Compositions for inhibiting absorption of cholesterol

• US 4,034,083 A
• Filed: 11/03/1975
• Issued: 07/05/1977
• Est. Priority Date: 11/03/1975
• Status: Expired

• Current Assignee: The Procter & Gamble Company
• Original Assignee: The Procter & Gamble Company
• Inventors: Mattson, Fred Hugh
• Primary Examiner(s): Rosen, Sam
• Application Number:
  US05/628,265
• Time in Patent Office: 610 Days
• Field of Search: 424/180, 424/312, 424/311, 424/236, 424/237, 424/284, 424/331, 424/344
• US Class Current: 514/53
• CPC Class Codes: A61K 31/07 Retinol compounds, e.g. vitamin A retinoic acids A61K31/203
• CPC Class Codes: A61K 31/12 Ketones
• CPC Class Codes: A61K 31/23 of acids having a carboxyl group bound to a chain of seven or more carbon atoms
• CPC Class Codes: A61K 31/355 Tocopherols, e.g. vitamin E
• CPC Class Codes: A61K 31/59 Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
• CPC Class Codes: A61K 31/70 Carbohydrates; Sugars; Derivatives thereof sorbitol A61K31/047
• CPC Class Codes: A61K 31/715 Polysaccharides, i.e. having more than five saccharide radicals attached to each other by glycosidic linkages; Derivatives thereof, e.g. ethers, esters
• CPC Class Codes: A61P 3/06 Antihyperlipidemics

Abstract

Polyol fatty acid polyesters having at least four fatty acid ester groups are fortified with fat-soluble vitamins and used in pharmaceutical compositions for treating and/or preventing hypercholesterolemia in animals, especially humans, and in low-calorie foods.

Claims

1. A composition of matter, comprising:

a non-absorbable, non-digestible polyol fatty acid polyester having at least 4 fatty acid ester groups, wherein the polyol is selected from the group consisting of sugars and sugar alcohols containing from 4 to 8 hydroxyl groups and wherein each fatty acid group has from about 8 to about 22 carbon atoms; and

sufficient fat-soluble vitamin selected from the group consisting of vitamin A, vitamin D, vitamin E and vitamin K, or mixtures thereof, to prevent abnormally low levels of any of said fat-soluble vitamins in animals ingesting said composition.

2. A composition according to claim 1 wherein the polyol fatty acid polyester contains no more than 2 free hydroxyl groups.

3. A composition according to claim 2 wherein the fatty acid ester groups contain from about 14 to about 18 carbon atoms.

4. A composition according to claim 3 wherein the polyol is a member selected from the group consisting of erythritol, xylitol, sorbitol, glucose and sucrose.

5. A composition according to claim 4 wherein the polyol is sucrose.

6. A composition according to claim 5 wherein the sucrose fatty acid polyester is a member selected from the group consisting of C₁₄, C₁₆ and C₁₈ hexa-, hepta-, and octa-esters, and mixtures thereof.

7. A composition according to claim 6 wherein the sucrose fatty acid polyester is a member selected from the group consisting of the hexaoleate, heptaoleate and octaoleate of sucrose, and mixtures thereof.

8. A composition according to claim 1 which comprises from about 98% to about 99.999% by weight of the non-absorbable, non-digestible polyol fatty acid polyester and from about 0.001% to about 2% by weight of a vitamin selected from the group consisting of vitamin A, vitamin D, vitamin E, vitamin K, and mixtures thereof.

9. A pharmaceutical composition in effective unit dosage amounts for inhibiting the absorption of cholesterol without interfering with the body'"'"'s stores of fat-soluble vitamins, comprising:

from about 0.1 gram to about 5 grams of a non-absorbable, non-digestible polyol fatty acid polyester having at least 4 fatty acid ester groups, wherein the polyol is selected from the group consisting of sugars and sugar alcohols containing from 4 to 8 hydroxyl groups and wherein each fatty acid group has from about 8 to about 22 carbon atoms; and

sufficient fat-soluble vitamin selected from the group consisting of vitamin A, vitamin D, vitamin E and vitamin K, or mixtures thereof, to prevent abnormally low levels of any of said fat-soluble vitamins in humans ingesting said composition.

10. A composition according to claim 9 wherein the polyol fatty acid polyester contains no more than 2 free hydroxyl groups.

11. A composition according to claim 10 wherein the fatty acid ester groups contain from about 14 to about 18 carbon atoms.

12. A composition according to claim 11 wherein the polyol is a member selected from the group consisting of erythritol, xylitol, sorbitol, glucose and sucrose.

13. A composition according to claim 12 wherein the polyol is sucrose.

14. A composition according to claim 13 wherein the sucrose fatty acid polyester is a member selected from the group consisting of C₁₄, C₁₆ and C₁₈ hexa-, hepta-, and octa-esters, and mixtures thereof.

15. A composition according to claim 14 wherein the sucrose fatty acid polyester is a member selected from the group consisting of the hexaoleate, heptaoleate and octaoleate of sucrose, and mixtures thereof.

16. A low calorie fat-containing food composition comprising non-fat ingredients and fat ingredients wherein from about 10% to about 100% of the total fat ingredients comprise a non-absorbable, non-digestible polyol fatty acid polyester having at least 4 fatty acid ester groups, wherein the polyol is selected from the group consisting of sugars and sugar alcohols containing from 4 to 8 hydroxyl groups and wherein each fatty acid group has from about 8 to about 22 carbon atoms, said food composition being fortified with sufficient fat-soluble vitamin selected from the group consisting of vitamin A, vitamin D, vitamin E and vitamin K, or mixtures thereof, over and above that naturally present in said food composition, to prevent abnormally low levels of any of said fat-soluble vitamins in animals ingesting said composition.

17. A composition according to claim 16 wherein the polyol fatty acid polyester contains no more than 2 free hydroxyl groups.

18. A composition according to claim 17 wherein the fatty acid ester groups contain from about 14 to about 18 carbon atoms.

19. A composition according to claim 18 wherein the polyol is a member selected from the group consisting of erythritol, xylitol, sorbitol, glucose and sucrose.

20. A composition according to claim 19 wherein the polyol is sucrose.

21. A composition according to claim 20 wherein the sucrose fatty acid polyester is a member selected from the group consisting of C₁₄, C₁₆ and C₁₈ hexa-, hepta-, and octa-esters, and mixtures thereof.

22. A composition according to claim 21 wherein the sucrose fatty acid polyester is a member selected from the group consisting of the hexaoleate, heptaoleate and octaoleate of sucrose, and mixtures thereof.

23. A method for inhibiting the absorption of cholesterol without decreasing the body'"'"'s stores of fat-soluble vitamins comprising systemically administering to an animal susceptible to or afflicted with hypercholesterolemia successive therapeutically effective doses of a non-absorbable and non-digestible polyol fatty acid polyester having at least 4 fatty acid ester groups, wherein the polyol is selected from the group consisting of sugars and sugar alcohols containing from 4 to 8 hydroxyl groups and wherein each fatty acid group has from about 8 to about 22 carbon atoms and sufficient fat-soluble vitamin to prevent abnormally low levels of said vitamin from developing in said animal.