WO2009134165A1 - Antioxidant and antihypoxant dihydroquercetin-based complex for cosmetic products - Google Patents

Abstract

The invention relates to the chemical, pharmaceutical and cosmetic industry. The inventive antioxidant and anti-hypoxant dihydroquercetin-based complex for cosmetic products comprises 6.0-16.0 % by weight soy phospholipides with a phosphatidylcholine (lecithin) content ranging from 50 to 100%, 0.5-12.0 % by weight water-soluble vegetable extracts, 2.0-5.0 % by weight carbohydrates, 2.0-5.0 % by weight distilled glycerin, 0.5-2.5 % by weight dihydroquercitin, 0.1-1.0 % by weight PP vitamin (nicotinamide), 0.05-0.5 % by weight water-soluble antioxidant and antihypoxant agents, 0.05-0.5 % by weight oil-soluble antioxidant and antihypoxant agents, 0.05-0.5 % by weight magnesium ascorbyl phosphate, 0.1-1.0 % by weight preservative and 6.0-14.0 % by weight ethyl alcohol, the rest being deionized water up to 100 % by weight.

Description

 Antioxidant and antihypoxant complex based on dihydroquercetin for cosmetics

Technical field

The invention relates to the pharmaceutical industry, in particular to the creation of biologically active complexes based on natural raw materials, which may find application in the composition of cosmetic products used in the cosmetic industry and medical and preventive medicine.

State of the art

It is widely known that in order to impart therapeutic and prophylactic properties to cosmetics, a wide variety of active substances are introduced into their composition, affecting the vital activity of the body. Natural and synthetic substances are known that impart useful properties to cosmetic products, for example, antioxidant, anti-inflammatory, etc.

(Chemical Dictionary, edited by I.L. Knunyants, M., Soviet Encyclopedia, 1963). Known biologically active additive for cosmetic products, including plant extract, Vitamin E, proteins, fatty acids, chlorophyll, minerals, etc. (RF patent 2053763 from 1996).

Most known dietary supplements have a highly specific biological effect.

Disclosure of invention

The present invention is the creation of a complex concentrate for the production of a variety of cosmetic products with a wide range of biological effects.

To solve this problem, a composition has been proposed in liposome form with antioxidant and antihypoxic properties, including oil-soluble ingredients such as phospholipids, dihydroquercetin (taxifolin), tocopherols (vitamin E), tetrahydroquinoline derivatives (6-ethoxy-2,2,4-trimethyl) , 2,3, 4-tetrahydroxinolin, 6-hydroxy-2, 2, 4-trimethyl-1,2,3,4-tetrahydroxinolin and others), 2,6-Di-tert-butyl-4-methylphenol, rutin and water-soluble ingredients, such as derivatives of hydroxypyridine succinate (2-ethyl-6-methyl-3-hydroxypyridine succinate and others), etc. tetrahydroquinoline hydrochloride derivatives (6-ethoxy-2,2,4-trimethyl-l, 2,3,4-tetrahydroxinoline hydrochloride and others), 1-hydroxyhermatran, as well as magnesium ascorbyl phosphate, water-soluble plant extracts selected from the group of plants: Gingko-biloba, Ginseng, Arnica, Iglitsa, Licorice, Chamomile, Badan, St. John's wort, Horse chestnut, Nettle, Soy, Green tea, Calendula, Milk Thistle, Sabelnik, Scutellaria, Sage and troxerutin in the following components, in weight. %: soy phospholipids with a content of 6.0 - 16.0 phosphatidylcholine (lecithin) from 50 to 100% water-soluble plant extracts 0.5 - 12.0 carbohydrates 2.0 - 5.0 distilled glycerin 2.0 - 5.0 dihydroquercetin 0.5 - 2.5 vitamin PP (Nicotinamide) 0.1 - 1.0 water soluble antioxidants - 0.05 - 0.5 antihypoxants oil soluble antioxidants - 0.05 - 0.5 antihypoxants magnesium ascorbyl phosphate 0.05 - 0, 5 preservative 0.1 - 1.0 ethyl alcohol 6.0 - 14.0 deionized water to 100,

while water-soluble plant extracts selected from the group of plants Gingko-biloba, Zhen-Shen, Arnica, Iglitsa, Licorice, Chamomile, Frankincense, St. John's wort,

