Vitamin formulation for cardiovascular health

• US 6,914,073 B2
• Filed: 01/14/2002
• Issued: 07/05/2005
• Est. Priority Date: 03/18/1999
• Status: Expired due to Fees

• Current Assignee: Bristol-Myers Squibb Company
• Original Assignee: Bristol-Myers Squibb Company
• Inventors: Desai, Jatin, Stillman, Robert, Martin, Neil, Boulos, Atef, Udwin, Marion
• Primary Examiner(s): Clardy, S. Mark
• Assistant Examiner(s): CHOI, FRANK I
• Application Number:
  US10/047,583
• Publication Number:
  US 20020172721A1
• Time in Patent Office: 1,268 Days
• Field of Search: 424/465, 424/469, 424/489, 424/490, 424/600, 424/464, 514/458, 514/769, 514/770, 514/781, 514/904, 514/905, 514/960, 514/961, 514/964, 514/965
• US Class Current: 514/458
• CPC Class Codes: A23L 33/15 Vitamins
• CPC Class Codes: A23V 2002/00 Food compositions, function of food ingredients or processes for food or foodstuffs
• CPC Class Codes: A23V 2200/224 Encapsulating agent
• CPC Class Codes: A23V 2250/156 Mineral combination undefined extract A23V2250/1638
• CPC Class Codes: A23V 2250/1578 Calcium
• CPC Class Codes: A23V 2250/161 Magnesium
• CPC Class Codes: A23V 2250/1628 Silicium
• CPC Class Codes: A23V 2250/1886 Stearic acid
• CPC Class Codes: A23V 2250/211 Carotene, carotenoids
• CPC Class Codes: A23V 2250/51084 Crystalline, microcrystalline cellulose
• 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 2250/712 Vitamin E
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 9/2009 Inorganic compounds
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system

Abstract

The invention concerns a composition containing a high level of Vitamin E in encapsulated form, preferably as beadlets or spray dried, and a high level of silicates. The composition is compressible into tablets or caplets that do not leach out Vitamin E into the tablet matrix during compression and/or storage. The composition preferably contains vitamins and minerals in doses optimized for cardiovascular health.

Claims

1. A composition comprising:

(i) an amount of encapsulated Vitamin E such that when the composition is divided into unit doses each unit dose contains at least 100 International Units Vitamin E,

(ii) from about 0.5% to about 10% by weight based on total weight of the composition, of precipitated silica,

(iii) from about 1% to about 10% by weight, based on total weight of the composition, of calcium silicate,

(iv) from about 5% to about 50% by weight, based on total weight of the composition, of microcrystalline cellulose,

(v) from 0 to about 5% by weight, based on total weight of the composition, of talc; and

(vi) an amount of vitamins in addition to Vitamin E and an amount of additional minerals;

wherein the precipitated silica and the calcium silicate is present in a total amount of over 4% by weight, based on total weight of the composition;

the encapsulated Vitamin E and the total amount of silica and calcium silicate is present in a ratio of from 3;

1 to 6;

1; and

the composition is compressible into stable tablet or caplet unit doses containing the encapsulated Vitamin E in the matrix of said tablet or caplet in which no Vitamin E leaches out of encapsulated Vitamin E into the tablet or caplet matrix when the tablet or caplet is stored at room temperature for a period of at least twelve months from the date of manufacture of the tablet or caplet or when stored for three months at 40°

C. and a relative humidity of 75%.

2. The composition, as claimed in claim 1, wherein each unit dose contains at least 200 International Units Vitamin E.

3. The composition, as claimed in claim 1, wherein the total amount of precipitated silica and calcium silicate is at least about 5%.

4. The composition, as claimed in claim 1, wherein the total amount of precipitated silica and calcium silicate is from about 5% to about 8%.

5. The composition, as claimed in claim 1, wherein the calcium silicate is present in an amount of about 4.5% and the precipitated silica is present in an amount of about 4%.

6. The composition, as claimed in claim 1, wherein the talc is present in an amount of from about 1% to about 5%.

7. The composition, as claimed in claim 1, wherein the proportion of encapsulated Vitamin E:

precipitated silica;

calcium silicate is 2-50;

1-10;

1-10.

8. The composition, as claimed in claim 1, wherein the microcrystalline cellulose is present in an amount of about 30%.

9. The composition, as claimed in claim 1, wherein the encapsulated Vitamin E is Vitamin E acetate beadlets.

10. The composition, as claimed in claim 1, wherein the encapsulated Vitamin E is spray dried Vitamin E.

11. The composition, as claimed in claim 1, wherein the additional minerals and vitamins are selected from Folic Acid, iron, lycopene, β

-carotene, β

-cryptoxanthin, lutein, α

-carotene, zeaxanthin, Vitamin B₆ Vitamin B₁₂, Magnesium, Vitamin C, Selenium, Vitamin K, Vitamin A, Vitamin D, Thiamin, Riboflavin, Niacin, Biotin, Pantothenic Acid, Calcium, Chromium, Copper, Manganese, Molybdenum, Zinc, Boron, Chloride, Iodine, Nickel, Phosphorous, Potassium, Silicon, Tin, Vanadium, and mixtures thereof.

12. A method of providing a cardiovascular benefit to a human comprising orally administering to said human a daily dose of one or more stable tablets or caplets prepared by compressing the composition of claim 1, said Vitamin E, additional minerals and vitamins being present in amounts effective to decrease homocysteine level in said human, and wherein each unit does contains at least 100 International Units Vitamin E.