A New Transmucosal Therapeutic System: Overview of Formulation Development and in Vitro/In Vivo Clinical Performance

Abstract

AbstractA new transmucosal therapeutic system (TmTs) was developed for controlled systemic delivery of drugs, which are labile to hepatic “first-pass” metabolism, through oral mucosa. It consists of a fast-release layer, which provides a rapid release of drug for prompt rise in blood drug concentration to reach the therapeutic level, and a sustained-release layer, which releases the drug continuously for sustained duration to maintain the therapeutic level for up to 12 hrs. The sustained-release layer also contains mucoadhesive composition, so TmTs can be applied on gingival mucosa for continuous transmucosal controlled administration of drugs. Using isosorbide dinitrate (ISDN), a well-known antianginal drug which is known to be subjected to extensive presystemic elimination when taken orally, the systemic bioavailability has been improved by 37 fold in beagle dogs and by almost 5 fold in humans compared to that of marketed oral sustained-release tablet and the plasma concentration profile has also been p...