RU2291684C2 - Active additive for cosmetic agents and method for production thereof - Google Patents

Abstract

FIELD: chemical and pharmaceutical and cosmetic industries, in particular composition and intermediates containing betulin and/or derivatives thereof as biologically active components.

SUBSTANCE: claimed additive contains betulin and/or derivatives thereof, vegetable oil, and surfactants. As surfactants it contains mixture of hydrophilic and lipophylic surfactants in ratio of 1:(0.65-4.0), respectively. Hydrophilic surfactants are selected from group containing oxyethylated alcohols, oxyethylated natural or hydrogenised castor oil, oxyethylated sorbitane and fat acid esters; and lipophylic surfactants are selected from group containing glycerol asters of fat acids, oxyethylated fat acids or alcohols; sorbitane and fat acid esters; emulsified wax, high fat alcohols, apian wax. As vegetable oil olive, soybean or castor oil is used. Also disclosed is method for production of said bioactive additive including treatment of betulin and/or derivatives thereof using vegetable oil by addition under stirring of dry betulin or derivative thereof into preliminary melted mixture of hydrophilic and lipophylic surfactants. Then vegetable oil is added, mixture is heated up to 100-120°C, conditioned to full dissolution, obtained solution is filtered in hot state and cooled.

EFFECT: effective bioactive additive with maximal distribution of surfactants on skin surface due to high disperse colloidal state of betulin and/or derivatives thereof.

11 cl, 2 tbl

Description

The invention relates to the chemical, pharmaceutical and cosmetic industries, in particular to compositions and intermediates containing betulin and / or its derivatives as a biologically active component.

Betulin and its derivatives (betulinic acid, lupeleol, betulin diacetate) are obtained from the crushed birch bark by extraction with various organic solvents, followed by purification (RU No. 2167892, 2172178, 2184120, 2206572). One of the most common commercial products of betulin is a dry birch extract, which, depending on the method of preparation, contains from 50 to 80% pure betulinol. Studies of betulin and its derivatives have shown their harmlessness and diverse biological activity:

anti-inflammatory, antimicrobial, antiviral, antitumor, antioxidant. It is shown that betulin reduces the level of a hangover syndrome and can be used as an additive to alcoholic beverages (RF No. 2184772).

It is known to use betulin and its derivatives in cosmetic and therapeutic agents for external use, for example

- powder powder (RU No. 2049462) containing betulin (2.0-4.0 parts by weight), copper derivatives of chlorophyll, talc, zinc oxide, starch; possesses anti-inflammatory properties;

- whitening and sunscreen composition (EP 1295587) includes betulin and / or its derivatives, vegetable oils and excipients.

However, the introduction of betulin and a number of its derivatives in the composition of cosmetic and therapeutic agents is difficult due to their specific properties, consisting in the fact that they are hydrophobic substances with relatively low solubility in water (about 0.15 mg / l), oils, physiologically acceptable solvents. As a result, in cosmetic and medicinal products for external use they are present in the form of sufficiently large particles, are poorly absorbed into the epidermis, are unevenly distributed over the surface, and cannot fully exhibit their pharmacological activity. Therefore, the task of improving their bioavailability is quite relevant. It is solved, for example, by chemical modification, obtaining new betulin derivatives in the form of quaternary ammonium salts, which have greater solubility and surface-active properties (US 5182337). However, such transformations can lead to a change in toxicity and biological activity.

The closest in composition to the proposed active additive is a product obtained by a method involving the treatment of dry betulin and / or its derivatives with an emollient, which is used as vegetable oil: sunflower, soybean, olive, palm, or alkyl-modified silicone. The components are dispersed in ethanol (2 parts by weight), followed by the addition of water (4 parts by weight) and homogenization. The ratio of betulin or its derivative: emollient is 1: (0.6 ÷ 1.5). The result is a sufficiently stable suspension, which is proposed to be used for the production of cosmetic, pharmaceutical and paint emulsions.

