Título : Effect of Common Excipients on Intestinal Drug Absorption in
Wistar Rats |
Autor : Ruiz Picazo, Alejandro Gonzalez-Alvarez, Marta Gonzalez-Alvarez, Isabel Bermejo, Marival |
Editor : American Chemical Society |
Departamento: Departamentos de la UMH::Ingeniería |
Fecha de publicación: 2020-05 |
URI : https://hdl.handle.net/11000/35148 |
Resumen :
Theaimof thepresentpaper is tostudytheeffectofcommonexcipientsonthepermeabilityofatenolol (asdrug absorbedmainlybypassivediffusion)andrhodamine(asP-glycoproteinsubstrate).Theapparentpermeabilitywasmeasuredbyan insituperfusionmethod inWistar ratsusing theclosed loopDoluisio’smethod. Permeabilityvalueswerecharacterized inthe absence andpresenceof 18commonlyusedexcipients. Excipient concentrationswere selectedbasedon the amounts inoral immediate releasedosage forms,which failedthe testduring thehumanbioequivalence studies.Atenololwas studiedwithand withoutexcipients inthewholesmall intestine,whereasrhodaminewastestedinthreedifferent intestinal segmentstoaccount for thedifferential expressionof P-glycoprotein, and itwas further on tested in the ileum, in thepresenceof excipients. Atenolol presentedhigherpermeabilityvalueswhenitwasadministeredwithcolloidal silica, croscarmellose,hydroxypropylmethylcellulose (HPMC),magnesiumstearate,MgCO3, poly(ethyleneglycol)400, poly(vinylpyrrolidone), sorbitol, starch, andTiO2 rhodamine showedhigherpermeabilityvalueswhenitwasadministeredwithcroscarmelloseandHPMC.Ontheonehand, themechanismsof actionwerenotdiscerniblewiththeproposedexperiments.Ontheotherhand, commercial formulationsdonotpresentasingle excipientbutseveral,whichcancounteracttheireffects.Theinsituperfusiontechniquecanbeusefulforapreliminaryscreeningand riskanalysis,whilethe invivopharmacokineticresultswouldbeneededtodefineconclusiveeffects.
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Palabras clave/Materias: permeability excipient passivediffusion P-glycoprotein |
Área de conocimiento : CDU: Ciencias aplicadas: Ingeniería. Tecnología |
Tipo de documento : info:eu-repo/semantics/article |
Derechos de acceso: info:eu-repo/semantics/closedAccess Attribution-NonCommercial-NoDerivatives 4.0 Internacional |
DOI : https://dx.doi.org/10.1021/acs.molpharmaceut.0c00023 |
Aparece en las colecciones: Artículos Ingeniería
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