RU2500384C1 - Mouth rinse formulation - Google Patents

Abstract

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to dentistry and may be used for making hygienic and therapeutic products for daily dental and oral care, namely to mouth rinses. A mouth rinse formulation contains troxerutin 0.1-0.3 wt % in a combination with ectoin 0.01-1.0 wt %, nicotinamide 0.05-0.1 wt % and a complex of bisabolol and ginger extract 0.01-0.03 wt %, as well as a cosmetically acceptable base containing a water-retaining additive, a structure-forming agent, a filming agent, an anti-caries additive, a flavouring agent and a target additive in the amounts to provide performing the above functions, a biologically active additive consisting of Aloe Vera and herbal infusion, while a medium is water.

EFFECT: formulation provides the effective repair action on the periodontal tissues and high cleansing properties when using the mouth rinse.

14 cl, 2 tbl

Description

The invention relates to dentistry and can be used for the manufacture of hygienic and therapeutic agents for daily care of teeth and oral cavity, namely, means for rinsing the oral cavity.

One of the most common problems a population encounters during daily oral care is bleeding gums during brushing. This is usually a symptom of inflammatory periodontal disease. The main cause of periodontal inflammation is bacteria, which, due to insufficient or improper oral hygiene, accumulate on the teeth in the form of plaque, and are subsequently converted to tartar.

The creation of oral care products used to treat periodontal inflammation and to prevent them is an urgent task.

To solve this problem, rinsing agents are widely known where medicinal herbs are used as the active ingredient. In particular, mouthwashes and elixirs for the oral cavity are known that contain extracts, decoctions and essential oils of medicinal herbs that have antiseptic, hemostatic, antioxidant properties, the ability to improve tissue respiration and metabolism, stimulate immune protective reactions, and promote tissue regeneration.

For example, a dental elixir is known that contains glycerin, ethyl alcohol, sodium fluoride, calcium hydroxyapatite, desorbent pectin, coltsfoot leaf extract, noble laurel, peppermint essential oils, ball eucalyptus and distilled water, taken in a certain ratio. The elixir prevents the formation of plaque and plaque, has remineralizing, effective anti-carious, cleansing and deodorizing effects (Patent RU No. 2355380, IPC A61K 8/18, A61K 8/97, A61Q 11/00, A61P 1/02, publ. 20.05. 2009).

Also known is a therapeutic and prophylactic elixir for oral care, which contains alcohol, a surfactant, glycerin, perfume, a biologically active additive with a chloroform extract of nettle, plantain, myrrh, chamomile and calendula flowers, vitamin “A”, sodium fluoride , anionic surfactant, antiseptic, as a preservative - nipagin, nipazole, perfume, dye. The elixir has a prolonged biological activity, anti-inflammatory ability and a pronounced desensitizing property and is used for gingivitis, periodontitis, for the prevention of dental caries (Patent RU No. 2334522, IPC A61K 36/68, A61K 36/28, A61K 36/185, A61K 8/21 , A61K 8/899, A61Q 11/00, A61P 1/02, published September 27, 2008).

Known transdermal elixir for the oral cavity, which contains biologically active substances isolated during chloroform extraction from a mixture of medicinal herbs, while their delivery to the epithelial cells of the oral mucosa is carried out by a liposome suspension. The elixir is evenly distributed when rinsing on the mucous membrane of the oral cavity, has anti-inflammatory and keratoplastic effects (Patent RU No. 2323245, IPC A61K 8/97, A61K 8/92, A61K 8/34, A61K 8/37, A61K 8/72, A61Q 11 / 00, published on June 27, 2008).

