| Autor: |
de Zeeuw RA; Groningen Centre for Drug Research, Bioanalysis and Toxicology Group, University of Groningen, The Netherlands., Herder RE, Wiechers JW, Drenth BF |
| Jazyk: |
angličtina |
| Zdroj: |
Pharmaceutical research [Pharm Res] 1990 Jun; Vol. 7 (6), pp. 638-43. |
| DOI: |
10.1023/a:1015878430173 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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