RU2190388C1 - Preparation on base of tea tree oil (versions) - Google Patents

Abstract

FIELD: medicinal cosmetology and dermatology. SUBSTANCE: preparation on base of tea tree oil contains gel-former, moistener, conserving agent, and water. As a gel-former, it contains a substance of polysaccharide origin separated from group of hydroxycellulose, hydroxypropylcellulose, sodium carboxymethylcellulose, hydroxypropylguar, xanthane resin, corragenan, and chitosan. As a conserving agent, preparation includes methylparabene or propylparabene. All components are used in determined quantitative ratio. The preparation is not toxic, easy in application, and has no side effects. EFFECT: protecting function of skin without disturbance of tissue respiration. 2 cl, 7 ex

Description

 The invention relates to the field of hygienic and auxiliary therapeutic agents, in particular to external agents in the field of medical cosmetology, dermatology and antibacterial therapy, in particular in obstetric and gynecological practice.

Known tool containing tea tree oil in its pure form, used for the treatment and prevention of inflammatory, including purulent diseases of the skin and mucous membranes, with colds and infectious diseases (Voitkevich S. A. Essential oils, fragrances, preservatives. Restrictions on use. M .: Food industry. 2000. 96 s.)
Disadvantages are: insufficient efficiency of penetration of the active components of tea tree oil through the skin and mucous membranes, the risk of burns to the skin and mucous membranes, the possibility of an allergic reaction due to 100% oil concentration, and unreasonably high oil consumption.

 A known cleansing and moisturizing agent manufactured by Oriflame (Oriflame catalog, spring 1999) containing tea tree oil, glycerol polymethacrylate, carbomer and tetrahydroxypropyl ethylenediamine as gelling agents, glycerin as a component that reduces the evaporation of water (humectant), propylene glycol solvent of ingredients and a moisture carrier, polysorbate-20 as a solubilizer, disodium ethylenediaminetetraacetate to reduce water hardness, methyl, ethyl, propyl and butyl parabens, imidazolidini l urea and phenoxyethanol as preservatives, menthol for a calming effect on the skin, benzophenone-4 as a sunscreen, yellow gentian extracts, peppermint to reduce sebum, perfumes, colorants CI 42090 and CI 19140.

 The disadvantages of the known gel-like funds are: the use of synthetic gelling agents; the use of a solubilizer that inactivates partially active components due to the strong intermolecular interaction; glycerol polymethacrylate and carbomer, increasing the acidity of the medium; the use of fragrances and dyes, which are potential allergens, menthol, which makes it impossible to use the gel in sensitive skin (eyes, skin around the lips) and especially on the mucous membranes; short contact with the skin, insufficient for the effective manifestation of the therapeutic effect.

 Known protective and prophylactic agent containing tea tree oil, whey proteins, which includes water and oil components, while the water component includes ascorbic acid, polyvidone iodine and water, and the oil component includes vaseline oil and cocoa butter (RF Patent 2150935, A61K 7 / 00, 2000).

 The disadvantages of the known funds include the use in its composition of liquid paraffin, which clogs the pores of the skin and, as a result, violates breathing. In addition, the composition does not provide sufficiently effective transport through the skin of biologically active substances.

 Thus, the authors were faced with the task of developing a composition of a tea tree-based product that would have bactericidal (antiseptic), fungicidal and healing properties, provide the most effective transport of active components through the skin and mucous membranes, and perform a protective function of the skin without disturbing tissue respiration. In addition, it was non-toxic, showed no undesirable side effects, and was convenient to use.

