JP2023033269A - external composition - Google Patents

Abstract

To provide an external composition that can clean a tooth, a gum, a tongue, an oral cavity even if the tooth or oral cavity is not polished by a brush, and can be drunk after cleaning, before cleaning or during cleaning, and is harmless and safe even it is taken into a body.SOLUTION: Sphinganine, sphingosine, sphingenine, sphingadienine, methyl-sphingadienine, or amino-methyl-octadecatriene-diol by 0.01 wt.% to 80 wt.%, and water, alcohol or oil by 10 wt.% to 90 wt.% are mixed. Sphinganine, sphingosine, sphingenine, sphingadienine, methyl-sphingadienine, or amino-methyl-octadecatriene-diol is contained in a sea cucumber or the like, has a cleaning effect, and is harmless and safe even taken into a body.SELECTED DRAWING: None

Description

TECHNICAL FIELD The present invention relates to external compositions such as toothpastes and mouthwashes, and to external compositions that are harmless and pose no problem even when taken into the body.

A wide variety of topical compositions, especially toothpastes and mouthwashes, have been considered for the prevention of tooth decay, periodontal disease, halitosis, and the like. Accordingly, various production methods have been considered.

JP 2010-265189 A Japanese Unexamined Patent Application Publication No. 2006-028148 JP 2005-073588 A Japanese Patent Application Laid-Open No. 2008-149802 Japanese Patent Publication No. 2004-500378 JP 2010-270157 A Japanese Patent Publication No. 2006-508182 JP-A-10-120510 JP-A-10-029927 Japanese Patent Application Laid-Open No. 2010-013400 Chinese Patent Application Publication No. 102058502 JP-A-2000-143437 Journal of Ethnopharmacology, 2004, vol.92

The present invention has been made to solve the above-mentioned problems, and an object of the present invention is to provide a composition for external use that is safe and harmless even if it is swallowed, eaten, or drunk and absorbed in the gastrointestinal tract. It is about providing things.

Therefore, the topical composition of the present invention contains sphinganine, sphingosine, sphingenine, sphingadienine, methyl-sphingadienine, or amino-methyl - 0.01% to 80% by weight of octodecatriene-diol and 10% to 90% by weight of water, alcohol or oil, not exceeding 100% by weight in total. and mixed.

Therefore, these ingredients can be swallowed, eaten, or drunk, and can be absorbed through the gastrointestinal tract without any problem or harm. The composition for external use (including toothpaste and mouthwash; the same shall apply hereinafter) can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and can be used after, before, and during cleaning. It is also possible to drink In particular, it is convenient for people who have difficulty in brushing their teeth or washing their mouths, such as the disabled and the elderly, and can provide a harmless and safe composition for external use even when taken into the body from the back of the throat. Of course, this composition for external use may also be used by healthy people.

(1) Composition of topical compositions (toothpaste, mouthwash) External compositions, such as toothpastes and mouthwashes, include sphinganine, sphingosine, sphingenine, and sphingadienine. , methyl-sphingadienine, or amino-methyl-octadecatriene-diol from 0.01% to 80% by weight, water, alcohol or oil 10% to 90% by weight, but not exceeding 100% by weight in total.

Here, one or more of the above sphinganine, sphingosine, sphingenine, sphingadienin, methyl-sphingadienine, amino-methyl-octodecatriene-diol may be excluded, or one of these One or more may be selected and mixed.

Sphinganine, sphingosine, sphingenine, sphingadienin, methyl-sphingadienine, or amino-methyl-octodecatriene-diol is 0.01% to 80% by weight, preferably 1% to 70% by weight. %, mixed.

The chemical formula of the above sphinganine is shown in "Chemical Formula 1", and this sphinganine is a long-chain aminoalcohol having 18 carbons. It forms the main part of sphingolipids and is a compound belonging to a group of cell membrane lipids including sphingomyelin, which is one of the important phospholipids, and has anti-inflammatory effects.

