RETINOL FORMULATION (II)

Abstract

The present invention relates to a new formulation, which comprises a high amount of retinol in a specific solvent and in the presence of mixed tocopherol.

Claims

1. A formulation comprising 40-75 weight-% (wt-%), based on the total weight of the formulation, of retinol, 20-55 wt-%, based on the total weight of the formulation, of at least one solvent, and 0.1-5 wt-%, based on the total weight of the formulation, of mixed tocopherol, wherein the at least one solvent is a compound of formula (I) ##STR00006## wherein w, x, y and z are independently from each other integers which sum up to 20, and R is a linear or branched C.sub.10-C.sub.18-alkyl moiety or a linear or branched C.sub.10-C.sub.18-alkylene moiety.

2. A formulation consisting (essentially) of 40-75 wt-%, based on the total weight of the formulation, of retinol, and 20-55 wt-%, based on the total weight of the formulation, of at least one solvent, and 0.1-5 wt-%, based on the total weight of the formulation, of mixed tocopherol, wherein the at least one solvent is a compound of formula (I) ##STR00007## wherein w, x, y and z are independently from each other integers which sum up to 20, and R is a linear or branched C.sub.10-C.sub.18-alkyl moiety or a linear or branched C.sub.10-C.sub.18-alkylene moiety.

3. The formulation according to claim 1, comprising 40-70 wt-%, based on the total weight of the formulation, of retinol.

4. The formulation according to claim 1, wherein the at least one solvent is a compound of formula (I), wherein w, x, y and z are independently from each other integers which sum up to 20, and R is a linear C.sub.11-alkyl, a linear C.sub.17-alkyl moiety or a linear C.sub.17-alkylene moiety (preferably of formula (CH.sub.2)CH?CH(CH.sub.2).sub.7CH.sub.3.).

5. The formulation according to claim 1, wherein the solvent is polysorbate 20.

6. The formulation according to claim 1, comprising 25-55 wt-%, based on the total weight of the formulation, of the at least one solvent.

7. The formulation according to claim 1, wherein the mixed tocopherol comprises up to 20 wt-%, based on the total weight of the mixed tocopherol, of ?-tocopherol and up to 5 wt-%, based on the total weight of the mixed tocopherol, of ?-tocopherol and up to 75 wt-%, based on the total weight of the mixed tocopherol, of ?-tocopherol and up to 35 wt-%, based on the total weight of the mixed tocopherol, of ?-tocopherol.

8. The formulation according to claim 1, wherein the formulation does not comprise any further antioxidants (other than the mixed tocopherol).

9. The formulation according to claim 1, comprising 0.2-4.5 wt-%, based on the total weight of the formulation, of mixed tocopherol.

10. Process of producing a formulation according to claim 1 comprising the following steps Mixing the retinol and the mixed tocopherol at elevated temperature (40 to 65? C.) Heating the at least one solvent up to a similar temperature as the retinol/mixed tocopherol mixture (40 to 65? C.) Adding the at least one solvent to the retinol/mixed tocopherol mixture (or vice versa) at elevated temperature (40 to 65? C.) and mixing it at this temperature Cool down the mixture slowly.

11. Use of at least one formulation according to claim 1 in food, feed, pharma and personal care products (preferably in personal care products).

12. Food, feed, pharma and personal care personal care products comprising at least one formulation according to claim 1.

13. Personal care personal care products comprising at least one formulation according to claim 1.

Description

EXAMPLES

[0138] All the following examples are made according to the following method: [0139] Melting and mixing the retinol and the mixed tocopherol a temperature of 63? C. to 65? C. for about 5 to 10min under nitrogen; [0140] Then heating the solvent to a temperature of 63? C. to 65? C. [0141] Then mixing (under stirring) the retinol/mixed tocopherol mixture and the solvent at 63? C. to 65? C. for a few minutes 2-5 minutes and the let the formulation cool down to room temperature slowly. [0142] Mixed tocopherol was Mixed Tocopherols 95 (from DSM)

TABLE-US-00001 TABLE 1 All values in the table are wt-%, based on the total weight of the formulation Example 1 2 3 Polysorbate 20 51 48 51.5 BHT 3.1 BHA 0.9 Mixed tocopherols 95 1 0.5 Retinol 48 48 48

[0143] To determine the stability of these formulations, they were stored (at 40? C.) for 2 weeks and 12 weeks. And the loss of retinol was measure (the initial value was 100%)

TABLE-US-00002 TABLE 2 the retinol content was determined after storage Example 1 2 3 Initial 100 100 100 2 weeks 98 94.4 70 6 weeks 96.9 89.4 54

[0144] It can be seen from the table that the formulations according to the present invention are very stable. The formulation 2 and 3 (comparison examples with BHA and BHT as antioxidant and without any antioxidants) show lower stability.

