LIQUID COMPOSITION CONTAINING A COMBINATION OF VITAMINS A, D, E AND K IN A LIQUID MATRIX

Abstract

The present invention relates to a liquid composition containing a combination of vitamins A, D, E and K or a suitable provitamin thereof in a liquid matrix, where the total amount of said vitamins and provitamins is at least 0.2% by weight of the total compositions. The invention further relates to the use of this vitamin formulation in the treatment of an existing or impending vitamin deficiency condition concerning at least one of vitamin A, D, E or K, in particular due to vitamin maldigestion. The present invention also relates to formulations for dietary purposes, cosmetic purposes or medical purposes, in particular to dosage forms for oral administration, to formulations for parenteral administration and to topical formulations. The present invention further relates to the use of the compositions for dietary purposes, including e.g. food supplementation and food for special purposes, such as a balanced diet. The present invention further relates to the use of the compositions for medical purposes and for cosmetic purposes.

Claims

1. A liquid composition containing the following components a) to h): a) at least one of vitamin A and esters of vitamin A; b) at least one of vitamin D and provitamin D; c) at least one of vitamin E and esters of vitamin E; d) at least one of vitamin K and provitamin K; e) 40 to 95% by weight, based on the total weight of the liquid composition, of at least one water miscible polyol; f) 1 to 40% by weight, based on the total weight of the liquid composition, of at least one edible triglyceride; g) 3 to 30% by weight, based on the total weight of the liquid composition, water; and h) 0.5 to 10% by weight, based on the total weight of the liquid composition, of a phospholipid composition containing phosphatidylcholine; wherein the total amount of components a) to d) is at least 0.3% by weight, based on the total weight of the liquid composition.

2. The liquid composition of claim 1 which is translucent.

3. The liquid composition of any one of the preceding claims, wherein the total amount of components a) to d) is in the range of 0.2 to 20% by weight, based on the total weight of the composition.

4. The liquid composition of any one of the preceding claims, where the concentrations of components a) to d) are as follows: a) 0.001 to 0.4% by weight, based on the total weight of the liquid composition, of component a), b) 0.00005 to 0.3% by weight, based on the total weight of the liquid composition, of component b), c) 0.1 to 19% by weight, based on the total weight of the liquid composition, of component c), d) 0.001 to 0.4% by weight, based on the total weight of the liquid composition, of component d); where the total concentration of components a), b), c) and d) is range of 0.2 to 20% by weight, based on the total weight of the composition.

5. The liquid composition of any one of the preceding claims further containing at least one carotenoid and/or an ester thereof as a component i).

6. The liquid composition of claim 5, wherein the carotenoid comprises -carotene.

7. The liquid composition of any one of claim 5 or 6, wherein the concentration of the carotenoid in the liquid composition is in the range of 0.01 to 10% by weight, in particular in the range of 0.02 to 5% by weight, based on the total weight of the liquid composition.

8. The liquid composition of any one of the preceding claims, wherein the components a), b) c) and d) and optionally the component i) is essentially present in dissolved form.

9. The liquid composition of any one of the preceding claims further containing a zinc salt, which is suitable for nutritional or dietary purposes or pharmaceutically acceptable.

10. The liquid composition of claim 9, wherein the zinc salt is selected from zinc sulfate, zinc gluconate, zinc bisglycinate, zinc acetate, zinc hydroxide carbonate, zinc lactate, zinc ascorbate, in particular zinc L-ascorbate, zinc hydrogen ascorbate, zinc aspartate, zinc hydrogen aspartate, such as zinc DL-hydrogen aspartate or zinc L-hydrogen aspartate, zinc citrate, zinc oxide, zinc stearate, zinc orotate, zinc picolinate and the hydrates thereof.

11. The liquid composition of any one of claim 9 or 10, wherein the concentration of the zinc salt in the liquid composition is in the range of 0.01 to 0.2% by weight, based on the total weight of the liquid composition and calculated as elemental zinc.

12. The liquid composition of any one of the preceding claims, wherein the weight ratio of the phosphatidylcholine to the triglyceride is in the range of 1:20 to 1:1.

13. The liquid composition of any one of the preceding claims, wherein the triglyceride is selected from the group consisting of oils of seed-oil plants, MCT oils, LCT oils and oils of marine organisms and combinations thereof, and where the triglyceride comprises a medium chain triglyceride as a main constituent.

14. The liquid composition of any one of the preceding claims, which has at least one of the following features a) to d), wherein a) the weight ratio of component f) to the total weight of components a), b) c) and d) and optionally the component i) is in the range of 1:1 to 100:1, in particular in the range of 2:1 to 50:1; b) the phospholipid composition contains phosphatidylcholine in an amount of at least 45% by weight, based on the total weight of the phospholipid composition; c) the liquid composition is characterized in that a dilution of the liquid composition in deionized water at 25 C. and at a concentration of 1% by weight forms droplets having a Z average particle diameter of at most 500 nm, as determined by dynamic light scattering; d) the liquid composition additionally contains a water-soluble organic anti-oxidant, which is in particular ascorbic acid or sodium ascorbate.