The numbers in the above and following chemical formulas are originally displayed in small sizes at the bottom right of the respective chemical symbols, but in the present application, they are displayed in large normal size for the sake of convenience to make them easier to read.

The chemical formula of the above sphingosine (2-amino-4-octadecene-1,3-diol) is shown in "Chemical 2", and this sphingosine is a long-chain aminoalcohol having 18 carbons and one unsaturated Contains hydrocarbon chains. It forms the main part of sphingolipids and is a compound belonging to a group of cell membrane lipids including sphingomyelin, which is one of the important phospholipids, and has anti-inflammatory effects.

This sphingosine is phosphorylated in vivo by two kinases, sphingosine kinase type 1 and type 2. This leads to the synthesis of sphingosine-1-phosphate, which serves as a signaling lipid. Metabolism of sphingolipids such as ceramide, sphingosine and sphingosine-1-phosphate becomes lipid signaling molecules in various intracellular reaction processes.

The chemical formula of the sphingenine is shown in Chemical Formula 3, and this sphingenine is a long-chain aminoalcohol having 18 carbons. It forms the main part of sphingolipids and is a compound belonging to a group of cell membrane lipids including sphingomyelin, which is one of the important phospholipids, and has anti-inflammatory effects.

The chemical formula of the above sphingadienin is shown in Chemical Formula 4, and this sphingadienin is a long-chain aminoalcohol having 18 carbons. It forms the main part of sphingolipids and is a compound belonging to a group of cell membrane lipids including sphingomyelin, which is one of the important phospholipids, and has anti-inflammatory effects.

The chemical formula of the above methyl-sphingadienine is shown in Chemical Formula 5, and this methyl-sphingadienine is a long-chain compound having 19 carbons and a methyl group. It forms the main part of sphingolipids and is a compound belonging to a group of cell membrane lipids including sphingomyelin, which is one of the important phospholipids, and has anti-inflammatory effects.

The chemical formula of the above amino-methyl-octodecatriene-diol is shown in Chemical Formula 6, and this amino-methyl-octodecatriene-diol is a long-chain compound having 19 carbons and a methyl group. It forms the main part of sphingolipids and is a compound belonging to a group of cell membrane lipids including sphingomyelin, which is one of the important phospholipids, and has anti-inflammatory effects.

The sphingenine may be other sphingenines, such as 8-sphingenine, 4-sphingenine, . The sphingadienines may be other sphingadienines, such as 4,8-sphingadienines, . . . The above methyl-sphingadienine may be other methyl-sphingadienines, other sphingadienines, such as 9-methyl-4,8-sphingadienine, .

The above amino-methyl-octadecatriene-diol is, for example, 2-amino-9-methyl-4,8,10-octodecatriene-1,3-diol, etc. amino-methyl-octodecatriene-diol, other methyl-octodecatriene-diol, other methyl-sphingadienine, other octodecatriene-diol, and other octodecatriene.

Examples of the above alcohols include butylene glycol (butanediol), ethylene glycol, styrene glycol, propylene glycol, propanol, ethanol, methanol, primary alcohols, secondary alcohols, ..., dihydric alcohols, trihydric alcohols, ..., ... Other alcohols such as

One or more of the above water, alcohol, and oil may be excluded, or only one of them may be selected and mixed. Water, alcohol or oil is mixed in an amount of 10% to 90% by weight, preferably 15% to 80% by weight. As a result, it becomes water-based, oil-based, and alcohol-based, and can be switched or used properly according to the nature of the dirt in the mouth.

(2) Washing Sphingenine, sphingosine, sphingenin, sphingadienin, methyl-sphingadienine, amino-methyl-octodecatriene-diol can be used on the surface of teeth, the surface of gums, the surface of the mouth, the surface of the tongue, etc. liberates, melts, removes, and decomposes various contaminants attached to The tooth includes enamel, cementum, crown, root, gingiva, dentin, and the like. These various stains include dental plaque, plaque, food debris, acid stains, alkaline stains, neutral stains, stains before putrefaction, stains after putrefaction, miscellaneous germs, bacteria, and the like.

