Multi-vitamin and mineral nutritional supplements

• US 20050214383A1
• Filed: 03/28/2005
• Published: 09/29/2005
• Est. Priority Date: 03/29/2004
• Status: Abandoned Application

• Current Assignee: Wyeth LLC (Pfizer Inc.)
• Original Assignee: Wyeth LLC (Pfizer Inc.)
• Inventors: Sutton, Bruce W., Poxon, Scott W., Walters, Denise L., Herman, Paul W., Vernon, Jeffrey V., Williams, Michael G., Moreines, Judith, Bubnis, William, Wittenberg, Neil, Cotter, Richard
• Application Number:
  US11/090,486
• Publication Number:
  US 20050214383A1
• Time in Patent Office: Days
• US Class Current: 424/641
• CPC Class Codes: A23L 33/105 Plant extracts, their artificial duplicates or their derivatives
• CPC Class Codes: A23L 33/11 Plant sterols or derivatives thereof, e.g. phytosterols
• CPC Class Codes: A23L 33/15 Vitamins
• CPC Class Codes: A23L 33/16 Inorganic salts, minerals or trace elements
• CPC Class Codes: A23P 10/20 Agglomerating; Granulating; Tabletting
• 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 2250/1572 Boron
• CPC Class Codes: A23V 2250/1578 Calcium
• CPC Class Codes: A23V 2250/1588 Copper
• CPC Class Codes: A23V 2250/1592 Iron
• CPC Class Codes: A23V 2250/1598 Iodine
• CPC Class Codes: A23V 2250/1608 Molybdenum
• CPC Class Codes: A23V 2250/161 Magnesium
• CPC Class Codes: A23V 2250/1612 Manganese
• CPC Class Codes: A23V 2250/1618 Phosphorus
• CPC Class Codes: A23V 2250/1626 Selenium
• CPC Class Codes: A23V 2250/1628 Silicium
• CPC Class Codes: A23V 2250/163 Tin
• CPC Class Codes: A23V 2250/1636 Vanadium
• CPC Class Codes: A23V 2250/1642 : Zinc
• CPC Class Codes: A23V 2250/213 : Lycopene
• CPC Class Codes: A23V 2250/2136 : Phytosterols, phytostanols
• CPC Class Codes: A23V 2250/304 : Choline
• CPC Class Codes: A23V 2250/702 : Vitamin A
• CPC Class Codes: A23V 2250/7044 : Vitamin B2
• CPC Class Codes: A23V 2250/7046 : Vitamin B3 niacin
• CPC Class Codes: A23V 2250/705 : Vitamin B5 pantothenic acid
• CPC Class Codes: A23V 2250/7052 : Vitamin B6
• CPC Class Codes: A23V 2250/7056 : Vitamin B8 Folic acid
• CPC Class Codes: A23V 2250/706 : Vitamin B12
• CPC Class Codes: A23V 2250/708 : Vitamin C
• CPC Class Codes: A23V 2250/71 : Vitamin D
• CPC Class Codes: A23V 2250/712 : Vitamin E
• CPC Class Codes: A23V 2250/714 : Vitamin K
• CPC Class Codes: A23V 2250/72 : Biotin
• 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 31/352 : condensed with carbocyclic rings, e.g. methantheline cannabinoids A61K31/658
• CPC Class Codes: A61K 31/355 : Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 31/375 : Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/51 : Thiamines, e.g. vitamin B1
• CPC Class Codes: A61K 31/525 : Isoalloxazines, e.g. riboflavins, vitamin B2
• CPC Class Codes: A61K 31/56 : Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/575 : substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• CPC Class Codes: A61K 31/675 : having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
• CPC Class Codes: A61K 31/714 : Cobalamins, e.g. cyanocobalamin, i.e. vitamin B12
• CPC Class Codes: A61K 33/00 : Medicinal preparations containing inorganic active ingredients
• CPC Class Codes: A61K 45/06 : Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/10 : Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00
• CPC Class Codes: A61K 9/20 : Pills, tablets, discs, rods A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/284 : obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• CPC Class Codes: A61P 3/02 : Nutrients, e.g. vitamins, minerals
• CPC Class Codes: A61P 3/06 : Antihyperlipidemics

Abstract

The invention provides a nutritional supplement which includes micronutrients to facilitate reduction of cholesterol, and/or reduction of homocystein and/or reduction of low-density lipoprotein-cholesterol (LDL-C) oxidation in humans. In one embodiment the supplement is a multi-vitamin, a mineral supplement which includes at least one component known to reduce cholesterol. The invention further provides a method for tableting one fourth to one half of the daily effective dosage of a phytosterol containing nutritional supplement in a practical sized tablet and a method for reducing blood cholesterol in humans.

