Compositions comprising lecithin oils and NSAIDs for protecting the gastrointestinal tract and providing enhanced therapeutic activity
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-009/107
A61K-031/192
A61K-031/195
A61K-031/405
A61K-047/24
A61K-031/4152
A61K-031/5415
A61K-031/616
A61K-031/167
A61K-031/685
A61K-047/44
A61K-047/48
A61K-031/196
A61K-009/00
출원번호
US-0144786
(2016-05-02)
등록번호
US-9687551
(2017-06-27)
발명자
/ 주소
Lichtenberger, Lenard M.
출원인 / 주소
THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
대리인 / 주소
Foley & Lardner LLP
인용정보
피인용 횟수 :
0인용 특허 :
27
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 microemulstion for internal, oral, direct or topical administration.
대표청구항▼
1. A method of reducing a gastrointestinal (GI) toxic effect of a non-steroidal anti-inflammatory drug (NSAID) in a subject who ingests the NSAID, comprising administering to the subject a pharmaceutical composition which is an NSAID-in-oil suspension, wherein: (a) the NSAID-in-oil suspension is the
1. A method of reducing a gastrointestinal (GI) toxic effect of a non-steroidal anti-inflammatory drug (NSAID) in a subject who ingests the NSAID, comprising administering to the subject a pharmaceutical composition which is an NSAID-in-oil suspension, wherein: (a) the NSAID-in-oil suspension is the product of a process that comprises admixing an NSAID in powder form into a lecithin oil;(b) the NSAID-in-oil suspension comprises from about 20 wt. % to about 80 wt. % phospholipids; (c) the NSAID in the NSAID-in-oil suspension is present in a therapeutically effective amount; and(c) the NSAID-in-oil suspension has a GI toxicity that is reduced relative to the NSAID alone. 2. The method of claim 1, wherein the oil-based carrier comprises between about 20 wt. % and about 60 wt. % phospholipids. 3. The method of claim 1, wherein the oil-based carrier comprises between about 20 wt. % and about 40 wt. % phosphatidylcholine. 4. The method of claim 1, wherein the NSAID is selected from the group consisting of aspirin, indomethacin, and ibuprofen. 5. The method of claim 1, wherein the NSAID is aspirin. 6. The method of claim 1, wherein the NSAID is ibuprofen. 7. The method of claim 1, wherein the NSAID is indomethacin. 8. The method of claim 1, 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. 9. The method of claim 1, wherein the weight ratio of NSAID to lecithin oil is about 1:1. 10. The method of claim 1, wherein the NSAID is associated with the phospholipid. 11. The method of claim 1, wherein the GI toxic effect is at least one effect selected from the group consisting of GI bleeding and GI tract ulceration. 12. The method of claim 1, wherein the subject suffers from at least one condition selected from the group consisting of tissue inflammation, tissue ulceration, pain, fever, cardiovascular disease, ovarian cancer, colon cancer, and Alzheimer's Disease. 13. The method of claim 1, wherein the subject suffers from cardiovascular disease. 14. A method of reducing a gastrointestinal (GI) toxic effect of a non-steroidal anti-inflammatory drug (NSAID) in a subject who ingests the NSAID, comprising administering to the subject a pharmaceutical composition which is an NSAID-in-oil suspension, wherein: (a) the NSAID-in-oil suspension is the product of a process that comprises admixing an NSAID in powder form into an oil-based carrier to obtain the NSAID-in-oil suspension, wherein the oil-based carrier comprises a lecithin oil and from about 20 wt. % to about 80 wt. % phospholipids;(b) the NSAID in the NSAID-in-oil suspension is present in a therapeutically effective amount; and(c) the NSAID-in-oil suspension has a GI toxicity that is reduced relative to that of the NSAID alone. 15. The method of claim 14, wherein the oil-based carrier comprises between about 20 wt. % and about 60 wt. % phospholipids. 16. The method of claim 14, wherein the oil-based carrier comprises between about 20 wt. % and about 40 wt. % phosphatidylcholine. 17. The method of claim 14, wherein the NSAID is selected from the group consisting of aspirin, indomethacin, and ibuprofen. 18. The method of claim 14, wherein the NSAID is aspirin. 19. The method of claim 14, wherein the NSAID is ibuprofen. 20. The method of claim 14, wherein the NSAID is indomethacin. 21. The method of claim 14, 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. 22. The method of claim 14, wherein the weight ratio of NSAID to lecithin oil is about 1:1. 23. The method of claim 14, wherein the NSAID is associated with the phospholipid. 24. The method of claim 14, wherein the GI toxic effect is at least one effect selected from the group consisting of GI bleeding and GI tract ulceration. 25. The method of claim 14, wherein the subject suffers from at least one condition selected from the group consisting of tissue inflammation, tissue ulceration, pain, fever, cardiovascular disease, ovarian cancer, colon cancer, and Alzheimer's Disease. 26. The method of claim 14, wherein the subject suffers from cardiovascular disease.
Lichtenberger, Lenard M., Compositions comprising lecithin oils and NSAIDs for protecting the gastrointestinal tract and providing enhanced therapeutic activity.
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