The problem is solved by using a tea tree oil based product containing a gelling agent, a moisturizer, preservatives and water, which contains a polysaccharide substance as a gelling agent selected from the group: hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl guar, xanthan gum, carotenan, carrageenan glycerin, sorbitol or propylene glycol as a humectant, and a mixture of methyl paraben and propyl paraben as a preservative, in the following ratio and the specified components, wt.%:
Tea Tree Oil - 1.00-1.50
A polysaccharide substance selected from the group: hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl guar, xanthan gum, carrageenan, chitosan - 1.10-2.00
Glycerin, sorbitol or propylene glycol - 6.00-20.00
A mixture of methyl paraben and propyl paraben - 0.14-0.30
Water - Up to 100
The problem was also solved by the use of tea tree oil-based products containing oil and water components, in which the oil component includes emulsion wax, cosmetic stearin, glycerol monostearate, stearol, vegetable oil, and the aqueous component includes triethanolamine, polyethylene glycol, preservatives and water with the following ratio of components wt.%:
Tea Tree Oil - 1.00-1.50
Emulsion Wax - 3.40-3.60
Cosmetic stearin - 3.80-4.20
Glycerol monostearate - 1.70-1.90
Stearol - 1.50-1.70
Vegetable oil - 14.30-14.40
Triethanolamine - 0.60-0.80
PEG-400 polyethylene glycol - 6.10-6.20
Preservatives - 0.40-0.50
Water - Up to 100
Currently, the composition of the product based on tea tree oil, which contains these components in the proposed qualitative and quantitative ratio, is unknown from the patent and scientific literature.

 The proposed tool based on tea tree oil, containing a substance of a polysaccharide nature, glycerin, sorbitol or propylene glycol, a mixture of methylparaben and propylparaben and water, can be obtained as follows. In a stainless steel reactor equipped with a propeller stirrer, a polysaccharide substance (1.10-2.00 wt.%), Glycerin, sorbitol or propylene glycol (6.00-20.00 wt.%) And a mixture of methyl paraben and propyl paraben ( 0.14-0.30 wt.%), Stirring is continued until a homogeneous suspension is formed (mixture 1). Mix water (91.76-76.20 wt.%) And tea tree oil (1.00-1.50 wt.%), Obtaining a mixture of 2. While continuing to mix mixture 1, gradually add to it a mixture of 2 and leave on 1 day. The finished product is packaged.

 The use of tea tree oil in the proposed tool in the specified amount (1.00-1.50 wt.%) Provides the most effective manifestation of its properties (bactericidal, antiseptic, fungicidal and healing) and does not cause adverse reactions, in particular it does not cause allergic phenomena and burns.

 As a gelling agent, substances of a polysaccharide nature (hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl guar, xanthan gum, carrageenan, chitosan) are used, which are substances of natural origin, predictably affecting the human body, capable of degrading, including into the natural physiological metabolic chains, funds and without exerting undesirable side effects. A gelling agent content of less than 1.10 wt.% Does not provide sufficient dispersion stability of the composition. When the content of the gelling agent is more than 2.00 wt.% There are technological difficulties in its preparation, namely, it is difficult to mix the solution and packaging of the finished product.

 As a humidifier in the proposed tool use glycerin, sorbitol or propylene glycol. Humidifier limits are due to the following reasons. If the content is less than 6.00 wt.%, The duration of preservation of the lubricating and moisturizing effect is reduced by reducing the ability of the composition to retain moisture. When the content is more than 20.00 wt.% There is no further increase in the moisturizing properties of the product.

 As preservatives, a mixture of methyl paraben and propyl paraben is used. The lower limit (0.13 wt.%) Of the preservative content is sufficient to prevent the emergence and reproduction of microorganisms during the expiration date. The upper limit (0.30 wt.%) Is due to the amount that does not yet have an undesirable effect on the human body.

The proposed tool based on tea tree oil containing oil and water components, in which the oil component includes emulsion wax, cosmetic stearin, glycerol monostearate, stearol, vegetable oil, and the aqueous component includes triethanolamine, polyethylene glycol, preservatives and water, can be obtained as follows . Cosmetic stearin (3.80-4.20 wt.%), Glycerol monostearate (1.70-1.90 wt.%), Stearol (1.50-1.70) are loaded into a stainless steel reactor equipped with a propeller stirrer. wt.%), emulsion wax (3.40-3.60 wt.%), vegetable oil (14.30-14.40 wt.%) and propyl paraben (0.10-0.14 wt.%), heated to 70-75 ^o C and stirring is continued until a uniform transparent mass is formed (mixture 1). Water (67.20-65.20 wt.%), Triethanolamine (0.60-0.80 wt.%), PEG-400 (6.10-6.20 wt.%) And methylparaben (0.30 are mixed) -0.36 wt.%) And heated to 70-75 ^o C (mixture 2). Pour mixture 2 to mixture 1, include a stirrer and dispersant, allow the mass to cool to 40 ^o C. Continuing mixing and dispersion, add tea tree oil (1.00-1.50 wt.%). At temperatures below 30 ^o With the mass of the vacuum. The finished product is packaged.

