EP1465592A2 — Formulation and dosage form for increasing oral bioavailability of hydrophilic macromolecules

USPTO Abstract

The present invention includes a formulation and dosage form for enhancing the bioavailability of orally administered hydrophilic macromolecules. The formulation of the present invention includes a permeation enhancer, a hydrophilic macromolecule, and a carrier that exhibits in-situ gelling properties, such as nonionic surfactant. The formulation of the present invention is delivered within the GI tract as a liquid having at least some affinity for the surface of the GI mucosal membrane. Once released, it is believed that the liquid formulation spreads across one or more areas of the surface of the GI mucosal membrane, where the carrier of the formulation then transitions into a biodhesive gel in-situ. As a bioadhesive gel, the formulation of the present invention present the hydrophilic macromolecule and the permeation enhancer at the surface of the GI mucosal membrane at concentrations sufficient to increase absorption of the hydrophilic macromolecule through the GI mucosal membrane over a period of time. The dosage form of the present invention incorporates the formulation of the present invention and may be designed to provide the controlled release of the formulation within the GI tract over a desired period of time.