Closest to the claimed invention is an mouth rinse, which as an aqueous medium contains a decoction of herbs obtained by maceration of crushed plant material in a fluidized bed under vacuum in an aqueous medium, followed by preservation with an alcohol-containing composition. The rinse agent also contains a biologically active additive, a water-retaining additive, which is used as glycerin, an anti-caries additive, which is used as sodium fluoride, a preservative, an antimicrobial additive, triclosan, a formative thickener, sodium carboxymethyl cellulose or a copolymer of methylvinyl ether and maleic acid anhydride; 40 hydrogenated castor oil, flavoring agent - sodium saccharinate, softener - Trilon B, traditional target additives: dye, aromatizing a supplement, a pH regulator, and the biologically active additive is a system of СО ₂ extract of woody green Siberian fir, water-alcohol or water-alcohol-glycerin extract of plant materials and aloe juice at a certain ratio of components. Mouthwash provides a combined effect of preventing the formation of dental deposits on the surface of the teeth with a pronounced anti-inflammatory and therapeutic effect for various gum diseases (Patent RU No. 2312657, IPC A61K 8/97, A61K 8/92, A61K 8/34, A61K 8 / 19, A61K 8/40, A61Q 11/00, publ. 12/20/2007).

A disadvantage of the known therapeutic products for oral care is their surface effect on the gums. Active substances that nourish the gums are quickly washed off and removed from the oral cavity, stopping exposure. In addition, when using known means, the therapeutic effect is not accumulated, i.e. exposure to periodontal tissue occurs during direct contact with rinse aid.

The objective of the present invention is to provide an effective means for caring for the oral cavity with the additional effect of deep exposure to periodontal tissues, tangible recovery from the inside, preventing re-inflammation and the accumulation of the above effects over time.

The problem is solved in that the rinse aid composition contains a cosmetically acceptable base, including a moisture-retaining additive, a structure-forming agent, a film-forming agent, an anti-caries additive, a flavoring additive and target additives in quantities that ensure the performance of these functions, a biologically active additive consisting of aloe vera and a decoction of herbs and as a medium - water, characterized in that it further contains active components, which use troxerutin in an amount of 0.1-0.3 wt.%, ectoin in an amount of 0.01-1.0 wt.%, nicotinamide in an amount of 0.05-0.1 wt.% and a complex of bisabolol and ginger extract in an amount of 0.01-0.03 wt.%

The inventive oral rinse composition as target additives may contain a preservative, a dye, a flavoring agent, a softener, a component that provides a cooling effect and a pH regulator, which are used in effective amounts to ensure that they perform the corresponding function.

Troxerutin is a drug, a flavonoid (a semi-synthetic derivative of rutin, γ-benzopyrone), which is used mainly in the treatment of vein diseases, is an angioprotector and corrector for microcirculation, has a venotonic, angioprotective, anti-inflammatory, anti-edematous, antioxidant effect.

Ectoine is a natural substance isolated from halophilic bacteria of the genus Halomonas Elongata, living in extreme conditions of salt marshes and solonchak deserts. Ectoin has unique protective, moisturizing, stimulating and immunomodulating properties, acts at the intracellular level. Introduced into the cellular system, ectoin interacts with free water molecules around biopolymers, forming a powerful “water cocoon” that is resistant to external influences.

Ectoine, acting together with troxerutin, stabilizes the external and internal (mitochondrial and nuclear) cell membranes not only of the capillary walls, but also of nearby tissue cells, thereby helping troxerutin to penetrate deeper and faster, and the moist environment created by ectoin is favorable for the course reactions.

Nicotinamide (synonyms - niacinamide, vitamin PP, vitamin B ₃ ) is a vitamin remedy that eliminates vitamin PP deficiency. This deficiency is often manifested in the oral cavity: glossitis, marginal gingivitis, ulcers on the interdental papillae, stomatitis, disappearance of the papillae of the tongue, increased secretion, and cracked lips.

Nicotinamide helps activate blood flow, thereby enhancing the transport of nutrients. Acting in conjunction with troxerutin, nicotinamide enhances the transport of troxerutin into the capillaries, which allows it to "absorb" in the gum tissue in a fairly short time, i.e. while rinsing the mouth.

The complex of bisabolol and ginger extract is known for its anti-inflammatory efficacy at the cellular level, proven by in vitro and in vivo studies, according to Symrise presentation materials.

Bisabolol is one of the most active components of chamomile oil. Bisabolol relieves tissue inflammation, eliminates irritation, and stimulates cell regeneration.

