EFFECT OF COD-LIVER OIL EXTRACT ON THE BUCCAL PERMEATION OF ERGOTAMINE TARTRATE

Ergotamine tartrate (ET) is used clinically in the treatment of migrai nes. However, the bioavailability of ET is rather poor following oral administration. Therefore, we tried to improve ET delivery using bucca l administration. The purpose of this study was td investigate the cha racteristics of the permeation of ET through the hamster cheek pouch i n vitro using a two-chamber diffusion cell, and to evaluate the effect of permeation enhancers on the transbuccal delivery of ET. Cod-liver oil extract (CLOE), polyoxyethylene hydrogenated castor oil (HCO 60), sodium glycocholate (GC), and sodium caprate (CA) were selected as per meation enhancers considering their low irritancy of the mucosa. When the enhancers were added to the donor cell at a 5% concentration each, the ET permeation rate markedly increased compared with that in a con trol not containing enhancer. Among these. enhancers, CLOE exhibited t he greatest effect. Because CLOE is composed of 16 kinds of fatty acid s, the enhancement action of each of the major components was separate ly determined As major fatty acids, palmitic acid oleic acid, eicosape ntaenoic acid (EPA), and docosahexaenoic acid (DHA) were selected and their enhancing effects were studied. The enhancing effect of each fat ty acid was significantly lower than that of CLOE.