Vitaminized compositions for treating hypercholesterolemia

• US 4,005,196 A
• Filed: 02/12/1976
• Issued: 01/25/1977
• Est. Priority Date: 02/12/1976
• Status: Expired

• Current Assignee: The Procter & Gamble Company
• Original Assignee: The Procter & Gamble Company
• Inventors: Jandacek, Ronald James, Mattson, Fred Hugh
• Primary Examiner(s): Rosen, Sam
• Application Number:
  US05/657,529
• Time in Patent Office: 348 Days
• Field of Search: 424/180, 424/312, 424/343, 424/236, 424/344, 424/284, 424/331, 426/658
• US Class Current: 514/23
• CPC Class Codes: A23D 9/013 Other fatty acid esters, e.g. phosphatides
• CPC Class Codes: A23L 33/26 Polyol polyesters, e.g. sucrose polyesters; Synthetic sugar polymers, e.g. polydextrose
• 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: A61K 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

Abstract

Anti-anal leakage agents are used in combination with vitamin-fortified liquid fatty acid polyester compositions to provide pharmaceutical and food compositions for treating and/or preventing hypercholesterolemia while avoiding undesired anal leakage of the polyesters.

Claims

1. A composition of matter, comprising

a. an edible, non-absorbable, non-digestible liquid 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;

b. sufficient anti-anal leakage agent to prevent leakage of said liquid polyester through the anal sphincter; and

c. sufficient fat-soluble vitamin selected from the group consisting of vitamin A, vitamin D, vitamin E and vitamin K 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 liquid polyol fatty acid polyester contains no more than about 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 the hexaoleate, heptaoleate and octaoleate of sucrose, and mixtures thereof.

7. A composition according to claim 1 wherein the anti-anal leakage agent is a member selected from the group consisting of:

edible C₁₂ and higher saturated fatty acids, and their edible salts;

edible, digestible sources of C₁₂ and higher saturated fatty acids;

edible, non-absorbable, non-digestible solid polyol fatty acid polyesters 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

edible, non-digestible esters of alpha-branched chain C₁₀ -C₁₈ fatty acids.

8. A composition according to claim 7 which comprises at least about 10% by weight of the anti-anal leakage agent.

9. A composition according to claim 7 which comprises at least about 20% by weight of the anti-anal leakage agent.

10. A composition according to claim 7 which comprises from about 20% to about 50% by weight of the anti-anal leakage agent.

11. A composition according to claim 7 which comprises from about 10% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible C₁₂ -C₂₄ saturated fatty acids and edible salts of C₁₂ -C₂₄ saturated fatty acids.

12. A composition according to claim 7 which comprises from about 10% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible, digestible sources of C₁₂ -C₂₄ saturated fatty acids, and mixtures thereof.

13. A composition according to claim 12 wherein the anti-anal leakage agent is a lower alkyl ester of C₁₂ -C₂₄ saturated fatty acids, or mixtures thereof.

14. A composition according to claim 12 wherein the anti-anal leakage agent comprises substantially saturated triglyceride esters of C₁₂ -C₂₄ fatty acids, or mixtures thereof.

15. A composition according to claim 14 wherein the anti-anal leakage agent is hydrogenated palm oil.

16. A composition according to claim 14 wherein the anti-anal leakage agent is natural or synthetic cocoa butter.

17. A composition according to claim 14 wherein the anti-anal leakage agent is an edible position-specific trigylceride selected from the group consisting of:

the 1-stearoyl, 1-palmitoyl, 1-arachidoyl and 1-behenoyl 2,3-dioleins;

the 2-oleoyl 1,3-distearins, 1,3-dipalmitins, 1,3-diarachidins and 1,3-dibehenins;

1-oleoyl distearin;

1-palmitoyl distearin;

1-arachidoyl distearin; and

1-behenoyl distearin; and

mixtures thereof.

18. A composition according to claim 17 which comprises from about 20% to about 40% by weight of the position-specific triglyceride.

19. A composition according to claim 7 which comprises from about 20% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible, non-absorbable, non-digestible solid polyol fatty acid polyesters 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.

20. A composition according to claim 19 wherein the anti-anal leakage agent is selected from the group consisting of C₁₀ -C₂₂ saturated fatty acid polyol esters.

