Claims
- 1. A self-emulsifying preconcentrate pharmaceutical composition capable of forming an oil-in-water microemulsion or emulsion upon dilution with an aqueous solution, comprising:a) a pharmaceutically effective amount of an omega-3 fatty acid oil; b) a therapeutically effective amount of a poorly water soluble therapeutic agent, wherein the poorly water soluble therapeutic agent is substantially soluble in the omega-3 fatty acid oil; and c) a surfactant system comprising at least one surfactant; wherein the composition contains minor amounts or is substantially free of a hydrophilic solvent system.
- 2. The composition of claim 1, wherein the composition is a microemulsion preconcentrate.
- 3. The composition of claim 1, wherein the composition is an emulsion preconcentrate.
- 4. The composition of claim 1, wherein the composition is adapted for oral administration.
- 5. The composition of claim 1, wherein the omega-3 fatty acid oil is present in an amount ranging from 5 to 70% by weight.
- 6. The composition of claim 1, wherein the therapeutic agent is a cyclosporin.
- 7. The composition of claim 1, wherein the omega-3 fatty acid oil comprises an omega-3 fatty acid oil selected from the group consisting of eicosapentaenoic acid, salts of eicosapentaenoic acid, docosahexaenoic acid, salts of docosahexaenoic acid, triglycerides of eicosapentaenoic acid, triglycerides of docosahexaenoic acid, ethyl esters of eicosapentaenoic acid, ethyl esters of docosahexaenoic acid and mixtures thereof.
- 8. The composition of claim 1, wherein the omega-3 fatty acid oil comprises a component of a fish oil or a mixture of fish oils.
- 9. The composition of claim 8, wherein the omega-3 fatty acid component of the fish oil or the mixture of fish oils is at least 50% by weight.
- 10. The composition of claim 8, wherein the omega-3 fatty acid component of the fish oil or the mixture of fish oils is at least 70% by weight.
- 11. The composition of claim 8, wherein the omega-3 fatty acid component of the fish oil or the mixture of fish oils is at least 80% by weight.
- 12. The composition of claim 1, wherein the omega-3 fatty acid oil comprises omega-3 fatty acid triglycerides.
- 13. The composition of claim 1, wherein the omega-3 fatty acid oil comprises omega-3 fatty acid ethyl esters.
- 14. The composition of claim 1, wherein the therapeutic agent is selected from the group consisting of an analgesic, anti-allergic agent, anti-fungal, anti-inflammatory agent, anti-arrythmic agent, antibiotic, anticoagulant, antidepressant, antidiabetic agent, anti-epilepsy agent, antihypertensive agent, anti-gout agent, anti-malarial, anti-migraine agent, antimuscarinic agent, antineoplastic agent, anti-protozoal agent, anxiolytic, thyroid, anti-thyroid, antiviral, anoretic, bisphosphonate, cardiac inotropic agent, cardiovascular agent, corticosteroid, diuretic, dopaminergic agent, gastrointestinal agent, hemostatic, histamin receptor antagonist, hypnotic, immunosuppressant, kidney protective agent, lipid regulating agent, muscle relaxant, neuroleptic, neurotropic agent, opioid agonist and antagonist, parasympathomimetic, protease inhibitor, prostglandin, sedative, sex hormone, stimulant, sympathomimetic, vasodilator and xanthin or mixtures thereof.
- 15. The composition of claim 1, wherein the composition is adapted for topical administration.
- 16. The composition of claim 1, wherein the composition is adapted for parenteral administration.
- 17. A microemulsion or emulsion pharmaceutical composition comprising the self-emulsifying preconcentrate of claim 1 diluted with an aqueous solution.
- 18. The composition of claim 17, wherein the composition is a microemulsion.
- 19. The composition of claim 17, wherein the composition is an emulsion.
- 20. The composition of claim 17, wherein the composition is adapted for oral administration.
- 21. The composition of claim 17, wherein the therapeutic agent is a cyclosporin.
- 22. The composition of claim 17, wherein the omega-3 fatty acid oil comprises an omega-3 fatty acid oil selected from the group consisting of eicosapentaenoic acid, salts of eicosapentaenoic acid, docosahexaenoic acid, salts of docosahexaenoic acid, triglycerides of eicosapentaenoic acid, triglycerides of docosahexaenoic acid, ethyl esters of eicosapentaenoic acid, ethyl esters of docosahexaenoic acid and mixtures thereof.
