A device for enhanced epithelial permeation of y2 receptor-binding peptides

Abstract

A pharmaceutical device comprising a composition comprising an aqueous solution of PYY(3-36), a cyclodextrin, and a compound selected from phosphatidylcholine or diglyceride, wherein the cyclodextrin and the compound selected from phosphatidylcholine or diglyceride are present in an amount sufficient to enhance epithelial permeation, and wherein the composition is present in a container; and an actuator fluidly connected to the container, wherein the actuator has a tip which defines a passage through which the solution is ejected to produce a spray of the solution.

Description

CROSS REFERENCE TO RELATED APPLICATIONS [0001] This application is a divisional claiming the benefit under 35 U.S.C. § 120 of U.S. patent application Ser. No. 10 / 780,325, filed Feb. 17, 2004, which is a continuation application and claims priority under 35 U.S.C. §120 of co-pending U.S. patent application Ser. No. 10 / 745,069 filed Dec. 23, 2003, which is a continuation-in-part of U.S. patent application Ser. No. 10 / 322,266, filed Dec. 17, 2002, and claims priority under 35 U.S.C. §119 (e) of U.S. Provisional Application No. 60 / 493,226, filed Aug. 7, 2003, U.S. Provisional Application No. 60 / 501,170, filed Sep. 8, 2003, U.S. Provisional Application No. 60 / 510,785, filed Oct. 10, 2003, U.S. Provisional Application No. 60 / 517,290, filed Nov. 4, 2003; U.S. Provisional Application No. 60 / 518,812, filed on Nov. 10, 2003; and PCT / US03 / 40538, filed on Dec. 17, 2003; the entire contents of these applications are incorporated herein by reference.BACKGROUND OF THE INVENTION [0002] The teaching...

AI Technical Summary

Benefits of technology

"The present invention provides novel methods and compositions for delivering Y2 receptor-binding peptides to the mucosal, especially nasal, tissue to treat obesity, induce satiety, promote weight-loss, and prevent or cure diabetes. The Y2 receptor-binding peptides are administered in the form of nasal sprays or other mucosal delivery methods that can increase the concentration of the peptides in the blood plasma of a mammal by at least 5 pmol when a dose of the peptide is administered intranasally. The formulation is preferably free of proteins or polypeptides that stabilize the formulation. The Y2 receptor-binding peptides can be administered in amounts ranging from 150 μg to 2000 μg per mammal. The formulation can also contain a solubilizing agent, such as a cyclodextrin, to facilitate the delivery of the peptides across the mucosal membrane."

Problems solved by technology

Obesity and its associated disorders are common and very serious public health problems in the United States and throughout the world.

It reduces life-span and carries a serious risk of co-morbidities above, as well disorders such as infections, varicose veins, acanthosis nigricans, eczema, exercise intolerance, insulin resistance, hypertension hypercholesterolemia, cholelithiasis, orthopedic injury, and thromboembolic disease.

However, for the treatment of obesity and related diseases, including diabetes, the mode of administration has been limited to intravenous IV infusion with no effective formulations optimized for alternative administration of PYY3-36.

However, the physical forces associated with droplet formation often destroys or denatures proteins and peptides.

Images