RU2135161C1 - Composition "ritsiniol" for cure and cosmetic care of mucous membranes, skin and hair - Google Patents

Abstract

FIELD: medicine and cosmetics. SUBSTANCE: composition in the form of emulsion includes, mas. %: used as components of fermentative or chemical hydrolysis of vegetable oils: ricinoleic acid, 50.0-70.0; oleic acid, 5.0-7.0; stearic acid, 1.0-3.0; linoleic acid, 1.0-3.0; 10-% glycerine aqueous solution, the balance up to 100%. EFFECT: antiseptic and regenerating action; strengthening of hair bulbs; dandruff elimination. 2 tbl, 7 ex

Description

 The invention relates to medicine, cosmetics and can be used as a tool for the treatment and cosmetic care of mucous membranes, skin and hair.

 Known drug, which is castor oil, obtained by pressing and subsequent cleaning of the seeds of the castor oil plant (M.D. Mashkovsky. Medicines // Pharmacotherapy manual for doctors. - M., "Medicine", 1977, part 1. - S. 335 - 336). The drug is used externally to treat burns, tongue, to soften the skin.

 The disadvantage of the drug with its external use is that it has a weak therapeutic effect, does not have bactericidal properties and is used mainly as a component of ointments and emulsions. There is no noticeable effect when used behind hair and scalp.

 Known skin care product containing vegetable cottonseed oil, plant extracts, including the oil composition of the extracts of succession, elecampane, lycoposia, clover, lemon balm, preservative, phytosterols and the oil fraction of copper derivatives of chlorophyll (Pat. RF N 2010563, IPC A 61 K 7 / 00, publ. 04/15/94). As a preservative, chemically synthesized substance vantole is used.

 The disadvantage of this tool is that it has insufficient preventive, hygienic and therapeutic effect associated with the prevention of diaper rash and skin irritation. The tool slightly inhibits the development of pathogenic microflora.

 In addition, the use of a chemically synthesized substance such as vantole (bronopol) as a preservative has a harmful effect on human skin. The bactericidal properties of vanola are determined primarily by the course of the denitration reaction with the formation of an active form of nitrogen dioxide, which can nitrosate biologically active amino acids and amino groups of proteins. Compounds formed in the form of nitrosoamines have pronounced mutagenic properties. Vanthol penetrates well through the skin and can cause erythema skin and even swelling.

Known tool for hair care "Ashten", containing (wt.%) Stearin 3,5-4,5; lanolin 1-3: emulsion wax 0.5-1.5; glycerol monostearate 1-2; triethanolamine 0.4-0.8; castor oil 2-4; polyethylene glycol stearate 1.5-2.5; distilled glycerin 3-5; primary synthetic higher alcohols of the fatty fraction C ₁₆ -C ₂₀ ; baliz-2 7-12; ethyl alcohol 2-4; paraform 0.03-0.05; dye 0.0008-0.0015; perfume 0.3-0.5; peppermint oil 0.02-0.05; water - the rest (RF patent N 2101004, IPC ⁶ A 61 K 7/06, publ. 10.01.98). The drug provides stimulation of hair growth due to the introduction of such a component as baliz-2, which is a product of bacterial fermentation.

 However, such a tool does not have an antiseptic effect on the skin, and chemically synthesized preservatives such as paraforms have a harmful effect on human skin and have pronounced mutagenic properties. Paraform penetrates well through the skin and with prolonged use as a cosmetic can cause erythema skin and even swelling.

 Known hair care product containing high molecular weight synthetic alcohols, polyvinylpyrrolidone, citric acid, formalin, perfume, water, nonionic hydroxyethylated fatty acid ether and polyglycerol, a cationic surfactant based on quaternary amines and a nonionic emulsifier, L-lecithin from plant materials, a composition comprising coffee fat and oil extract, propolis oil extract and hop extract in a ratio of 1.5: -1: 1 (ed. certificate of the USSR N 1738284, MKI A 61 K 7/06, publ. 07.06.92). The product effectively protects hair and scalp from ultraviolet radiation.