Claims

1. A nutritional supplement for administration to humans comprising:

an effective amount of at least one vitamin selected from the group consisting of Vitamin A;

Vitamin C;

Vitamin B₆;

Vitamin B₂;

folate;

Vitamin B₁₂;

Vitamin E; and

an effective amount of at least one cholesterol reducing agent selected from the group consisting of phytostanols;

phytosterols, policosanols, and statins.

8. The nutritional supplement of any of claims 1-7 further comprising a diluent.

9. The nutritional supplement of claim 8 wherein the diluent is selected from the group consisting of calcium compounds, magnesium compounds, microcrystalline cellulose, starch and a combination thereof.

10. The nutritional supplement of any of claims 1-9 further comprising an absorbent.

11. The nutritional supplement of claim 10 wherein the absorbent is silicon dioxide.

12. The nutritional supplement of claim 11 wherein the silicon dioxide is selected from the group consisting of fumed silicon dioxide, precipitated silicon dioxide and a mixture thereof.

13. A method of a nutritional supplementation for a human which facilitates reduction of blood cholesterol comprising providing a human an effective amount of the nutritional supplement of any one of claims 1-12.

24. The supplement of any of claims 1 to 12, wherein the supplement is in the form selected from a tablet, a caplet, a capsule, a chewable dosage unit or a sachet.

25. The supplement of claim 24, wherein the supplement is in the form of a tablet.

26. The supplement of claim 25, wherein the tablet is coated.

27. The supplement of claim 26, wherein the coating is a film coating.

28. The supplement of claim 27, wherein the film coat comprises polyvinyl alcohol.

29. A method of a nutritional supplementation for a human, wherein the supplementation lowers or reduces cholesterol, lowers or reduces homocystine levels or lowers or reduces low-density lipoprotein cholesterol oxidation comprising providing a human an effective amount of the nutritional supplement of any of claims 1-12.

30. The nutritional supplement of any of claims 1 to 12 wherein a daily efficacious amount of nutritional supplement comprises two tablets and wherein each of the two tablets has a volume less than about 2 cubic centimeters.

31. The nutritional supplement of any of claims 1 to 12 wherein a daily efficacious amount comprises four tablets or fewer and wherein each tablet has a volume less than 1.5 cubic centimeters.

32. The nutritional supplement of claims 30 and 31 wherein the tablets have an oblong, capsule, modified oval or oval shape.

33. The nutritional supplement of any of claims 30-32 wherein the tablets are coated with a film coating comprising polyvinyl alcohol.

2. A nutritional supplement for administration to humans comprising:

an effective amount of at least one mineral selected from the group consisting of selenium, chromium and zinc, and an effective amount of at least one cholesterol reducing agent selected from the group consisting of phytosterols, phytostanols, policosanols, and statins.

3. A nutritional and mineral supplement for administration to humans comprising:

an effective amount of Vitamin A;

an effective amount of Vitamin C;

an effective amount of Vitamin B₆;

an effective amount of Vitamin B₂;

an effective amount of folate;

an effective amount of Vitamin B₁₂;

an effective amount of Vitamin E; and

at least one cholesterol reducing agent selected from the group consisting of phytosterols, phytostanols, policosanols, and statins wherein the at least one cholesterol reducing agent is present in an amount effective to reduce cholesterol.

4. The composition of claim 3 further comprising at least one of an effective amount of lycopene and an effective amount of selenium.

5. A nutritional supplement for administration to humans, the supplement comprising:

at least about 800 mg of a phytosterol;

at least about 3500 I.U. of vitamin A and vitamin A precursors;

at least about 60 mg of Vitamin C;

at least about 400 I.U. of Vitamin D;

at least about 30 I.U. of vitamin E;

at least about 25 mcg of vitamin K;

at least about 1.5 mg of thiamin;

at least about 1.7 mg of vitamin B₂ (riboflavin);

at least about 20 mg of niacin;

at least about 5 mg of vitamin B₆;

at least about 800 mcg of folic acid;

at least about 200 mcg of vitamin B₁₂;

at least about 30 mcg of biotin;

at least about 10 mg of pantothenic acid;

at least about 6 mg of iron dosed in the form of a pharmaceutically acceptable iron compound;

at least about 150 mcg of iodine dosed in the form of a pharmaceutically acceptable iodine compound;

