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Claims for Patent: 6,365,180

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Claims for Patent: 6,365,180

Title: Oral liquid compositions
Abstract:The present invention relates to novel, liquid and semi-solid pharmaceutical compositions which can be administered in liquid form or can be used for preparing capsules containing such pharmaceutical compositions. Also provided are methods of using and processes for preparing the pharmaceutical compositions of the present invention.
Inventor(s): Meyer; Glenn A. (Wilmington, NC), Trespidi; Laura A. (89073 Ulm, DE), Wilson; Edward S. (Wilmington, NC), Clark; Christy M. (Southport, NC), Desai; Ashok J. (Wilmington, NC), Sancilio; Frederick D. (Wilmington, NC)
Assignee:
Application Number:09/354,982
Patent Claims: 1. A pharmaceutical composition comprising:

one or more pharmaceutically active agent wherein said pharmaceutically a active agent is selected from the group consisting of said agents wherein at least one of said agents having at least one acid moiety, and at least one of said agents having at least one ester group or other chemically active moiety in which the terminal moiety to said ester group or other chemically active moiety is hydrolyzed or otherwise removed in situ or in vivo forming at least one acid moiety; and wherein said pharmaceutically active agent is soluble in acid at a ratio of about 3:1 (acid to solute) to about 10,000:1 (acid to solute) or a pharmaceutically acceptable salt thereof;

at least one dispersing agent selected from the group consisting of polymer-based dispersing agents and carbohydratebased dispersing agents, wherein the ratio of said one or more pharmaceutically active agent to said at least one polymer-based dispersing agent is from about 3:1 (w/w) to about 1:50 (w/w) and wherein the ratio of said one or more pharmaceutically active agent to said at least one carbohydrate-based dispersing agent is from about 3:1 (w/w) to about 1:20 (w/w); and

at least one solubilizing agent; and, optionally,

at least one surfactant; and further optionally,

at least one plasticizing agent.

2. A pharmaceutical composition according to claim 1 wherein said one or more polymer-based dispersing agent is polyvinylpyrrolidone.

3. A pharmaceutical composition according to claim 2 wherein said polyvinylpyrrolidone is polyvinylpyrrolidone K29-32.

4. A pharmaceutical composition according to claim 1 wherein said one or more carbohydrate-based dispersing agent is selected from the group consisting of hydroxypropylcellulose, hydroxypropylmethylcellulose, and cyclodextrin.

5. A pharmaceutical composition according to claim 1 wherein the concentration of said one or more solubilizing agent is from about zero percent to about 99 percent (w/w) of the total composition.

6. A pharmaceutical composition according to claim 5 wherein said one or more solubilizing agent is selected from the group consisting of water and polyethylene glycol.

7. A pharmaceutical composition according to claim 6 wherein the molecular weight of said polyethylene glycol is from about 200 to about 8,000.

8. A pharmaceutical composition according to claim 6 wherein the concentration of said polyethylene glycol is from about 20 percent to about 99 percent (w/w) of the total composition.

9. A pharmaceutical composition according to claim 5 wherein the concentration of said water is from about zero percent to about 99 percent (w/w) of the total composition.

10. A pharmaceutical composition according to claim 1 wherein said one or more pharmaceutically active agent is selected from the group consisting of non-steroidal anti-inflammatory drugs, quinapril, fluvastatin, lovastatin, pravastatin, cervistatin, atorvastin, simvastatin, fexofenadine, cromolyn, omeprazole, gemfibrozil, ciprofibrate, ciprofloxacin, lomeflloxacin, ofloxacin, carbidopa, levodopa, retinoic acid, carboprost, penicillins, beta lactams, cephalosporins, liothryonine and probenecid.

11. A pharmaceutical composition according to claim 10 wherein said non-steroidal anti-inflammatory drugs are selected from the group consisting of aralkylcarboxylic acids and arylcarboxylic acids.

