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Synthesis and transdermal permeation-enhancing activity of ketone, amide, and alkane analogs of Transkarbam 12
Holas T., Vávrová K., Klimentová J., Hrabálek A.
Jazyk angličtina Země Velká Británie
- MeSH
- adjuvancia farmaceutická farmakologie chemická syntéza chemie MeSH
- alkany chemie MeSH
- amidy chemie MeSH
- financování organizované MeSH
- karbamáty farmakologie chemická syntéza chemie MeSH
- ketony chemie MeSH
- kožní absorpce účinky léků MeSH
- molekulární modely MeSH
- prasata MeSH
- theofylin farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- zvířata MeSH
Transkarbam 12 (5-(dodecyloxycarbonyl)pentylammonium-5-(dodecyloxycarbonyl)pentylcarbamate, T12) is a highly active transdermal permeation enhancer. In this study, ketone, amide, and alkane analogs of T12 have been synthesized and evaluated for their permeation-enhancing activity using porcine skin and theophylline as a model drug. Replacement of ester by methylene and ketone, respectively, led to a significant decrease of activity. Amide analogs displayed lower activity in 60% propylene glycol and were comparable to T12 in isopropyl myristate. An intramolecular H-bond between ester and ammonium-carbamate group was suggested to be important for the permeation-enhancing activity of T12.
Citace poskytuje Crossref.org
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