Emisphere Technologies, Inc.

Evgueni N Barantsevitch

Sam J Milstein

Andrea Leone-Bay

Donald J Sarubbi

Noemi B Santiago

Nai Fang Wang

Duncan R Paton

Martin L Kantor

Susan Haas

Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Compounds and compositions for delivering active agents

The present invention relates to an oral drug delivery system, and in particular to modified amino acids and modified amino acid derivatives for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids and derivatives can form non-covalent mixtures with active biological agents and in an alternate embodiment can releasably carry active agents. Modified amino acids can also form drug containing microspheres. These mixtures are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids are also disclosed.

Oral drug delivery compositions and methods

Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: Additionally, mimetics and methods for preparing mimetics are contemplated.

Active agent transport systems

The present invention relates to compositions and methods for orally delivering antigens. The antigen and an adjuvant are combined with an acylated amino acid or polyamino acid and, a sulfonated amino acids or polyamino acid, or a salt of the foregoing.

Compositions for the delivery of antigens

This invention provides an encapsulated fragrance in which the fragrance is controlled can be released by exposing the encapsulated fragrance to a solution of a predetermined pH. The invention also contemplates a process for preparing encapsulated fragrances.

Microencapsulated fragrances and method for preparation

The present invention relates to an oral drug delivery system, and in particular to modified amino acids and modified amino acid derivatives for use as a delivery system of sensitive agents such as bioactive peptides. The modified amino acids and derivatives can form non-covalent mixtures with active biological agents and in an alternate embodiment can releasably carry active agents. Modified amino acids can also form durg containing microspheres. These mixtures are suitable for oral administration of biologically active agents to animals. Methods for the preparation of such amino acids are also disclosed.

Orally deliverable supramolecular complex

Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of:

Methods for transporting a biologically active agent across a cellular membrane or a lipid bilayer. A first method includes the steps of: (a) providing a biologically active agent which can exist in a native conformational state, a denatured conformational state, and an intermediate conformational state which is reversible to the native state and which is conformationally between the native and denatured states; (b) exposing the biologically active agent to a complexing perturbant to reversibly transform the biologically active agent to the intermediate state and to form a transportable supramolecular complex; and (c) exposing the membrane or bilayer to the supramolecular complex, to transport the biologically active agent across the membrane or bilayer. The perturbant has a molecular weight between about 150 and about 600 daltons, and contains at least one hydrophilic moiety and at least one hydrophobic moiety. The supramolecular complex comprises the perturbant non-covalently bound or complexed with the biologically active agent. In the present invention, the biologically active agent does not form a microsphere after interacting with the perturbant. A method for preparing an orally administrable biologically active agent comprising steps (a) and (b) above is also provided as are oral delivery compositions. Additionally, mimetics and methods for preparing mimetics are contemplated.

Oral delivery composition comprising supramolecular complex

Modified hydrolyzed vegetable protein microspheres and methods for their preparation and use as oral delivery systems for pharmaceutical agents are described.

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New Rochelle, NY, United States of America

Evgueni N Barantsevitch