12. A pharmaceutical composition according to claim 11 wherein said aralkylcarboxylic acids are selected from the group consisting of diclofenac, fenoprofen, flurbiprofen, ibuprofen, indomethacin, ketoprofen, ketorolac, naproxen, sulindac, etodolac, and tometin.

13. A pharmaceutical composition according to claim 11 wherein said arylcarboxylic acids are selected from the group consisting of diflunisal, mefenamic acid, meclofenamic acid, and flufenamic acid.

14. A pharmaceutical composition according to claim 10 wherein said penicillins are selected from the group consisting of amoxicillins and ampicillins.

15. A pharmaceutical composition according to claim 1 wherein the concentration of said optional at least one plasticizing agent is from about zero percent to about 75 percent (w/w) of the total composition.

16. A pharmaceutical composition according to claim 15 wherein said plasticizing agent is selected from the group consisting of glycerin, propylene, glycol, and sorbitol.

17. A pharmaceutical composition according to claim 5 wherein the concentration of said optional at least one plasticizing agent is from about zero percent to about 75 percent (w/w) of the total composition.

18. A pharmaceutical composition according to Claim 17 wherein said plasticizing agent is selected from the group consisting of glycerin, propylene, glycol, and sorbitol.

19. A pharmaceutical composition according to claim 15 wherein the concentration of said optional at least one surfactant is from about zero percent to about 10 percent (w/w) of the total composition.

20. A pharmaceutical composition according to claim 17 wherein the concentration of said optional at least one surfactant is from about zero percent to about 10 percent (w/w) of the total composition.

21. A method of improving the rate of absorption of one or more pharmaceutically active agent in mammals, wherein said pharmaceutically active agent is selected from the group consisting of said agent wherein:

at least one of said agents having at least one acid moiety, and

at least one of said agents having at least one ester or other chemically active moiety in which the terminal moiety to said ester group or other chemically active moiety is hydrolyzed or otherwise removed in situ or in vivo forming at least one add moiety; and

wherein said pharmaceutically active agent is soluble in acid at a ratio of about 3:1 (acid to solute) to about 10,000:1 (acid to solute), or a pharmaceutically acceptable salt thereof, comprising administering to a mammal in need of treatment of said pharmaceutically active agent an effective amount of a composition according to claim 1 providing said composition comprises said optional surfactant.

22. A method of improving the onset of the therapeutic benefit of one or more pharmaceutically active agent in mammals, wherein said pharmaceutically active agent is selected from the group consisting of said agent wherein:

at least one of said agents having at least one acid moiety, and

at least one of said agents having at least one ester or other chemically active moiety in which the terminal moiety to said ester group or other chemically active moiety is hydrolyzed or otherwise removed in situ or in vivo forming at least one acid moiety; and

wherein said pharmaceutically active agent is soluble in add at a ratio of about 3:1 (acid to solute) to about 10,000:1 (acid to solute), or a pharmaceutically acceptable salt thereof, comprising administering to a mammal in need of treatment of said pharmaceutically active agent an effective amount of a composition according to claim 1 providing said composition comprises said optional surfactant.

23. A method of inhibiting gastroirritation in a mammal caused by the ingestion of one or more non-steroidal anti-inflammatory drugs comprising administering a composition according to claim 1 wherein at least one of said pharmaceutically active agents is an effective amount of a non-steroidal anti-inflammatory drug.

24. A method of treating mammals in need of the treatment provided by one or more pharmaceutically active agent, wherein said pharmaceutically active agent is selected from the group consisting of said agents wherein:

at least one of said agents having at least one acid moiety, and

at least one of said agents having at least one ester or other chemically active moiety in which the terminal moiety to said ester or other chemically active moiety is hydrolyzed or otherwise removed in situ or in vivo forming at least on acid moiety; and

wherein said pharmaceutically active agent is soluble in acid at a ratio of about 3:1 (acid to solute) to about 10,000:1 (acid to solute), or a pharmaceutically acceptable salt thereof, comprising administering to a mammal in need of treatment of said pharmaceutically active agent an effective amount of a pharmaceutical composition according to claim 1.