at least about 40 mg of magnesium dosed in the form of a pharmaceutically acceptable magnesium compound;

at least about 7.5 mg of zinc dosed in the form of a pharmaceutically acceptable zinc compound;

at least about 20 mcg of selenium dosed in the form of a pharmaceutically acceptable selenium compound;

at least about 0.7 mg of copper dosed in the form of a pharmaceutically acceptable copper compound;

at least about 2 mg of manganese dosed in the form of a pharmaceutically acceptable manganese compound;

at least about 108 mg calcium dosed in the form of a pharmaceutically acceptable calcium compound;

at least about 80 mg of phosphorus dosed in a pharmaceutically acceptable phosphorus compound;

at least about 75 mcg of molybdenum dosed in a pharmaceutically acceptable molybdenum compound;

at least about 32 mcg boron dosed in a pharmaceutically acceptable boron compound;

at least about 5 mcg nickel dosed in a pharmaceutically acceptable nickel compound;

at least about 2 mg silicon dosed in a pharmaceutically acceptable silicon compound;

at least about 10 mcg tin dosed in a pharmaceutically acceptable tin compound;

at least about 10 mcg vanadium dosed in a pharmaceutically acceptable vanadium compound;

at least about 120 mcg of chromium dosed in the form of a pharmaceutically acceptable chromium compound;

at least about 64 mg of potassium dosed in the form of a pharmaceutically acceptable potassium compound;

at least about 58 mg of chloride dosed in the form of a pharmaceutically acceptable chloride compound;

at least about 300 mcg of lycopene dosed in the form of a pharmaceutically acceptable lycopene compound; and

at least about 250 mcg lutein dosed in the form of a pharmaceutically acceptable lutein compound.

6. A nutritional supplement for administration to humans, the supplement comprising:

about 800 mg to about 3 g phytosterols;

about 1300 I.U. to about 12,000 I.U. of vitamin A;

about 45 mg to about 250 mg of vitamin C;

about 200 I.U. to about 2000 I.U. of vitamin D;

about 20 I.U. to about 200 I.U. of vitamin E;

about 10 mcg to about 90 mcg of vitamin K;

about 1.2 mg to about 4.5 mg of thiamin;

about 1.3 mg to about 5.1 mg of vitamin B₂ (riboflavin);

about 0 mg to about 550 mg of choline;

about 5 mg to about 40 mg of niacin;

about 1 mg to about 8 mg of vitamin B₆;

about 0 mcg to about 1400 mcg of folic acid;

about 2.4 mcg to about 400 mcg of vitamin B₁₂;

about 0 mcg to 300 mcg of biotin;

about 0 mg to about 16mg of pantothenic acid;

about 0 mg to about 18 mg of iron dosed in the form of a pharmaceutically acceptable iron compound;

about 0 mcg to about 300 mcg of iodine dosed in the form of a pharmaceutically acceptable iodine compound;

about 0 mg to about 100 mg of magnesium dosed in the form of a pharmaceutically acceptable magnesium compound;

about 3 mg to about 15 mg of zinc dosed in the form of a pharmaceutically acceptable zinc compound;

about 15 mcg to about 75 mcg of selenium dosed in the form of a pharmaceutically acceptable selenium compound;

about 0 mg to about 10 mg of copper dosed in the form of a pharmaceutically acceptable copper compound;

about 0 mg to about 6 mg of manganese dosed in the form of a pharmaceutically acceptable manganese compound;

about 0 mg to about 200 mg calcium dosed in the form of a pharmaceutically acceptable calcium compound;

about 0 mg to about 750 mg of phosphorus dosed in a pharmaceutically acceptable phosphorus compound;

about 0 mcg to about 250 mcg of molybdenum dosed in a pharmaceutically acceptable molybdenum compound;

about 0 mg to about 1.35 mg boron dosed in a pharmaceutically acceptable boron compound;

about 0 mcg to about 100 mcg nickel dosed in a pharmaceutically acceptable nickel compound;

about 0 mg to about 40 mg silicon dosed in a pharmaceutically acceptable silicon compound;

about 0 mcg to about 35 mcg tin dosed in a pharmaceutically acceptable tin compound;

about 6 mcg to about 25 mcg vanadium dosed in a pharmaceutically acceptable vanadium compound

about 0 mcg to about 300 mcg of chromium dosed in the form of a pharmaceutically acceptable chromium compound;

about 0 mg to about 125mg of potassium dosed in the form of a pharmaceutically acceptable potassium compound;

about 0 mg to about 120 mg of chloride dosed in the form of a pharmaceutically acceptable chloride compound;

about 0 g to about 3 g of omega-3 fatty acids;

about 0 g to about 3 g of lycopene dosed in the form of a pharmaceutically acceptable lycopene compound.;

about 0 g to about 3 g of zeaxanthin dosed in the form of a pharmaceutically acceptable zeaxanthin compound; and

about 0 g to about 3 g lutein dosed in the form of a pharmaceutically acceptable lutein compound.