These stains cause various oral diseases such as periodontal disease, caries, periodontitis, gingivitis, alveolar pyorrhea, halitosis, and stomatitis. Fingadienin, Amino-Methyl-Octodecatriene-Diol, is intended to prevent/treat these diseases by removing said stains.

Such stain removal acts like a surfactant, but cleanses the teeth, gums, tongue, mouth, and mouth to liberate, melt, and remove the stain without brushing the teeth or oral cavity. , can be decomposed. After such cleansing, the topical composition, toothpaste, mouthwash is harmless if swallowed, eaten, drunk, gastrointestinal absorption, ingestion, or ingestion into the body. and safe.

For the above cleaning, the topical composition, toothpaste, and mouthwash may be rinsed in the mouth, but the mouth may be opened and sprayed into the mouth. / Air flow / gas flow, or impregnated with cleaning cloth, paper, normal cloth, paper, etc. with uneven surface, surface of teeth, surface of gums, surface of mouth, back surface of tongue, etc. may be wiped or polished.

(3) Production method of external composition (toothpaste, mouthwash) sea cucumber, sea urchin).

Since sea cucumbers are edible, they are harmless and safe even if taken deep into the body. The sea cucumber is a general term for echinoderms of the sea cucumber class. The body is cylindrical and bilaterally symmetrical, with three rows of tube feet on the ventral surface, many tentacles around the mouth, and a flexible outer skin. has tiny spicules. Widely distributed in shallow to deep waters, deep-sea ones have agar-agar bodies. Sea cucumbers such as manamako, kinko, and wisteria sea cucumber are eaten raw, and the dried ones are called 'iriko' and used as an ingredient in Chinese cuisine. This is called.

The sea cucumber may be dried or wet, finely chopped or ground, or as such, soaked in alcohol, such as ethanol, at room temperature (0°C to 20°C), or water (0°C to 20°C). ° C.) or hot water (20° C.-100° C.) and optionally hydrolyzed with potassium hydroxide (4M KOH in ethanol).

As a result, components such as sphinganine, sphingosine, sphingenin, sphingadienin, methyl-sphingadienine, amino-methyl-octodecatriene-diol contained in sea cucumber are extracted into this alcohol, water or hot water, and these components are refined.

Such alcoholic and aqueous solutions form a series of amphiphilic compounds called sphingoid bases. Amphiphilic compounds are compounds that combine hydrophobic and hydrophilic moieties and are capable of liberating, dissolving, removing and decomposing water-based soils and dissolving, dissolving, removing and decomposing oil-based soils.

The remaining sea cucumber from which the above components have been extracted is usually filtered from the alcohol and water and discarded, but may be left in the alcohol and water. In this case, 0.01% to 80% by weight of the above components are mixed with 10% to 90% by weight of alcohol or water. By such extraction and purification, the alcoholic solution and aqueous solution become the alcoholic solution and aqueous solution of the above components.

This alcoholic or aqueous solution may optionally further contain a wetting agent such as 0.001% to 5% by weight, preferably 0.01% to 2.5% by weight of glycyrrhizic acid, an abrasive such as calcium carbonate 1% by weight. % to 60% by weight, preferably 10% to 40% by weight, a sweetener such as xylitol 0.1% to 20% by weight, preferably 0.5% to 5% by weight, a humectant such as glycerin 1% by weight. % to 50% by weight, preferably 5% to 30% by weight, a wetting agent such as 0.1% to 20% by weight, preferably 1% to 10% by weight of sorbitol, are added, mixed and thoroughly stirred. The temperature is maintained at 0°C to 20°C while heating until reaching 20°C to 100°C as the case may be. Sterilization is also performed by this heating.

