Por favor, use este identificador para citar o enlazar este ítem: https://hdl.handle.net/11000/35148

Effect of Common Excipients on Intestinal Drug Absorption in Wistar Rats


no-thumbnailVer/Abrir:

 6 Effect of Common Excipients on Intestinal Drug Absorption (1).pdf



1,18 MB
Adobe PDF
Compartir:

Este recurso está restringido

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.
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



Creative Commons La licencia se describe como: Atribución-NonComercial-NoDerivada 4.0 Internacional.