Effect of cod-liver oil extract on the buccal permeation of ergotamine tartrate
K Tsutsumi1, Y Obata, K Takayama
1Department of Pharmaceutics, Hoshi University, Tokyo, Japan.
Abstract:
Ergotamine tartrate (ET) is used clinically in the treatment of migraines. However, the bioavailability of ET is rather poor following oral administration. Therefore, we tried to improve ET delivery using buccal administration. The purpose of this study was to investigate the characteristics of the permeation of ET through the hamster cheek pouch in 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 premeation 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 control not containing enhancer. Among these enhancers, CLOE exhibited the greatest effect. Because CLOE is composed of 16 kinds of fatty acids, the enhancement action of each of the major components was separately determined. As major fatty acids, palmitic acid, oleic acid, eicosapentaenoic acid (EPA), and docosahexaenoic acid (DHA) were selected and their enhancing effects were studied. The enhancing effect of each fatty acid was significantly lower than that of CLOE.
Related Concept Videos
Drug Delivery: Enteral Route
Drugs in...
Factors Influencing Drug Absorption: Presystemic Elimination
First Pass Effect
Depending on the route of administration, drugs can be metabolized in the liver, intestine, lungs, and vasculature. Orally administered drugs are first absorbed through the...
Routes of Drug Administration: Enteral
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
Cholinergic Antagonists: Pharmacokinetics
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