21. A composition according to claim 1 which comprises from about 50% to about 90% by weight of the non-absorbable, non-digestible liquid polyol fatty acid polyester, at least about 10% by weight of the anti-anal leakage agent, 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.

22. A method for inhibiting the absorption of cholesterol without decreasing the body'"'"'s stores of fat-soluble vitamins or causing an anal leakage effect comprising systemically administering to an animal susceptible to or afflicted with hypercholesterolemia successive therapeutically effective doses of a composition comprising a non-absorbable, non-digestible liquid 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;

sufficient anti-anal leakage agent to prevent leakage of said liquid polyester through the anal sphincter; and

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

23. A method according to claim 22 wherein the anti-anal leakage agent is a member selected from the group consisting of:

edible C₁₂ -C₂₄ saturated fatty acids, and their edible salts;

edible, digestible sources of C₁₂ -C₂₄ saturated fatty acids;

edible, nonabsorbable, non-digestible solid polyol fatty acid polyesters 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

edible, non-digestible esters of alpha-branched chain C₁₀ -C₁₈ fatty acids.

24. A method according to claim 23 wherein the composition comprises at least about 10% by weight of the anti-anal leakage agent.

25. A method according to claim 23 wherein the composition comprises at least about 20% by weight of the anti-anal leakage agent.

26. 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. a portion comprising an edible, non-absorbable, non-digestible liquid 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

b. sufficient anti-anal leakage agent to prevent leakage of said liquid polyester through the anal sphincter,

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.

27. A composition according to claim 26 wherein the liquid polyol fatty acid polyester contains no more than about 2 free hydroxyl groups.

28. A composition according to claim 27 wherein the fatty acid ester groups contain from about 14 to about 18 carbon atoms.

29. A composition according to claim 28 wherein the polyol is a member selected from the group consisting of erythritol, xylitol, sorbitol, glucose and sucrose.

30. A composition according to claim 29 wherein the polyol is sucrose.

31. A composition according to claim 30 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.

32. A composition according to claim 31 wherein the anti-anal leakage agent is a member selected from the group consisting of:

edible C₁₂ and higher saturated fatty acids, and their edible salts;

edible, digestible sources of C₁₂ and higher saturated fatty acids;

edible, non-absorbable, non-digestible solid polyol fatty acid polyesters 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

edible, non-digestible esters of alpha-branched chain C₁₀ -C₁₈ fatty acids.

33. A composition according to claim 26 wherein the liquid polyester portion of the fat ingredients comprises at least about 10% by weight of the anti-anal leakage agent.

34. A composition according to claim 33 wherein the liquid polyester portion of the fat ingredients comprises at least about 20% by weight of the anti-anal leakge agent.

35. A composition according to claim 34 wherein the liquid polyester portion of the fat ingredients comprises from about 20% to about 50% by weight of the anti-anal leakage agent.

36. A composition according to claim 32 wherein the liquid polyester portion of the fat ingredients comprises from about 10% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible, digestible C₁₂ -C₂₄ fatty acids and edible salts of C₁₂ -C₂₄ fatty acids.

37. A composition according to claim 32 wherein the liquid polyester portion of the fat ingredients comprises from about 10% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible, digestible sources of C₁₂ -C₂₄ saturated fatty acids, and mixtures thereof.

38. A composition according to claim 37 wherein the anti-anal leakage agent is a lower alkyl ester of C₁₂ -C₂₄ saturated fatty acids, or mixtures thereof.

39. A composition according to claim 37 wherein the anti-anal leakage agent comprises substantially saturated triglyceride esters of C₁₂ -C₂₄ fatty acids, or mixtures thereof.

40. A composition according to claim 39 wherein the anti-anal leakge agent is hydrogenated palm oil.

41. A composition according to claim 39 wherein the anti-anal leakage agent is natural or synthetic cocoa butter.

42. A composition according to claim 39 wherein the anti-anal leakage agent is an edible position-specific triglyceride selected from the group consisting of:

the 1-stearoyl, 1-palmitoyl, 1-arachidoyl and 1-behenoyl 2,3-dioleins;

the 2-oleoyl 1,3-distearins, 1,3-dipalmitins, 1,3-diarachidins and 1,3-dibehenins;

1-oleoyl distearin;

1-palmitoyl distearin;

1-arachidoyl distearin; and

1-behenoyl distearin; and

mixtures thereof.

