# US 10,869,955 B2 · Joint fat pad formulations, and methods of use thereof

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- Number: US 10,869,955 B2
- Document ID: US10869955B2
- Status: Granted
- Kind: B2
- Application number: 15/540,103
- Filed: 2016-01-28
- Published: 2017-12-28
- Granted: 2020-12-22
- Earliest claimed: 2015-01-28
- Assignees: Allergan, Inc.
- Applicants: Allergan, Inc.
- Inventors: Guang-Liang Jiang; Catherine C. Turkel; Michael E. Stern; Christopher S. Schaumberg; Wendy M. Blanda
- Web page: https://patentgrep.com/patent/US10869955B2

## CPC

- A61L 31/042: {Polysaccharides}
- A61K 31/573: substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
- A61L 31/145: {Hydrogels or hydrocolloids}
- A61L 31/16: Biologically active materials, e.g. therapeutic substances {(A61L31/047 takes precedence)}
- A61P 19/02: for joint disorders, e.g. arthritis, arthrosis
- A61P 23/00: Anaesthetics
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/02: Immunomodulators
- A61P 37/06: Immunosuppressants, e.g. drugs for graft rejection
- A61L 2300/402: Anaestetics, analgesics, e.g. lidocaine
- A61L 2300/41: Anti-inflammatory agents, e.g. NSAIDs
- A61L 2300/426: Immunomodulating agents, i.e. cytokines, interleukins, interferons
- A61L 2300/43: Hormones, e.g. dexamethasone
- A61L 2300/622: Microcapsules
- A61L 2300/624: Nanocapsules
- A61L 2400/06: Flowable or injectable implant compositions
- A61L 2430/24: for joint reconstruction
- A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K)
- 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

The present invention relates to formulations for administration to a joint fat pad of a subject, and to methods of treating joint pain, inflammation or disease. The disclosed formulations are intended for local administration to the joint fat pad to provide sustained release of a therapeutic agent to the joint cavity and surrounding tissues. The joint may be an arthritic joint, an injured joint or a surgically replaced joint. The therapeutic agent may be an analgesic agent, an anti-inflammatory agent or an immunosuppressive agent. A single administration of the formulation to the joint fat pad delivers a therapeutically effective amount of the therapeutic agent with reduced systemic exposure relative to a single systemic or a single intra-articular administration of a therapeutic dose of an identical therapeutic agent.

## Claims

### Claim 1

A method of treating pain, inflammation, or a combination thereof, in a joint of a subject in need of such treatment, the method comprising administering a gel suspension formulation into a fat pad of the joint, thereby relieving the joint from the pain, inflammation, or combination thereof;
wherein the formulation comprises:
a non-crosslinked hyaluronic acid present at a concentration ranging from 2% to 10% (wt/wt) of the formulation; and
dexamethasone, or a salt thereof, which is suspended in the formulation and present at a concentration ranging from 0.1% to 50% (wt/wt) of the formulation;
wherein the formulation provides sustained release of the dexamethasone, or the salt thereof, to the joint;
wherein the method provides consisting of reduced systemic exposure relative to a systemic or an intra-articular administration of a therapeutic dose of dexamethasone; and
wherein a single administration of the formulation to the joint fat pad provides equivalent or superior relief of the pain or inflammation of the joint relative to a single systemic or intra-articular administration of a therapeutic dose of dexamethasone; and
wherein the administering comprises injecting, embedding or implanting the formulation into the joint fat pad.

### Claim 2 (depends on 1)

The method of claim 1 wherein the dexamethasone, or the salt thereof, is present at a concentration ranging from 0.5% to 30% (wt/wt) of the formulation.

### Claim 3 (depends on 1)

The method of claim 1, wherein the hyaluronic acid is sodium hyaluronan.

### Claim 4 (depends on 1)

The method of claim 1 wherein the hyaluronic acid is present at a concentration ranging from 2% to 5% (wt/wt) of the formulation.

### Claim 5 (depends on 1)

The method of claim 1, wherein the formulation further comprises an anesthetic agent.

### Claim 6 (depends on 5)

The method of claim 5, wherein the anesthetic agent is lidocaine.

### Claim 7 (depends on 1)

The method of claim 1, wherein the joint is an arthritic joint, an injured joint or a surgically replaced joint.

### Claim 8 (depends on 1)

The method of claim 1, wherein the joint is a synovial joint.

### Claim 9 (depends on 1)

The method of claim 1, wherein the joint is a knee joint, and the fat pad is an infrapatellar fat pad.

### Claim 10 (depends on 1)

The method of claim 1, wherein the pain, inflammation or the combination thereof is associated with osteoarthritis, rheumatoid arthritis, juvenile arthritis, calcium pyrophosphate dehydrate crystal deposition disease (pseudo gout), post-operative pain, joint replacement surgery pain or a combination thereof.

### Claim 11 (depends on 1)

The method of claim 1, comprising a single injection of the gel formulation into the joint fat pad.

### Claim 12 (depends on 2)

The method of claim 2, wherein the dexamethasone, or the salt thereof, is present at a concentration ranging from 1% to 25% (wt/wt) of the formulation.

### Claim 13 (depends on 2)

The method of claim 2, wherein the dexamethasone, or the salt thereof, is present at a concentration ranging from 2% to 20% (wt/wt) of the formulation.

### Claim 14 (depends on 1)

The method of claim 1, wherein the hyaluronic acid is present at a concentration of 2% (wt/wt) of the formulation, and the dexamethasone, or the salt thereof, is present at a concentration of 10% (wt/wt) of the formulation.

### Claim 15 (depends on 1)

The method of claim 1, wherein: the formulation is a gel suspension; the dexamethasone, or the salt thereof, is present at a concentration ranging from 1% to 25% (wt/wt) of the formulation; the hyaluronic acid is present at a concentration ranging from 2% to 5% (wt/wt) of the formulation; and the formulation delivers pharmacodynamic concentrations of the dexamethasone to the joint for up to about 6 months after the administration.

### Claim 16 (depends on 1)

The method of claim 1, wherein the hyaluronic acid is present at a concentration of 2% (wt/wt) of the formulation, and the dexamethasone, or the salt thereof, is present at a concentration of 20% (wt/wt) of the formulation.