Horse chestnut, Nettle, Soybeans, Green tea, Calendula, Milk thistle, Cinquefoil, Scutellaria, Sage and / or water-soluble biologically active compound Troxerutin; carbohydrates are selected from the group: fructose, glucose, xylitol, sorbitol, invert sugar; water-soluble antioxidants, antihypoxants are selected from the group: 2-ethyl-6-methyl-3-hydroxypyridine succinate and / or 6-ethoxy-2,2,4-trimethyl-1, 2,3,4-tetrahydroxinoline hydrochloride and / or 1- germatran hydroxides or mixtures thereof; oil-soluble antioxidants - antihypoxants selected from the group: 6-ethoxy-2,2,4-trimethyl-l, 2,3,4-tetrahydroquinoline and / or 6-hydroxy-2,2,4-trimethyl-l, 2,3, 4- tetrahydroquinoline and / or 2,6-Dieth-butyl-4-methylphenol and / or tocopherol (nicotinamide, linoleate, acetate, alpha) or mixtures thereof and / or a biologically active compound rutin; the preservative is selected from the group: phenoxyethanolamine, methylparaben, ethylparaben, propylparaben, butylparaben, isobutylparaben or biosol, sodium benzoate, potassium sorbate.

The technical result consists in obtaining an additional effect of transdermal transfer during topical application of antioxidant and antihypoxic properties. The best example of carrying out the invention

The invention is illustrated by the following examples: Technological recipe for the preparation of liposomal concentrates:

1. Preparation of the aqueous phase.

2. Preparation of the oil phase.

3. Preparation of a coarse dispersion of Flavosomes. 4. Preparation of liposome concentrate

Example 1

1. When preparing the aqueous phase in a separate container with a capacity of 2.0 liters in 551, Or warm deionized water (55 - 60 ⁰ C), with stirring, add and dissolve 8.0 g of sodium benzoate (Preservative), 0.5 g of a mixture of water-soluble antioxidants-hypoxants ( 6-ethoxy-2,2,4-trimethyl-l, 2,3,4-tetrahydroxinoline hydrochloride and 1-hydroxyl germatrane in a 1: 1 ratio), l, 0 g nicotinamide, 2.0 g magnesium ascorbyl phosphate, 30.0 g glycerol distilled (farm.), 40.0 g of carbohydrate (Xylitol), 40.0 g of Gingko-Biloba and mix thoroughly until completely dissolved.

2. When preparing the oil phase in a separate container with a capacity of 0.5 liters we add 140, Or ethyl alcohol and dissolve 25, Or dihydroquercetin when heated to 40 - 55 ⁰ C, then add 160.0 g of soy phospholipids (content of phosphatidylcholine 70%), 0.5 g of oil-soluble antioxidants-antihypoxants - 6-ethoxy-2,2,4-trimethyl- 1,2,3,4-tetrahydroxinoline and tocopherol acetate in a 1: 2 ratio, 2.0 g of paraoxybenzoic acid propyl ester are heated to 55-60 ⁰ C and dissolved with stirring until the components are completely dissolved in alcohol. 3. When preparing a coarse dispersion in the aqueous phase

(672.5 g) obtained according to claim 1, we add 327.5 g of the oil phase according to claim 2. when mixing with a working high-speed turbo mixer at a temperature of 55-60 ⁰ C and disperse for 5-10 minutes until a coarse dispersion is obtained. 4. In the preparation of a fine dispersion, a coarse dispersion according to p.Z. we homogenize in an argon (nitrogen) atmosphere in a high-pressure homogenizer (in particular, the Menton Gaulin model with a capacity of (80 - 100) l / h, USA or any other high-pressure homogenizer) while cooling the liposome concentrate to an average temperature of not higher than 35 - 50 ⁰ C in the following technological mode:

1 - 3 cycles of homogenization at an overpressure of 150 - 250 ati, 1-2 pressure homogenization cycles

300 - 400 ati,

1 - 2 cycles of homogenization at an excess pressure of about 600 ati, 1 - 2 cycles of homogenization at an excess pressure

300 - 450 ati,

1 - 3 cycles of homogenization at an excess pressure of 150 - 200 ati.

The total number of homogenization cycles is from 6 to 14. The pH value is in the range of 5.0 - 7.5.

