Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the format...

Autores
Delrivo, Alicia; Aloisio, Carolina; Longhi, Marcela Raquel; Granero, Gladys Ester
Año de publicación
2018
Idioma
inglés
Tipo de recurso
artículo
Estado
versión publicada
Descripción
We propose an in vitro permeability assay by using a modified lipid membrane to predict the in vivo intestinal passive permeability of drugs. Two conditions were tested, one with a gradient pH (pH 5.5-donor/pH 7.4-receptor) and the other with an iso-pH 7.4. The predictability of the method was established by correlating the obtained apparent intestinal permeability coefficients (Papp) and the oral dose fraction absorbed in humans (fa) of 16 drugs with different absorption properties. The Papp values correlated well with the absorption rates under the two conditions and the method showed high predictability and good reproducibility. On the other hand, with this method, we successfully predicted the transport characteristics of oral sulfadiazine (SDZ). Also, the tradeoff between the increase in the solubility of SDZ by its complex formation with cyclodextrins and/or aminoacids and its oral permeability was assessed. Results suggest that SDZ is transported through the gastrointestinal epithelium by passive diffusion in a pH-dependent manner. These results support the classification of SDZ as a high/low borderline permeability compound and are in agreement with the Biopharmaceutics Classification Systems (BCS). This conclusion is consistent with the in vivo pharmacokinetic properties of SDZ.
Fil: Delrivo, Alicia. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina
Fil: Aloisio, Carolina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Longhi, Marcela Raquel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Granero, Gladys Ester. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Materia
SULFADIAZINE
ß-CYCLODEXTRIN
AMINOACIDS
BINARY AND TERNARY COMPLEXES
IN VITRO PERMEABILITY METHOD
INTESTINAL ABSORPTION
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:11336/91909
Acceder
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oai_identifier_str oai:ri.conicet.gov.ar:11336/91909
network_acronym_str CONICETDig
repository_id_str 3498
network_name_str CONICET Digital (CONICET)
spelling Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrinsDelrivo, AliciaAloisio, CarolinaLonghi, Marcela RaquelGranero, Gladys EsterSULFADIAZINEß-CYCLODEXTRINAMINOACIDSBINARY AND TERNARY COMPLEXESIN VITRO PERMEABILITY METHODINTESTINAL ABSORPTIONhttps://purl.org/becyt/ford/1.4https://purl.org/becyt/ford/1We propose an in vitro permeability assay by using a modified lipid membrane to predict the in vivo intestinal passive permeability of drugs. Two conditions were tested, one with a gradient pH (pH 5.5-donor/pH 7.4-receptor) and the other with an iso-pH 7.4. The predictability of the method was established by correlating the obtained apparent intestinal permeability coefficients (Papp) and the oral dose fraction absorbed in humans (fa) of 16 drugs with different absorption properties. The Papp values correlated well with the absorption rates under the two conditions and the method showed high predictability and good reproducibility. On the other hand, with this method, we successfully predicted the transport characteristics of oral sulfadiazine (SDZ). Also, the tradeoff between the increase in the solubility of SDZ by its complex formation with cyclodextrins and/or aminoacids and its oral permeability was assessed. Results suggest that SDZ is transported through the gastrointestinal epithelium by passive diffusion in a pH-dependent manner. These results support the classification of SDZ as a high/low borderline permeability compound and are in agreement with the Biopharmaceutics Classification Systems (BCS). This conclusion is consistent with the in vivo pharmacokinetic properties of SDZ.Fil: Delrivo, Alicia. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; ArgentinaFil: Aloisio, Carolina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Longhi, Marcela Raquel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaFil: Granero, Gladys Ester. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; ArgentinaSpringer2018-02info:eu-repo/semantics/articleinfo:eu-repo/semantics/publishedVersionhttp://purl.org/coar/resource_type/c_6501info:ar-repo/semantics/articuloapplication/pdfapplication/pdfapplication/pdfhttp://hdl.handle.net/11336/91909Delrivo, Alicia; Aloisio, Carolina; Longhi, Marcela Raquel; Granero, Gladys Ester; Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins; Springer; AAPS Pharmscitech; 19; 2-2018; 1437-14471530-9932CONICET DigitalCONICETenginfo:eu-repo/semantics/altIdentifier/url/http://link.springer.com/10.1208/s12249-018-0965-8info:eu-repo/semantics/altIdentifier/doi/10.1208/s12249-018-0965-8info:eu-repo/semantics/openAccesshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/reponame:CONICET Digital (CONICET)instname:Consejo Nacional de Investigaciones Científicas y Técnicas2025-10-22T11:06:27Zoai:ri.conicet.gov.ar:11336/91909instacron: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:34982025-10-22 11:06:27.341CONICET Digital (CONICET) - Consejo Nacional de Investigaciones Científicas y Técnicasfalse
dc.title.none.fl_str_mv Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
title Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
spellingShingle Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
Delrivo, Alicia
SULFADIAZINE
ß-CYCLODEXTRIN
AMINOACIDS
BINARY AND TERNARY COMPLEXES