Ginger has a powerful antimicrobial and strong immunomodulatory effect.

Bisabolol and ginger extract are anti-irritants known in cosmetics. Together with troxerutin, a complex of bisabolol and ginger extract promotes the regeneration of damaged and pathologically altered capillary cells and periodontal tissues, providing an unexpectedly high recovery effect.

As a complex of bisabolol and ginger extract, Symrise Symrelief can be used.

As the water-retaining substance, glycerin can preferably be used.

As the builder, PEG-40 hydrogenated castor oil can preferably be used.

As the film former, a PVM / MA copolymer (copolymer of molyvinyl methyl ether with maleic anhydride - PVM / MA copolymer) can preferably be used.

Sodium fluoride may preferably be used as an anti-caries additive.

As a flavoring agent, saccharin (sodium saccharinate) can preferably be used.

As a dietary supplement, aloe vera gel and a decoction of herbs can be used.

A decoction of herbs can be made by maceration of crushed plant material in a fluidized bed in an aqueous medium, followed by preservation with an alcohol-containing composition, i.e., by the method described in patent RU No. 2306922. The following types of medicinal herbs can be used as plant raw materials for decoction: Stinging nettle (Urtica dioica), Chamomile (Chamomilla recutita), Yarrow (Achilla millefolium), Hypericum perforatum (Hypericum perforatum) Large celandine (Chelidonium majus) preferably in equal parts.

As a preservative, for example, bronopol can be used.

As a colorant, a blue colorant CI 42090 and / or a yellow colorant CI 19140 and / or other known colorants may be used.

As a flavoring agent, Frozen Sage Flavor 508826T flavoring agent may be used, including eugenol and linalool, or other known flavorings.

As a component providing a cooling effect, for example, menthol can be used.

As a pH regulator, for example, sodium hydroxide can be used.

Unexpectedly, we found that even a relatively small administration of troxerutin together with ectoin, nicotinamide, and a complex of bisabolol and ginger extract as part of a therapeutic and prophylactic rinse significantly increases their effectiveness in periodontal inflammation.

Studies conducted at the Ural State Medical Academy (Russia, Yekaterinburg) confirmed that the introduction of troxerutin, ectoin, nicotinamide and a complex of bisabolol and ginger extract in the composition of the claimed rinse significantly reduces bleeding, soreness and swelling of the gums, i.e. the claimed result is achieved, due to the property of troxerutin to quickly penetrate into capillaries, restore their structure and thereby correct blood flow in periodontal tissues, and also due to the properties of ectoin, nicotinamide and a complex of bisabolol and ginger extract, affect the speed and depth of penetration of troxerutin, as well as restoration morphology of periodontal tissues and mucosa.

The inventive composition is prepared as follows.

The estimated amount of decoction of herbs with a structurant is loaded into the cooking apparatus, the resulting mixture is heated with stirring to a temperature of 40-55 ° C. Enter the estimated amount of decoction of herbs, pre-diluting with water - 1 part of a concentrated decoction of herbs with a content of extractive substances of 5.1% per 80 parts of water. A decoction of herbs is used as a biologically active additive to create a biologically active water base of the rinse and is introduced in an amount usual for biologically active additives of 0.1-3.0 wt.%. The resulting mass is cooled to the temperature of the working room and with stirring, the calculated amount of a moisture-retaining substance is used, which is used as glycerin, a flavoring additive, which uses sodium saccharin, an additional biologically active additive, which is used as an aloe vera in the form of a gel, troxerutin, ectoin, nicotinamide, a complex of bisabolol and softener ginger extract, an anti-caries component, which uses sodium fluoride, a dye, in the quality of which is used blue dye CI 42090 and / or dye yellow CI 19140, a preservative, which is used as a bronopol, structure-forming agent, which is used as polyethylene glycol, for example, brand PEG-40, a film former, which is used as a PVM / MA copolymer, component providing a cooling effect, which is used as menthol, a pH regulator, which is used as sodium hydroxide, and an acceptable flavor, for example, Frozen Sage Flavor 508826T, in the following ratio and components, wt.%:

