRO
title_short In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
title_full In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
title_fullStr In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
title_full_unstemmed In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
title_sort In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats
dc.creator.none.fl_str_mv Cárdenas, Paola Andrea
Kratz, Jadel Müller
Hernández, Aura
Costa, Geison Modesti
Ospina, Luis Fernando
Baena, Yolima
Simões, Cláudia Maria Oliveira
Jimenez Kairuz, Alvaro Federico
Aragón, Marcela
author Cárdenas, Paola Andrea
author_facet Cárdenas, Paola Andrea
Kratz, Jadel Müller
Hernández, Aura
Costa, Geison Modesti
Ospina, Luis Fernando
Baena, Yolima
Simões, Cláudia Maria Oliveira
Jimenez Kairuz, Alvaro Federico
Aragón, Marcela
author_role author
author2 Kratz, Jadel Müller
Hernández, Aura
Costa, Geison Modesti
Ospina, Luis Fernando
Baena, Yolima
Simões, Cláudia Maria Oliveira
Jimenez Kairuz, Alvaro Federico
Aragón, Marcela
author2_role author
author
author
author
author
author
author
author
dc.subject.none.fl_str_mv 6-METHYLCOUMARIN/DISTRIBUTION
6-METHYLCOUMARIN/PHARMACOKINETICS/RATS
INTESTINAL PERMEABILITY/STUDY
INTESTINAL PERMEABILITY/STUDY/IN VITRO
topic 6-METHYLCOUMARIN/DISTRIBUTION
6-METHYLCOUMARIN/PHARMACOKINETICS/RATS
INTESTINAL PERMEABILITY/STUDY
INTESTINAL PERMEABILITY/STUDY/IN VITRO
purl_subject.fl_str_mv https://purl.org/becyt/ford/3.1
https://purl.org/becyt/ford/3
dc.description.none.fl_txt_mv 6-Methylcoumarin (6MC) is a semisynthetic coumarin with important in vitro and in vivo anti-inflammatory activity. In order to continue the pre-clinical characterization of this molecule, in vitro intestinal permeability, plasma profile and tissue distribution after oral administration in rats were studied. The permeability of 6MC was evaluated by the Caco-2 cellular model in both the apical-basal (A-B) and basal-apical (B-A) directions. The pharmacokinetics and biodistribution were evaluated in rats after oral and intraperitoneal administration at doses of 200 mg/kg. Transport experiments with Caco-2 cells showed that 6MC presented high permeability at all concentrations evaluated. This finding suggested that 6MC could be transported across the gut wall by passive diffusion. The plasma concentration-time curve showed that the maximum concentration (Cmax) was 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration, with elimination constant of (Ke) 0.0070 min-1 and a short life half time of (T1/2) lower that 120 min. The distribution study showed that 6MC has high accumulation in the liver, and widespread distribution in all the organs evaluated.
Fil: Cárdenas, Paola Andrea. Universidad Nacional de Colombia. Departamento de Farmacia. Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
Fil: Kratz, Jadel Müller. Universidade Federal de Santa Catarina. Departamento de Ciências Farmacêuticas. Grupo de Análise e Desenvolvimento de Fármacos de Origem Natural; Brasil
Fil: Hernández, Aura. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
Fil: Costa, Geison Modesti. Universidad Nacional de Colombia. Departamento de Química. Grupo de Estudio y Aprovechamiento de Productos Naturales Marinos y Frutas de Colombia ; Colombia
Fil: Ospina, Luis Fernando. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo de Principios Bioactivos de Plantas Medicinales; Colombia
Fil: Baena, Yolima. Universidad Nacional de Colombia. Departamento de Farmacia.Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
Fil: Simões, Cláudia Maria Oliveira. Universidade Federal de Santa Catarina. Departamento de Ciências Farmacêuticas. Grupo de Análise e Desenvolvimento de Fármacos de Origem Natural; Brasil
Fil: Jimenez Kairuz, Alvaro Federico. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Ciencias Farmacéuticas; Argentina
Fil: Aragón, Marcela. Universidad Nacional de Colombia. Departamento de Farmacia. Grupo Sistemas de Liberación Modificada de Moléculas Biológicamente Activas; Colombia
description 6-Methylcoumarin (6MC) is a semisynthetic coumarin with important in vitro and in vivo anti-inflammatory activity. In order to continue the pre-clinical characterization of this molecule, in vitro intestinal permeability, plasma profile and tissue distribution after oral administration in rats were studied. The permeability of 6MC was evaluated by the Caco-2 cellular model in both the apical-basal (A-B) and basal-apical (B-A) directions. The pharmacokinetics and biodistribution were evaluated in rats after oral and intraperitoneal administration at doses of 200 mg/kg. Transport experiments with Caco-2 cells showed that 6MC presented high permeability at all concentrations evaluated. This finding suggested that 6MC could be transported across the gut wall by passive diffusion. The plasma concentration-time curve showed that the maximum concentration (Cmax) was 17.13 ± 2.90 µg/mL at maximum time (Tmax) of 30 min for the oral route and Cmax 26.18 ± 2.47 µg/mL at 6.0 min for the intraperitoneal administration, with elimination constant of (Ke) 0.0070 min-1 and a short life half time of (T1/2) lower that 120 min. The distribution study showed that 6MC has high accumulation in the liver, and widespread distribution in all the organs evaluated.
publishDate 2017
dc.date.none.fl_str_mv 2017-04-20
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/11336/65859
Cárdenas, Paola Andrea; Kratz, Jadel Müller; Hernández, Aura; Costa, Geison Modesti; Ospina, Luis Fernando; et al.; In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats; Universidade de São Paulo; Brazilian Journal Of Pharmaceutical Sciences; 53; 1; 20-4-2017
1984-8250
2175-9790
CONICET Digital
CONICET
url http://hdl.handle.net/11336/65859
identifier_str_mv Cárdenas, Paola Andrea; Kratz, Jadel Müller; Hernández, Aura; Costa, Geison Modesti; Ospina, Luis Fernando; et al.; In vitro intestinal permeability studies, pharmacokinetics and tissue distribution of 6-methylcoumarin after oral and intraperitoneal administration in Wistar rats; Universidade de São Paulo; Brazilian Journal Of Pharmaceutical Sciences; 53; 1; 20-4-2017
1984-8250
2175-9790
CONICET Digital
CONICET
dc.language.none.fl_str_mv eng
language eng
dc.relation.none.fl_str_mv info:eu-repo/semantics/altIdentifier/url/http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502017000100621&lng=en&nrm=iso&tlng=en
info:eu-repo/semantics/altIdentifier/doi/10.1590/s2175-97902017000116081
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 Universidade de São Paulo
publisher.none.fl_str_mv Universidade de São Paulo
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 13.13397

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