Solid solution compositions and use in chronic inflammation

Patent metadata

Field	Value
Publication number	US-9308213-B2
Application number	US-201414155108-A
Country	US
Kind code	B2
Filing date	Jan 14, 2014
Priority date	Oct 29, 2010
Publication date	Apr 12, 2016
Grant date	Apr 12, 2016

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 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 in an amount of at least 30% by weight of the pharmaceutical composition;
c) one or more pharmaceutically-acceptable monoglycerides or acetylated monoglycerides that is liquid at room temperature in an amount of less than 30% 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 therapeutic compounds is about 25% to about 35% by weight of the pharmaceutical composition.

3. 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.

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

5. The solid solution pharmaceutical composition according to claim 1 , wherein the amount of the one or more pharmaceutically-acceptable monoglycerides or an acetylated monoglycerides is less than 25% 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 6 , wherein the one or more pharmaceutically-acceptable hard fats comprise one or more glycerolipids.

8. The solid solution pharmaceutical composition according to claim 7 , 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 .

9. The solid solution pharmaceutical composition according to claim 8 , 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.

10. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more pharmaceutically-acceptable monoglycerides or an acetylated monoglycerides comprise 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.

11. The solid solution pharmaceutical composition according to claim 10 , wherein the one or more pharmaceutically-acceptable monoglycerides monoglycerides or an acetylated monoglycerides comprise glycerol monolinoleate.

12. The solid solution pharmaceutical composition according to claim 1 , wherein the solid solution pharmaceutical composition further comprises one or more stabilizing agents and/or one or more neutralizing agents.

13. The solid solution pharmaceutical composition according to claim 12 , wherein the one or more stabilizing agents comprises about 1% to about 5% by weight of the pharmaceutical composition.

14. The solid solution pharmaceutical composition according to claim 13 , wherein the one or more stabilizing agents comprises a liquid glycol polymer, a monohydric alcohol, isosorbide dimethyl ether, and diethylene glycol monoethyl ether (2-(2-ethoxyethoxy)ethanol).

15. The solid solution pharmaceutical composition according to claim 14 , wherein the liquid glycol polymer is a liquid polyethylene glycol (PEG) polymer and/or a liquid polypropylene glycol (PPG) polymer.

16. The solid solution pharmaceutical composition according to claim 14 , wherein the liquid glycol polymer in an amount of about 5% to about 15% by weight of the pharmaceutical composition.

17. The solid solution pharmaceutical composition according to claim 12 , wherein the one or more neutralizing agents comprises about 5% to 55% by weight of the pharmaceutical composition.

18. The solid solution pharmaceutical composition according to claim 17 , wherein the one or more neutralizing agents comprises one or more fatty acids, sodium acetate, or triethanolamine.

19. The solid solution pharmaceutical composition according to claim 18 , wherein the one or more fatty acids comprises a C 16 -C 18 fatty acid.

20. The solid solution pharmaceutical composition according to claim 16 , wherein the liquid glycol polymer in an amount of about 9% to about 12% by weight of the pharmaceutical composition.

21. The solid solution pharmaceutical composition according to claim 1 , wherein the one or more NSAIDs comprises a non-selective cyclo-oxygenase inhibitor, a selective cyclooxygenase 1 inhibitor, a selective cyclooxygenase 2 inhibitor or any combination thereof.

22. The solid solution pharmaceutical composition according to claim 1 or claim 2 , wherein the one or more NSAIDs comprises a pharmaceutically-acceptable form of a salicylate derivative NSAID, a pharmaceutically-acceptable form of a p-amino phenol derivative NSAID, a pharmaceutically-acceptable form of a propionic acid derivative NSAID, a pharmaceutically-acceptable form of an acetic acid derivative NSAID, a pharmaceutically-acceptable form of an enolic acid derivative NSAID, a pharmaceutically-acceptable form of a fenamic acid derivative NSAID, an ester of the NSAID, or any combination thereof.

23. The solid solution pharmaceutical composition according to claim 3 , wherein the propionic acid derivative NSAID comprises a pharmaceutically-acceptable form of an Alminoprofen, a pharmaceutically-acceptable form of a Benoxaprofen, a pharmaceutically-acceptable form of a Dexketoprofen, a pharmaceutically-acceptable form of a Fenoprofen, a pharmaceutically-acceptable form of a Flurbiprofen, a pharmaceutically-acceptable form of an Ibuprofen, a pharmaceutically-acceptable form of an Indoprofen, a pharmaceutically-acceptable form of a Ketoprofen, a pharmaceutically-acceptable form of a Loxoprofen, a pharmaceutically-acceptable form of a Naproxen, a pharmaceutically-acceptable form of an Oxaprozin, a pharmaceutically-acceptable form of a Pranoprofen, or a pharmaceutically-acceptable form of a Suprofen.

24. The solid solution pharmaceutical composition according to claim 23 , wherein the propionic acid derivative NSAID is a pharmaceutically-acceptable form of an Ibuprofen.

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

26. The solid solution pharmaceutical composition according to claim 25 , wherein the PEG polymer comprises PEG 100, PEG 200, PEG 300, PEG 400, PEG 500, PEG 600, PEG 700, PEG 800, PEG 900, PEG 1000, or any combination thereof.

Assignees

• Infirst Healthcare Ltd

Inventors

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

Classifications

• A61K31/60

  Salicylic acid; Derivatives thereof · CPC title

• A61K31/25

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

• A61K47/14

  Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters · CPC title

• A61K9/2013

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

• A61K9/08

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