 The use of tea tree oil in the proposed tool in the specified amount (1.00-1.50 wt.%) Provides the most effective manifestation of its properties (bactericidal, antiseptic, fungicidal and healing) and does not cause adverse reactions, in particular, does not cause allergic phenomena and burns.

 In the proposed tool, emulsion wax is an artificial wax with good emulsifying properties and hydrophilicity, as well as cosmetic stearin and glycerin monostearate, used as emulsifiers. The compounds proposed as an emulsifier mix well with water and significantly improve the water-dispersible properties. The lower limit provides the formation of a stable emulsion, the upper - easy mixing with water and, therefore, quick removal after use.

 As an additional emulsifier, triethanolamine is used - low molecular weight alcohol, hygroscopic, highly soluble in polar solvents, which is also a soft base.

Cosmetic stearin, glycerol monostearate and stearol are used as thickeners. Cosmetic stearin also serves as an auxiliary emulsifier. Glycerin monostearate is an emulsifier that stabilizes and structures the component. Stearol (a mixture of esters of stearic and palmitic acids and high molecular weight alcohols C ₁₇ -C ₁₈ ) is a structure-forming agent. The content of thickeners within the specified limits provides the desired consistency and texture of the product, in particular, allows you to fix the tool on the body.

 Vegetable oil and polyethylene glycol PEG-400 (non-ionic oxygen-containing high molecular weight compound that improves adhesion to the skin and creates a feeling of smoothness) are used as solvents. Content within the claimed limits provides the desired consistency and texture.

 A mixture of methyl paraben and propyl paraben is used as a preservative. The lower limit (0.04 wt.%) Of the preservative content is sufficient to prevent the emergence and multiplication of microorganisms during the expiration date. The upper limit (0.13 wt.%) Is due to the amount that does not yet have an undesirable effect on the human body.

 The proposed technical solution is illustrated by the following examples.

 Example 1. In a stainless steel reactor equipped with a propeller stirrer, 110.0 g of hydroxyethyl cellulose (1.10 wt.%), 600.0 g of glycerin (6.00 wt.%), 10.0 g of methyl paraben (0, 10 wt.%) And 4.0 g of propyl paraben (0.04 wt.%), Stirring is continued until a homogeneous suspension is formed. 9176.0 g of water (91.76 wt.%) And 100.0 g of tea tree oil (1.00 wt.%) Are mixed. Continuing the stirring of mixture 1, mixture 2 is gradually added to it and left for 1 day. Get the final product ready for packaging.

 Example 2. In a stainless steel reactor equipped with a propeller stirrer, 200.0 g of hydroxyethyl cellulose (2.00 wt.%), 2000.0 g of glycerin (20.00 wt.%), 23.0 g of methyl paraben (0, 23 wt.%) And 7.0 g of propyl paraben (0.07 wt.%), Stirring is continued until a homogeneous suspension is formed. 7620.0 water (76.20 wt.%) And 150.0 g of tea tree oil (1.50 wt.%) Are mixed. Continuing the stirring of mixture 1, mixture 2 is gradually added to it and left for 1 day. Get the final product ready for packaging.

