Compositions, methods and kits for reducing lipid levels

• US 9,895,357 B2
• Filed: 06/09/2017
• Issued: 02/20/2018
• Est. Priority Date: 03/15/2013
• Status: Active Grant

• Current Assignee: Nusirt Sciences, Inc.
• Original Assignee: Nusirt Sciences, Inc.
• Inventors: Zemel, Michael, Bruckbauer, Antje
• Primary Examiner(s): LOVE, TREVOR M
• Application Number:
  US15/619,406
• Publication Number:
  US 20170340615A1
• Time in Patent Office: 256 Days
• CPC Class Codes: A23L 33/15 Vitamins
• CPC Class Codes: A23L 33/175 Amino acids
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A23V 2200/3262 having an effect on blood cholesterol
• CPC Class Codes: A23V 2250/0628 Leucine
• CPC Class Codes: A23V 2250/7046 Vitamin B3 niacin
• 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 31/05 Phenols cannabinoids A61K31/658
• 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 31/435 having six-membered rings with one nitrogen as the only ring hetero atom
• CPC Class Codes: A61K 31/455 Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
• CPC Class Codes: A61K 31/706 containing six-membered rings with nitrogen as a ring hetero atom
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

Compositions, methods, and kits useful for treating hyperlipidemic conditions are provided herein. Such compositions can contain synergizing amounts of nicotinic acid, nicotinamide riboside and/or nicotinic acid metabolites in combination with leucine and/or a leucine metabolite, with or without resveratrol.

Claims

1. A kit comprising:

i. a composition comprising;

a. at least 250 mg of leucine and/or at least 25 mg of one or more leucine metabolites, wherein the leucine metabolite is selected from the group consisting of keto-isocaproic acid (KIC), alpha-hydroxy-isocaproic acid, and hydroxymethylbutyrate (HMB); and

b. at least 1 mg of nicotinic acid and/or nicotinamide riboside and/or one or more nicotinic acid metabolites, wherein the nicotinic acid metabolite is selected from the group consisting of nicotinyl CoA, nicotinuric acid, nicotinate mononucleotide, nicotinate adenine dinucleotide, and nicotinamide adenine dinucleotide;

wherein the composition is substantially free of alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, valine, isoleucine and tyrosine,

ii. instructions.

2. The kit of claim 1, wherein the composition is substantially free of nicotinamide.

3. The kit of claim 1, wherein the component (a) in the composition is leucine and the component (b) in the composition is nicotinic acid.

4. The kit of claim 1, wherein the amount of leucine and/or one or more leucine metabolites is less than about 1300 mg.

5. The kit of claim 1, wherein the amount of nicotinic acid and/or nicotinamide riboside and/or one or more nicotinic acid metabolites is less than about 250 mg.

6. The kit of claim 1, wherein the amount of nicotinic acid and/or nicotinamide riboside and/or one or more nicotinic acid metabolites is about 1-100 mg.

7. The kit of claim 1, wherein the composition further comprises resveratrol.

8. The kit of claim 1, wherein the composition is a tablet, a capsule, or a pill.

9. The kit of claim 1, wherein the composition contains less than about 10% of non-leucine amino acids.

10. The kit of claim 1, wherein the composition contains less than about 0.1% of alanine, arginine, asparagine, aspartic acid, cysteine, glutamic acid, glutamine, glycine, histidine, lysine, methionine, phenylalanine, proline, serine, threonine, tryptophan, valine, isoleucine and tyrosine.

11. The kit of claim 1, wherein the composition is formulated in a unit dosage form.

12. The kit of claim 1, wherein a portion of the leucine and/or one or more leucine metabolites is in a free form.

13. The kit of claim 1, wherein the composition when administered to a subject in need thereof synergistically reduces lipid content in the subject.

14. The kit of claim 1, wherein the composition when administered to a subject in need thereof synergistically enhances a decrease in weight gain, enhances an increase in fat oxidation, and/or enhances an increase in activation of Sirt1 in the subject.

15. The kit of claim 1, wherein the composition further comprises a pharmaceutically active agent.

16. The kit of claim 15, wherein the pharmaceutically active agent is an anti-hyperlipidemic agent.

17. The kit of claim 16, wherein the anti-hyperlipidemic agent is selected from the group consisting of HMG-CoA inhibitor, fibrate, bile acid sequestrant, ezetimibe, lomitapide, phytosterols, CETP antagonist, orlistat, dextrothyroxine sodium, icosapent, and any combination thereof.

18. The kit of claim 16, wherein the anti-hyperlipidemic agent comprises a HMC-CoA inhibitor selected from the group consisting of atorvastatin, fluvastatin, pravastatin, lovastatin, simvastatin, pitavastatin, cerivastatin, rosuvastatin, and lovastatin/niacin ER.

19. The kit of claim 16, wherein the anti-hyperlipidemic agent comprises simvastatin and ezetimibe.

20. The kit of claim 16, wherein the anti-hyperlipidemic agent comprises a fibrate selected from the group consisting of gemifibrozil, fenofibrate, fenofibric acid, clofibrate, and micronized fenofibrate.

21. The kit of claim 16, wherein the anti-hyperlipidemic agent comprises a bile acid sequestrant selected from the group consisting of colestipol, cholestyramine and colesevelam.

22. The kit of claim 1, wherein component (a) and (b) are provided in a single composition.

23. The kit of claim 1, wherein component (a) is provided in a separate composition from component (b).