- 23. The composition of claim 17, wherein the omega-3 fatty acid oil comprises a component of a fish oil or a mixture of fish oils.
- 24. The composition of claim 23, wherein the omega-3 fatty acid component of the fish oil or the mixture of fish oils is at least 50% by weight.
- 25. The composition of claim 23, wherein the omega-3 fatty acid component of the fish oil or the mixture of fish oils is at least 70% by weight.
- 26. The composition of claim 23, wherein the omega-3 fatty acid component of the fish oil or the mixture of fish oils is at least 80% by weight.
- 27. The composition of claim 17, wherein the therapeutic agent is selected from the group consisting of an analgesic, anti-allergic agent, anti-fungal, anti-inflammatory agent, anti-arrythmic agent, antibiotic, anticoagulant, antidepressant, antidiabetic agent, anti-epilepsy agent, antihypertensive agent, anti-gout agent, anti-malarial, anti-migraine agent, antimuscarinic agent, antineoplastic agent, anti-protozoal agent, anxiolytic, thyroid, anti-thyroid, antiviral, anoretic, bisphosphonate, cardiac inotropic agent, cardiovascular agent, corticosteroid, diuretic, dopaminergic agent, gastrointestinal agent, hemostatic, histamine receptor antagonist, hypnotic, immunosuppressant, kidney protective agent, lipid regulating agent, muscle relaxant, neuroleptic, neurotropic agent, opioid agonist and antagonist, parasympathomimetic, protease inhibitor, prostglandin, sedative, sex hormone, stimulant, sympathomimetic, vasodilator and xanthin or mixtures thereof.
- 28. The composition of claim 17, wherein the omega-3 fatty acid oil comprises omega-3 fatty acid triglycerides.
- 29. The composition of claim 17, wherein the omega-3 fatty acid oil comprises omega-3 fatty acid ethyl esters.
- 30. The composition of claim 17, wherein the composition is adapted for topical administration.
- 31. The composition of claim 17, wherein the composition is adapted for parenteral administration.
- 32. The composition of claim 17, wherein the amount of aqueous solution to preconcentrate is 1:1 or greater.
- 33. A method of lowering the therapeutically effective amount of a poorly water soluble therapeutic agent comprising administering to a human in need of a therapeutically effective amount of the therapeutic agent the self-emulsifying preconcentrate of claim 1, wherein the omega-3 fatty acid oil exerts an additive effect or synergistic effect to the therapeutic effect of the therapeutic agent.
- 34. A method of reducing the side effects of a poorly water soluble therapeutic agent comprising administering to a human in need of a therapeutically effective amount of the therapeutic agent the self-emulsifying preconcentrate of claim 1, wherein the omega-3 fatty acid oil mediates at least one negative side effect of the therapeutic agent.
- 35. A method of lowering the therapeutically effective amount of a poorly water soluble therapeutic agent comprising administering to a human in need of a therapeutically effective amount of the therapeutic agent the microemulsion or emulsion of claim 17, wherein the omega-3 fatty acid oil exerts an additive effect or synergistic effect to the therapeutic effect of the therapeutic agent.
- 36. A method of reducing the side effects of a poorly water soluble therapeutic agent comprising administering to a human in need of a therapeutically effective amount of the therapeutic agent the microemulsion or emulsion of claim 17, wherein the omega-3 fatty acid oil mediates at least one negative side effect of the therapeutic agent.
- 37. The method according to any of claims 33, 34, 35 or 36, wherein the poorly water soluble therapeutic agent is a cyclosporin.
- 38. A hard or softgel capsule formulation comprising the composition of claim 1.
- 39. A self-emulsifying preconcentrate pharmaceutical composition capable of forming an oil-in-water microemulsion or emulsion upon dilution with an aqueous solution, comprising:a) a pharmaceutically effective amount of an omega-3 fatty acid oil; b) a therapeutically effective amount of a poorly water soluble therapeutic agent, wherein the poorly water soluble therapeutic agent is substantially soluble in the omega-3 fatty acid oil; and c) a surfactant system comprising at least one surfactant.
Parent Case Info
This application claims priority from U.S. Provisional Application 60/084,516, filed May 7, 1998 and is a continuation-in-part of U.S. application Ser. No. 08/988,270, filed Dec. 10, 1997, now abandoned.
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Provisional Applications (1)
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Number |
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|
60/084516 |
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Continuation in Parts (1)
|
Number |
Date |
Country |
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08/988270 |
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US |
Child |
09/209066 |
|
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