25. A method according to claim 24 wherein said pharmaceutical composition is used to fill one or more capsule, which are optionally coated, for said administration to said mammal.

26. A method according to claim 25 wherein said capsule is selected from the group consisting of soft gelatin capsules and hard gelatin capsules.

27. A method according to claim 24 wherein said one or more pharmaceutically active agent is one or more non-steroidal anti-inflammatory drugs and, optionally, a motility agent, and said mammal is in need of analgesic treatment.

28. A method according to claim 27 wherein said one or more non-steroidal anti-inflammatory drugs is selected from the group consisting of diclofenac, indomethacin, and sulindac.

29. A method according to claim 28 wherein said mammal is also in need of anti-inflammatory treatment.

30. A method according to claim 28 wherein said composition is based to fill one or more capsules, which are optionally coated, for said administration to said mammal.

31. A method according to claim 24 wherein said one or more pharmaceutically active agent is fexofenadine and said mammal is in need of antihistamine treatment.

32. A method according to claim 24 wherein said one or more pharmaceutically active agent is omeprazole and said mammal is in need of inhibition of gastric acid secretion.

33. A method according to claim 32 wherein said proton pump inhibitor is omeprazole.

34. A method according to claim 33 wherein said composition is used to fill one or more capsules, which are optionally coated, for administration to said mammal.

35. A process for preparing a pharmaceutical composition according to claim 1 wherein said at least one acid moiety of said one or more pharmaceutically active agent is acid labile comprising:

forming a solution of at least one dispersing agent and at least one solubilizing agent and, optionally, one or more lower (C.sub.1 -C.sub.4) alkanol;

adding sufficient base to establish said solution at a pH of at least 9.0; and

adding said one or more pharmaceutically active agent while maintaining said solution at a pH of at least 9.0; and optionally,

one or more surfactant; and further optionally,

one or more plasticizing agent.

36. A process according to claim 35 wherein the concentration of said one or more solubilizing agent is from about 0 percent to about 99 percent (w/w) of the total composition.

37. A process according to claim 35 wherein said at least one polymer-based dispersing agent is polyvinylpyrrolidone, said at least one carbohydrate-based dispersing agent is selected from the group consisting of hydroxypropylcellulose, hydroxypropylmethylcellulose, and cyclodextrin, and said at east one or more solubilizing agent is selected from the group consisting of polyethylene glycol and water.

38. A process according to claim 37 comprising the additional step of filling a capsule with pharmaceutical composition.

39. A process according to claim 38 wherein said capsule is selected from the group consisting of soft gelatin capsules and hard gelatin capsules.

40. A process according to claim 35 comprising the additional step of filling a capsule with said pharmaceutical composition.

41. A process according to claim 40 wherein said capsule is selected from the group consisting of soft gelatin capsules and hard gelatin capsules.

42. A process according to claim 35 wherein said one or more pharmaceutically active agent is a proton pump inhibitor.

43. A process according to claim 42 wherein said proton pump inhibitor is omeprazole.

44. A process according to claim 39 wherein said one or more pharmaceutically active agent is a proton pump inhibitor.

45. A process according to claim 44 wherein said proton pump inhibitor is omeprazole.

46. A pharmaceutical composition when prepared by a process according to claim 35.

47. A pharmaceutical composition according to claim 46 wherein said one or more pharmaceutically active agent is omeprazole.

48. A process according to claim 40 comprising the additional step of coating said capsule with a non-toxic, pharmaceutically acceptable coating.

49. A process according to claim 48 wherein said coating is an enteric coating.

50. A process according to claim 44 comprising the additional step of coating said capsule with a non-toxic, pharmaceutically acceptable coating.

51. A process according to claim 50 wherein said coating is an enteric coating.

52. A method according to claim 34 wherein said optional coating is an enteric coating.

53. A method according to claim 28 wherein said optional motility agent is metoclopromide.
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