Formulation and dosage form for increasing oral bioavailability of hydrophilic macromolecules

摘要

A formulation and dosage form for enhancing the bioavailability of orally administered hydrophilic macromolecules includes a permeation enhancer, a hydrophilic macromolecule, and a carrier such as a nonionic surfactant that exhibits in-situ gelling properties. The formulation 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 bioadhesive gel in-situ. As a bioadhesive gel, the formulation presents 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. A dosage form incorporates the formulation and may be designed to provide the controlled release of the formulation within the GI tract over a desired period of time.