Linked Life Data

14603506

Source:http://linkedlifedata.com/resource/pubmed/id/14603506

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:issue
11
pubmed:dateCreated
2003-11-6
pubmed:abstractText
Utilization of carrier-mediated transport systems in the gastrointestinal tract to increase the bioavailability of drugs is of great interest. In the present study, an increased supply of the driving force for peptide transporter PEPT1 by utilizing a proton-releasing polymer, Eudragit L100-55, was employed to increase the intestinal transport activity. Intestinal absorption of zwitterionic cefadroxil and dianionic cefixime was studied in rats by using in situ ileal closed loops and by in vivo oral administration of the drugs concomitantly with Eudragit L100-55. The results showed that Eudragit L100-55 decreased the pH in the intestinal loops, and increased the disappearance of both cefadroxil and cefixime from the loops. In rats, the plasma concentration after oral administration was increased significantly by coadministration of Eudragit L100-55, whereas a proton-nonreleasing analogous polymer, Eudragit RSPO, did not have any effect. Furthermore, the increased absorption of cefixime caused by Eudragit L100-55 was blocked by simultaneous administration of cefadroxil, a PEPT1 substrate/inhibitor, in a concentration-dependent manner. These results demonstrate that improvement of intestinal absorption of peptide-mimetics via a peptide transporter is possible by optimizing the transporter activity through coadministration of a proton-releasing polymer that supplies the driving force for the transporter.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/Acrylic Resins, http://linkedlifedata.com/resource/pubmed/chemical/Anti-Bacterial Agents, http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Cefixime, http://linkedlifedata.com/resource/pubmed/chemical/Cephalosporins, http://linkedlifedata.com/resource/pubmed/chemical/Eudragit L100-55, http://linkedlifedata.com/resource/pubmed/chemical/PepT1 protein, http://linkedlifedata.com/resource/pubmed/chemical/Pharmaceutical Preparations, http://linkedlifedata.com/resource/pubmed/chemical/Polymers, http://linkedlifedata.com/resource/pubmed/chemical/Protons, http://linkedlifedata.com/resource/pubmed/chemical/Slc15a1 protein, rat, http://linkedlifedata.com/resource/pubmed/chemical/Symporters
pubmed:status
MEDLINE
pubmed:month
Nov
pubmed:issn
0022-3549
pubmed:author
pubmed:copyrightInfo
Copyright 2003 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 92:2208-2216, 2003
pubmed:issnType
Print
pubmed:volume
92
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
2208-16
pubmed:dateRevised
2006-11-15
pubmed:meshHeading
pubmed:year
2003
pubmed:articleTitle
Enhanced intestinal absorption of drugs by activation of peptide transporter PEPT1 using proton-releasing polymer.
pubmed:affiliation
Faculty of Pharmaceutical Sciences, Department of Molecular Biopharmaceutics, Tokyo University of Science, 2641 Yamazaki, Noda, Chiba 278-8510, Japan.
pubmed:publicationType
Journal Article, Research Support, Non-U.S. Gov't