[0145] As stated above, the inventive retinol formulations of the present invention can be incorporated into a variety of compositions.

[0146] For example, in the following personal care compositions listed in the following tables (all values are given in weight-%, based on the total weight of the composition)

TABLE-US-00003 Examples: O/W-Emulsions 4 5 6 Cetearyl Alcohol + Sodium 3.00 3.00 2.00 Cetylstearylsulfat Glycerylstearat SE 2.00 2.00 4.00 Octyldodecanol 2.00 2.00 2.00 C.sub.12-15 Alkylbenzoate 1.00 1.00 1.00 C13-16 Isoparaffin 3.00 3.00 3.00 Undecane, tridecane 2.00 2.00 2.00 Glycerine 5.00 5.00 6.00 Dimethicone 0.50 0.50 0.50 Sodium ascorbylphosphate 0.10 Ethylhexylsalicylate 0.50 0.50 0.50 Glycyrrhetic acid 0.10 Retinol formulation of Example 1 0.1 0.16 0.02 BEL-EVEN? 0.50 Grape seed oil 0.50 0.50 0.50 Dihydroxyacetone 2.00 Paraffinum Liquidum + 0.25 0.25 0.25 Ginkgo Biloba Extract Citric acid 0.09 0.09 0.09 Sodium citrate 0.17 0.17 0.17 Xanthan gum 0.10 Ammonium Acryloyldimethyltaurate/ 0.40 0.40 VP Copolymer Carbomer 0.30 Parabene 0.30 0.30 0.30 Phenoxyethanol 0.50 0.50 0.50 Alcohol Denat. 3.50 3.50 3.50 Perfume q.s q.s q.s Water ad 100 ad 100 ad 100

TABLE-US-00004 Examples: Hydrodispersions 7 8 9 Glyceryl Stearate Citrate 0.4 Sodium Carbomer Acrylates/C.sub.10-30 Alkyl Acrylate 0.1 0.2 Crosspolymer Ceteareth-20 Potassium Cetyl Phosphate Xanthan Gum 0.5 0.2 Dimethicone/Vinyl Dimethicone 3 1.5 Crosspolymer 2-(4-Diethylamino-2-hydroxybenzoyl)- 1.5 benzoic Acid Hexylester 2,4,6-Tribiphenyl-4-yl-1,3,5 Triazine 0.5 Butyl Methoxydibenzoylmethane 5 Ethylhexyl 2 Bis-Isopentylbenzoxazolylphenyl Melamine Bis-Ethylhexyloxyphenol 2 Methoxyphenyltriazine Disodium Phenyl Dibenzimidazole 1 Tetrasulfonate Phenylbenzimidazole Sulfonic Acid 1 Ethylhexyl Methoxycinnamate 8 Ethylhexyl Salicylate Homosalate Diethylhexyl Butamido Triazone Ethylhexyl Triazone 3 1 Octocrylene Polysilicone-15 0.9 Methylbenzylidene Camphor 2 BEL-EVEN? 0.5 Titanium Dioxide 2 1 2 Drometrizole Trisiloxane 0.5 Terephthalidene Dicamphor 0.75 Sulfonic Acid C.sub.12-15 Alkyl Benzoate Butylene Glycol Dicaprylate/ Dicaprate Dicaprylyl Carbonate 3 Dicaprylylether 2 Cyclomethicone 3 2-Phenylethylbenzoate Diethylhexylnaphthalate Tridecylsalicylate 3 0.5 3 PVP Hexadecene Copolymer 1 Glycerin 5 8 Butylene Glycol 7 Glycine Soja 1 Vitamin E Acetate 0.25 1 0.25 Alpha-Glycosylrutin Retinol formulation of Example 1 0.1 0.02 0.1 DHA 1.0 Erythrulose 0.5 Trisodium EDTA 0.1 0.1 Tromethamine Ethanol 10 1 Preservatives q.s q.s q.s Fragrance, Colours q.s q.s q.s Water Ad 100 Ad 100 Ad 100