43. A composition according to claim 42 wherein the liquid polyester portion of the fat ingredients comprises from about 20% to about 40% by weight of the position-specific triglyceride.

44. A composition according to claim 32 wherein the liquid polyester portion of the fat ingredients comprises from about 20% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible, non-absorbable, non-digestible solid polyol fatty acid polyesters 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.

45. A composition according to claim 44 wherein the anti-anal leakage agent is selected from the group consisting of C₁₀ -C₂₂ saturated fatty acid polyol esters.

46. A pharmaceutical composition in effective unit dosage amounts for inhibiting the absorption of cholesterol without causing an anal leakage effect or interfering with the body'"'"'s stores of fat-soluble vitamins, comprising:

a. from about 0.1 gram to about 5 grams of an edible, non-absorbable, non-digestible liquid 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;

b. sufficient anti-anal leakage agent to prevent leakage of said liquid polyester through the anal sphincter; and

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

47. A composition according to claim 46 wherein the liquid polyol fatty acid polyester contains no more than about 2 free hydroxyl groups.

48. A composition according to claim 47 wherein the fatty acid ester groups contain from about 14 to about 18 carbon atoms.

49. A composition according to claim 48 wherein the polyol is a member selected from the group consisting of erythritol, xylitol, sorbitol, glucose and sucrose.

50. A composition according to claim 49 wherein the polyol is sucrose.

51. A composition according to claim 50 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.

52. A composition according to claim 46 wherein the anti-anal leakage agent is a member selected from the group consisting of:

edible C₁₂ and higher saturated fatty acids, and their edible salts;

edible, digestible sources of C₁₂ and higher saturated fatty acids;

edible, non-absorbable, non-digestible solid polyol fatty acid polyesters 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

edible, non-digestible esters of alpha-branched chain C₁₀ -C₁₈ fatty acids.

53. A composition according to claim 52 which comprises at least about 10% by weight of the anti-anal leakage agent.

54. A composition according to claim 52 which comprises at least about 20% by weight of the anti-anal leakage agent.

55. A composition according to claim 52 which comprises from about 20% to about 50% by weight of the anti-anal leakage agent.

56. A composition according to claim 52 which comprises from about 10% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible C₁₂ -C₂₄ saturated fatty acids and edible salts of C₁₂ -C₂₄ fatty acids.

57. A composition according to claim 52 which comprises from about 10% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible, digestible sources of C₁₂ -C₂₄ saturated fatty acids, and mixtures thereof.

58. A composition according to claim 57 wherein the anti-anal leakage agent is a lower alkyl ester of C₁₂ -C₂₄ saturated fatty acids, or mixtures thereof.

59. A composition according to claim 57 wherein the anti-anal leakage agent comprises substantially saturated triglyceride esters of C₁₂ -C₂₄ fatty acids, or mixtures thereof.

60. A composition according to claim 59 wherein the anti-anal leakage agent is hydrogenated palm oil.

61. A composition according to claim 59 wherein the anti-anal leakage agent is natural or synthetic cocoa butter.

62. A composition according to claim 59 wherein the anti-anal leakage agent is an edible position-specific triglyceride selected from the group consisting of:

the 1-stearoly, 1-palmitoyl, 1-arachidoyl and 1-benhenoyl 2,3-dioleins;

the 2-oleoyl 1,3-distearins, 1,3-dipalmitins, 1,3-diarachidins and 1,3-dibehenins;

1-oleoyl distearin;

1-palmitoyl distearin;

1-arachidoyl distearin; and

1-behenoyl distearin; and

mixtures thereof.

63. A composition according to claim 62 which comprises from about 20% to about 40% by weight of the position-specific triglyceride.

64. A composition according to claim 52 which comprises from about 20% to about 50% by weight of an anti-anal leakage agent selected from the group consisting of edible, non-absorbable, non-digestible solid polyol fatty acid polyesters 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.

65. A composition according to claim 64 wherein the anti-anal leakage agent is selected from the group consisting of C₁₀ -C₂₂ saturated fatty acid polyol esters.

66. A composition in accordance with claim 46 which contains at least about 0.1 RDA of a vitamin selected from the group consisting of vitamin A, vitamin D, vitamin E, vitamin K, and mixtures of said vitamins.