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Rapid CommunicationShort Communication

Increased Absorption of the Antiviral Ester Prodrug Tenofovir Disoproxil in Rat Ileum by Inhibiting Its Intestinal Metabolism

Jan Van Gelder, Sven Deferme, Pieter Annaert, Lieve Naesens, Erik De Clercq, Guy Van den Mooter, Renaat Kinget and Parick Augustijns
Drug Metabolism and Disposition December 2000, 28 (12) 1394-1396;
Jan Van Gelder
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Sven Deferme
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Pieter Annaert
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Lieve Naesens
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Erik De Clercq
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Guy Van den Mooter
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Renaat Kinget
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Parick Augustijns
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Abstract

Previous studies have shown that strawberry extract increases the transepithelial transport of tenofovir disoproxil, an esterase-sensitive prodrug of the antiviral compound tenofovir (formerly PMPA), across Caco-2 monolayers. This increase in transport was at least partially due to inhibition of its intestinal metabolism. To further study the feasibility of this absorption enhancing strategy, the influence of various concentrations of strawberry extract (0–2%) on the intestinal absorption of tenofovir disoproxil (100 μM) was assessed using an in situ perfusion model with immediate blood sampling from the mesenteric vein, a model closer to the in vivo situation than the in vitro Caco-2 system. Inclusion of strawberry extract (1%) resulted in a 7-fold increase in the appearance of tenofovir equivalents. The metabolism of tenofovir disoproxil in the intestinal perfusate was significantly lower in the presence of strawberry extract (1%), showing that the metabolism of tenofovir disoproxil is reduced by the flavoring extract.

Footnotes

  • Send reprint requests to: Patrick Augustijns, Ph.D., Laboratorium voor Farmacotechnologie en Biofarmacie, Katholieke Universiteit Leuven, Campus Gasthuisberg, Onderwijs en Navorsing, B-3000 Leuven, Belgium. E-mail:patrick.augustijns{at}farm.kuleuven.ac.be

  • This study was supported by grants from the Fonds voor Wetenschappelijk Onderzoek (FWO, Flanders) and from the Onderzoeksfonds of the K. U. Leuven, Belgium. Jan Van Gelder and Pieter Annaert received a scholarship from the Vlaams Instituut voor de Bevordering van Wetenschappelijk-Technologisch Onderzoek in de Industrie (IWT), Belgium.

  • Abbreviations used are::
    PMPA
    tenofovir (9-[(R)-2-(phosphonomethoxy)propyl]adenine)
    LDH
    lactate dehydrogenase
    • Received May 12, 2000.
    • Accepted August 17, 2000.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 28 (12)
Drug Metabolism and Disposition
Vol. 28, Issue 12
1 Dec 2000
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Rapid CommunicationShort Communication

Increased Absorption of the Antiviral Ester Prodrug Tenofovir Disoproxil in Rat Ileum by Inhibiting Its Intestinal Metabolism

Jan Van Gelder, Sven Deferme, Pieter Annaert, Lieve Naesens, Erik De Clercq, Guy Van den Mooter, Renaat Kinget and Parick Augustijns
Drug Metabolism and Disposition December 1, 2000, 28 (12) 1394-1396;

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Rapid CommunicationShort Communication

Increased Absorption of the Antiviral Ester Prodrug Tenofovir Disoproxil in Rat Ileum by Inhibiting Its Intestinal Metabolism

Jan Van Gelder, Sven Deferme, Pieter Annaert, Lieve Naesens, Erik De Clercq, Guy Van den Mooter, Renaat Kinget and Parick Augustijns
Drug Metabolism and Disposition December 1, 2000, 28 (12) 1394-1396;
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