IN VITRO PERMEABILITY METHOD
INTESTINAL ABSORPTION
title_short Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
title_full Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
title_fullStr Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
title_full_unstemmed Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
title_sort Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins
dc.creator.none.fl_str_mv Delrivo, Alicia
Aloisio, Carolina
Longhi, Marcela Raquel
Granero, Gladys Ester
author Delrivo, Alicia
author_facet Delrivo, Alicia
Aloisio, Carolina
Longhi, Marcela Raquel
Granero, Gladys Ester
author_role author
author2 Aloisio, Carolina
Longhi, Marcela Raquel
Granero, Gladys Ester
author2_role author
author
author
dc.subject.none.fl_str_mv SULFADIAZINE
ß-CYCLODEXTRIN
AMINOACIDS
BINARY AND TERNARY COMPLEXES
IN VITRO PERMEABILITY METHOD
INTESTINAL ABSORPTION
topic SULFADIAZINE
ß-CYCLODEXTRIN
AMINOACIDS
BINARY AND TERNARY COMPLEXES
IN VITRO PERMEABILITY METHOD
INTESTINAL ABSORPTION
purl_subject.fl_str_mv https://purl.org/becyt/ford/1.4
https://purl.org/becyt/ford/1
dc.description.none.fl_txt_mv We propose an in vitro permeability assay by using a modified lipid membrane to predict the in vivo intestinal passive permeability of drugs. Two conditions were tested, one with a gradient pH (pH 5.5-donor/pH 7.4-receptor) and the other with an iso-pH 7.4. The predictability of the method was established by correlating the obtained apparent intestinal permeability coefficients (Papp) and the oral dose fraction absorbed in humans (fa) of 16 drugs with different absorption properties. The Papp values correlated well with the absorption rates under the two conditions and the method showed high predictability and good reproducibility. On the other hand, with this method, we successfully predicted the transport characteristics of oral sulfadiazine (SDZ). Also, the tradeoff between the increase in the solubility of SDZ by its complex formation with cyclodextrins and/or aminoacids and its oral permeability was assessed. Results suggest that SDZ is transported through the gastrointestinal epithelium by passive diffusion in a pH-dependent manner. These results support the classification of SDZ as a high/low borderline permeability compound and are in agreement with the Biopharmaceutics Classification Systems (BCS). This conclusion is consistent with the in vivo pharmacokinetic properties of SDZ.
Fil: Delrivo, Alicia. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Departamento de Farmacia; Argentina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba; Argentina
Fil: Aloisio, Carolina. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Longhi, Marcela Raquel. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
Fil: Granero, Gladys Ester. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Córdoba. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica. Universidad Nacional de Córdoba. Facultad de Ciencias Químicas. Unidad de Investigación y Desarrollo en Tecnología Farmacéutica; Argentina
description We propose an in vitro permeability assay by using a modified lipid membrane to predict the in vivo intestinal passive permeability of drugs. Two conditions were tested, one with a gradient pH (pH 5.5-donor/pH 7.4-receptor) and the other with an iso-pH 7.4. The predictability of the method was established by correlating the obtained apparent intestinal permeability coefficients (Papp) and the oral dose fraction absorbed in humans (fa) of 16 drugs with different absorption properties. The Papp values correlated well with the absorption rates under the two conditions and the method showed high predictability and good reproducibility. On the other hand, with this method, we successfully predicted the transport characteristics of oral sulfadiazine (SDZ). Also, the tradeoff between the increase in the solubility of SDZ by its complex formation with cyclodextrins and/or aminoacids and its oral permeability was assessed. Results suggest that SDZ is transported through the gastrointestinal epithelium by passive diffusion in a pH-dependent manner. These results support the classification of SDZ as a high/low borderline permeability compound and are in agreement with the Biopharmaceutics Classification Systems (BCS). This conclusion is consistent with the in vivo pharmacokinetic properties of SDZ.
publishDate 2018
dc.date.none.fl_str_mv 2018-02
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/11336/91909
Delrivo, Alicia; Aloisio, Carolina; Longhi, Marcela Raquel; Granero, Gladys Ester; Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins; Springer; AAPS Pharmscitech; 19; 2-2018; 1437-1447
1530-9932
CONICET Digital
CONICET
url http://hdl.handle.net/11336/91909
identifier_str_mv Delrivo, Alicia; Aloisio, Carolina; Longhi, Marcela Raquel; Granero, Gladys Ester; Artificial lipid membrane permeability method for predicting intestinal drug transport: Probing the determining step in the oral absorption of sulfadiazine; Influence of the formation of binary and ternary complexes with cyclodextrins; Springer; AAPS Pharmscitech; 19; 2-2018; 1437-1447
1530-9932
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://link.springer.com/10.1208/s12249-018-0965-8
info:eu-repo/semantics/altIdentifier/doi/10.1208/s12249-018-0965-8
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
application/pdf
dc.publisher.none.fl_str_mv Springer
publisher.none.fl_str_mv Springer
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 12.982451

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