Troxerutin 0.1-0.3 Ectoin 0.01-1.0 Nicotinamide 0.05-0.1 Complex of bisabolol and ginger extract 0.01-0.03 Moisture retention additive 3.0-5.0 Anti-caries supplement up to 0.05

Dietary supplement, including:

Aloe vera gel 1,0-2,0 (dietary supplement) Decoction of herbs 0.1-3.0 (dietary supplement) Structure former 0.5-2.0 Film former 1.5-3.0 Softener 0.01-0.15 Flavoring Additive 0.01-0.1 PH regulator 0.01-1.0 Preservative up to 0.05 Dye 0,0003-0,021 Flavoring 0.1-0.224 Cooling component up to 0.04 Water rest

The resulting composition is homogenized, pumped to the hopper for settling, and then to the filling hopper, from where it enters the packaging machines.

The specific contents of the ingredients of the claimed composition, with the exception of troxerutin, ectoin, nicotinamide and a complex of bisabolol and ginger extract, are preferred and can be changed down or up based on the desired consumer properties of the mouthwash (taste, color, aroma, consistency , expiration date, etc.). A slight change in the content of the ingredients of the claimed compositions, with the exception of troxerutin, ectoin, nicotinamide and a complex of bisabolol and ginger extract, does not have a significant effect on the claimed technical result - a profound effect on periodontal tissues, a noticeable recovery from the inside and prevention of re-inflammation, as well as accumulation these effects over time.

The introduction of troxerutin, ectoin, nicotinamide, and a complex of bisabolol and ginger extract into the rinse composition in excessive amounts exceeding the declared values can lead to irritation and allergic reactions, and the introduction of an amount less than the declared amounts will not lead to a significant result.

The inventive rinse aid composition is illustrated by Examples of specific performance No. 1, 2, 3 (according to the invention), are presented in Table 1.

The inventive rinse according to Example 1 is made as follows.

The estimated amount of decoction of herbs preliminarily diluted with the calculated amount of water is loaded into the cooking apparatus, and the structure-forming agent is heated, the resulting mixture is heated to 40-55 ° C with stirring. The resulting mass is cooled to the temperature of the working room and with stirring, the calculated amount of the remaining ingredients of the inventive composition of Example 1 is loaded into the apparatus. The finished compositions are homogenized, pumped to the silo for settling, and then to the filling hopper, from where it enters the packaging machines.

The decoction of herbs according to Example 1 was made by maceration of crushed plant material in a fluidized bed in an aqueous medium, followed by preservation with an alcohol-containing composition, i.e. by the method described in the patent of the Russian Federation No. 2306922, owned by the applicant. The following types of medicinal herbs were used as a plant raw material for decoction: Stinging nettle (Urtica dioica), Chamomilla chemist (Chamomilla recutita), Yarrow (Achilla millefolium), Hypericum perforatum (Hypericum perforatum), Large celandine (Chelidonium majus) equal shares. A decoction of herbs is added to the rinse aid composition as a biologically active additive.

The rinse aid of Examples 2 and 3 was made in a similar manner.

The properties of the claimed oral rinse composition according to Examples 1, 2, 3 were investigated at the Department of Therapeutic Dentistry of the Ural State Medical Academy (Russia, Yekaterinburg). The tests were conducted in a specially formed group of probes of both sexes (full-time students of the dental faculty) in the amount of 30 people. The group of probes possessed the same level of hygiene skills, had at least 20 teeth in the dental status without caries, periodontitis, crowns and fillings of class V, with local foci of inflammation of the oral mucosa that arose as a result of acute trauma, with signs of gingivitis. The average age was 20.5 years. The probants had no medical contraindications and pledged to use only the rinse aid issued by them and to conscientiously rinse their mouth, according to the manufacturer's recommendations, and brush their teeth with a placebo toothpaste. No other forms of hygienic oral care were allowed during the study period. All study participants were advised to use the same manual toothbrushes, with a Medium bristle hardness of the same manufacturer.

