초록 ▼

A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gas

A novel pharmaceutical composition is provided by which nonsteroidal anti-inflammatory drugs (NSAIDs) are added directly to phospholipid-containing oil such as lecithin oils or to a bio-compatible oil to which an phospholipid has been added to make a NSAID-containing formulation that possess low gastrointestinal (GI) toxicity and enhanced therapeutic activity to treat or prevent inflammation, pain, fever, platelet aggregation, tissue ulcerations and/or other tissue disorders. The composition of the invention are in the form of a non-aqueous solution, paste, suspension, dispersion, colloidal suspension or in the form of an aqueous emulsion or microemulsion for internal, oral, direct or topical administration.

대표청구항 ▼

1. A method for producing a pharmaceutical composition comprising admixing an NSAID in powder form into an oil-based carrier to obtain an NSAID-in-oil suspension, wherein: (a) the oil-based carrier comprises a phospholipid and a bio-compatible oil;(b) the NSAID is present in a therapeutically effect

1. A method for producing a pharmaceutical composition comprising admixing an NSAID in powder form into an oil-based carrier to obtain an NSAID-in-oil suspension, wherein: (a) the oil-based carrier comprises a phospholipid and a bio-compatible oil;(b) the NSAID is present in a therapeutically effective amount; and(c) the NSAID-in-oil suspension has a gastrointestinal toxicity that is reduced relative to the NSAID alone. 2. The method of claim 1, wherein the oil based carrier comprises from about 20 wt. % to about 80 wt. % phospholipids. 3. The method of claim 1, wherein the NSAID is selected from the group consisting of propionic acid drugs, acetic acid drugs, ketone drugs, fenamate drugs, oxicam drugs, salicylic acid drugs, pyrazolin acid drugs, acetaminophen, and COX-2 inhibitors. 4. The method of claim 1, wherein the NSAID is selected from the group consisting of aspirin, fenoprofen, flurbiprofen, suprofen, benoxaprofen, ibuprofen, ketoprofen, naproxen, oxaprozin, diclofenac, etodolac, indomethacin, ketorolac tromethamine, ketorolac, nabumetone, sulindac, tolmetin, meclofenamate, mefenamic acid, piroxicam, diflunisal, oxyphenbutazone, phenylbutazone, acetaminophen, celecoxib, rofecoxib, and mixtures or combinations thereof. 5. The method of claim 1, wherein the bio-compatible oil is selected from the group consisting of vegetable oils, hydrogenated vegetable oils, and mixtures or combinations thereof. 6. The method of claim 5, wherein the oils are selected from the group consisting of peanut oil, canola oil, avocado oil, safflower oil, olive oil, corn oil, soy bean oil, sesame oil, vitamin A, vitamin D, vitamin E, and mixtures or combinations thereof. 7. The method of claim 1, wherein the weight ratio of NSAID to oil-based carrier present in the NSAID-in-oil suspension is from about 4:1 to about 1:4. 8. The method of claim 7, wherein the weight ratio of NSAID to oil-based carrier is about 1:1. 9. The method of claim 1, wherein the oil-based carrier comprises between about 20 wt. % and about 60 wt. % phospholipids. 10. The method of claim 1, wherein the oil-based carrier comprises between about 20 wt. % and about 40 wt. % phosphatidylcholine. 11. The method of claim 1, wherein the NSAID associates with the phospholipid. 12. A pharmaceutical composition that is a non-steroidal anti-inflammatory drug (NSAID)-in-oil suspension comprising an NSAID in powder form and a lecithin oil, wherein: (a) the NSAID-in-oil suspension comprises from about 20 wt. % to about 80 wt. % phospholipids;(b) the NSAID is present in a therapeutically effective amount; and(c) the composition has a gastrointestinal (GI) toxicity that is reduced relative to the NSAID alone. 13. The composition according to claim 12, wherein the NSAID-in-oil suspension comprises from about 20 wt. % to about 80 wt. % phospholipids. 14. The composition of claim 12, wherein the NSAID is selected from the group consisting of propionic acid drugs, acetic acid drugs, ketone drugs, fenamate drugs, oxicam drugs, salicylic acid drugs, pyrazolin acid drugs, acetaminophen, and COX-2 inhibitors. 15. The composition of claim 12, wherein the NSAID is selected from the group consisting of aspirin, fenoprofen, flurbiprofen, suprofen, benoxaprofen, ibuprofen, ketoprofen, naproxen, oxaprozin, diclofenac, etodolac, indomethacin, ketorolac tromethamine, ketorolac, nabumetone, sulindac, tolmetin, meclofenamate, mefenamic acid, piroxicam, diflunisal, oxyphenbutazone, phenylbutazone, acetaminophen, celecoxib, rofecoxib, and mixtures or combinations thereof. 16. The composition according to claim 12, wherein the weight ratio of NSAID to lecithin oil present in the NSAID-in-oil suspension is from about 4:1 to about 1:4. 17. The composition according to claim 16, wherein the weight ratio of NSAID to lecithin oil is about 1:1. 18. The composition of claim 11, wherein the NSAID is associated with the phospholipid. 19. A pharmaceutical composition that is an NSAID-in-oil suspension and that is the product of a process that comprises admixing an NSAID in powder form into an oil-based carrier, to obtain a NSAID-in-oil suspension, wherein the oil-based carrier comprises a lecithin oil and from about 20 wt. % to about 80 wt. % phospholipids, wherein: (a) the NSAID is present in a therapeutically effective amount; and(b) the composition has a GI toxicity that is reduced relative to that of the NSAID alone. 20. The composition of claim 19, wherein the NSAID-in-oil suspension comprises from about 20 wt. % to about 60 wt. % phospholipids. 21. The composition of claim 19, wherein the NSAID is selected from the group consisting of propionic acid drugs, acetic acid drugs, ketone drugs, fenamate drugs, oxicam drugs, salicylic acid drugs, pyrazolin acid drugs, acetaminophen, and COX-2 inhibitors. 22. The composition of claim 19, wherein the NSAID is selected from the group consisting of aspirin, fenoprofen, flurbiprofen, suprofen, benoxaprofen, ibuprofen, ketoprofen, naproxen, oxaprozin, diclofenac, etodolac, indomethacin, ketorolac tromethamine, ketorolac, nabumetone, sulindac, tolmetin, meclofenamate, mefenamic acid, piroxicam, diflunisal, oxyphenbutazone, phenylbutazone, acetaminophen, celecoxib, rofecoxib, and mixtures or combinations thereof. 23. The composition according to claim 19, wherein the bio-compatible oil is selected from the group consisting of vegetable oils, hydrogenated vegetable oils, and mixtures or combinations thereof. 24. The composition according to claim 19, wherein the weight ratio of NSAID to oil-based carrier present in the NSAID-in-oil suspension is from about 4:1 to about 1:4. 25. The composition according to claim 24, wherein the weight ratio of NSAID to oil-based carrier is about 1:1. 26. The composition of claim 19, wherein the NSAID is associated with the phospholipid.