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Transdermal absorption of dimethindene in man
1Institute of Pharmaceutical Chemistry, University of Münster, Germany.
Archiv Der Pharmazie
|February 1, 1995
Summary
Dermal administration of dimethindene leads to minimal excretion of the drug and its metabolite N-demethyldimethindene in urine. This suggests some skin absorption occurs after topical application.
Area of Science:
- Pharmacology
- Toxicology
- Analytical Chemistry
Background:
- Dimethindene is an antihistamine used for allergic conditions.
- Understanding drug absorption through the skin is crucial for safety and efficacy.
- Previous studies have investigated oral administration routes.
Purpose of the Study:
- To quantify dimethindene and its metabolite N-demethyldimethindene in human urine following dermal administration.
- To assess the extent of skin absorption of dimethindene.
Main Methods:
- High-Performance Liquid Chromatography (HPLC) was employed for drug determination.
- Urine samples were collected from 8 healthy volunteers over 32 hours.
- Dermal administration of a dimethindene formulation was performed.
Main Results:
- An average of 0.023% of the dimethindene dose was excreted in urine.
- An average of 0.022% of the N-demethyldimethindene metabolite was excreted.
- Excretion levels were comparable to those observed after oral administration.
Conclusions:
- Dermal administration of dimethindene results in measurable, albeit low, systemic absorption.
- The findings indicate that dimethindene can penetrate the skin barrier.
- Further research may explore optimizing dermal formulations for enhanced delivery or reduced systemic exposure.