COMPOSITIONS AND METHODS FOR TREATMENT OF CHRONIC FATIGUE

• US 20150250761A1
• Filed: 05/06/2015
• Published: 09/10/2015
• Est. Priority Date: 06/24/2011
• Status: Abandoned Application

• Current Assignee: K-PAX Pharmaceuticals, Inc.
• Original Assignee: K-PAX Pharmaceuticals, Inc.
• Inventors: Kaiser, Jon D.
• Application Number:
  US14/705,573
• Publication Number:
  US 20150250761A1
• Time in Patent Office: Days
• US Class Current: 1/1
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/137 Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
• CPC Class Codes: A61K 31/138 Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine atenolol A61K31/165; pindolol A61K31/404; timolol A61K31/5377
• CPC Class Codes: A61K 31/145 having sulfur, e.g. thiurams (>N—C(S)—S—C(S)—N< and >N—C(S)—S—S—C(S)—N<), Sulfinylamines (—N=SO), Sulfonylamines (—N=SO2) isothiourea A61K31/155
• CPC Class Codes: A61K 31/165 having aromatic rings, e.g. colchicine, atenolol, progabide
• CPC Class Codes: A61K 31/185 Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids hydroxamic acids A61K31/16; peroxy acids A61K31/327
• CPC Class Codes: A61K 31/198 Alpha-amino acids, e.g. alanine or edetic acid [EDTA] betaine A61K31/205; proline A61K31/401; tryptophan A61K31/405; histidine A61K31/4172; peptides not degraded to individual amino acids A61K38/00
• CPC Class Codes: A61K 31/205 Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
• CPC Class Codes: A61K 31/385 having two or more sulfur atoms in the same ring
• CPC Class Codes: A61K 31/4415 Pyridoxine, i.e. Vitamin B6 pyridoxal phosphate A61K31/675
• CPC Class Codes: A61K 31/4458 only substituted in position 2, e.g. methylphenidate
• CPC Class Codes: A61K 31/522 having oxo groups directly attached to the heterocyclic ring, e.g. hypoxanthine, guanine, acyclovir
• CPC Class Codes: A61K 31/714 Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 21/00 Drugs for disorders of the muscular or neuromuscular system
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 25/28 for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Pharmaceutical compositions and methods for the treatment of chronic fatigue in human patients comprising a central nervous system (CNS) stimulant in a daily low-dosage amount in combination with therapeutically effective daily amounts of micronutrients, comprising acetyl L-carnitine, L-tyrosine, N-acetyl cysteine, and alpha-lipoic acid. The CNS and micronutrient components may be in an oral dosage composition containing a low dosage amount of CNS stimulant such as about 2.5 mg methylphenidate HCl together with about 60-250 mg acetyl L-carnitine, 50-200 mg L-tyrosine, 60-250 mg N-acetyl cysteine, and 25-100 mg alpha-lipoic acid.

Claims

1. An oral dosage composition for the treatment of chronic fatigue, comprising:

a central nervous system stimulant in a therapeutically effective low-dosage amount;

a therapeutically effective amount of a micronutrient stimulant component comprising L-carnitine and L-tyrosine; and

a therapeutically effective amount of a micronutrient antioxidant component comprising N-acetyl cysteine and alpha-lipoic acid.

2. The composition of claim 1, wherein acetyl L-carnitine is present in a range of 60 to 250 mg.

3. The composition of claim 1, wherein acetyl L-carnitine is present in a range of 100 to 150 mg.

4. The composition of claim 1, wherein L-tyrosine is present in a range of 50 to 200 mg.

5. The composition of claim 1, wherein L-tyrosine is present in a range of 80 to 100 mg.

6. The composition of claim 1, wherein N-acetyl cysteine is present in a range of 60 to 250 mg.

7. The composition of claim 1, wherein N-acetyl cysteine is present in a range of 100 to 150 mg.

8. The composition of claim 1, wherein alpha-lipoic acid is present in a range of 25 to 100 mg.

9. The composition of claim 1, wherein alpha-lipoic acid is present in a range of 40 to 60 mg.

10. The composition of claim 1, further comprising about 25 to 100 mg L-taurine.

11. The composition of claim 10, wherein L-taurine is present in a range of 35 to 75 mg.

12. The composition of claim 1, wherein the central nervous system stimulant is atomoxetine HCl in an amount of about 2 mg to 20 mg.

13. The composition of claim 1, wherein the central nervous system stimulant is methylphenidate HCl in the amount of about 0.75 mg to 7.5 mg.

14. The composition of claim 1, wherein the central nervous system stimulant is dexmethylphenidate HCl in the amount of about 0.5 mg to 5 mg.

15. The composition of claim 1, wherein the central nervous system stimulant is modafinil in the amount of about 4 mg to 40 mg.

16. The composition of claim 1, wherein the central nervous system stimulant is armodafinil in the amount of 4 mg to 40 mg.

17. The composition of claim 1, wherein the central nervous system stimulant is an amphetamine in the amount of about 1 mg to 10 mg.

