TRANSDERMAL IONTOPHORESIS OF TACRINE IN VIVO Ⅰ -CLINICAL RELEVANCE

摘要

Oral administration of tacrine involves problems like low bioavailability, short elimination half-life, dose-dependent hepatotoxicity, and peripheral cholinenergic side effects. Thus, by transdermal delivery we attempted to avoid the adverse effects of oral tacrine delivery. Methods to control tacrine delivery were iontophoresis and the use of ion-exchange fiber. In this study we demonstrated in human volunteers, that 1) clinically relevant plasma concentrations of tacrine could be achieved by transdermal iontophoresis in vivo and 2) the variability of iontophoretic tacrine permeation was not significantly improved by the ion-exchange approach.