Example 3. In a stainless steel reactor equipped with a propeller stirrer, cosmetic stearin 380.0 g (3.80 wt.%), Glycerol monostearate 170.0 g (1.70 wt.%), Stearol 150.0 g ( 1.50 wt.%), Emulsion wax 340.0 g (3.40 wt.%), Vegetable oil 1430.0 g (14.30 wt.%) And propyl paraben 10.0 g (0.10 wt.%) ), heated to 70-75 ^o C and continue stirring until a uniform transparent mass is formed (mixture 1). Water is mixed 6720.0 g (67.20 wt.%), Triethanolamine 60.0 g (0.60 wt.%), PEG-400 610.0 g (6.10 wt.%) And methyl paraben 30.0 g (0.30 wt.%) And heated to 70-75 ^o C (mixture 2). Pour mixture 2 to mixture 1, include a stirrer and dispersant, allow the mass to cool to 40 ^o C. Continuing mixing and dispersion, add tea tree oil 100.0 g (1.00 wt.%). At temperatures below 30 ^o With the mass of the vacuum. The finished product is packaged.

Example 4. In a stainless steel reactor equipped with a propeller stirrer, cosmetic stearin 420.0 g (4.20 wt.%), Glycerol monostearate 190.0 g (1.90 wt.%), Stearol 170.0 g ( 1.70 wt.%), Emulsion wax 360.0 g (3.60 wt.%), Vegetable oil 1440.0 g (14.40 wt.%) And propyl paraben 14.0 g (0.14 wt.%) ), heated to 70-75 ^o C and continue stirring until a uniform transparent mass is formed (mixture 1). Water is mixed 6520.0 g (65.20 wt.%), Triethanolamine 80.0 g (0.80 wt.%), PEG-400 620.0 g (6.20 wt.%) And methyl paraben 36.0 g (0.36 wt.%) And heated to 70-75 ^o C (mixture 2). Pour mixture 2 to mixture 1, include a stirrer and dispersant, allow the mass to cool to 40 ^o C. Continuing mixing and dispersion, add tea tree oil 150.0 g (1.50 wt.%). At temperatures below 30 ^o With the mass of the vacuum. The finished product is packaged.

 Example 5. Patient M., 28 years old, underwent a course of treatment with a papulopustular form of acne. For 9 days, the patient applied a gel-like product based on tea tree oil to the inflamed areas of the face and neck 2 times a day with a complete rejection of the use of oily creams and decorative cosmetics. On the 4th day of use, a decrease in the total area of inflammation, rapid drying of the crusts was observed. On the 8th-9th day, skin functions were almost completely normal.

 Example 6. Patient K., 32 years old, underwent a course of wellness treatment. After mechanical cleaning of the face for 2 days, the patient applied a gel-like agent based on tea tree oil to the inflamed areas of the face and neck 2 times a day. Further treatment consisted of the use of a creamy product based on tea tree oil due to the fact that the patient had thin dry skin and the use of the gel caused a feeling of tightness of the skin of the face. The product was applied in the morning as a base for makeup and in the evening. On the 4th day of using the product, almost complete healing of the skin after cleansing was observed, an even tone of the face, the absence of foci of inflammation were noted.

 In total, 27 patients with various forms of acne, oily seborrhea, and also after mechanical cleansing of the face were treated. Due to the violation of the integrity of the skin and its barrier functions, the structure of the lipid mantle, the reaction of the skin to topical therapy is ambiguous, the use of many cosmetics, including, in addition to therapeutic ones, components such as lipid structurants, polymer stabilizers, etc., is limited. The duration of treatment depends on the type of disease: with practically healthy skin after mechanical cleaning and with oily seborrhea, the course is 3-5 days (a gel-like product is applied to the skin 2 times a day), with mild and moderate forms of acne - at least 7 days, with cystic form - 7-30 days. No adverse reactions noted.

 Thus, the proposed tool based on tea tree oil has the properties necessary for use in medical cosmetology, namely: bactericidal action, high penetrating ability of the antiseptic factor, protective ability without disturbing tissue respiration, healing effect (affects reparative processes, creates a film effect ), antipruritic effect. When treated with a tea tree oil-based product, there is a significant decrease in inflammatory processes, post-traumatic erythema, the absence of itching, and a decrease in skin greasiness.