Then, optionally, an abrasive such as hydroxyapatite 0.1% to 10% by weight, preferably 0.5% to 5% by weight, is added, mixed and maintained at temperature for 1 minute to 100 minutes. , and stir well.

and optionally a binder such as carrageenan 0.001% to 5%, preferably 0.01% to 2.5%, a binder such as xanthan gum 0.01% to 10% by weight. , desirably 0.3% to 5% by weight, are added, mixed, and thoroughly stirred for 1 minute to 200 minutes while maintaining the temperature.

and, optionally, a cooling agent such as mint oil 0.001% to 5%, preferably 0.01% to 2.5% by weight, a flavoring agent such as sea salt or table salt or other salt 1% by weight. 50% to 50% by weight, preferably 5% to 30% by weight, are added, mixed, and thoroughly stirred for 10 minutes to 180 minutes while maintaining the temperature at 10°C to 60°C. It is used as a topical composition, toothpaste and mouthwash. Here, water is contained in an amount of 10% to 90% by weight.

Mixing and stirring of the abrasive, such as the hydroxyapatite, or the cooling agent, such as the peppermint oil, may be omitted. Also, the mixing and stirring of the humectant, such as the xanthan gum, or the binding agent, such as the carrageenan, or the humectant, such as the glycyrrhizic acid, may be omitted.

Further, mixing and stirring of the wetting agent, such as the sorbitol, or the sweetener, such as the xylitol, may be omitted. Still further, the mixing and stirring of the flavoring agent, such as the sea salt or table salt or other salt, may be omitted. Furthermore, the mixing and stirring of the abrasive, such as the calcium carbonate, or the wetting agent, such as the glycerin, may be omitted.

(4) Other Embodiments/Examples The present invention is not limited to the above-described examples, and some steps can be omitted without departing from the scope of the present invention. For example, the water may be partially or wholly replaced with alcohol or oil, or the alcohol and water may be further mixed with alcohol, water or oil.

The above sphinganine, sphingosine, sphingenin, sphingadienin, methyl-sphingadienine, and amino-methyl-octodecatriene-diol are collected and extracted from sea cucumber, other edible fish and shellfish, and edible animals and plants. may be The composition for external use, toothpaste, and mouthwash of the present invention may not be taken into the body, but may be spit out or washed with a toothbrush or the like.

In this case, 10% to 90% by weight, preferably 20% to 60% by weight of alcohol, or 10% by weight of oil, to 10% to 90% by weight, preferably 20% to 60% by weight of water. % to 90% by weight, preferably 20% to 60% by weight.

In this case, 0.1 wt % to 20 wt %, preferably 0.5 wt % to 10 wt % of surfactant may be mixed. As a result, the composition for external use or the aqueous solution becomes an emulsion or microemulsion.

Examples of alcohols include methanol, ethanol, propanol, butanol, hexane, lower alcohols, and higher alcohols. The above oils may be derived from plant seeds such as cottonseed, rice bran, rapeseed, palm, palm, soybean, corn, sesame, hexane, and the like, and from plants such as fruits, but animal oils may also be included.

The sphinganine, sphingosine, sphingenine, sphingadienin, methyl-sphingadienine, amino-methyl-octodecatriene-diol are ” With respect to the chemical formula of “Chem. 6”, the parts shown in “Chem. 7”, “Chem. 8”, “Chem. 9”, “Chem. However, they may be isomers, and each atom may be an isotope.

For example, the portion of “Chem. or 13 in total, or any other number may be used. Similarly, the double bond or single bond portion of "Chem. 7", "Chem. 8", "Chem. 9", "Chem. 10", "Chem. 11", and "Chem. Other numbers may be used.

The above double bond or single bond may be a single bond, double bond, triple bond, . The double bond portion of "Chemical 9", "Chemical 10", "Chemical 11", and "Chemical 12" may be a single bond, a triple bond, . . . A double bond, a triple bond, . . .

Substances with these chemical structures are also extracted from sea cucumbers, have a cleansing effect, and are safe and harmless when taken into the body. In addition to toothpastes and mouthwashes, the above external compositions include soaps, ointments, body lotions, facial cleansing lotions, hair lotions, skin creams, hair creams, hair shampoos, hair rinses, hair conditioners, skin hair conditioners, cosmetics, and lotions. , kitchen detergent, ware detergent, building detergent, etc.