7. A nutritional supplement for administration to humans, the supplement comprising:

up to about 3 g phytosterols or phytostanols,

up to about 20 mg of policosanol;

up to about 40 to 80 mg of statins;

up to about 10,000 I.U. of vitamin A and vitamin A precursors;

up to about 2 g of vitamin C;

up to about 2000 I.U. of vitamin D;

up to about 1500 I.U. of vitamin E;

up to about 1 mg of vitamin K;

up to about 100 mg of thiamin;

up to about 40 mg of vitamin B2 (riboflavin);

up to about 500 mg of niacin;

up to about 10 mg of vitamin B6;

up to about 1.5 mg of folic acid;

up to about 2 mg of vitamin B12;

up to about 900 mcg of biotin;

up to about 200 mg of pantothenic acid;

up to about 3500 mg of choline dosed in the form of a pharmaceutically acceptable choline compound;

up to about 18 mg of iron dosed in the form of a pharmaceutically acceptable iron compound;

up to about 1100 mcg of iodine dosed in the form of a pharmaceutically acceptable iodine compound;

up to about 400 mg of magnesium dosed in the form of a pharmaceutically acceptable magnesium compound;

up to about 40 mg of zinc dosed in the form of a pharmaceutically acceptable zinc compound;

up to about 400 mcg of selenium dosed in the form of a pharmaceutically acceptable selenium compound;

up to about 10 mg of copper dosed in the form of a pharmaceutically acceptable copper compound;

up to about 12 mg of manganese dosed in the form of a pharmaceutically acceptable manganese compound;

up to about 1500 mg calcium dosed in the form of a pharmaceutically acceptable calcium compound;

up to about 1250 mg of phosphorus dosed in a pharmaceutically acceptable phosphorus compound;

up to about 2000 mcg of molybdenum dosed in a pharmaceutically acceptable molybdenum compound;

up to about 20 mg boron dosed in a pharmaceutically acceptable boron compound;

up to about 1 mg nickel dosed in a pharmaceutically acceptable nickel compound;

up to about 500 mg silicon dosed in a pharmaceutically acceptable silicon compound;

up to about 200 mcg tin dosed in a pharmaceutically acceptable tin compound;

up to about 1.8 mg vanadium dosed in a pharmaceutically acceptable vanadium compound;

up to about 10 mg of chromium dosed in the form of a pharmaceutically acceptable chromium compound;

up to about 3900 mg of potassium dosed in the form of a pharmaceutically acceptable potassium compound;

up to about 150 mg of chloride dosed in the form of a pharmaceutically acceptable chloride compound;

up to about 6 g of omega-3 fatty acids;

up to about 6 g of lycopene dosed in the form of a pharmaceutically acceptable lycopene compound;

up to about 6 g of zeaxanthin dosed in the form of a pharmaceutically acceptable zeaxanthin compound; and

up to about 6 g lutein dosed in the form of a pharmaceutically acceptable lutein compound.

14. A method of making a granulation for use in tableting a nutritional supplement which comprises at least one phytosterol, the method comprising:

providing at least one phytosterol and at least one diluent;

granulating the phytosterol and the at least one diluent under high shear granulation conditions to form a granulation;

milling the granulation; and

adding an absorbent to the granulation,

and compressing the granulation to form a tablet.

15. The method of claim 14 is further comprising, adding at least one nutrient selected from the group consisting of vitamins and minerals and mixtures thereof.

16. The method of claim 14 further comprising drying the granulation.

17. The method of claim 16 wherein the drying is performed in a fluid bed dryer.

18. The method of claim 14 wherein is the diluent comprises at least one mineral.

19. The method of claim 14 wherein at least a portion of the diluent is selected from a calcium compound and a magnesium compound or a mixture thereof.

20. The method of claim 14 wherein the absorbent is silicon dioxide.

21. The method of claim 20 wherein the silicon dioxide is selected from fumed silicon dioxide, precipitated silicon dioxide and a mixtures thereof.

22. The method of claim 14 wherein once formed the tablet is coated.

23. The method of claim 22 wherein the tablet is coated with a film coat the film coat comprising polyvinyl alcohol.