Formulation and dosage form for increasing oral bioavailability of hydrophilic macromolecules
First Claim
1. A formulation for increasing the bioavailability of an orally administered hydrophilic macromolecule, the formulation comprising a hydrophilic macromolecule, a permeation enhancer, and a carrier capable of forming a bioadhesive gel, the formulation being formulated such that the formulation is released within the gastrointestinal tract as a liquid and forms a bioadhesive gel in-situ after the formulation has had some opportunity to spread across the surface of the gastrointestinal mucosal membrane.
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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 a 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 bioadhesive gel in-situ. As a bioadhesive gel, the formulation of the present invention 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. 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.
86 Citations
20 Claims
- 1. A formulation for increasing the bioavailability of an orally administered hydrophilic macromolecule, the formulation comprising a hydrophilic macromolecule, a permeation enhancer, and a carrier capable of forming a bioadhesive gel, the formulation being formulated such that the formulation is released within the gastrointestinal tract as a liquid and forms a bioadhesive gel in-situ after the formulation has had some opportunity to spread across the surface of the gastrointestinal mucosal membrane.
- 14. A formulation for enhancing the bioavailability of an orally administered hydrophilic macromolecule, the formulation comprising a hydrophilic macromolecule, a permeation enhancer, and a carrier capable of forming a bioadhesive gel, wherein the hydrophilic macromolecule comprises between about 0.01 wt % and about 50 wt % of the formulation, the permeation enhancer comprises between about 11% and about 30% of the formulation, and the carrier comprising between about 35% and 88% of the formulation.
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16. A dosage form comprising:
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a formulation comprising a hydrophilic macromolecule, a permeation enhancer, and a carrier capable of forming a bioadhesive gel, the formulation being formulated such that the formulation is released within the gastrointestinal tract as a liquid and forms a bioadhesive gel in-situ after the formulation has had some opportunity to spread across a surface of a gastrointestinal mucosal membrane; and
a delivery device configured to release the formulation within the gastrointestinal tract of a subject at a controlled rate over a period of time. - View Dependent Claims (17, 18, 19)
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20. A controlled release dosage form comprising:
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a liquid formulation comprising a hydrophilic macromolecule, the formulation being capable of enhancing the oral bioavailability of the hydrophilic macromolecule; and
a deliver device configured to deliver the formulation over a desired period of time.
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Specification