Metabolic Conversion of Cyoctol During Skin Passage in Humans

Rokus A. De Zeeuw*, Renella E. Herder, Johann W. Wiechers, Ben F. H. Drenth

*Corresponding author for this work

    Research output: Contribution to journalArticleAcademicpeer-review

    4 Citations (Scopus)

    Abstract

    Upon application of 14C-labeled cyoctol to the forearm of healthy volunteers, no parent cyoctol was detectable in ipsilateral blood plasma. The 14C activity was largely accounted for by a component with higher lipophilicity than the parent compound, as justified from their HPLC retention. Thus, this study suggests that human skin is capable of nearly complete cutaneous first-pass metabolism, resulting in negligible systemic availability of cyoctol. In a comparable experiment, rabbits were also able to convert cyoctol during skin absorption to a more lipophilic metabolite, which was identified as the palmitoleic acid ester of O-demethylated cyoctol by GC/MS. However, chromatographic evidence indicates that the human ipsilateral metabolite differs from the rabbit cyoctol metabolite.
    Original languageEnglish
    Pages (from-to)638-643
    Number of pages6
    JournalPharmaceutical Research
    Volume7
    Issue number6
    DOIs
    Publication statusPublished - Jun-1990

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