Formulation of fat-soluble vitamin

Patent metadata

Field	Value
Publication number	US-11090276-B2
Application number	US-201515308926-A
Country	US
Kind code	B2
Filing date	May 5, 2015
Priority date	May 5, 2014
Publication date	Aug 17, 2021
Grant date	Aug 17, 2021

Abstract

The invention relates to a composition comprising A) microcapsules comprising at least one fat-soluble active substance selected from a vitamin K compound or a provitamin or a prodrug of a vitamin K compound embedded in a matrix comprising a hydrocolloid and optionally one or more other matrix components, and B) at least one dietary mineral; as well as uses and products comprising such compositions.

First claim

The invention claimed is:

1. A composition comprising:
A) a first component being microcapsules consisting of at least one fat-soluble active substance selected from a vitamin K compound or a provitamin or a prodrug of a vitamin K compound embedded in a matrix comprising a hydrocolloid and optionally one or more other matrix components; and
B) a separate second component being at least one dietary mineral, wherein the dietary mineral is selected from a calcium salt, a magnesium salt, calcium carbonate or magnesium oxide.

2. The composition according to claim 1 , wherein said at least one fat-soluble active substance is vitamin K1, vitamin K2, provitamins and prodrugs of vitamin K1 or vitamin K2, MK-6, MK-7, MK-8, or a mixture thereof.

3. The composition according to claim 1 , wherein the content of said active substance is from 0.01 to 15%, 0.1 to 10%, 0.2 to 5%, or 1 to 3% of the total weight of the microcapsules.

4. The composition according to claim 1 , wherein the content of said microcapsules is from 0.001 to 15%, 0.01 to 10%, or 0.1 to 6% of the total weight of the composition.

5. The composition according to claim 1 , wherein the content of said at least one dietary mineral is at least 10%, at least 20%, or at least 30% of the total weight of the composition.

6. The composition according to claim 1 , further comprising one or more additional active substances selected from the group consisting of vitamin D2, vitamin D3, vitamin E, vitamin E-acetate, vitamin A, a monounsaturated fatty acid, a polyunsaturated fatty acid (PUFA), a PUFA oil, β-carotene, zeaxanthin, lycopene, lutein and Q10.

7. The composition according to claim 1 , wherein said microcapsules comprise vitamin K2 in the MK-7 form as the at least one fat-soluble active substance, and wherein said at least one dietary mineral is calcium carbonate or magnesium oxide.

8. The composition according to claim 1 , wherein said microcapsules comprise vitamin K1 as the at least one fat-soluble active substance, and wherein said at least one dietary mineral is calcium carbonate or magnesium oxide.

9. A unit dosage form comprising the composition according to claim 1 , wherein the content of said active substance is from 10 to 500 μg, 25 to 250 μg, or 50 to 200 μg, and wherein the content of said at least one dietary mineral is at least 10%, at least 20%, or at least 30% of the total weight of the dosage form.

10. The unit dosage form according to claim 9 which is a daily unit dosage form.

11. A process for preparing the unit dosage form according to claim 9 in the form of a tablet, comprising:
a) blending microcapsules comprising at least one fat-soluble active substance selected from a vitamin K compound or a provitamin or a prodrug of a vitamin K compound embedded in a matrix comprising a hydrocolloid and optionally one or more other matrix components in an amount of from 10 to 500 μg with at least 10% by weight of the total weight of the dosage form of at least one dietary mineral; and
b) compressing the resulting blend to form a tablet.

12. The composition according to claim 1 , wherein said hydrocolloid is an acacia gum, a protein or a starch.

13. The composition according to claim 1 , wherein said matrix further contains antioxidants and/or carbohydrates.

14. A product comprising the composition according to claim 1 .

15. The product according to claim 14 , which is a food, a food supplement, a beverage, a pharmaceutical or veterinary product, a feed or feed supplement, a personal care product, or a household product.

16. The product according to claim 14 , which is a nutraceutical or pharmaceutical product for oral administration.

17. The product according to claim 14 for use:
a) in the treatment of a condition associated with vitamin K deficiencies;
b) in the treatment of osteoporosis;
c) in the treatment of conditions of the cardiovascular system;
d) in the treatment of arteriosclerosis; or
e) in assisting blood clotting.

18. A method of treating a condition associated with vitamin K1 or K2, comprising administering to a patient in need thereof an effective amount of the composition according to claim 1 .

Assignees

• Basf Se

Inventors

• Aukrust Inger Reidun
• Larsson Helena M
• Rove Thomas

Classifications

• A61K9/1623

  Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules · CPC title

• A61K9/2077

  Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets · CPC title

• A61K31/593

  9,10-Secocholestane derivatives, e.g. cholecalciferol, i.e. vitamin D3 · CPC title

• A61K31/592

  9,10-Secoergostane derivatives, e.g. ergocalciferol, i.e. vitamin D2 · CPC title

• A61K33/08

  Oxides; Hydroxides · CPC title