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Claims for Patent: RE39030

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Claims for Patent: RE39030

Title:Fluoxetine enteric pellets and methods for their preparation and use
Abstract:A superior enteric formulation of the antidepressant drug, fluoxetine, is in the form of enteric pellets of which the enteric layer comprises hydroxypropylmethylcellulose acetate succinate.
Inventor(s): Anderson; Neil Robert (West Lafayette, IN), Harrison; Roger Garrick (Zionsville, IN), Lynch; Daniel Frederick (Indianapolis, IN), Oren; Peter Lloyd (Fishers, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:10/058,891
Patent Claims: 1. An enteric fluoxetine pellet comprising a) a core consisting of fluoxetine and one or more pharmaceutically acceptable excipients; b) an optional separating layer comprising a non-reducing sugar and one or more pharmaceutically acceptable excipients; c) an enteric layer comprising hydroxypropylmethylcellulose acetate succinate (HPMCAS) and one or more pharmaceutically acceptable excipients; d) an optional finishing layer..].

.[.2. A pellet of claim 1 wherein the HPMCAS is partially neutralized with ammonium ions to the degree that from about 0% to about 25% of the succinic acid groups are neutralized..].

.[.3. A pellet of claim 2 wherein the HPMCAS is partially neutralized to the degree that from about 0% to about 15% of the succinic acid groups are neutralized..].

.[.4. A pellet of claim 1 wherein the separating layer is present..].

.[.5. A pellet of claim 1 wherein the average particle size of the fluoxetine is about 50 .mu.m or less..].

.[.6. A pellet of claim 5 wherein the core comprises an inert core on which the fluoxetine is deposited as a layer comprising in addition a pharmaceutically acceptable excipient..].

.[.7. A pellet of claim 6 wherein the separating layer is present..].

.[.8. A pellet of claim 7 wherein the HPMCAS is partially neutralized with ammonium ions to the degree that from about 0% to about 25% of the succinic acid groups are neutralized..].

.[.9. A pellet of claim 4 wherein the separating layer comprises a pharmaceutically acceptable sugar..].

.[.10. A pellet of claim 9 wherein the sugar is sucrose..].

.[.11. A process for preparing an enteric fluoxetine pellet comprising a) providing a core consisting of fluoxetine and one or more pharmaceutically acceptable excipients; b) optionally, applying to the core a separating layer comprising a non-reducing sugar and one or more pharmaceutically acceptable excipients; c) applying an enteric layer comprising HPMCAS and one or more pharmaceutically acceptable excipients, wherein the HPMCAS is supplied as an aqueous solution or suspension and the application takes place in an apparatus of the fluid bed type; d) optionally, applying a finishing layer..].

.[.12. A process of claim 11 wherein the HPMCAS is fully or partially neutralized with ammonium ions..].

.[.13. A process of claim 12 wherein the HPMCAS is neutralized to the degree that from about 25% to about 100% of the succinic acid groups are neutralized..].

.[.14. A process of claim 11 wherein the separating layer is applied..].

.[.15. A process of claim 14 wherein the separating layer comprises a pharmaceutically acceptable sugar..].

.[.16. A process of claim 15 wherein the sugar is sucrose..].

.[.17. A process of claim 11 wherein the core is prepared by applying fluoxetine and one or more pharmaceutically acceptable excipients to an inert core..].

.[.18. A process of claim 17 wherein the separating layer is applied and comprises a pharmaceutically acceptable sugar..].

19. A formulation of .[.claim 1 containing 20-100.]. .Iadd.enteric fluoxetine pellets sufficient to administer 60-120 .Iaddend.mg base equivalent of fluoxetine.Iadd., wherein the pellets comprise a core consisting of fluoxetine and one or more pharmaceutically acceptable excipients and an enteric layer comprising hydroxypropyl-methylcellulose acetate succinate (HPMCAS) and one or more pharmaceutically acceptable excipients.Iaddend..

20. A formulation of claim 1.Iadd.9 .Iaddend..[.containing.]. .Iadd.administering .Iaddend.about 80-90 mg base equivalent of fluoxetine.

