# US 9,750,810 B2 · Compositions and methods for treating chronic inflammation and inflammatory diseases

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- Number: US 9,750,810 B2
- Document ID: US9750810B2
- Status: Granted
- Kind: B2
- Application number: 15/043,327
- Filed: 2016-02-12
- Published: 2016-06-09
- Granted: 2017-09-05
- Earliest claimed: 2010-10-29
- Assignees: Infirst Healthcare Limited
- Applicants: Infirst Healthcare Limited
- Inventors: Robin M. Bannister; John Brew; Wilson Caparros-Wanderely; Suzanne J. Dilly; Olga Pleguezeulos Mateo; Gregory A. Stoloff
- Web page: https://patentgrep.com/patent/US9750810B2

## CPC

- A61K 47/14: Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A61K 9/08: Solutions {(composition of solutions A61K47/00)}
- A61K 9/2013: {Organic compounds, e.g. phospholipids, fats}
- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/60: Salicylic acid; Derivatives thereof
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- A61K 47/44: Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin (synthetic glycerides, e.g. medium-chain triglycerides, A61K47/14)
- A61K 31/19: Carboxylic acids, e.g. valproic acid (salicylic acid A61K31/60)
- A61K 31/202: having three or more double bonds, e.g. linolenic (eicosanoids, e.g. leukotrienes A61K31/557)
- A61K 31/25: with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol
- A61K 31/337: having four-membered rings, e.g. taxol
- A61K 31/704: attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin {(digitoxin A61K31/7048)}
- 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)

## Abstract

The present specification discloses pharmaceutical compositions, methods of preparing such pharmaceutical compositions, and methods and uses of treating a chronic inflammation and/or an inflammatory disease in an individual using such pharmaceutical compositions.

## Claims

### Claim 1

A pharmaceutical composition comprising:
a) about 10% to 30% of a propionic acid derivative NSAID by weight of the pharmaceutical composition;
b) about 5% to about 15% of a polyethylene glycol (PEG) polymer by weight of the pharmaceutical composition;
c) about 20% to about 50% of a hard fat comprising a triglyceride or a triester of glycerol by weight of the pharmaceutical composition; and
d) about 10% to about 30% of a liquid fat comprising a mono-glyceride by weight of the pharmaceutical composition,
wherein the pharmaceutical composition is formulated to be a solid at a temperature of about 15° C. or lower and have a melting point temperature in the range of about 25° C. or higher.

### Claim 2 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the propionic acid derivative NSAID is about 20% to about 30% by weight of the pharmaceutical composition.

### Claim 3 (depends on 2)

The pharmaceutical composition according to claim 2, wherein the propionic acid derivative NSAID is in an amount from about 25% to about 30% by weight of the pharmaceutical composition.

### Claim 4 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the propionic acid derivative NSAID comprises an Alminoprofen, a Benoxaprofen, a Dexketoprofen, a Fenoprofen, a Flurbiprofen, an Ibuprofen, an Indoprofen, a Ketoprofen, a Loxoprofen, a Naproxen, an Oxaprozin, a Pranoprofen, or a Suprofen.

### Claim 5 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the propionic acid derivative NSAID is a pharmaceutically-acceptable form of an Ibuprofen.

### Claim 6 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the hard fat or the triester of glycerol is in an amount from about 30% to about 50% by weight of the pharmaceutical composition.

### Claim 7 (depends on 6)

The pharmaceutical composition according to claim 6, wherein the hard fat or the triester of glycerol is in an amount from about 35% to about 45% by weight of the pharmaceutical composition.

### Claim 8 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the hard fat or the triester of glycerol has a melting point of about 40° C. to about 46° C.

### Claim 9 (depends on 8)

The pharmaceutical composition according to claim 8, wherein the hard fat comprises a mixture of saturated C10-C18 triglycerides having a melting point of between 41° C. to 45° C.

### Claim 10 (depends on 9)

The pharmaceutical composition according to claim 9, wherein the hard fat comprises a mixture of saturated C10-C18 triglycerides having a melting point of about 43° C.

### Claim 11 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the liquid fat is in an amount from about 15% to about 25% by weight of the pharmaceutical composition.

### Claim 12 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the liquid fat further comprises a diglyceride, a triglyceride, or any combination thereof.

### Claim 13 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the monoglyceride is glyceryl monolinoleate.

### Claim 14 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the PEG polymer is in an amount from about 8% to about 15% by weight of the pharmaceutical composition.

### Claim 15 (depends on 14)

The pharmaceutical composition according to claim 14, wherein the PEG polymer is in an amount from about 7% to about 13% by weight of the pharmaceutical composition.

### Claim 16 (depends on 15)

The pharmaceutical composition according to claim 15, wherein the pharmaceutically-acceptable PEG polymer is in an amount from about 8% to about 12% by weight of the pharmaceutical composition.

### Claim 17 (depends on 16)

The pharmaceutical composition according to claim 16 wherein the PEG polymer is in an amount from about 9% to about 11% by weight of the pharmaceutical composition.

### Claim 18 (depends on 1)

The pharmaceutical composition according to claim 1, wherein the PEG polymer is a liquid PEG polymer.

### Claim 19 (depends on 18)

The pharmaceutical composition according to claim 18, wherein the pharmaceutically-acceptable PEG polymer is less than about 2,000 g/mol.

### Claim 20 (depends on 19)

The pharmaceutical composition according to claim 19, wherein the liquid PEG polymer is a PEG 100, a PEG 200, a PEG 300, a PEG 400, a PEG 500, a PEG 600, a PEG 700, a PEG 800, a PEG 900, a PEG 1000, or a combination thereof.
