DELIVERY OF RENIN INHIBITOR THROUGH MOUTH MUCOSA

The aim of this work was to investigate the efficiency of transporting the orally inactive renin inhibitor A-64662 through oral mucosa-floor of mouth, cheek, or gum-using the dog as an animal model. It has been demonstrated that A-64662, can be effectively delivered to the bloods tream through mouth mucosa with various dosage forms. Compared to bucc al adsorption, a relatively fast onset was observed after sublingual a dministration of an aqueous solution. A slightly higher bioavailabilit y but lower C-max and extended plasma drug levels were observed after sublingual administration of a slow-release gel formulation. This work has also shown that mucoadhesive patch application can provide sustai ned and controlled release of A-64662 by either buccal or gum administ ration. The absorption through the gum is slower than the cheek.