18. The composition of claim 1, further comprising one or more of vitamin B6 (pyridoxine) and vitamin B12.

19. The composition of claim 1, further comprising one or more of vitamin C, vitamin E, beta carotene, zinc and selenium.

20. The composition of claim 1, wherein the composition comprises acetyl L-carnitine, L-tyrosine, vitamin B6 (pyridoxine), vitamin B12, N-acetyl cysteine, alpha-lipoic acid, L-taurine, vitamin C, vitamin E and beta carotene.

21. The composition of claim 20, further comprising of one or more additional vitamins or minerals selected from the group consisting of zinc, selenium, mixed tocopherols, vitamin B1 (thiamine), vitamin B2 (riboflavin), niacinamide, calcium pantothenate, choline (bitartrate), inositol, folic acid (folacin), biotin, vitamin D3 (cholicalciferol), calcium, magnesium, iron, iodine, copper, manganese, potassium, chromium, molybdenum and boron.

22. The composition of claim 1, wherein the stimulant and micronutrient components are combined together in a pill, tablet, capsule or liquid dosage form.

23. A method for treating chronic fatigue in a human patient comprising:

administering a daily low-dosage amount of a central nervous system stimulant; and

administering daily therapeutically effective dosages of acetyl L-carnitine,

L-tyrosine,

N-acetyl cysteine, and

alpha lipoic acid.

24. The method of claim 23, wherein acetyl L-carnitine is administered in a range of about 100 to 2000 mg/d.

25. The method of claim 23, wherein acetyl L-carnitine is administered in a range of about 400 to 1600 mg/d.

26. The method of claim 23, wherein L-tyrosine is administered in a range of about 100 to 2000 mg/d.

27. The method of claim 23, wherein L-tyrosine is administered in a range of 350 to 1400 mg/d.

28. The method of claim 23, wherein N-acetyl cysteine is administered in a range of 100 to 2000 mg/d.

29. The method of claim 23, wherein N-acetyl cysteine is administered in a range of 250 to 1250 mg/d.

30. The method of claim 23, wherein alpha-lipoic acid is administered in a range of 50 to 1000 mg/d.

31. The method of claim 23, wherein alpha-lipoic acid is administered in a range of 150 to 600 mg/d.

32. The method of claim 23, wherein said administering is conducted on a continuous basis for at least 12 weeks.

33. The method of claim 23, wherein the chronic fatigue is associated with Chronic Fatigue Syndrome.

34. The method of claim 23, wherein the chronic fatigue is associated with fibromyalgia.

35. The method of claim 23, wherein the chronic fatigue is associated with a condition selected from the group of cancer, HIV/AIDS, chronic hepatitis B &

C, autoimmune disorders, Lyme'"'"'s disease, Parkinson'"'"'s disease, Alzheimer'"'"'s disease, psychological disorders including depression, ADD and ADHD, multiple sclerosis, sickle cell anemia, and congestive heart failure.

36. The method of claim 23, wherein the CNS stimulant, acetyl L-carnitine, L-tyrosine, N-acetyl cysteine, and alpha lipoic acid are orally administered together in a combined dosage form.

37. The method of claim 23, wherein the CNS stimulant comprises methylphenidate.

38. The method of claim 37, wherein the methylphenidate is administered in an amount of 2.5 to 40 mg/day.

39. The method of claim 38, wherein the methylphenidate is administered in an amount less than 20 mg/day.

40. The method of claim 23, wherein the CNS stimulant comprises modafinil.

41. The method of claim 37, wherein the modafinil is administered in an amount of 30 to 100 mg/day.

42. The method of claim 38, wherein the modafinil is administered in an amount of 30 to 50 mg/day.

43. The method of claim 23, wherein the CNS stimulant comprises armodafinil.

44. The method of claim 37, wherein the armodafinil is administered in an amount of 20 to 80 mg/day.

45. The method of claim 38, wherein the armodafinil is administered in an amount of 20 to 40 mg/day.

46. The method of claim 23, wherein the CNS stimulant comprises dexmethylphenidate.

47. The method of claim 37, wherein the dexmethylphenidate is administered in an amount of 2.5 to 10 mg/day.

48. The method of claim 38, wherein the dexemthylphenidate is administered in an amount of 2.5 to 5 mg/day.

49. The method of claim 23, wherein the CNS stimulant comprises an amphetamine.

50. The method of claim 37, wherein the amphetamine is administered in an amount of 2.5 to 20 mg/day.

51. The method of claim 38, wherein the amphetamine is administered in an amount of 2.5 to 10 mg/day.

52. The method of claim 23, wherein the CNS stimulant comprises atomoxetine.

53. The method of claim 37, wherein the atomoxetine is administered in an amount of 20 to 50 mg/day.

54. The method of claim 38, wherein the atomoxetine is administered in an amount of 20 to 25 mg/day.

55. The method of claim 23, wherein the CNS stimulant comprises caffeine.

56. The method of claim 55, wherein the caffeine is administered in an amount of 15 to 200 mg/day.

57. The method of claim 55, wherein the caffeine is administered in an amount of 30 to 125 mg/day.