Prepared liposome concentrate 1000.0 g.

Example 2

1. When preparing the aqueous phase in a separate container with a capacity of 2.0 l in 620.0 g of warm deionized water (55 - 60 ⁰ C), with stirring, add and dissolve 8.0 g of sodium benzoate (Preservative), 5.0 g of a mixture of water-soluble antioxidants-hypoxants (2-ethyl-6-methyl-3-hydroxyxypyridine hydrochloride and 1-hydroxy germatrane in a 1: 1 ratio), 10.0 g of nicotinamide, 5, Or magnesium ascorbyl phosphate, 50.0 g of distilled glycerol (farm.), 50.0 g carbohydrate (Fructose), 120.0 g (Troxerutin and Sabelnik in a 5: 1 ratio) and mix thoroughly until completely dissolved. 2. When preparing the oil phase in a separate container with a capacity of 0.5 l, add 60.0 g of ethyl alcohol and dissolve 5, Or dihydroquercetin when heated to 40 - 55 ⁰ C, then add 60.0 g of soy phospholipids (100% phosphatidylcholine content), 5, 0 g of oil-soluble antioxidants, antihypoxants - (6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroxinolin and tocopherol acetate in a ratio of 1: 2), 2.0 g of paraoxybenzoic acid propyl ester are heated to 55 - 60 ⁰ C and dissolve with stirring until the components are completely dissolved in alcohol.

3. When preparing a coarse dispersion in the aqueous phase (868.0 g), obtained according to claim 1. make (132.0 g) of the oil phase according to claim 2. when mixing with a working high-speed turbo mixer at a temperature of 55-60 ⁰ C and disperse for 5-10 minutes until a coarse dispersion is obtained.

4. When preparing a fine dispersion according to item 3, we homogenize the coarse dispersion in an argon (nitrogen) atmosphere in a high-pressure homogenizer (in particular, the Menton Gaulin model with a capacity of (80–100) l / h, USA, or any other high-pressure homogenizer ) when cooling the liposomal concentrate to an average temperature of not higher than 35 - 50 ⁰ C in the following technological mode: 1 - 2 cycles of homogenization at an excess pressure of 150 - 250 ati,

1 - 2 cycles of homogenization at an excess pressure of 400 - 450 ati, 1 - 2 cycles of homogenization at an excess pressure of about 600 ati,

1 - 2 cycles of homogenization at an excess pressure of 300 - 350 ati,

1 - 2 cycles of homogenization at an excess pressure of 150 - 200 ati.

The total number of homogenization cycles is from 5 to 10.

PH values in the range of 5.0 - 7.5.

Prepared liposome concentrate 1000.0 g.

Example 3

1. When preparing the aqueous phase in a separate container with a capacity of 2.0 l in 565.0 g of warm deionized water (55 - 60 ⁰ C) with stirring, add and dissolve 5, Or sodium benzoate (Preservative), 2.0 g of a mixture of water-soluble antioxidants - antihypoxants (2-ethyl-6-methyl-3-hydroxypyridine succinate and 1-hydroxyl germatrane in a 1: 1 ratio), 2.0 g nicotinamide, l, 0 g magnesium ascorbyl phosphate, 30.0 g distilled glycerol (farm.), 30.0 g carbohydrate (Sorbitol), 100.0g Troxerutin and mix thoroughly until completely dissolved.

2. When preparing the oil phase in a separate container with a capacity of 0.5 l, add 120.0 g of ethyl alcohol and dissolve 20, Or dihydroquercetin when heated to 40 - 55 ⁰ C, then add 120.0 g of soy phospholipids (60% phosphatidylcholine content), 3, 0 g of oil-soluble antioxidants - antihypoxants (6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroxinolin and tocopherol nicotinamide in a ratio of 1: 2), 2.0 g of paraoxybenzoic acid propyl ester are heated to 55 - 60 ⁰ C and dissolve with stirring until the components are completely dissolved in alcohol.

3. When preparing a coarse dispersion in the aqueous phase (735.0 g) obtained according to claim 1, we add 265, Or of the oil phase according to claim 2. when mixing with a working high-speed turbo mixer at a temperature of 55-60 ⁰ C and disperse for 5-10 minutes until a coarse dispersion is obtained.