The main disadvantage of the production method is that the treatment proposed by him does not increase the dispersion of the initial betulin and its derivatives, and the target product contains ethyl alcohol, which limits its use for the manufacture of many cosmetic and pharmaceutical forms:

creams, ointments, emulsions.

The objective of the invention is to develop an active additive for cosmetics, including betulin and / or its derivatives, in the form of a highly dispersed stable colloid, which will make it suitable for many cosmetic and pharmaceutical forms, and a method for its preparation.

The task is implemented by the proposed active additive for cosmetics, including betulin and / or its derivatives, vegetable oil and surface-active substances (surfactants) in the following ratio of components (parts by weight):

Betulin and / or its derivatives 5-35 Surfactant 45-80 Vegetable oil 10-45

As a surfactant, it contains a mixture of hydrophilic (HF) and lipophilic (LF) surfactants in the following ratio: hydrophilic: lipophilic as 1: (0.65 ÷ 4), and as hydrophilic surfactants substances, the mixture contains substances selected from the group: ethoxylated alcohols, ethoxylated natural or hydrogenated castor oil, ethoxylated esters of sorbitan and fatty acids, and lipophilic surfactants are selected from the group: glycerol and fatty ethers acids, ethoxylated fatty acids or alcohols, sorbitan and fatty acid esters, emulsion wax, higher fatty alcohols, beeswax. As betulin and / or its derivatives, you can take dry birch bark extract. Vegetable oil is used olive, soy or castor.

The task is also realized by the proposed method for producing an active additive for cosmetics, which involves the processing of betulin or its derivatives using vegetable oil. The method consists in the fact that, while stirring, dry betulin and / or its derivatives are introduced into a pre-molten mixture of hydrophilic (HF) and lipophilic (LF) surfactants (surfactants), then vegetable oil is added, the temperature is brought to 100-120 ° C , stirred until complete dissolution, the resulting solution was filtered hot and then cooled. A mixture of GF surfactant and LF surfactant is taken in the ratio: GF: LF as 1: (0.65 ÷ 4). At the same time, substances selected from the group are used as HF surfactants: hydroxyethylated alcohols, ethoxylated natural or hydrogenated castor oil, ethoxylated esters of sorbitan and fatty acids, and as LF surfactants, substances selected from the group are used: glycerol and fatty acid esters, hydroxyethylated fatty acids acids or alcohols, sorbitan fatty acid esters, emulsion wax, higher fatty alcohols, beeswax. Vegetable oil is used olive, soy or castor.

Examples of the invention are shown in table 1.

A method of obtaining an active additive for cosmetics is as follows.

The surfactant mixture in accordance with the selected composition (Table 1) is melted at 80-90 ° C, powder of dry birch bark extract (50-80%) or purified betulin and / or its derivative is added with stirring, the calculated amount of vegetable oil is added, the mixture is heated with stirring to 100-120 ° C. The resulting clear solution is filtered, cooled and poured onto a baking sheet or in a mold.

Ready active additive (AD) at room temperature is a solid waxy mass or flakes from dark yellow to brown, odorless. Quality indicators are given in table 2.

When 10-15% of the finished blood pressure is added to hot water with stirring, a uniform creamy emulsion is formed, stable in a wide temperature range. During storage and stability tests (centrifugation, exposure at 50 ° C for up to 14 days, 5-fold freezing-thawing), no particles of betulin or its derivatives, or significant separation of the emulsion, are observed (table 2).

Thus, the proposed active additive for cosmetics and the method for its preparation make it possible to obtain any form of cosmetics in a technologically standardized way. In this case, due to the conversion of betulin or its derivatives to a highly dispersed colloidal state, the maximum degree of distribution of biologically active substances in cosmetics on the skin surface is achieved, their penetration into the stratum corneum of the epidermis and thereby increases their effectiveness. In addition, the proposed method allows to transfer to a finely dispersed state any commodity forms of betulin, including dry birch bark extract.