 The disadvantage of this tool is that it has insufficient strengthening and anti-inflammatory effect on the hair and scalp, and also does not eliminate dandruff and itching of the scalp. Surfactants used in the product are harmful to the skin, as they irreversibly block the work of skin enzymes, changing their structure ("turning" the molecule). Formalin, used as a preservative in the product, also creates an irritating effect, denatures skin proteins and enzymes, and to some extent disrupts the normal functioning of the skin's cellular system.

 Known means to stimulate hair growth, including oleic acid (carboxylic unsaturated fatty acid) in an amount of 0.01-10% and testosterone-5L-reductase - the rest (Application of Japan 59-152308, MKI A 61 K 7/06, publ. 1984 )

 However, this hormonal drug should be used only under the supervision of a doctor. In addition, it does not have antiseptic and regenerative effects on the skin.

 The closest technical solution (prototype) is the drug "Linetol", obtained from linseed oil and containing a mixture of ethyl esters of unsaturated fatty acids: oleic (about 15%), linoleic (about 15%) and linolenic (about 57%); the content of saturated acids is 9-11% (MD Mashkovsky. Medicines // Pharmacotherapy manual for doctors. - M., "Medicine", 1977, part 2. - p.14-15). Linetol is used externally for burns, radiation injuries of the skin.

 However, this drug does not have a bactericidal (antiseptic) effect, does not provide for the healing of mucous membranes, the strengthening of hair follicles and the elimination of dandruff.

 The objective of the invention is the creation of such a composition in the form of an emulsion, which would have a wider scope of application due to giving this composition an antiseptic, regenerating effect on the skin, as well as strengthening hair follicles and eliminating dandruff.

This problem is solved in that in the composition for the treatment and cosmetic care of the mucous membranes, skin and hair, including components of the enzymatic or chemical hydrolysis of vegetable oils, according to the invention it additionally contains a 10% aqueous glycerol solution, and as components of the enzymatic or chemical hydrolysis using ricinoleic, oleic, linoleic and stearic acid, in the following quantitative ratio of the components of the composition (wt.%):
ricinoleic acid - 50.0 - 70.0
oleic acid - 5.0 - 7.0
stearic acid - 1.0 - 3.0
linoleic acid - 1.0 - 3.0
10% aqueous glycerol solution - the rest is up to 100%
With a decrease in the composition of the quantitative content of the components below the indicated concentrations, they do not provide the optimal therapeutic and cosmetic effect, and when these concentrations of the components of the composition are exceeded, there is no significant increase in the therapeutic and cosmetic effect.

 It was found that ricinoleic acid in a mixture with other carboxylic acids has an effective bactericidal effect.

 In addition, fatty carboxylic acids have a stabilizing effect on cell membranes, restore their integrity and protect against adverse external influences. They are lighter than the vegetable oils (in particular castor oil), which they are part of, penetrate into the deeper layers of the skin, hair follicles, accelerating the metabolic processes occurring there and participating in them as plastic substances.

 Glycerin (TU 46-4904560-01-91), providing a softening and moisturizing effect, additionally facilitates the transport of substances through the epidermis.

 The invention meets the criteria of patentability, in particular, novelty and inventive step, since the composition of Riciniol as the biologically active components was first introduced by a mixture of fatty carboxylic acids such as ricinoleic, oleic, stearic and linoleic acids, which simultaneously provide bactericidal, regenerating, purifying, painkillers, decongestants, nourishing and strengthening hair roots properties.

 The following are examples of formulations of the proposed composition "Riciniol".

Example 1. Emulsion "Riciniol" for the treatment of mucous membranes
ricinoleic acid - 70.0
oleic acid, - 7.0
stearic acid - 3.0
linoleic acid - 3.0
10% aqueous glycerol solution - the rest is up to 100%
In the early stages of sore throat, pharyngitis, laryngitis, dry nasal mucosa with bleeding, sinusitis are instilled into the nose: children 1-3 drops, and adults up to 10 drops 2-3 times a day. In the case of tonsillitis, the tonsils and the back wall of the throat are additionally lubricated, and in case of stomatitis with a swab moistened with the Riciniol composition, the oral mucosa is lubricated. Recovery occurs in 3-5 days. In the later stages of the disease, the drug can be used in conjunction with other therapeutic drugs.

