RU2247555C1 - Antibacterial gel - Google Patents

Abstract

FIELD: cosmetology.

SUBSTANCE: the present innovation deals with cosmetic preparation for taking care of skin, in particular. The suggested antibacterial gel consists of either hydroxypropylcellulose or hydroxyethylcellulose, propylene glycol or diethylene glycol compound, polyguanidine or its synergistic mixture with quaternary ammonium compound, chitosan, oxyethylated ether of sorbitane, polyvinyl pyrrolidone at molecular weight ranged 10000 - 40000 or copolymer of polyvinylpyrrolidone, trilon-B - sodium salt of ethylene diamintetraacetic acid, perfumery composition, vitamin constituent and water. The present innovation provides increased regenerating formula of skin and its enhanced barrier function, improves homogeneity of the composition mentioned and its stability.

EFFECT: higher efficiency of application.

5 cl, 4 ex, 3 tbl

Description

The invention relates to the field of cosmetology, in particular to means for skin care, and can be used to care for the skin of the face, hands, legs and other parts of the body.

Known gel for antiseptic treatment of the skin, containing in its composition a modified derivative of cellulose, an antiseptic - miramistin and water (Pat. RF No. 2185157, class A 61 K 31/14, 2000).

However, the miramistin used does not have a prolonged effect and is effective for a narrow field of use.

The closest solution to the proposed is a hygienic gel of the following composition, wt.%: Carbopol - 0.1-10.0; triethanolamine - 0.1-10.0; liposomal preparation “Sorceress-2” (anti-acne) - 1-30; distilled glycerin PK-94 - 1-15; rectified ethyl alcohol of the highest purification - 0.1-5.0; water-alcohol-glyceric burdock extract - 0.1-5.0; water-alcohol-glyceric extract of horsetail - 0.1-5.0; triclosan - 0.1-1.0; synthetic camphor - 0.01-1.0; dye C1 42090 - 0.1-1.0; perfume composition - 0.1-1.5; drinking water - the rest (Pat. RF No. 2150264, class A 61 K 7/00, 1999).

The disadvantages of the known gel include the fact that the applied triclosan is a dichlorinated derivative of bis-phenol, which is close in structure to the extremely dangerous substance dioxin. It is known that triclosan may contain an admixture of dioxin, an extremely toxic and dangerous substance. In addition, it is known that chlorinated phenols with simple heating are easily converted to dioxins. At the same time, the antibacterial activity of triclosan is extremely low.

The technical problem solved by this invention is to reduce the toxicity of the gel through the use of low-toxic disinfectants with improved dermatological effect and prolonged effect, contributing to an increase in the regenerative function of the skin and enhance its barrier function. In addition, the homogeneity of the composition and its stability are improved.

To solve the technical problem in an antibacterial gel, including an alkyl hydroxyl compound, a disinfectant, a perfume composition and water, propylene glycol or diethylene glycol is used as an alkyl hydroxyl compound, a polyguanidine compound or its synergistic hydroxyethylacetate or synergistic hydroxyethylacetate are used as a disinfectant. , chitosan, ethoxylated sorbitan ester, polyvinylpyrrolidone with mol acous- weight of from 10,000 to 40,000 or a copolymer of polyvinyl pyrrolidone, Trilon B - sodium salt of ethylenediaminetetraacetic acid, a vitamin component, and water at the following ratio of components in wt.%:

- hydroxypropyl cellulose or

hydroxyethyl cellulose 0.3-3.0

- propylene glycol or diethylene glycol 0.2-15.0

- a compound of polyguanidine or its synergistic

quaternary ammonium compound

in the ratio 1: 1 0.5-3.0

- chitosan 0.1-2.0

- ethoxylated ester of sorbitan 0.01-1.0

- polyvinylpyrrolidone with a molecular weight of 10,000

up to 40,000 or a copolymer of polyvinylpyrrolidone 0.01-0.5

- trilon B - sodium salt

ethylenediaminetetraacetic acid 0.1-2.0

- perfume composition 0.2-0.5

- vitamin component 0.1-2.0

- water the rest

In the antibacterial gel, poly- (4,9-dioxadodecane-1,12-guanidine) phosphate, or polyhexamethylene guanidine citrate / formate, or polyhexamethylene guanidine gluconate / benzoate, or polyhexamethylene guanidine chloride are used as the polyguanidine gel.

In an antibacterial gel, dimethylbenzyl dodecylammonium sulfate is used as a quaternary ammonium compound, and tween-20, or tween-40, or tween-60, or tween-80 are used as the ethoxylated sorbitan ester.

In the antibacterial gel, vitamin A, or vitamin E, or provitamin B ₅ , or a mixture thereof in equal parts is used as the vitamin component.

