Fexofenadine の消化管吸収におけるラット oatp3 の関与 Transporter-mediated Intestinal Absorption of Fexofenadine in Rats

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著者

    • KIKUCHI Akihiro
    • Faculty of Pharmaceutical Sciences, Tokyo University of Science (RIKADAI)
    • NOZAWA Takashi
    • Faculty of Pharmaceutical Sciences, Tokyo University of Science (RIKADAI)
    • WAKASAWA Takeru
    • Faculty of Pharmaceutical Sciences, Tokyo University of Science (RIKADAI)
    • MAEDA Tomoji
    • Faculty of Pharmaceutical Sciences, Tokyo University of Science (RIKADAI)
    • TAMAI Ikumi
    • Faculty of Pharmaceutical Sciences, Tokyo University of Science (RIKADAI)

抄録

  Both influx and efflux transporters are thought to be involved in the intestinal absorption of fexofenadine. The present study examined the influx transporter-mediated intestinal absorption of fexofenadine in rats, focusing on the role of rat oatp3 (Oatp1a5). The intestinal permeability of fexofenadine was evaluated by means of the Ussing chamber method in the presence of a P-glycoprotein inhibitor to block efflux transport. The permeability of fexofenadine from the mucosal to the serosal side was higher than that from the serosal side to the mucosal side. Transport of fexofenadine was saturable, and was significantly decreased by an organic anion transporting polypeptide (oatp) inhibitor. Furthermore, uptake of fexofenadine by <i>Xenopus</i> oocytes expressing rat oatp3 was significantly greater than that by water-injected oocytes, and the affinity of oatp3 for fexofenadine (<i>K</i>m) was about 60 μM, which is comparable with the value obtained by the Ussing chamber method using rat intestinal tissues. These results indicate that oatp3 plays a role as an influx transporter in the intestinal absorption of fexofenadine in rats.<br>

収録刊行物

  • Drug metabolism and pharmacokinetics  

    Drug metabolism and pharmacokinetics 21(4), 308-314, 2006-08-31 

    The Japanese Society for the Study of Xenobiotics

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各種コード

  • NII論文ID(NAID)
    10018042931
  • NII書誌ID(NCID)
    AA1162652X
  • 本文言語コード
    ENG
  • 資料種別
    ART
  • ISSN
    13474367
  • データ提供元
    CJP書誌  CJP引用  J-STAGE 
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