15. A method for producing a liquid composition of any one of the preceding claims, which comprises e) mixing the components of the liquid composition and f) homogenizing the mixture obtained in step a).

16. A formulation comprising a liquid composition according to any one of claims 1 to 14 and a carrier or vehicle, which is a formulation for topical administration or for oral administration.

17. A composition according to any one of claims 1 to 14 for use in the treatment of an existing or impending vitamin deficiency condition concerning at least one of vitamin A, D, E or K.

18. The composition of any one of claims 1 to 14 for use in a medical co-treatment of a disease with a therapeutic agent different from vitamin A, D, E and K, where the disease or the treatment with the therapeutic agents causes or may cause vitamin deficiency condition concerning at least one of vitamin A, D, E or K.

19. The use of a composition of any one of claims 1 to 14 for dietary purposes or cosmetic purposes.

Description

EXAMPLE 1: COMPOSITION OF COMPONENTS A) TO I) CONTAINING A ZINC SALT AND SODIUM Ascorbate

TABLE-US-00001 Batch size: 600 g Phase A Medium-chain triglycerides 30.0000% 180.0 g Tocopherol acetate 0.6210% 3.73 g beta-Carotin (30%) 0.1389% 0.83 g LIPOID P 75 5.0000% 30.0 g Phase B Sodium Ascorbate 0.0500% 0.30 g Glycerin (86%) 60.0251% 360.2 g Water 2.0000% 12.0 g Phase C Retinyl palmitate 0.0061% 37 mg Vitamin K.sub.1 0.0029% 17 mg Vitamin D.sub.3 (2.5%) .sup.0.0033% .sup.1) 20 mg Phase D Zinc-bisglycinate 0.1527% 0.92 g Water 2.0000% 12.0 g .sup.1) % amount refers to the 2.5 solution of vitamin D.sub.3 and corresponds to a concentration of vitamin D.sub.3 in the formulation of 0.0000825%.

[0107] Phase A: -Carotin was dissolved in MCT oil at 60 C. After cooling the solution to 50 C., LIPOID P 75 and tocopherol acetate were added and dissolved. To prepare phase B, sodium ascorbate was dissolved with stirring in water at 20-25 C. Glycerin was added, and the solution was heated to 50 C. Components of phase C were added to phase A with stirring to obtain a mixture AC. Phase B was added to the mixture AC and mixed for further 30 min at 50 C. to obtain a mixture ABC. Zinc-bisglycinate was dissolved in water at 20-25 C., and the solution was added to the pre-emulsion ABC. The resulting pre-emulsion was then homogenized using a high-pressure homogenizer in two passes at a pressure of 900 bar. Temperature was kept at 50 C. to 70 C. during homogenization.

Analytical Data:

[0108] Red, transparent, slightly viscous liquid [0109] pH value: 8.1 [0110] Average particle size (Pdl): 241 nm

Stability: 6 Months at Room Temperature:

[0111] Appearance unchanged [0112] pH value: 6.9 [0113] Average particle size (Pdl): 271 nm

6 Month at +2-8 C.:

[0114] Appearance unchanged [0115] pH value: 7.1 [0116] Average particle size (Pdl): 270 nm

EXAMPLE 2: COMPOSITION OF COMPONENTS A) TO H)

TABLE-US-00002 Batch size: 300 g Phase A Medium-chain triglycerides 10.0000% 30.0 g Tocopherol acetate 3.0311% 9.09 g Retinyl palmitate 0.0373% 0.112 g Vitamin K.sub.2 (5%) .sup.0.1695% .sup.1) 0.509 g Vitamin D.sub.3 .sup.0.0678% .sup.2) 0.203 g Phase B LIPOID P 75 4.0000% 12.0 g Glycerin (86%) 82.6943% 248.08 g .sup.1) % amount refers to the 5% solution of vitamin K.sub.2 and corresponds to a concentration of vitamin K.sub.2 in the formulation of 0.008475%. .sup.2) % amount refers to the 2.5 solution of vitamin D.sub.3 and corresponds to a concentration of vitamin D.sub.3 in the formulation of 0.001695%.

[0117] Phase A: The vitamins were added to MCT oil and dissolved with stirring at 20-25 C. To prepare phase B, LIPOID P 75 was completely dispersed in glycerin with stirring at 20-30 C.

[0118] The oil phase A was added to the dispersion phase B and stirred until a homogenous mixture was obtained. The resulting pre-emulsion was then homogenized using a high-pressure homogenizer in two passes at a pressure of 900 bar. Temperature was kept at max. 50 C. during homogenization.

Analytical Data:

[0119] Yellow to light brown, transparent, slightly viscous liquid [0120] pH value: 7.0 [0121] Average particle size (Pdl): 79 nm

Stability: 4 Weeks at Room Temperature:

[0122] Appearance unchanged [0123] pH value: 6.0 [0124] Average particle size (Pdl): 81 nm

4 Weeks at +2-8 C.:

[0125] Appearance unchanged [0126] pH value: 6.0 [0127] Average particle size (Pdl): 88 nm