Example 2. Emulsion "Riciniol" for the treatment of skin of the face, hands and body
ricinoleic acid - 60.0
oleic acid, - 6.0
stearic acid - 2.0
linoleic acid - 2.0
10% aqueous glycerol solution - the rest is up to 100%
In case of bruises, bleeding cuts, burns, a tampon impregnated with Riciniol composition is applied to sore spots. Timely treatment of the burn relieves pain, reduces swelling, prevents the formation of "bubbles" and inflammatory reactions. In case of wounds, cuts, the product provides a stop of bleeding, the tissues heal softly, elasticly without the formation of scars and adhesions.

 It is recommended to rub into the skin with allergies: the rash decreases, the itching is relieved. For osteochondrosis, arthrosis, massage with the use of Riciniol emulsion is recommended. The remedy causes a warming effect, the "stiffness" of the joints and spine is removed, the pain syndrome is removed.

 When used in cosmetics, the product softens the skin, increases its elasticity and tone, has a cleansing and easy exfoliating effect. The emulsion can be used as an independent cosmetic product and as a basis for cosmetic and therapeutic compositions.

Example 3. Emulsion "Riciniol" for the treatment of hair and scalp
ricinoleic acid - 50.0
oleic acid - 5.0
stearic acid - 1.0
linoleic acid - 1.0
10% aqueous glycerol solution - the rest is up to 100%
The Riciniol emulsion has a beneficial effect on the hair follicles and the hair itself, improving their appearance, restoring a healthy structure, giving them a natural shine and elasticity, and eliminating dandruff.

 Before washing, a small amount of Riciniol emulsion is rubbed into the hair roots, followed by moisturizing all the hair. The procedure is carried out for 30 minutes, after which the drug is washed off with shampoo.

Example 4. The technology for the production of emulsion "Riciniol"
The main components of the composition (ricinoleic, oleic, linoleic and stearic acid) are purchased from manufacturers or obtained in other ways. For example, one of the methods for producing ricinoleic, oleic, linoleic and stearic acids is the enzymatic or chemical hydrolysis of castor oil. As an enzyme, lipase can be used. Chemically, ricinoleic acid is obtained by acid or alkaline hydrolysis of castor oil, followed by low-temperature crystallization from methanol or acetone. Oleic, stearic and linoleic acid is obtained by similar hydrolysis of any vegetable oil (linseed, cottonseed, sunflower, etc.) with subsequent fractionation of these acids or their combined use in the proposed composition.

 Glycerin is used in accordance with TU 46-4904560-01-91.

In the reactor with a stirrer at room temperature load in the indicated concentrations (examples 1-3) preheated at 100 ^o C for 30 minutes ricinoleic, oleic, linoleic and stearic acid, as well as a 10% aqueous solution of glycerol. Mixing of all components is carried out in a homogenizer for 5-10 minutes at room temperature, after which the finished Riciniol emulsion is packaged in a container.

 As a result of the experimental selection of the components of the proposed composition "Riciniol" (example 1-3), their synergistic effect in the indicated quantitative ratios is maximally manifested, which ensures maximum therapeutic, preventive and cosmetic effects than the known analogues.

Example 5. Data on testing cosmetic emulsion "Riciniol"
Tests of the proposed emulsion "Riciniol" was carried out on several groups of healthy women from 10-15 people aged 30-50 years with dry, aging and normal skin type. On examination (before the experiment), some patients had dry skin, peeling, sagging, i.e. Signs of premature skin aging. To identify individual sensitivity to the agent, the possibility of its long-term use, preliminary tests were performed, including applying one or two drops of the agent to a clean surface of the elbow bend and monitoring the condition of the skin for 0.5-1 hours. If the surface of the skin at the place of application of the product has not changed, then patchwork was applied to the skin with an exposure of 24 hours. In the case of a negative patch test, the agent was then applied for 3 weeks by applying a thin layer to the skin of the face and neck 1 time per day for 25-30 minutes. The remaining funds were removed with a napkin. During testing, the agents noted its effect on skin color, the presence of wrinkles, fat content and vascular reactions.

