RU2367409C1 - Antioxidant and antihypoxant dihydroquercetin for cosmetic products - Google Patents

Abstract

FIELD: medicine.

SUBSTANCE: invention refers to chemical-pharmaceutical industry, namely to creation of biologically active complexes based on natural raw materials to be applied in cosmetic products used in cosmetic industry, and therapeutic medicine. There is offered antioxidant and antohypoxant dihydroquercetin complex for cosmetic products, characterised by that it contains soya phospholipids, water-soluble vegetative extracts, carbohydrates, distilled glycerine, dihydroquercetin, vitamin PP (nicotinamide), water-soluble antioxidants-antihypoxants, poorly soluble antioxidants-antihypoxants, magnesium ascorbyl phosphate, preserving agent, ethanol, deionized water.

EFFECT: declared invention provides transdermal delivery speed of complex oil- and water-soluble antioxidants and antohypoxants increased by 20-50%.

6 cl, 3 ex

Description

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

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.

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.

A composition is 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-1,2,3,3 , 4-tetrahydroquinoline, 6-hydroxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline 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), tetrahydride derivatives oquinoline hydrochloride (6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline hydrochloride and others), 1-hydroxyhermatran, as well as magnesium ascorbyl phosphate, water-soluble plant extracts selected from the plant group: Gingko- biloba, ginseng, arnica, iglitza, licorice, chamomile, incense, St. John's wort, horse chestnut, nettle, soybeans, green tea, calendula, milk thistle, sabelnik, shlemnik, sage and troxerutin in the following components, in wt.%:

soy phospholipids containing phosphatidylcholine (lecithin) from 50 to 100% 6.0-16.0 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 antihypoxic antioxidants 0.05-0.5 oil soluble antioxidants antihypoxants 0.05-0.5 magnesium ascorbyl phosphate 0.05-0.5 preservative 0.1-1.0 ethanol 6.0-14.0 deionized water up to 100,

while water-soluble plant extracts are 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, Shlemnik, Sage and / or a water-soluble biologically active compound Troxerutin;

carbohydrates are selected from the group: fructose, glucose, xylitol, sorbitol, invert sugar;

water-soluble antioxidant antihypoxants selected from the group: 2-ethyl-6-methyl-3-hydroxypyridine succinate and / or 6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline hydrochloride and / or 1- hydroxy germatran or mixtures thereof;

oil soluble antioxidant antihypoxants selected from the group: 6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline and / or 6-hydroxy-2,2,4-trimethyl-1,2,3, 4-tetrahydroquinoline and / or 2,6-di-tert-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 invention is illustrated by the following examples.

Technological prescriptions 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 l in 551.0 g of warm deionized water (55-60 ° 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-1,2,3,4-tetrahydroquinoline hydrochloride and 1-hydroxyhermatran in a 1: 1 ratio), 1.0 g of nicotinamide, 2.0 g of magnesium ascorbyl phosphate , 30.0 g of distilled glycerol (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 l, we add 140.0 g of ethyl alcohol and dissolve 25.0 g of dihydroquercetin when heated to 40-55 ° C, then we add 160.0 g of soy phospholipids (70% phosphatidylcholine content ), 0.5 g of oil-soluble antioxidant antihypoxants - 6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline and Tocopherol acetate in a 1: 2 ratio, 2.0 g of paraoxybenzoic acid propyl ester, we heat everything up to 55-60 ° C and dissolve 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 while stirring with a working high-speed turbo mixer at a temperature of 55-60 ° C and for 5 -10 minutes dispersed to obtain a coarse dispersion.

4. When preparing a fine dispersion, the coarse dispersion according to claim 3. we homogenize in an argon (nitrogen) atmosphere in a high-pressure homogenizer (in particular, the Menton Gaulin model with a productivity of 80-100 l / h, USA or any other high-pressure homogenizer) when the liposome concentrate is cooled to an average temperature of no higher than 35-50 ° С following technological mode:

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

1-2 cycles of homogenization at an excess pressure of 300-400 ati,

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

1-2 cycles of homogenization at an excess pressure of 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.