Examples of the abrasive include, in addition to calcium carbonate and hydroxyapatite, heavy calcium carbonate, silica, titanium oxide, calcium hydrogen phosphate, hydrated silicic acid, dicalcium pyrophosphate, calcium pyrophosphate, sodium pyrophosphate, microcrystalline wax, Dicalcium phosphate, calcium hydrogen phosphate, sodium hydrogen phosphate, sodium carbonate, titanium oxide, anhydrous silicic acid, egg shell, aluminum hydroxide, sodium bicarbonate, and the like may also be used.

Examples of the humectant include glycerin, sorbitol and glycyrrhizic acid, as well as polyethylene glycol, propylene glycol and glycerol. Examples of the binder include xanthan gum, carrageenan, carboxymethyl cellulose sodium, carboxymethyl sodium, sodium alginate, CMC, and the like.

As the sweetener, in addition to xylitol, fruit oils such as orange oil, orange peel oil, grapefruit fruit oil, and grapefruit peel oil, synthetic sweeteners, artificial sweeteners, and the like may be used. Examples of the flavoring agent include sea salt, table salt, and other salts, as well as saccharin sodium, menthols, mints, orange oil, and orange peel oil.

Foaming agents such as sodium lauryl sulfate, sodium lauroyl sarcosine, and sucrose fatty acid esters may be mixed and stirred with the external composition, toothpaste, and mouthwash. Preservatives such as sodium benzoate and parapenes may be mixed and stirred with the external composition, toothpaste, and mouthwash. The cooling agent may be mint oil, menthol, carvone, or the like.

The external composition, toothpaste, and mouthwash are almost non-viscous liquids such as toothpaste, powder toothpaste, liquid toothpaste, solid toothpaste, cream toothpaste, sol-like toothpaste, gel-like toothpaste, gel-like toothpaste, There are viscous toothpastes such as paste toothpastes, foam toothpastes, and various others. In addition, this toothpaste and mouthwash can be applied to a toothbrush or the like to brush teeth, or to be put in the mouth for rinsing, gargling, massage with fingers, etc., applying as described above, There are wipes and sprays.

(5) Effects of other inventions [1] sphinganine, sphingosine, sphingenine, sphingadienine, methyl-sphingadienine, or amino- 0.01% to 80% by weight of amino-methyl-octadecatriene-diol, 10% to 90% by weight of water, alcohol or oil, not exceeding 100% by weight in total A topical composition characterized in that it is mixed in a range.

[2] The composition for external use according to [1], wherein the composition for external use is a toothpaste or mouthwash. As a result, the composition for external use can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and has a cleaning effect, and can be drunk after cleaning, before cleaning, and during cleaning. It is harmless and safe even if taken into the body.

[3] The above-mentioned toothpaste or mouthwash cleanses the teeth, gums, tongue and oral cavity without brushing the teeth or the oral cavity, and can be taken into the back of the throat after cleaning. 2. The composition for external use according to 2 above. As a result, the composition for external use can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and has a cleaning effect, and can be drunk after cleaning, before cleaning, and during cleaning. It is harmless and safe even if taken into the body.

[4] The external composition according to [3], which is a toothpaste or mouthwash for preventing and treating periodontal disease. Thus, the composition for external use can prevent or treat periodontal disease, can be drunk after washing, before washing, or during washing, and is harmless and safe even if taken into the body.

[5] The composition for external use according to [3], wherein the composition for external use is a toothpaste or mouthwash for preventing and treating caries. Thus, the composition for external use can prevent or treat caries, can be drunk after washing, before washing, or during washing, and is harmless and safe even if taken into the body.

[6] The composition for external use according to [4] or [5], wherein the sphingenine is 8-sphingenine. As a result, the composition for external use can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and has a cleaning effect, and can be drunk after cleaning, before cleaning, and during cleaning. It is harmless and safe even if taken into the body.