21. A formulation of claim 1.Iadd.9 .Iaddend..[.containing.]. .Iadd.administering .Iaddend.about 90 mg base equivalent of fluoxetine.

22. A formulation of claim 19 wherein the fluoxetine is present as fluoxetine hydrochloride.

23. A formulation of claim 20 wherein the fluoxetine is present as fluoxetine hydrochloride.

24. A formulation of claim 21 wherein the fluoxetine is present as fluoxetine hydrochloride.

25. A gelatin capsule containing .[.the formulation of claim 1.]. .Iadd.enteric fluoxetine pellets sufficient to administer 60-120 mg base equivalent of fluoxetine, wherein the pellets comprise a core consisting of fluoxetine and one or more pharmaceutically acceptable excipients and an enteric layer comprising hydroxypropylmethylcellulose acetate succinate (HPMCAS) and one or more pharmaceutically acceptable excipients.Iaddend..

26. A gelatin capsule .[.containing the formulation.]. of claim .[.24.]. .Iadd.25, wherein about 80-90 base equivalents of fluoxetine are administered.Iaddend..

27. A formulation of claim 1.Iadd.9 .Iaddend.containing the following: TABLE-US-00005 Cores Sucrose-starch nonpareils, 30-35 mesh 100-150 Fluoxetine layer Fluoxetine hydrochloride 100.5-100.8 mg Sucrose 20-30 mg Hydroxypropylmethylcellulose 10-15 mg Separating layer Hydroxypropylmethylcellulose 4-12 mg Sucrose 15-35 mg Talc, 500 mesh 25-60 mg Enteric layer HPMCAS-LF 60-90 mg Triethyl citrate 10-20 mg Talc, 500 mesh 15-25 mg Finishing layer Color mixture white (HPMC + titanium dioxide) 35-55 mg HPMC 5-15 mg Talc Trace.

28. A gelatin capsule .[.containing the formulation.]. of claim .[.24.]. .Iadd.25, wherein about 90 mg base equivalent of fluoxetine are administered.Iaddend..

29. A formulation according to claim 1.Iadd.9 .Iaddend.wherein the formulation additionally contains pindolol.

30. A method of treating .[.people.]. .Iadd.a patient .Iaddend.suffering from depression, obsessive-compulsive disorder, bulimia, pain, obsessive-compulsive personality disorder, post-traumatic stress disorder, hypertension, atherosclerosis, anxiety, anorexia nervosa, panic, social phobia, stuttering, sleep disorders, chronic fatigue, Alzheimer's disease, alcohol abuse, appetite disorders, weight loss, agoraphobia, improving memory, amnesia, smoking cessation, nicotine withdrawal symptoms, disturbances of mood and/or appetite associated with pre-menstrual syndrome, depressed mood and/or carbohydrate craving associated with pre-menstrual syndrome, disturbances of mood, disturbances of appetite or disturbances which contribute to recidivism associated with nicotine withdrawal, circadian rhythm disorder, borderline personality disorder, hypochondriasis, pre-menstrual syndrome (PMS), late luteal phase dysphoric disorder, pre-menstrual dysphoric disorder, trichotillomania, symptoms following discontinuation of other antidepressants, aggressive/intermittent explosive disorder, compulsive gambling, compulsive spending, compulsive sex, psychoactive substance use disorder, sexual disorder, schizophrenia, premature ejaculation, or psychiatric symptoms selected from stress, worry, anger, rejection sensitivity, and lack of physical energy comprising administering a formulation of claim 1.Iadd.9.Iaddend..

31. A method of claim 30 employing a formulation .[.containing 20-100.]. .Iadd.administering about 80-90 .Iaddend.mg base equivalent of fluoxetine.

32. A method of claim 30 employing a formulation .[.containing.]. .Iadd.administering .Iaddend.about 90 mg base equivalent of fluoxetine.