During the study, in accordance with the manufacturer's recommendations, the rinse should be used independently, at home, at least twice a day, after brushing your teeth with a placebo toothpaste, for 60 seconds, 10-15 ml of the solution. At the end of the procedure, it is advisable not to eat or drink for one hour.

Dental examinations were carried out at the Department of Therapeutic Dentistry of the UGMA (before the study, after the first application, after 3, after 7, after 14 days).

Before the study, all participants were conducted:

- inspection;

- training in oral hygiene - the rules of brushing your teeth according to the Pakhomov method;

- professional hygienic treatment of the oral cavity with the removal of soft dental deposits and tartar, followed by polishing of teeth and fillings;

- determination of the initial level of oral hygiene (Green-Vermilion Hygiene Index, OHI-S);

- determination of bleeding gums in inflammatory periodontal disease (IR);

- determination of the severity of gingivitis (PMA index).

During and at the end of the tests, the probants gave an analog-visual assessment of the effect of the claimed mouth rinse, based on subjective sensations.

Table 2 presents the indicators of the hygiene index, bleeding index, the severity of gingivitis when testing the composition of the claimed rinse aid in Example 1. The indicators in examples 2 and 3 throughout the study period were identical. According to the data of Table 2, throughout the entire period of the study there was a fairly uniform decrease in the digital indicators of the hygiene index OHI-S, which indicates a good cleaning effect of the claimed rinse aid. There was also a decrease in bleeding and soreness of the gums, and, in addition, strengthening of the gums, as evidenced by the regression of the bleeding index. Objectively, the gums became denser, wounds, swelling and tension of the soft tissues disappeared, which was confirmed by a change in the PMA index.

As a result of the evaluation of analog-visual data, the probants noted the disappearance of pain, hyperemia, edema in local lesions immediately after using the claimed rinse aid. In addition, the probants noted a long-lasting sensation of a refreshing (deodorizing) effect, the absence of unpleasant sensations and irritating effects, after the first use and within 14 days of use.

The inventive mouth rinse:

- provides daily preventive care for gums;

- prevents the appearance of gum disease;

- relieves the first signs of gum disease (inflammation, swelling, swelling, bleeding, pain in the gums);

- stimulates the process of restoration of periodontal tissues;

- strengthens the blood vessels of the gums;

- normalizes microcirculation in the gums;

- strengthens periodontal tissues;

- improves epithelization of gum tissue;

- improves the general condition of the oral cavity.

Systemic use of the claimed rinse provides a clinically significant reduction in the rate of formation of plaque, has a cleansing effect. In 100% of the probans who regularly used the claimed mouthwash, the condition of the gums improved after the first use. Rinse aid does not cause an allergenic or local irritant effect on the oral mucosa.

Comparison of the data obtained with the data on the prototype allows you to identify the following: the hygiene index compared with the prototype is higher by 12%, while the parameters of the prototype were taken after 4 weeks of use, and the indicators according to the invention after 2 weeks, which indicates a significant increase in the effectiveness of the claimed rinse aid in comparison with the prototype and the accumulation of the result. Indicators of the severity index of gingivitis (gingival index) are comparable with each other, while using the composition of the prototype, the indicators were taken after 4 weeks, and when using the inventive rinse aid - after 2 weeks.

Thus, the studies show that the combined use of troxerutin, ectoin, nicotinamide and a complex of bisabolol and ginger extract as part of a therapeutic and oral mouth rinse leads to new results, namely, it stimulates the restoration and strengthening of periodontal tissues, strengthens the blood vessels of the gums and normalizes microcirculation in them after the first application.

The claimed rinse aid composition combines an effective regenerative effect on periodontal tissues and high cleaning properties, providing an accumulation of positive effects over time.