[7] The composition for external use according to [4] or [5], wherein the sphingadienine is 4,8-sphingadienine. As a result, the composition for external use can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and has a cleaning effect, and can be drunk after cleaning, before cleaning, and during cleaning. It is harmless and safe even if taken into the body.

[8] The composition for external use according to [4] or [5], wherein the methyl-sphingadienine is 9-methyl-4,8-sphingadienine. As a result, the composition for external use can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and has a cleaning effect, and can be drunk after cleaning, before cleaning, and during cleaning. It is harmless and safe even if taken into the body.

[9] The amino-methyl-octadecatriene-diol is 2-amino-9-methyl-4,8,10-octodecatriene-1,3-diol The composition for external use according to claim 4 or 5, characterized by: As a result, the composition for external use can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and has a cleaning effect, and can be drunk after cleaning, before cleaning, and during cleaning. It is harmless and safe even if taken into the body.

[10] The composition for external use according to [4] or [5], wherein the alcohol is butylene glycol (butanediol). As a result, the composition for external use can clean teeth, gums, tongue, and oral cavity without brushing teeth or oral cavity, and has a cleaning effect, and can be drunk after cleaning, before cleaning, and during cleaning. It is harmless and safe even if taken into the body.

[11] The sphinganine, sphingosine, sphingenine, sphingadienin, methyl-sphingadienine, or amino-methyl-octodecatriene-diol is an amphipathic compound having both hydrophobic and hydrophilic moieties. The composition for external use according to claim 4 or 5, characterized in that there is As a result, water-based stains can be liberated, melted, removed, and decomposed, and oil-based stains can also be liberated, melted, removed, and decomposed.

[12] 0.01% to 80% by weight of sphinganine, sphingosine, sphingenine, sphingadienin, methyl-sphingadienine, or amino-methyl-octodecatriene-diol, and 10% by weight of water, alcohol, or oil A method for producing a composition for external use, characterized by mixing in a range of weight % to 90 weight %, not exceeding 100 weight % in total.

It can clean teeth, gums, tongue and oral cavity without brushing teeth or oral cavity, and can be drunk after cleaning, before cleaning, or during cleaning, and is harmless and safe even if taken into the body. 0.01% to 80% by weight of sphinganine, sphingosine, sphingenine, sphingadienin, methyl-sphingadienine, or amino-methyl-octodecatriene-diol, and 10% to 90% by weight of water, alcohol, or oil , mixed.

Sphinganine, sphingosine, sphingenin, spungadienine, methyl-sphingadienine, or amino-methyl-octodecatriene-diol, which is contained in sea cucumber and the like, has a cleansing action, and is harmless and safe to be taken into the body.

Claims (9)

sphinganine, sphingosine, sphingenine, sphingadienine, methyl-sphingadienine, or amino-methyl-octodecatriene-amino-methyl -octadecatriene-diol) from 0.01% to 80% by weight and water, alcohol or oil from 10% to 90% by weight, in a range not exceeding 100% by weight in total. A composition for external use. 2. The composition for external use according to claim 1, wherein said composition for external use is a toothpaste or mouthwash. 3. The toothpaste or mouthwash cleansing teeth, gums, tongue, and oral cavity without brushing the teeth or oral cavity with a brush, and can be taken into the back of the throat after cleaning. External composition. 4. The composition for external use according to claim 3, wherein the composition for external use is a toothpaste or mouthwash for preventing and treating periodontal disease. 4. The composition for external use according to claim 3, wherein the composition for external use is a toothpaste or mouthwash for preventing and treating caries. 6. The composition for external use according to claim 4 or 5, wherein the sphingenine is 8-sphingenine. 6. The composition for external use according to claim 4 or 5, wherein the sphingadienine is 4,8-sphingadienine. The composition for external use according to claim 4 or 5, wherein the methyl-sphingadienine is 9-methyl-4,8-sphingadienine. The amino-methyl-octadecatriene-diol is 2-amino-9-methyl-4,8,10-octodecatriene-1,3-diol. The composition for external use according to claim 4 or 5.