Transdermal administration of emedastine.

Transdermal administration of emedastine was tested in vitro and in vivo. In the diffusion cell method in vitro, emedastine free base was more permeable by transdermal administration than emedastine difumarate. Emedastine had higher permeability in hydrophobic vehicles than in hydrophilic vehicles, and was most permeable in fatty acid monoesters. It was suggested that the change in permeability of emedastine from these vehicles was dependent on the change in its partition from the vehicle to the skin. In studies using rabbits in vivo, emedastine had high permeability from fatty acid monoesters and fatty acid diesters as found in in vitro studies, and bioavailability of the drug after transdermal administration was greater than that after peroral administration. The flux of emedastine in vitro was correlative with the pharmacokinetic parameters in vivo. Consequently, it is clear that transdermal permeability of emedastine is very high and that the drug may be efficacious in the system after administration by these means.