 In all patients, patchwork samples were negative. Long-term observations showed that the specified cosmetic product is intended for any type of skin. Absorbency of the composition is good. It softens the skin, relieves the effects of dryness, peeling, inflammation, and has a hydrant effect.

Example 6. The method of medical-cosmetic application of the emulsion "Riciniol" on the scalp and hair
For treatment, the emulsion is applied in small portions to the scalp and hair surface, evenly distributed over the entire length, and rubbed with a light massage. Withstand at least 15 - 30 minutes. Then the hair and head are washed with warm water and dried with a towel.

 To confirm the effect of reducing the formation of dandruff and itching of the scalp when using the proposed composition when comparing with the prototype, special studies were conducted. The data are given in table. 1.

 When comparing the data, it was found that the optimal decrease in dandruff occurs when using the drug and for 3-4 weeks by 95% (Table 1).

 When applying the proposed composition for hair care, an improvement in the physicochemical properties of the hair is additionally provided, and the elasticity and shine of the hair are restored.

 A positive anti-inflammatory effect when using hair care products in comparison with the prototype are given in table. 2.

 During medical procedures, the proposed composition "Riciniol" within 3-4 weeks, the inflammatory phenomena completely disappear (table. 2).

Example 7. Data on the clinical trial of the emulsion "Riciniol"
1. At the Department of Dermatovenereology of the Novosibirsk Medical Institute (conclusion of April 13, 1998), the proposed composition "Riciniol" was tested. The drug was prescribed locally, in the presence of skin rashes, 2 times a day from 3 to 20 days, depending on the severity of the disease, as prescribed by a dermatologist and a cosmetologist. The bactericidal and bacteriostatic effect of "Riciniol" on gram-positive, gram-negative, spore and yeast-like microflora was noted. The product, penetrating into the deeper layers of the skin, regulates the proliferation of fibers of the reticular dermis, increasing their elasticity, reducing swelling, affects the regeneration processes, normalizes skin tone. As a result of clinical trials of Riciniol, a number of indications for use in dermatology and cosmetology have been identified:
- Dermatoses, accompanied by dry skin, hyperkeratinization, peeling;
- diaper rash of the skin;
- some superficial streptoderma;
- decrease in skin elasticity, signs of wilting;
- local swelling of the skin, including with insect bites;
- prevention of foot mycoses;
- protection of the skin from the adverse effects of the environment.

 2. At the Department of Microbiology and Virology of the Novosibirsk Medical Institute, the antibacterial activity of the composition “Riciniol” was tested. The antibacterial effect of the drug was evaluated by diffusion in meat-peptone agar (MPA). For this, in MPA, after planting a test culture on it, the wells were cut with a 10 mm diameter into the test drug using the "lawn" method.

Castor oil was used as a control. Museum cultures of Staph were used as test cultures. aureus, E. coli, P. aeruginosa. Petri dishes were kept for 24 hours at a temperature of 37 ^o C, after which the presence of a zone of lack of growth of the bacteria culture test around the well was determined.

 As a result, it was found that the composition "Riciniol" inhibited the growth of Staph cultures. aureus, E. coli, but did not affect the growth of P. aeruginosa culture. Taken as a control, castor oil did not have an antibacterial effect against all bacterial test cultures.

 Industrial applicability. Cosmetic and therapeutic agent can be used in medicine and cosmetics.

Claims (1)

Composition for the treatment and cosmetic care of mucous membranes, skin and hair, including a 10% aqueous solution of glycerol and, as components of enzymatic or chemical hydrolysis of vegetable oils, ricinoleic, oleic, linoleic and stearic acid in the following quantitative ratio of the components of the composition, wt. %:
Ricinoleic acid - 50.0-70.0
Oleic acid - 5.0-7.0
Stearic acid - 1.0-3.0
Linoleic acid - 1.0-3.0
10% aqueous glycerol solution - The rest is up to 100%

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