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dc.contributor.author
Delrivo, Alicia
dc.contributor.author
Aloisio, Carolina
dc.contributor.author
Longhi, Marcela Raquel
dc.contributor.author
Granero, Gladys Ester
dc.date.available
2019-12-10T17:41:39Z
dc.date.issued
2018-02
dc.identifier.citation
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
dc.identifier.uri
http://hdl.handle.net/11336/91909
dc.description.abstract
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.
dc.format
application/pdf
dc.language.iso
eng
dc.publisher
Springer
dc.rights
info:eu-repo/semantics/openAccess
dc.rights.uri
https://creativecommons.org/licenses/by-nc-sa/2.5/ar/
dc.subject
SULFADIAZINE
dc.subject
ß-CYCLODEXTRIN
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AMINOACIDS
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BINARY AND TERNARY COMPLEXES
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IN VITRO PERMEABILITY METHOD
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INTESTINAL ABSORPTION
dc.subject.classification
Otras Ciencias Químicas
dc.subject.classification
Ciencias Químicas
dc.subject.classification
CIENCIAS NATURALES Y EXACTAS
dc.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
dc.type
info:eu-repo/semantics/article
dc.type
info:ar-repo/semantics/artículo
dc.type
info:eu-repo/semantics/publishedVersion
dc.date.updated
2019-10-23T21:11:21Z
dc.identifier.eissn
1530-9932
dc.journal.volume
19
dc.journal.pagination
1437-1447
dc.journal.pais
Alemania
dc.description.fil
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
dc.description.fil
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
dc.description.fil
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
dc.description.fil
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
dc.journal.title
AAPS Pharmscitech
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/url/http://link.springer.com/10.1208/s12249-018-0965-8
dc.relation.alternativeid
info:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1208/s12249-018-0965-8
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