Compositions and methods for treating chronic inflammation and inflammatory diseases

Patent metadata

Field	Value
Publication number	US-10653778-B2
Application number	US-201816206789-A
Country	US
Kind code	B2
Filing date	Nov 30, 2018
Priority date	Oct 29, 2010
Publication date	May 19, 2020
Grant date	May 19, 2020

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.

First claim

The invention claimed is:

1. A pharmaceutical composition comprising:
a) a peroxisome proliferator-activator receptor gamma (PPAR-γ) agonist;
b) a pharmaceutically-acceptable lipid in an amount of at least 50% by weight of the pharmaceutical composition, the pharmaceutically-acceptable lipid comprising a pharmaceutically-acceptable hard fat in an amount of at least 30% by weight of the pharmaceutical composition, the hard fat including a triglyceride or a triester of glycerol and a pharmaceutically-acceptable liquid fat in an amount of at least 20% by weight of the pharmaceutical composition, the liquid fat including a monoglyceride or an acetylated monoglyceride; and
c) a pharmaceutically-acceptable liquid polyethylene glycol (PEG) polymer in an amount less than about 20% 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 has a melting point temperature of about 25° C. or higher.

2. The pharmaceutical composition according to claim 1 , wherein the PPAR-γ agonist is about 10% to about 30% by weight of the pharmaceutical composition.

3. The pharmaceutical composition according to claim 2 , wherein the PPAR-γ agonist is about 20% to about 30% by weight of the pharmaceutical composition.

4. The pharmaceutical composition according to claim 3 , wherein the PPAR-γ agonist is in an amount from about 25% to about 30% by weight of the pharmaceutical composition.

5. The pharmaceutical composition according to claim 1 , wherein the PPAR-γ agonist comprises a non-steroidal anti-inflammatory drug (NSAID), a fibrate, a thiazolidinedione, or a combination thereof.

6. The pharmaceutical composition according to claim 5 , wherein the NSAID comprises a non-selective cyclooxygenase inhibitor, a selective cyclooxygenase 1 inhibitor, a selective cyclooxygenase 2 inhibitor or any combination thereof.

7. The pharmaceutical composition according to claim 5 , wherein the NSAID comprises a salicylate derivative NSAID, a p-amino phenol derivative NSAID, a propionic acid derivative NSAID, an acetic acid derivative NSAID, an enolic acid derivative NSAID, a fenamic acid derivative NSAID or a combination thereof.

8. The pharmaceutical composition according to claim 7 , wherein the propionic acid derivative NSAID comprises a pharmaceutically-acceptable form of 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.

9. The pharmaceutical composition according to claim 5 , wherein the fibrate comprises a Bezafibrate, a Ciprofibrate, a Clofibrate, a Gemfibrozil, a Fenofibrate, or a combination thereof.

10. The pharmaceutical composition according to claim 1 , wherein the pharmaceutically-acceptable lipid in an amount of at least 60% by weight of the pharmaceutical composition.

11. The pharmaceutical composition according to claim 1 , wherein the hard fat is in an amount from about 20% to about 50% by weight of the pharmaceutical composition.

12. The pharmaceutical composition according to claim 11 , wherein the hard fat is in an amount from about 30% to about 50% by weight of the pharmaceutical composition.

13. The pharmaceutical composition according to claim 12 , wherein the hard fat is in an amount from about 35% to about 45% by weight of the pharmaceutical composition.

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

15. The pharmaceutical composition according to claim 14 , wherein the hard fat comprises a mixture of saturated C10-C18 triglycerides having a melting point of between 41° C. to 45° C.

16. The pharmaceutical composition according to claim 1 , wherein the liquid fat is in an amount from about 10% to about 30% by weight of the pharmaceutical composition.

17. The pharmaceutical composition according to claim 16 , wherein the liquid fat is in an amount from about 15% to about 25% by weight of the pharmaceutical composition.

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

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

20. The pharmaceutical composition according to claim 1 , wherein the PEG polymer is in an amount from about 5% to about 15% by weight of the pharmaceutical composition.

Assignees

• Infirst Healthcare Ltd

Inventors

• Bannister Robin M
• Brew John
• Caparros-Wanderely Wilson
• Dilly Suzanne J
• Pleguezeulos Mateo Olga
• Stoloff Gregory A

Classifications

• A61K9/08

  Solutions {(composition of solutions A61K47/00)} · CPC title

• A61K31/25

  with polyoxyalkylated alcohols, e.g. esters of polyethylene glycol · CPC title

• A61K47/44

  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) · CPC title

• A61K31/337

  having four-membered rings, e.g. taxol · CPC title

• A61K47/10

  Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers · CPC title