Table 1 Ingredients Quantity, parts by weight / No. of examples one 2 3 four 5 6 7 8 9 10 Betulin 10 - - - - 35 - fifteen 5 35 Dry birch bark extract - twenty - - thirty - - - - - Betulinic acid - - 5 - - - - - - - Betulinol (90%) - - - 5 - - 10 - - - Hydrophilic surfactants drug OS-20 twenty - 10 - - - - fifteen - 10 tsetaret-23 - - - 5 - - - - - - stareth-20 - - - - - 5 - - - - RO-40 - twenty - - 10 - fifteen fifteen 10 - Rh-40 - - fifteen 10 - - - - - 10 twin 80 - - - 5 10 - - 10 - 10 twin 60 - - - - - 10 - - - - Lipophilic surfactants monoglycerides diets. thirty 25 twenty 10 10 10 thirty 10 fifteen thirty deg stearate - - - - 10 10 twenty - fifteen - spen 60 - - 10 - 10 - - 10 - - higher alcohols C ₁₆ -C ₂₀ - - 10 10 - - - - - 10 emulsion wax thirty 25 - -10 - 10 10 5 5 - beeswax - - 5 - - - - - - 10 The ratio of GF surfactant / LF surfactant 1: 3 1: 2.5 1: 1.8 1: 1,5 1: 1,5 1: 2 1: 4 1: 0.6 1: 3,5 1: 1.67 Oils soybean oil 10 - 25 - twenty twenty - - 10 25 castor oil - - - - - - fifteen twenty olive oil - 10 - 45 - - - - twenty

Claims (11)

1. An active additive for cosmetics, including betulin and / or its derivatives and vegetable oil, characterized in that it further comprises hydrophilic and lipophilic surface-active substances (surfactants) in a ratio of hydrophilic: lipophilic as 1: (0.65-4) in the following ratio of components wt. hours: Betulin and / or its derivatives 5-35 Surfactant 45-80 Vegetable oil 10-45 2. The active additive for cosmetics according to claim 1, characterized in that as the betulin and / or its derivatives contains dry birch bark extract. 3. The active additive for cosmetics according to claim 3, characterized in that as hydrophilic surfactants it contains substances selected from the group of ethoxylated alcohols, ethoxylated natural or hydrogenated castor oil, ethoxylated esters of sorbitan and fatty acids. 4. The active additive for cosmetics according to claim 4, characterized in that as lipophilic surfactants contains substances selected from the group of esters of glycerol and fatty acids, ethoxylated fatty acids or alcohols, esters of sorbitan and fatty acids, emulsion wax, higher fatty alcohols, beeswax. 5. The active additive for cosmetics according to claim 5. characterized in that as vegetable oil contains olive, soy or castor oil. 6. A method of obtaining an active additive for cosmetics, comprising the processing of betulin and / or its derivatives using vegetable oil, characterized in that dry betulin or its derivatives are added to the pre-molten mixture of hydrophilic and lipophilic surfactants, then vegetable oil, bring the temperature to 100-120 ° C, maintain until complete dissolution, the resulting solution is filtered and then cooled. 7. The method according to claim 7, characterized in that the dry birch bark extract is used as betulin and / or its derivatives. 8. The method according to claim 8, characterized in that the mixture of hydrophilic and lipophilic surfactants has a hydrophilic: lipophilic ratio of 1- (0.65-4). 9. The method according to claim 9, characterized in that as hydrophilic surfactants use substances selected from the group of ethoxylated alcohols, ethoxylated natural or hydrogenated castor oil, ethoxylated esters of sorbitan and fatty acids. 10. The method according to claim 10, characterized in that as lipophilic surfactants use substances selected from the group of esters of glycerol and fatty acids, ethoxylated fatty acids or alcohols, esters of sorbitan and fatty acids, emulsion wax, higher fatty alcohols, beeswax 11. The method according to claim 11, characterized in that olive, soy or castor oil is used as vegetable oil.