Solid solution compositions and use in chronic inflammation

Patent metadata

Field	Value
Publication number	US-9775820-B2
Application number	US-201615061661-A
Country	US
Kind code	B2
Filing date	Mar 4, 2016
Priority date	Oct 29, 2010
Publication date	Oct 3, 2017
Grant date	Oct 3, 2017

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 solid solution pharmaceutical composition comprising:
a) one or more propionic acid derivative non-steroidal anti-inflammatory drugs (NSAIDs) in an amount of about 20% to about 40% by weight of the pharmaceutical composition;
b) one or more pharmaceutically-acceptable hard fats comprising one or more glycerolipids in an amount of at least 30% by weight of the pharmaceutical composition;
c) one or more pharmaceutically-acceptable monoglycerides in an amount of less than 30% by weight of the pharmaceutical composition, and
d) one or more liquid glycol polymers in an amount of about 5% to about 18% by weight of the pharmaceutical composition
wherein the solid solution pharmaceutical composition is formulated to be a solid at a temperature of about 15° C. or lower.

2. The solid solution pharmaceutical composition according to claim 1 , wherein the amount of the one or more propionic acid derivative NSAIDS is about 25% to about 35% by weight of the pharmaceutical composition.

3. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more propionic acid derivative NSAID is 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.

4. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more propionic acid derivative NSAID is an Ibuprofen.

5. The solid solution pharmaceutical composition according to claim 1 , wherein the amount of the one or more pharmaceutically-acceptable hard fats is about 35% to about 45% by weight of the pharmaceutical composition.

6. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more pharmaceutically-acceptable hard fats have a melting point of about 40° C. to about 50° C.

7. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more glycerolipids comprise a triglyceride with one saturated or unsaturated fatty acid having a carbon length of C 12 -C 24 , two saturated or unsaturated fatty acids each having a carbon length of C 12 -C 24 , or three saturated or unsaturated fatty acids each having a carbon length of C 12 -C 24 .

8. The solid solution pharmaceutical composition according to claim 7 , wherein the one or more glycerolipids comprise a mixture of saturated C 10 -C 18 triglycerides having a melting point range of about 41° C. to 45° C.

9. The solid solution pharmaceutical composition according to claim 1 , wherein the amount of the one or more pharmaceutically-acceptable monoglycerides is about 8% to about 30% by weight of the pharmaceutical composition.

10. The solid solution pharmaceutical composition according to claim 1 , wherein the amount of the one or more pharmaceutically-acceptable monoglycerides is less than 25% by weight of the pharmaceutical composition.

11. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more pharmaceutically-acceptable monoglycerides is glycerol monomyristoleate, glycerol monopalmitoleate, glycerol monosapienate, glycerol monooleate, glycerol monoelaidate, glycerol monovaccenate, glycerol monolinoleate, glycerol monolinoelaidate, glycerol monolinolenate, glycerol monostearidonate, glycerol monoeicosenoate, glycerol monomeadate, glycerol monoarachidonate, glycerol monoeicosapentaenoate, glycerol monoerucate, glycerol monodocosahexaenoate, or glycerol mononervonate.

12. The solid solution pharmaceutical composition according to claim 11 , wherein the one or more pharmaceutically-acceptable monoglycerides is glycerol monolinoleate.

13. The solid solution pharmaceutical composition according to claim 1 , wherein the liquid glycol polymer in an amount of about 7% to about 15% by weight of the pharmaceutical composition.

14. The solid solution pharmaceutical composition according to claim 13 , wherein the liquid glycol polymer in an amount of about 9% to about 12% by weight of the pharmaceutical composition.

15. The solid solution pharmaceutical composition according to claim 1 , wherein the liquid glycol polymer is no more than about 1,000 g/mol.

16. The solid solution pharmaceutical composition according to claim 1 , wherein the liquid glycol polymer is a liquid polyethylene glycol (PEG) polymer and/or a liquid polypropylene glycol (PPG) polymer.

17. The solid solution pharmaceutical composition according to claim 16 , wherein the liquid PEG polymer is PEG 100, PEG 200, PEG 300, PEG 400, PEG 500, PEG 600, PEG 700, PEG 800, PEG 900, PEG 1000, or any combination thereof.

18. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more propionic acid derivative NSAID is an Ibuprofen, wherein the one or more pharmaceutically-acceptable hard fats is one or more glycerolipids comprising a mixture of saturated C 10 -C 18 triglycerides having a melting point range of about 41° C. to 45° C., wherein the one or more pharmaceutically-acceptable monoglycerides is glycerol monolinoleate, and wherein the liquid glycol polymer is a liquid PEG polymer no more than about 1,000 g/mol.

19. The solid solution pharmaceutical composition according to claim 18 , wherein the amount of the one or more propionic acid derivative NSAIDS is about 25% to about 35% by weight of the pharmaceutical composition, wherein the amount of the one or more pharmaceutically-acceptable hard fats is about 35% to about 45% by weight of the pharmaceutical composition, wherein the amount of the one or more pharmaceutically-acceptable monoglycerides is about 8% to about 30% by weight of the pharmaceutical composition, and wherein the liquid glycol polymer in an amount of about 9% to about 12% by weight of the pharmaceutical composition.

20. A solid solution pharmaceutical composition comprising:
a) one or more propionic acid derivative non-steroidal anti-inflammatory drugs (NSAIDs) in an amount of about 25% to about 35% by weight of the pharmaceutical composition;
b) one or more pharmaceutically-acceptable hard fats comprising one or more glycerolipids in an amount of about 35% to about 45% by weight of the pharmaceutical composition;
c) one or more pharmaceutically-acceptable monoglycerides in an amount of about 8% to about 30% by weight of the pharmaceutical composition, and
d) one or more liquid glycol polymers in an amount of about 9% to about 12% by weight of the pharmaceutical composition
wherein the solid solution pharmaceutical composition is formulated to be a solid at a temperature of about 15° C. or lower.

Assignees

• Infirst Healthcare Ltd

Inventors

• Bannister Robin M
• Brew John
• Reiley Iii Richard R
• Caparros Wanderley Wilson

Classifications

• A61K31/121

  acyclic · CPC title

• A61K47/22

  Heterocyclic compounds, e.g. ascorbic acid, tocopherol or pyrrolidones · CPC title

• A61K9/2013

  Organic compounds, e.g. phospholipids, fats · CPC title

• A61K31/616

  by carboxylic acids, e.g. acetylsalicylic acid · CPC title

• A61K31/25

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