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Titolo:
Intestinal drug efflux: formulation and food effects
Autore:
Wagner, D; Spahn-Langguth, H; Hanafy, A; Koggel, A; Langguth, P;
Indirizzi:
Univ Mainz, Sch Pharm, Dept Biopharmaceut & Pharmaceut Technol, D-55099 Mainz, Germany Univ Mainz Mainz Germany D-55099 rmaceut Technol, D-55099 Mainz, Germany Univ Halle Wittenberg, Dept Pharmaceut Chem, D-06120 Halle Saale, Germany Univ Halle Wittenberg Halle Saale Germany D-06120 0 Halle Saale, Germany
Titolo Testata:
ADVANCED DRUG DELIVERY REVIEWS
, volume: 50, anno: 2001, supplemento:, 1
pagine: S13 - S31
SICI:
0169-409X(20011001)50:<S13:IDEFAF>2.0.ZU;2-0
Fonte:
ISI
Lingua:
ENG
Soggetto:
MULTIDRUG-RESISTANCE PHENOTYPE; ORGANIC CATION/CARNITINE TRANSPORTER; P-GLYCOPROTEIN TRANSPORTERS; BETA-LACTAM ANTIBIOTICS; CACO-2 CELL MONOLAYERS; GRAPEFRUIT JUICE; TISSUE DISTRIBUTION; GASTROINTESTINAL-TRACT; CREMOPHOR EL; IN-VITRO;
Keywords:
efflux pumps; multidrug resistance protein family; P-glycoprotein; intestinal perfusion; intestinal secretion; site-dependent absorption; intestinal permeability;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
87
Recensione:
Indirizzi per estratti:
Indirizzo: Langguth, P Univ Mainz, Sch Pharm, Dept Biopharmaceut & Pharmaceut Technol, Staudingerweg 5, D-55099 Mainz, Germany Univ Mainz Staudingerweg 5 MainzGermany D-55099 inz, Germany
Citazione:
D. Wagner et al., "Intestinal drug efflux: formulation and food effects", ADV DRUG DE, 50, 2001, pp. S13-S31

Abstract

The intestine, primarily regarded as an absorptive organ, is also preparedfor the elimination of certain organic acids, bases and neutral compounds depending on their affinity to intestinal carrier systems. Several of the transport systems known to mediate efflux in the major clearing organs - liver and kidney - are also expressed in the intestine. Examples of secretory transporters in the intestine are P-glycoprotein, members of the multidrug resistance associated protein family, breast cancer resistance protein, organic cation transporters and members of the organic anion polypeptide family. In this communication, the P-glycoprotein mediated intestinal secretion of talinolol, a model compound showing metabolic stability, has been investigated in the jejunum, ileum and colon of rat intestine by single-pass perfusion. A model has been developed which demonstrates an increase in carrier-mediated secretion in the order jejunum < ileum < colon. Furthermore, the potency of common excipients in peroral drug products towards inhibition ofP-gp mediated secretion has been investigated using a radioligand-binding assay and transport studies in Caco-2 cell monolayers. Finally, evidence isprovided which demonstrates that constituents of grapefruit juice not onlymay influence intestinal drug metabolism, but can also interfere with secretory transport systems, leading to a new and yet undescribed mechanism in drug-food interactions. (C) 2001 Elsevier Science BY. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 13/07/20 alle ore 18:02:24