Oral suspensions comprising a non-steroidal anti-inflammatory drug (NSAID)
The present specification discloses pharmaceutical compositions formulated as a suspension for oral administration, the suspension comprising solid particles of a non-steroidal anti-inflammatory drug (NSAID) in an oil carrier comprising one or more free fatty acids, a glycerolipid, and a phospholipid as well as 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.
1. A pharmaceutical composition formulated as a suspension for oral administration, the suspension comprising solid particles of a non-steroidal anti-inflammatory drug (NSAID) in an oil carrier, the NSAID solid particles in an amount of at least 20% by weight of the pharmaceutical composition, the oil carrier in an amount of at least 30% by weight of the pharmaceutical composition, and the oil carrier comprising at least 10% of one or more free fatty acids, each of the one or more free fatty acids having at least 8 carbon atoms and being a liquid at room temperature; (ii) at least 25% of a glycerolipid; and (iii) a phospholipid.
2. The pharmaceutical composition of claim 1 , wherein NSAID solid particles are in an amount of about 25% to about 50% by weight of the pharmaceutical composition.
3. The pharmaceutical composition of claim 1 , wherein the NSAID is an acetic acid derivative NSAID, an enolic acid derivative NSAID, a fenamic acid derivative NSAID, or a propionic acid derivative NSAID.
4. The pharmaceutical composition of claim 1 , wherein the NSAID is an aspirin, a diclofenac, an ibuprofen, a mefenamic acid, a naproxen, or a piroxicam.
5. The pharmaceutical composition of claim 1 , wherein the oil carrier is in an amount of at least 40% by weight of the pharmaceutical composition.
6. The pharmaceutical composition of claim 5 , wherein the oil carrier is in an amount of at least 45% by weight of the pharmaceutical composition.
7. The pharmaceutical composition of claim 1 , wherein the oil carrier comprises at least 25% of the one or more free fatty acids.
8. The pharmaceutical composition of claim 7 , wherein the oil carrier comprises at least 35% of the one or more free fatty acids.
9. The pharmaceutical composition of claim 8 , wherein the oil carrier comprises at least 40% of the one or more free fatty acids.
10. The pharmaceutical composition of claim 9 , wherein the oil carrier comprises at least 45% of the one or more free fatty acids.
11. The pharmaceutical composition of claim 1 , wherein the amount of the one or more free fatty acids is at least 20% by weight of the pharmaceutical composition.
12. The pharmaceutical composition of claim 1 , wherein the amount of the one or more free fatty acids is at least 25% by weight of the pharmaceutical composition.
13. The pharmaceutical composition of claim 1 , wherein the one or more free fatty acids comprises a saturated free fatty acid, an unsaturated free fatty acid, or both saturated and unsaturated free fatty acids.
14. The pharmaceutical composition of claim 1 , wherein the oil carrier comprises one free fatty acid having at least 8 carbon atoms.
15. The pharmaceutical composition of claim 14 , wherein the one free fatty acid is an oleic acid.
16. The pharmaceutical composition of claim 1 , wherein the oil carrier comprises a plurality of different free fatty acids, each of the plurality of different free fatty acids having at least 8 carbon atoms.
17. The pharmaceutical composition of claim 16 , wherein the plurality of different free fatty acids comprises a palmitic acid, a stearic acid, an oleic acid, a linoleic acid, a linolenic acid, or any combination thereof.
18. The pharmaceutical composition of claim 1 , wherein the one or more free fatty acids is a lauric acid, a tridecylic acid, a myristic acid, a myristoleic acid, a pentadecyclic acid, a palmitic acid, a palmitoleic acid, a sapienic acid, a margaric acid, a stearic acid, an oleic acid, an elaidic acid, a vaccenic acid, a linoleic acid, a linoelaidic acid, an α-Linolenic acid, a γ-Linolenic acid, a stearidonic acid, a nonadecylic acid, an arachidic acid, an eicosenoic acid, a dihomo-γ-linolenic acid, a mead acid, an arachidonic acid, an eicosapentaenoic acid, a heneicosylic acid, a behenic acid, an erucic acid, a docosahexaenoic acid, a tricosylic acid, a lignoceric acid, a nervonic acid, or any combination thereof.
19. The pharmaceutical composition of claim 1 , wherein the oil carrier comprises at least 30% the glycerolipid.
20. The pharmaceutical composition of claim 19 , wherein the oil carrier comprises at least 35% the glycerolipid.
21. The pharmaceutical composition of claim 20 , wherein the oil carrier comprises at least 40% the glycerolipid.
22. The pharmaceutical composition of claim 1 , wherein the amount of the glycerolipid is at least 20% by weight of the pharmaceutical composition.
23. The pharmaceutical composition of claim 22 , wherein the amount of the glycerolipid is at least 25% by weight of the pharmaceutical composition.
24. The pharmaceutical composition of claim 1 , wherein the glycerolipid comprises one or more triglycerides.
25. The pharmaceutical composition of claim 24 , wherein the glycerolipid comprises one or more monoglycerides, one or more diglycerides, or combinations thereof.
26. The pharmaceutical composition of claim 1 , wherein the phospholipid comprises a phosphodiacylglyceride or a phosphosphingolipid.
27. The pharmaceutical composition of claim 1 , wherein the phospholipid is a phosphatidylcholine, a phosphatidylserine, a phosphatidylethanolamine, a phosphatidylinositol, a sphingomyelin, or any combination thereof.
28. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition is formulated in the absence of a solvent.
29. A pharmaceutical composition formulated as a suspension for oral administration, the suspension comprising solid particles of a non-steroidal anti-inflammatory drug (NSAID) in an oil carrier, the NSAID solid particles being in an amount of about 25% to about 50% by weight of the pharmaceutical composition, the oil carrier being in an amount of at least 40% by weight of the pharmaceutical composition, and the oil carrier comprising (i) at least 25% of one or more free fatty acids, each of the one or more free fatty acids having at least 8 carbon atoms and being a liquid at room temperature; (ii) at least 25% of a triglyceride;
and (iii) a phospholipid.
30. A pharmaceutical composition formulated as a suspension for oral administration, the suspension comprising solid particles of a non-steroidal anti-inflammatory drug (NSAID) in an oil carrier, the NSAID solid particles being in an amount of about 25% to about 50% by weight of the pharmaceutical composition, the oil carrier being in an amount of at least 40% by weight of the pharmaceutical composition, and the oil carrier comprising (i) at least 40% of one or more free fatty acids, each of the one or more free fatty acids having at least 8 carbon atoms and being a liquid at room temperature; (ii) at least 40% of a triglyceride;
and (iii) a phospholipid.