 Example 7. Patient B., 32 years old, during 2000 treated four times with symptoms of recurrent herpes simplex: hyperemia and erosion on the face (lips and nose), pain, burning and itching. Treatment with a gel-like tea tree oil-based agent was started on the second day of relapse. The gel was applied by the patient on his own three times a day. On the 3rd day of relapse (2nd day of treatment), a decrease in burning and itching was observed, on the 4th-5th day, crust formation was observed. A complete disappearance of symptoms was observed on the 6th day of relapse (5th day of treatment), while in the usual course of relapse lasted 8-9 days.

 A total of 40 patients with various forms of herpes virus infection were treated (19 men, 21 women, the average age of patients was 30.1 years). External treatment with a gel-like agent based on tea tree oil was prescribed in the first 24-28 hours from the onset of relapse and was carried out in combination with oral administration of acyclovir. The tool was used by patients on their own 3-4 times a day at the clinical stage of the disease in the form of vesicle elements, erosion, crusts.

 As a result of the use of tea tree oil-based products in 100% of patients, the total duration of relapse was reduced by more than 2 times (from 8.46 ± 2.03 to 4.71 ± 0.13 days), crust formation occurred on day 2-3 treatment, subjective sensations in the form of itching, burning and soreness in the area of rashes decreased or disappeared for 1-2 days. Thus, the effectiveness of external therapy is estimated as a significant improvement in 75% of cases and an improvement in 25%.

 In addition, all patients noted a good appearance of the product based on tea tree oil and a convenient consistency for use. An agent based on tea tree oil can be used as an effective external therapy in the treatment of simple and genital herpes.

 Tea tree oil-based agent can be used to treat bacterial vaginosis in pregnant women, because it contains a natural broad-spectrum bactericidal component (non-specific), which has an advantage over most known antibiotics, does not cause complications during pregnancy, maintains a satisfactory condition of the placental complex, reduces the likelihood complications during childbirth and, therefore, the need for prompt delivery, stimulates the immune system and is tsya effective in topical treatment in the field of obstetrics and gynecology.

 Tea tree oil-based product can be used for inflammatory, post-traumatic and postoperative diseases of the oral cavity (gums, teeth), for injuries (wounds, cuts, burns) in various parts of the body, for colds for inhalations and rinses, as an antifungal (fungicidal ) facilities.

 Thus, the use of the proposed composition based on tea tree oil components in the specified combination and ratio provides the most efficient transport of active components through the skin and mucous membranes, performs a protective function of the skin without disturbing tissue respiration. Along with this tool based on tea tree oil is non-toxic, convenient to use. Undesirable side effects were not detected. The composition based on tea tree oil does not include components prohibited for use in products intended for contact with skin and mucous membranes.

Claims (1)

1. Tool based on tea tree oil, containing a gelling agent, a moisturizer, preservatives and water, characterized in that it contains a polysaccharide substance as a gelling agent selected from the group: hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl guar, xanthan gum, carotenan , as a humectant, glycerin, sorbitol or propylene glycol, and as a preservative, methylparaben or propylparaben, or a mixture thereof, in the following ratio of these components ntov, wt.%:
Tea Tree Oil - 1.00-1.50
A polysaccharide substance selected from the group: hydroxyethyl cellulose, hydroxypropyl cellulose, sodium carboxymethyl cellulose, hydroxypropyl guar, xanth gum, carrageenan, chitosan - 1.10-2.00
Glycerin, sorbitol or propylene glycol - 6.00-20.00
A mixture of methyl paraben and propyl paraben - 0.14-0.30
Water - Up to 100
2. A tool based on tea tree oil containing oil and water components, characterized in that the oil component includes emulsion wax, cosmetic stearin, glycerol monostearate, stearol, vegetable oil, and the aqueous component includes triethanolamine, polyethylene glycol, preservatives and water in the following ratio components. wt.%:
Tea Tree Oil - 1.00-1.50
Emulsion Wax - 3.40-3.60
Cosmetic stearin - 3.80-4.20
Glycerol monostearate - 1.70-1.90
Stearol - 1.50-1.70
Vegetable oil - 14.30-14.40
Triethanolamine - 0.60-0.80
PEG-400 polyethylene glycol - 6.10-6.20
A mixture of methylapraben and propyl paraben - 0.40-0.50
Water - Up to 100E