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J Pharm Sci ; 105(1): 339-42, 2016 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-26852864

RESUMO

We investigated the influence of sweet and umami (savory) tastants on the intestinal absorption of cephalexin (CEX), a substrate of peptide transporter 1 (PEPT1, SLC15A1) in rats. After oral administration of glucose or mannitol to rats, CEX was administered together with a second dose of glucose or mannitol. Western blot analysis indicated that expression of PEPT1 in rat jejunum membrane was decreased by glucose, compared to mannitol. Furthermore, the maximum plasma concentration (Cmax) of orally administered CEX was reduced by glucose compared to mannitol. The effect of glucose was diminished by nifedipine, a L-type Ca(2+) channel blocker. We also found that Cmax of orally administered CEX was reduced by treatment with L-glutamic acid, compared to D-glutamic acid. Thus, excessive intake of glucose and L-glutamic acid may impair oral absorption of PEPT1 substrates.


Assuntos
Glucose/farmacologia , Ácido Glutâmico/farmacologia , Células Receptoras Sensoriais/efeitos dos fármacos , Simportadores/metabolismo , Papilas Gustativas/efeitos dos fármacos , Animais , Bloqueadores dos Canais de Cálcio/farmacologia , Cefalexina/farmacocinética , Absorção Intestinal , Jejuno/efeitos dos fármacos , Jejuno/metabolismo , Masculino , Manitol/farmacologia , Membranas/efeitos dos fármacos , Membranas/metabolismo , Nifedipino/farmacologia , Transportador 1 de Peptídeos , Transporte Proteico/efeitos dos fármacos , Ratos , Ratos Wistar , Simportadores/efeitos dos fármacos
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