# US 7,612,176 B2 · Polymer-based sustained release device

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- Number: US 7,612,176 B2
- Document ID: US7612176B2
- Status: Granted
- Kind: B2
- Application number: 11/826,535
- Filed: 2007-07-16
- Published: 2008-05-29
- Granted: 2009-11-03
- Earliest claimed: 2004-04-15
- Assignees: Alkermes, Inc.
- Inventors: Steven G. Wright; Troy Christensen; Thean Yeoh; Michael E. Rickey; Joyce M. Hotz; Rajesh Kumar; Henry R. Costantino
- Web page: https://patentgrep.com/patent/US7612176B2

## CPC

- A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence)
- A61K 9/0024: {Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue (compositions for intravenous administration, normal injectable solutions or dispersions for, e.g. subcutaneous administration A61K9/0019; brain implants A61K9/0085; (coated) prostheses, catheters or stents A61L)}
- A61K 9/1647: {Polyesters, e.g. poly(lactide-co-glycolide)}
- A61K 9/1694: {resulting in granules or microspheres of the matrix type containing more than 5% of excipient}
- A61K 38/2278: {Vasoactive intestinal peptide [VIP]; Related peptides (e.g. Exendin)}
- A61K 38/26: Glucagons
- A61K 47/26: Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/08: for glucose homeostasis (pancreatic hormones A61P5/48)
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 7/12: Antidiuretics, e.g. drugs for diabetes insipidus (ADH A61P5/10)
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K 9/1623: {Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules}
- A61K 47/38: Cellulose; Derivatives thereof
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.

## Claims

### Claim 1

A composition for sustained release of a polypeptide, consisting essentially of: a biocompatible polymer having the polypeptide dispersed therein so as to be present at about 3% (w/w) to about 5% (w/w) of the weight of the composition, and a sugar dispersed therein so as to be present at about 2% (w/w) of the weight of the composition, wherein the composition is free from additional ingredients that alter the rate of release of the polypeptide from the composition.

### Claim 2 (depends on 1)

The sustained release composition of claim 1, wherein the biocompatible polymer is selected from poly(lactides), poly(glycolides), poly(lactide-co-glycolides), poly(lactic acid)s, poly(glycolic acid)s, poly(lactic acid-co-glycolic acid)s, and blends and copolymers thereof.

### Claim 3 (depends on 2)

The sustained release composition of claim 2, wherein the biocompatible polymer is poly(lactide-co-glycolide) with a lactide:glycolide ratio of about 1:1.

### Claim 4 (depends on 1)

The sustained release composition of claim 1, wherein the polypeptide is present at about 5% (w/w) of the weight of the composition.

### Claim 5 (depends on 3)

The sustained release composition of claim 3, wherein the polypeptide is present at about 5% (w/w) of the weight of the composition.

### Claim 6 (depends on 1)

The sustained release composition of claim 1, wherein the sugar is selected from a monosaccharide, a disaccharide, a sugar alcohol, and combinations thereof.

### Claim 7 (depends on 6)

The sustained release composition of claim 6, wherein the sugar is selected from sucrose, mannitol, and a combination thereof.

### Claim 8 (depends on 7)

The sustained release composition of claim 7, wherein the sugar is sucrose.

### Claim 9 (depends on 1)

The sustained release composition of claim 1, wherein the polypeptide is present at about 5% (w/w) of the weight of the composition, and the sugar is sucrose.

### Claim 10 (depends on 1)

The sustained release composition of claim 1, wherein the polypeptide is selected from a glucoregulatory peptide and pharmaceutically acceptable salts thereof.

### Claim 11 (depends on 10)

The sustained release composition of claim 10, wherein the glucoregulatory peptide is selected from glucagon, glucagon-like peptides, exendins, agonists of glucagon-like peptides, vasoactive intestinal peptide, insulin, and growth hormone.

### Claim 12 (depends on 11)

The sustained release composition of claim 11, wherein the glucoregulatory peptide is selected from GLP-1, GLP-2, exendin-3, exendin-4, and combinations thereof.

### Claim 13 (depends on 12)

The sustained release composition of claim 12, wherein the biocompatible polymer is poly(lactide-co-glycolide) with a lactide:glycolide ratio of about 1:1.

### Claim 14 (depends on 12)

The sustained release composition of claim 12, wherein the sugar is sucrose.

### Claim 15 (depends on 12)

The sustained release composition of claim 12, wherein the glucoregulatory peptide is selected from exendin-3 and exendin-4.

### Claim 16

A method of treating a patient having Type 2 diabetes, the method comprising:
administering a therapeutically effective amount of a sustained release composition consisting essentially of a biocompatible polymer having a glucoregulatory peptide dispersed therein so as to be present at about 3% (w/w) to about 5% (w/w) of the weight of the composition, and a sugar dispersed therein so as to be present at about 2% (w/w) of the weight of the composition, wherein the composition is free from additional ingredients that alter the rate of release of the glucoregulatory peptide from the composition.

### Claim 17 (depends on 16)

The method of claim 16, wherein the biocompatible polymer is poly(lactide-co-glycolide) with a lactide:glycolide ratio of about 1:1.

### Claim 18 (depends on 16)

The method of claim 16, wherein the glucoregulatory peptide is present at about 5% (w/w) of the weight of the composition.

### Claim 19 (depends on 16)

The method of claim 16, wherein the sugar is selected from a monosaccharide, a disaccharide, a sugar alcohol, and combinations thereof.

### Claim 20 (depends on 16)

The method of claim 16, wherein the biocompatible polymer is poly(lactide-co-glycolide) with a lactide:glycolide ratio of about 1:1, wherein the glucoregulatory peptide is present at about 5% (w/w) of the weight of the composition, and the sugar is sucrose.

### Claim 21 (depends on 20)

The method of claim 20, wherein the sustained release composition is administered by injection.