33. A method of claim 30 wherein the fluoxetine is present as fluoxetine hydrochloride.

34. A method of claim 31 wherein the fluoxetine is present as fluoxetine hydrochloride.

35. A method of claim 32 wherein the fluoxetine is present as fluoxetine hydrochloride.

36. A method of claim 30 employing a formulation containing the following: TABLE-US-00006 Cores Sucrose-starch nonpareils, 30-35 mesh 100-150 Fluoxetine layer Fluoxetine hydrochloride 100.5-100.8 mg Sucrose 20-30 mg Hydroxypropylmethylcellulose 10-15 mg Separating layer Hydroxypropylmethylcellulose 4-12 mg Sucrose 15-35 mg Talc, 500 mesh 25-60 mg Enteric layer HPMCAS-LF 60-90 mg Triethyl citrate 10-20 mg Talc, 500 mesh 15-25 mg Finishing layer Color mixture white (HPMC + titanium dioxide) 35-55 mg HPMC 5-15 mg Talc Trace.

37. A method of claim 30 of treating .[.people.]. .Iadd.a patient .Iaddend.suffering from pain, further comprising the coadministration of morphine, codeine or dextropropoxyphene.

38. A method of claim 37 employing a formulation .[.containing about 20-100.]. .Iadd.administering about 80-90 .Iaddend.mg base equivalent of fluoxetine.

39. A method of claim 37 employing a formulation .[.containing.]. .Iadd.administering .Iaddend.about 90 mg base equivalent of fluoxetine.

.Iadd.40. A formulation of claim 19, wherein the pellets further comprise a separating layer..Iaddend.

.Iadd.41. A formulation of claim 40, wherein the separating layer comprises a non-reducing sugar and one or more pharmaceutically acceptable excipients..Iaddend.

.Iadd.42. A formulation of claim 19, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.43. A formulation of claim 40, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.44. A formulation of claim 41, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.45. A formulation of claim 21, wherein the pellets further comprise a separating layer..Iaddend.

.Iadd.46. A formulation of claim 45, wherein the separating layer comprises a non-reducing sugar and one or more pharmaceutically acceptable excipients..Iaddend.

.Iadd.47. A formulation of claim 21, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.48. A formulation of claim 45, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.49. A formulation of claim 46, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.50. A gelatin capsule of claim 25, wherein the pellets further comprise a separating layer..Iaddend.

.Iadd.51. A gelatin capsule of claim 50, wherein the separating layer comprises a non-reducing sugar and one or more pharmaceutically acceptable excipients..Iaddend.

.Iadd.52. A gelatin capsule of claim 25, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.53. A gelatin capsule of claim 50, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.54. A gelatin capsule of claim 51, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.55. A gelatin capsule of claim 28, wherein the pellets further comprise a separating layer..Iaddend.

.Iadd.56. A gelatin capsule of claim 55, wherein the separating layer comprises a non-reducing sugar and one or more pharmaceutically acceptable excipients..Iaddend.

.Iadd.57. A gelatin capsule of claim 28, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.58. A gelatin capsule of claim 55, wherein the pellets further comprise finishing layer..Iaddend.

.Iadd.59. A gelatin capsule of claim 56, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.60. A method of claim 30, wherein the pellets further comprise a separating layer..Iaddend.

.Iadd.61. A method of claim 60, wherein the separating layer comprises a non-reducing sugar and one or more pharmaceutically acceptable excipients..Iaddend.

.Iadd.62. A method of claim 30, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.63. A method of claim 60, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.64. A method of claim 61, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.65. A method of claim 32, wherein the pellets further comprise a separating layer..Iaddend.

.Iadd.66. A method of claim 65, wherein the separating layer comprises a non-reducing sugar and one or more pharmaceutically acceptable excipients..Iaddend.

.Iadd.67. A method of claim 32, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.68. A method of claim 65, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.69. A method of claim 66, wherein the pellets further comprise a finishing layer..Iaddend.

.Iadd.70. A method of claim 30 without an increase in nausea..Iaddend.

.Iadd.71. A method of claim 32 without an increase in nausea..Iaddend.

.Iadd.72. A method of claim 36 without an increase in nausea..Iaddend.

.Iadd.73. A method of claim 37 without an increase in nausea..Iaddend.

.Iadd.74. A method of claim 38 without an increase in nausea..Iaddend.

.Iadd.75. A method of claim 39 without an increase in nausea..Iaddend.
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