The highly active polyguanidine compound or its synergistic mixture with a quaternary ammonium compound, dimethylbenzylammonium sulfate, used as a gel, has a wide spectrum of biocidal activity: antibacterial, fungicidal, virucidal. It has low toxicity, does not penetrate intact skin (hazard class IY), remains on it for a long time, protecting it from microorganism attacks.

Dimethylbenzyl dodecylammonium sulfate is synthesized in two stages, starting from benzylamine, dodecyl chloride and dimethyl sulfate.

First, 97 g (1 mol) of benzylamine with 205 g (1 mol) of dodecyl chloride and 40 g (1 mol) of sodium hydroxide are heated at a temperature of 60-80 ° C in an alcohol solution until the precipitation of NaCl. The solution of benzyldodecylamine is filtered off from the NaCl precipitate and quaternized by adding 126 g (1 mol) of dimethyl sulfate and 20 g (0.5 mol) of sodium hydroxide.

The resulting dimethylbenzyl dodecylammonium sulfate is dried at a temperature not exceeding 60 ° C to constant weight. In its antimicrobial activity, the drug is superior to catamine AB and benzalkonium chloride.

Used in the proposed composition as a gelling component, hydroxylpropyl cellulose or hydroxyethyl cellulose refers to non-ionic cellulose ethers and is a white powder material with a content of the main component of at least 97% by weight, polymerization degree of at least 500 (TU 6-05-1857-87).

Methyl ethers of lower alcohols - propylene glycol (TU 6-09-2434-81) and diethylene glycol (GOST 10136-77) possess preservative, sterilizing and bactericidal properties. The hygroscopicity of propylene glycol allows the gel to maintain the desired consistency. The introduction of propylene glycol into the gel increases permeability through the skin.

Chitosan - poly1,4-2-amino-2 deoxy-D-glucan (TU No. 9289-002-11418234-99) used in the proposed composition is a cationic polysaccharide, a structural analogue of cellulose obtained by deacetylation of chitin - a natural biopolymer, which is included in the composition of shells of crustaceans and insects, forms the cellular structures of most fungi and some algae. Chitosan stimulates the body cells involved in immunological defense against pathogenic microorganisms, accelerates wound healing. Chitosan is introduced into the gel as an immunomodulator, viscosity regulator, antiseptic and modifier. In addition, it enhances the action of the main antibacterial component - polyguanidine or its synergistic mixture with a quaternary ammonium compound.

The ethoxylated esters of sorbitan (sorbitals, twins) are nonionic surfactants. They are distinguished by the acid entering the molecule (stearic, oleic, lauric, palmitic) and the degree of hydroxyethylation (5 or 20). They dissolve in water, ethanol, benzene, but do not dissolve in petroleum ether, mineral oils.

Tween-80 (sorbital O-20) sorbitan polyoxyethylene monooleate is a light yellow oily liquid with a basic substance content of 98% (FS 42-2540-88).

Tween-60 (S-20 Sorbital) sorbitan polyoxyethylene monooleate is a light yellow oily liquid with a basic substance content of 96% (TU 6-14-1050-81).

Tween-40 (TL-N) and tween-20 (TL-W) are products of Cao Chemical, Japan.

The ethoxylated esters of sorbitan are introduced to improve the penetration of the gel and improve the stability of the composition.

Polyvinylpyrrolidone (molecular weight from 10,000 to 40,000) is a white powder, readily soluble in water and most organic solvents (FS 42-2238-98).

Polyvinylpyrrolidone (PVP) gives the gel a prolonged effect and is a well-known detoxifier (hemodez). In combination with polyguanidine forms complexes with reduced toxicity. In addition, PVP in the gel composition changes the structure of water in which GHGs are dissolved, which helps to increase the stability and homogeneity of the gel composition.

The copolymers of polyvinylpyrrolidone with acrylates substituted with alkyl amines are products of ISP VAN DYK (USA):

poly (vinylpyrrolidone / dimethylaminoethyl methacrylate) - COPOLIMER 845; and COPOLIMER - 937; poly (vinylpyrrolidone and methacrylamidopropyltrimethylammonium chloride) - POLIQUTENIUM-28 and poly (vinylpyrrolidone / dimethylaminoethyl methacrylate) - POLIQUTENIUM - N.

Trilon B (GOST 10652) is a sodium salt of ethylenediaminetetraacetic acid, complexone III is an organic chelating compound, crystalline, soluble in water, ethanol and most organic solvents.

It is used as titrant in complexometry, for the separation and separation of metal ions, for dissolving and preventing the formation of various deposits, caused, for example, by hardness of water, for the release of toxic metals from the body, stabilization of food products, as water softeners, as components of detergents.

The perfume composition is an oily liquid with a characteristic odor and is introduced into the gel to give it a pleasant smell.