Table 1 The composition of the claimed rinse name of raw materials Mass fraction of components,% Example according to the invention No. 1 An example according to the invention No. 2 An example according to the invention No. 3 Moisture-retaining additive: Glycerol 3.0 4.0 5,0 Structuring agent: PEG-40 hydrogenated castor oil 1,2 0.5 2.0 Anti-caries supplement: Sodium Fluoride 0.05 0.05 0.05 Film former: PVM / MA Copolymer 2,5 1,5 3.0 Softener: Disodium ethylenediamine-N, N, N'N'-tetraacetic acid salt, 2-aqueous (Trilon B) 0.15 0.01 0.1 Dietary supplement: Aloe vera gel 2.0 1.0 1,5 Decoction of herbs 0.1 1,0 3.0 Active components: Troxerutin 0.2 0.1 0.3 Nicotinamide 0.05 0.08 0.1 Ectoin 0,03 0.05 1,0 Symrelief complex of bisabolol and ginger extract 0,03 0.01 0.02 PH regulator: Sodium hydroxide 0.01 0.05 1,0 Flavoring Additive: Sodium saccharinate 0.01 0.05 0.1 Preservative: Bronopol 0.05 0.05 0.05 Dye: Dye yellow C1 19140 0,0002 0.02 0.005 Dye blue C1 42090 0.0001 0.001 0.001

Fragrance: Frozen Sage Flavor 508826T 0.224 0.15 0.1 Component providing a cooling effect: Menthol 0.04 0.04 0.04 Water 90,3557 91,339 82,634

Claims (14)

1. The composition of the mouth rinse, containing a cosmetically acceptable base, including a moisture-retaining additive, a structure-forming agent, a film-forming agent, an anti-caries additive, a flavoring additive, a targeted additive and a biologically active additive consisting of aloe vera and a decoction of herbs, in quantities that ensure the performance of these functions, and as a medium - water, characterized in that it additionally contains active components, which use troxerutin in an amount of 0.1-0.3 wt.%, ectoine in an amount ve 0.01-1.0 wt.%, nicotinamide in an amount of 0.05-0.1 wt.% and a complex of bisabolol and ginger extract in an amount of 0.01-0.03 wt.%. 2. The rinse aid composition according to claim 1, characterized in that as a water-retaining additive contains glycerin in an amount of 3.0-5.0 wt.%. 3. The rinse aid composition according to claim 1, characterized in that the structure-forming agent comprises PEG-40 hydrogenated castor oil in an amount of 0.5-2.0 wt.%. 4. The rinse aid composition according to claim 1, characterized in that the film former contains PVM / MA Copolymer in an amount of 1.5-3.0 wt.%. 5. The rinse aid composition according to claim 1, characterized in that it contains sodium fluoride in an amount of up to 0.05 wt.% As an anti-caries additive. 6. The rinse aid composition according to claim 1, characterized in that, as a flavoring additive, it contains sodium saccharin in an amount of 0.01-0.1 wt.%. 7. The rinse aid composition according to claim 1, characterized in that as a biologically active additive contains aloe vera gel in an amount of 1.0-2.0 wt.% And a decoction of herbs obtained by maceration of a mixture of nettle, yarrow, celandine, St. John's wort and chamomile in a fluidized bed in an aqueous medium, followed by preservation with an alcohol-containing composition in an amount of 0.1-3.0 wt.%. 8. The rinse aid composition according to claim 1, characterized in that as the target additive contains a pH regulator, which is used as sodium hydroxide in an amount of 0.01-0.1 wt.% 9. The rinse aid composition according to claim 1, characterized in that the target additive contains dye in an amount of 0.0003-0.021 wt.%. 10. The rinse aid composition according to claim 1, characterized in that as a target additive contains a component that provides a cooling effect, which is used menthol in an amount up to 0.04 wt.%. 11. The rinse aid composition according to claim 1, characterized in that as the target additive contains a preservative in an amount up to 0.05 wt.%. 12. The rinse aid composition according to claim 1, characterized in that as the target additive contains a flavoring agent in an amount of 0.1-0.224 wt.% 13. The rinse aid composition according to claim 1, characterized in that as the target additive contains a softener in an amount of 0.01-0.15 wt.%. 14. The rinse aid composition according to claim 1, characterized in that the complex of bisabolol and ginger extract contains the drug Symrelief.