PH values 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 ° 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-hydroxypyridine hydrochloride and 1-hydroxy germatrane in a 1: 1 ratio), 10.0 g of nicotinamide, 5.0 g of magnesium ascorbyl phosphate, 50.0 g of distilled glycerol (farm .), 50.0 g of 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, we add 60.0 g of ethyl alcohol and dissolve 5.0 g of dihydroquercetin when heated to 40-55 ° C, then add 60.0 g of soy phospholipids (100% phosphatidylcholine content) ), 5.0 g of oil-soluble antioxidant antihypoxants - (6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline and Tocopherol acetate in a 1: 2 ratio), 2.0 g of paraoxybenzoic propyl ester acid, we heat everything up to 55-60 ° 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, add (132.0 g) the oil phase according to claim 2 with stirring with a working high-speed turbo mixer at a temperature of 55-60 ° C and in disperse for 5-10 minutes until a coarse dispersion is obtained.

4. When preparing a fine dispersion according to claim 3, we homogenize the coarse dispersion in an argon (nitrogen) atmosphere in a high-pressure homogenizer (in particular, the Menton Gaulin model with a productivity of 80-100 l / h, USA, or any other high-pressure homogenizer) under cooling liposome concentrate to an average temperature of not higher than 35-50 ° 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 overpressure 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 ° C), with stirring, add and dissolve 5.0 g of sodium benzoate (Preservative), 2.0 g of a mixture of water-soluble antioxidants, antihypoxants (2-ethyl-6-methyl-3-hydroxypyridine succinate and 1-hydroxy germatran in a 1: 1 ratio), 2.0 g of nicotinamide, 1.0 g of magnesium ascorbyl phosphate, 30.0 g of distilled glycerol (farm .), 30.0 g of carbohydrate (Sorbitol), 100.0 g of 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 20.0 g of dihydroquercetin when heated to 40-55 ° C, then add 120.0 g of soy phospholipids (60% phosphatidylcholine content ), 3.0 g of oil-soluble antioxidant antihypoxants (6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline and Tocopherol nicotinamide in a 1: 2 ratio), 2.0 g of paraoxybenzoic acid propyl ester , we heat everything up to 55-60 ° 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 265.0 g of the oil phase according to claim 2. when mixing with a working high-speed turbo mixer at a temperature of 55-60 ° C and disperse for 5-10 minutes until a coarse dispersion is obtained.

4. When preparing a fine dispersion according to claim 3, we homogenize the coarse dispersion in an argon (nitrogen) atmosphere in a high-pressure homogenizer (in particular, the Menton Gaulin model with a productivity 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 40-50 ° C in the following technological mode:

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

1-3 cycles of homogenization at an excess pressure of 300-400 ati,

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

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.

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 (31 volunteers) aged 20 to 54 years. The course of taking a variety of cosmetic products has shown 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-complex is increased by 20-50% and water soluble antioxidants and antihypoxants.

Claims (6)

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, antioxidants, antihypoxants, oil ascorbyl phosphate, preservative, ethyl alcohol, deionized water in the following components, wt.%:
soybean phospholipids containing phosphatidylcholine (lecithin) from 50 to 100% 6.0-16.0 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 antihypoxic antioxidants 0.05-0.5 oil soluble antioxidants antihypoxants 0.05-0.5 magnesium ascorbyl phosphate 0.05-0.5 preservative 0.1-1.0 ethanol 6.0-14.0 deionized water up 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-biloba, Zhen-Shen, Arnika, Iglitsa, Licorice, Chamomile, Badan, St. John's wort, Horse chestnut, Nettle, Soy, Green tea , Calendula, Milk Thistle, Sabelnik, Scutellaria, Sage and / or water-soluble biologically active compounds - 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 antihypoxic complex according to claim 1, wherein the water-soluble antioxidant 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-tetrahydroquinoline hydrochloride, and / or 1-hydroxy germatran, or mixtures thereof. 5. The antioxidant and antihypoxant complex according to claim 1, wherein the oil-soluble antioxidant antihypoxants are selected from the group of 6-ethoxy-2,2,4-trimethyl-1,2,3,4-tetrahydroquinoline, and / or 6-hydroxy-2 , 2,4-trimethyl-1,2,3,4-tetrahydroquinoline, and / or 2,6-di-tert-butyl-4-methylphenol and / or tocopherol (linoleate, acetate, alpha-tocopherol), 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.