English  |  正體中文  |  简体中文  |  Items with full text/Total items : 12340/13424 (92%)
Visitors : 1973766      Online Users : 147
RC Version 6.0 © Powered By DSPACE, MIT. Enhanced by NTU Library IR team.
Scope Tips:
  • please add "double quotation mark" for query phrases to get precise results
  • please goto advance search for comprehansive author search
    •  Adv. Search
    Home ‧ Login ‧ Upload ‧ Help ‧ About ‧ Administer Goto mobile version


    Please use this identifier to cite or link to this item: http://ir.nhri.org.tw/handle/3990099045/1221


    Title: Pharmacokinetics of anti-SARS-CoV agent niclosamide and its analogs in rats
    Authors: Chang, YW;Yeh, TK;Lin, KT;Chen, WC;Yao, HT;Lan, SJ;Wu, YS;Hsieh, HP;Chen, CM;Chen, CT
    Contributors: Division of Biotechnology and Pharmaceutical Research
    Abstract: Niclosamide has been demonstrated with inhibitory activity on the replication of SARS-CoV in Vero E6 cells. This study examined the pharmacokinetics and oral bioavailability of niclosamide and its two analogs, BPR1H366 and BPR1H369, in male Sprague-Dawley rats. After a single 2-mg/kg intravenous dose, the total body clearance (CL) of niclosamide, BPR1H366 and BPR1H369 was 20.0 +/- 2.9, 26.7 +/- 4.4 and 39.4 +/- 6.7 mL/kg/min, and the volume of distribution at steady state (Vss) was 0.9 +/- 0.4, 0.3 +/- 0.1 and 1.1 +/- 0.2 L/kg, respectively. The half-life (t(1/2)) of BPR1H366 and BPR1H369 was 2.6 +/- 0.3 and 3.7 +/- 1.1 hr, respectively, shorter than 6.7 +/- 2.0 hr of niclosamide. The AUC was 1413 +/- 118, 1019 +/- 203 and 750 +/- 113 ng/mL x hr for niclosamide, BPR1H366 and BPR1H369, respectively. After a single 5-mg/kg oral dose, all three compounds were rapidly absorbed. Niclosamide showed the highest C-max of 354 +/- 152 ng/mL within 30 min after oral gavage. The oral bioavailability of niclosamide, BPR1H366 and BPR1H369 was 10%, 12% and 15%, respectively. Our results demonstrated that the extents of drug exposure of the three compounds were comparable in rats. The pharmacokinetic properties of the compounds in humans are needed to be determined before their potential uses in SARS-CoV infected patients.
    Keywords: Food Science & Technology;Pharmacology & Pharmacy
    Date: 2006-12
    Relation: Journal of Food and Drug Analysis. 2006 Dec;14(4):329-333.
    Link to: http://www.fda.gov.tw/publish_periodical.aspx?publish_periodicalsn=274&keyword=&classifysn=210&belongsn=214&periodicallistsn=4
    JIF/Ranking 2023: http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcAuth=NHRI&SrcApp=NHRI_IR&KeyISSN=1021-9498&DestApp=IC2JCR
    Cited Times(WOS): https://www.webofscience.com/wos/woscc/full-record/WOS:000243186700003
    Cited Times(Scopus): http://www.scopus.com/inward/record.url?partnerID=HzOxMe3b&scp=33847011311
    Appears in Collections:[陳炯東] 期刊論文
    [葉燈光] 期刊論文
    [謝興邦] 期刊論文

    Files in This Item:

    File Description SizeFormat
    000243186700003.pdf299KbAdobe PDF475View/Open


    All items in NHRI are protected by copyright, with all rights reserved.

    Related Items in TAIR

    DSpace Software Copyright © 2002-2004  MIT &  Hewlett-Packard  /   Enhanced by   NTU Library IR team Copyright ©   - Feedback