Esters of 6-dimethylaminohexanoic acid as skin penetration enhancers
Language English Country Germany Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
11082838
Knihovny.cz E-resources
- MeSH
- Aminocaproates * MeSH
- Skin Absorption drug effects MeSH
- Aminocaproic Acid chemistry pharmacology MeSH
- Humans MeSH
- Magnetic Resonance Spectroscopy MeSH
- Excipients chemistry MeSH
- Spectrophotometry, Infrared MeSH
- In Vitro Techniques MeSH
- Theophylline pharmacokinetics MeSH
- Vasodilator Agents pharmacokinetics MeSH
- Chromatography, High Pressure Liquid MeSH
- Structure-Activity Relationship MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Aminocaproates * MeSH
- Aminocaproic Acid MeSH
- Excipients MeSH
- Theophylline MeSH
- Vasodilator Agents MeSH
We prepared a series of five esters of 6-dimethylaminohexanoic acid, and characterised the compounds by their NMR and IR spectra. Their ability to function as transdermal penetration enhancers was subsequently evaluated using excised human skin as a membrane, modified Franz diffusion cells, and theophylline as a model permeant. The penetration-enhancing efficiency of esters 1-5 was studied in the donor media of propylene glycol and isopropyl myristate, and expressed as the corresponding enhancement factors (EF). All the esters increased the penetration of theophylline through the skin. The enhancement factor for the most active substance, undecyl 6-dimethylaminohexanoate, was 118.5 (+/- 19) from propylene glycol.
Coupling reactions of alpha-bromocarboxylate with non-aromatic N-heterocycles