Use a perfume composition with the following odor: apple, peach, apricot, banana, vanilla, cherry, grapefruit, jasmine, honeysuckle, cocoa, cinnamon, kiwi, lavender, lily of the valley, lemon, lime blossom, mango, chamomile, calendula, green tea, fruit -floral and fruit-grassy (mint, burdock, St. John's wort, rosemary, wormwood, eucalyptus, sage, thyme, hops, violet, string).

Manufacturing firms can be: CFF (Italy), “Bell flowers and fragrances” (Germany), or AOZT “Phytotechnology” (St. Petersburg).

Vitamin A affects the metabolic processes of the skin, has a wound healing effect.

Provitamin B ₅ (panthenol) stimulates skin regeneration.

Vitamin E has a regenerating effect, protects the immune system, is an effective antioxidant, and stabilizes the composition.

The quantitative content of the gel components is optimal and is selected on the basis of numerous experiments. Table 1 presents data confirming the optimality of the declared limits.

The process of preparing an antibacterial gel has the following stages. The first - preparation of raw materials and equipment - includes checking the purity of the mixing reactor and weighing the ingredients. The second stage is the dispersion of non-ionic cellulose ethers (hydroxyethyl cellulose or hydroxypropyl cellulose) in diethylene glycol or propylene glycol for 30 minutes at a temperature of 35-40 ° C with periodic mixing of the mass. The mixing mode and design features of the reactor should prevent foaming.

The third stage is the sequential introduction of a weighed amount of water, ethoxylated ester of sorbitan, trilon B, chitosan, polyvinylpyrrolidone or its copolymer into the resulting dispersion with stirring. Next, the mixture is heated to a temperature of 35-40 ° C for 2-4 hours to obtain a homogeneous viscous solution.

The fourth stage is the preparation of an aqueous solution of a disinfectant in a mixer at a temperature of 30-40 ° C for 1.5-2 hours.

The fifth stage is the mixing of components in a reactor-mixer, which is a cylindrical container with a thermostatically controlled stainless steel jacket with a ratio of diameter and height of 1-1.5: 1-2, equipped with a removable cover, inlet fittings and an anchor or turbine type mixer. The prepared homogeneous viscous solution obtained as a result of the third stage of the process, an aqueous solution of a disinfectant, a perfume composition and a vitamin component are poured into the reactor. Water is added to the resulting mass and stirred continuously at a temperature of 25-30 ° C for 1 hour.

Examples of specific performance of the gel.

Example No. 1. Gel antibacterial for hands contains the following components, wt.%:

- hydroxypropyl cellulose 1.5

- propylene glycol 7.0

- phosphate poly- (4.9 dioxadodecane 1.12-guanidine) 1.5

- chitosan 1.0

- twin 20 0.5

- PVP 0.3

- Trilon B 1.0

- perfume composition 0.3

- provitamin B ₅ 1,0

- water the rest

It is used to protect the skin of the hands from the penetration of pathogenic microbes and bacteria. After applying the gel, a thinnest film forms on the skin, which does not dry the skin and does not upset the pH balance.

Example No. 2.

The antibacterial gel for the face contains the following components in wt.%:

- hydroxypropyl cellulose 0.3

diethylene glycol 15.0

- citrate / formate pgmg 0.5

- chitosan 2.0

- twin 60 0.01

- PVP 0.01

- Trilon B 0.1

- perfume composition 0.1

- a mixture of vitamins E and A in a ratio of 1: 1 2,0

- water the rest

It is used for problem skin, does not have an irritating and allergic effect.

Example No. 3. The antibacterial gel for the legs contains the following components in wt.%:

- hydroxyethyl cellulose 3.0

- propylene glycol 0.2

- synergistic mixture of PHMG chloride and

dimethylbenzyl dodecylammonium sulfate 3.0

- chitosan 0.1

- twin 60 1.0

- PVP copolymer with a molecular weight of 10,000 0.5

- Trilon B 2.0

- perfume composition 0.5

- provitamin B ₅ , vitamin E, vitamin A

in the ratio 1: 1: 1 0.1

- water the rest

Eliminates the smell of sweat, protects against infection by fungus and other skin diseases, kills pathogens.

Example No. 4

- hydroxypropyl cellulose 2.5

- propylene glycol 12.0

- gluconate / benzoate PGMG 2.5

- chitosan 1.5

- twin 80 0.05

- PVP 0.3

- Trilon B 0.5

- perfume composition 0.4

- vitamin A 1,5

- water the rest

Eliminates the smell of sweat, protects against infection by fungus and other skin diseases, kills pathogens.