4. When preparing a fine dispersion according to item 3, we homogenize the coarse dispersion in argon (nitrogen) atmosphere in a high-pressure homogenizer (in particular, the Menton Gaulin model with a capacity of 80-100 l / h, USA or any other high-pressure homogenizer) while cooling the liposome concentrate to medium temperature not higher than 40 - 50 ° С in the following technological mode:

1 - 3 cycles of homogenization at an overpressure of 150 - 250 ati, 1 - 3 cycles of homogenization at an overpressure

300 - 400 ati,

1 - 2 cycles of homogenization at an overpressure of about 600 atm,

1 - 2 cycles of homogenization at an excess pressure of 400 - 500 ati,

1 - 2 cycles of homogenization at an excess pressure of 150 - 200 ati.

The total number of homogenization cycles is from 5 to 12.

PH values in the range of 5.0 - 7.5. Prepared liposome concentrate 1000.0 g.

Industrial applicability

The obtained liposome concentrate with various compositions can be used in cosmetic products for gel and foot cream, hand cream, face serum, head masks, etc.

Liposomal concentrate does not have side effects. Tests were conducted on volunteers aged 20 to 54 years. The course of taking various cosmetic products showed that due to the combination of oil and water-soluble antioxidants and antihypoxants in the liposome form and the systemic interaction of the above ingredients in this composition, the result is that the rate of transdermal transfer of the oil-oil complex is increased by 20 - 50% and water soluble antioxidants and antihypoxants.

Claims

Claim 1. Antioxidant and antihypoxant complex based on dihydroquercetin for cosmetics, characterized in that it contains soy phospholipids, water-soluble plant extracts, carbohydrates, distilled glycerin, dihydroquercetin, vitamin PP (Nicotinamide), water-soluble antioxidants, antihypoxants, oil soluble antioxidants, antihypoxants, magnesium ascorbyl phosphate, preservative, ethyl alcohol, deionized water with the following components, in wt.%: Soy phospholipids with a content of 6.0 - 16.0 phosphatidylcholine (lecithin) 50 to 100% water-soluble plant extracts 0.5 - 12.0 carbohydrates 2.0 - 5.0 distilled glycerin 2.0 - 5.0 dihydroquercetin 0.5 - 2.5 vitamin PP (Nicotinamide) 0, 1 - 1 , 0 water soluble antioxidants - 0.05 - 0.5 antihypoxants oil soluble antioxidants - 0.05 - 0.5 antihypoxants magnesium ascorbyl phosphate 0.05 - 0.5 preservative 0.1 - 1.0 ethyl alcohol 6.0 - 14.0 deionized water to 100, 2. The antioxidant and antihypoxic complex according to claim 1, in which the water-soluble plant extracts are selected from the group of plants: Gingko-beat both, Zhen-Shen, Arnika, Iglitsa, Licorice, Chamomile, Badan, St. John’s Wort, Horse chestnut, Nettle, Soy, Green tea, Calendula, Milk Thistle, Sabelnik, Troxerutin, Shlemnik, Sage and / or a water-soluble biologically active compound - Troxerutin. 3. The antioxidant and antihypoxic complex according to claim 1, wherein the carbohydrates are selected from the group: fructose, glucose, xylitol, sorbitol, invert sugar. 4. The antioxidant and antihypoxant complex according to claim 1, wherein the water soluble antioxidants - antihypoxants are selected from the group: 2-ethyl-6-methyl-3-hydroxypyridine succinate and / or 6-ethoxy-2,2,4-trimethyl-1, 2,3,4-tetrahydroxinolin hydrochloride and / or 1-hydroxyl germatrane or mixtures thereof. 5. The antioxidant and antihypoxic complex according to claim 1, wherein the oil-soluble antioxidants - antihypoxants are selected from the group of 6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroxinolin and / or 6-hydroxy-2, 2,4-trimethyl 1,2,3,4-tetrahydroxinolin and / or 2,6-di-tert-butyl-4-methylphenol and / or tocopherol (nicotinamide, linoleate, acetate, alpha) or mixtures thereof, and / or biologically active compound rutin . 6. The antioxidant and antihypoxant complex according to claim 1, wherein the preservative is selected from the group of phenoxyethanolamine, methylparaben, ethylparaben, propylparaben, butylparaben, isobutylparaben or biosol, sodium benzoate, potassium sorbate.