When conducting tests of the antimicrobial activity of the developed antibacterial gel, zones of suppression of microorganisms were determined during the diffusion of the test substance into a solid nutrient medium (Fedorov Yu.A., Koren V.N. “Microbiological methods for the study of dental hygiene products” in the book “Fundamentals of oral hygiene”. L., “Medicine”, 1973, p.3-215).

For this, 20 ml of a dense nutrient medium was poured into a Petri dish. A 24-hour microbial suspension of test microorganisms with a concentration of 5 · 10 ⁵ CFU / ml was prepared and 1 ml of suspension was applied to the surface of the nutrient medium. It was dried for 30 min, and then, in a nutrient medium, wells with a diameter of 6 mm were made into which samples of the developed disinfecting gel were applied. The number of holes should not exceed 6 per Petri dish. For 30 minutes, Petri dishes were kept at room temperature (20 ° C), then they were placed in a thermostat for 24-48 hours at a temperature of 37 ° C and, after this period, the zones of inhibition of microbial growth, including the diameter of the wells, were taken into account. By the size of the zones of growth inhibition of test microorganisms, the antimicrobial effect of the test substance was judged, although it should be borne in mind that the diffusion rate of polymer disinfectants is lower than the diffusion rate of low polymer disinfectants.

To obtain reliable test results for each test substance, it is necessary to carry out in 2-3 series of replicates.

The determination of the minimum time necessary for complete suppression of the growth and development of test microorganisms was carried out for the developed antibacterial gel as follows.

A suspension of test microorganisms was added to the test substance in an amount of 10 ⁵ CFU / ml; for this, 1 ml of the test substance was poured into test tubes. The tubes were shaken and, at intervals of 2-5-10 and 30 minutes, were sown on solid nutrient media. Petri dishes were placed for 24-48 hours in a thermostat at 37 ° C. After this period, the number of colonies grown was counted and the bactericidal activity of the test substance was judged by this indicator.

The results of the studies are presented in table.2.

From the data presented in Table 2, it follows that gram-positive microorganisms (S. aureus) were more sensitive to the tested drugs. All tested agents formed growth retardation zones from 19 to 24 mm, which corresponds to a fairly high activity. The high activity of the preparation according to Example 3 to gram-negative microorganisms of the species E. coli and Ps.aeruginosa is noteworthy.

When determining the rate of manifestation of antimicrobial activity to the tested drugs, the results were obtained, which are presented in table 3.

From the data presented in Table 3, it follows that the antibacterial effect of the developed formulations develops very quickly. After 2 minutes of contact, in no case was live microflora detected after contamination with Escherichia coli.

Tests of the disinfectant gel were carried out on 100 volunteers without a burdened allergic history for 30 days. According to patchwork and application samples, it is shown that the gel is harmless, does not have an irritating and allergenic effect.

Claims (5)

1. An antibacterial gel, including an alkyl hydroxyl compound, a disinfectant, a perfume composition and water, characterized in that propylene glycol or diethylene glycol is used as an alkyl hydroxyl compound, a polyguanidine compound or its synergistic mixture with quaternary additional ammonium or ammonium hydroxy compound is used as a disinfectant, or hydroxypropyl cellulose, chitosan, ethoxylated sorbitan ester, polyvinylpyrrolidone with molecular th weight 10,000-40,000 or copolymer of polyvinylpyrrolidone, Trilon B - sodium salt of ethylenediaminetetraacetic acid, a vitamin component, and water at the following ratio, wt.%: hydroxypropyl cellulose or hydroxyethyl cellulose 0.3-3.0 propylene glycol or diethylene glycol 0.2-15.0 polyguanidine compound or its quaternary synergistic mixture ammonium compound in the ratio 1: 1 0.5-3.0 chitosan 0.1-2.0 ethoxylated sorbitan ester 0.01-1.0 polyvinylpyrrolidone with molecular weighing 10000-40000 or copolymer polyvinylpyrrolidone 0.01-0.5 Trilon B-sodium salt ethylenediaminetetraacetic acid 0.1-2.0 perfume composition 0.2-0.5 vitamin component 0.1-2.0 water rest 2. The antibacterial gel according to claim 1, characterized in that poly- (4,9-dioxadodecane-1,12-guanidine) phosphate or polyhexamethylene guanidine citrate / formate or polyhexamethylene guanidine gluconate or polyhexamethylene guanidine chloride . 3. The antibacterial gel according to claim 1, characterized in that dimethylbenzyl dodecylammonium sulfate is used as a quaternary ammonium compound. 4. The antibacterial gel according to claim 1, characterized in that tween 20, or tween 40, or tween 60, or tween 80 are used as the ethoxylated sorbitan ester. 5. The antibacterial gel according to claim 1, characterized in that vitamin A, or vitamin E, or provitamin B ₅ , or a mixture thereof in equal parts, is used as the vitamin component.