Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
  • A61K8/33—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
  • A61K8/37—Esters of carboxylic acids
  • A61K8/375—Esters of carboxylic acids the alcohol moiety containing more than one hydroxy group
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K8/00—Cosmetics or similar toiletry preparations
  • A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
  • A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
  • A61K8/84—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
  • A61K8/88—Polyamides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
  • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
  • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
  • A61Q11/00—Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Definitions

• the present invention relates to a liquid or liquid oral composition and a tongue coating adhesion inhibitor having a high effect of inhibiting tongue coating adhesion.
• Patent Document 2 Japanese Patent Laid-Open No. 2001-161720
• Patent Document 3 Japanese Patent Laid-Open No. 10-182387
• Patent Document 3 describes a technique for removing tongue coating using a condensed phosphate, but it is difficult to say that taste and oral mucosal irritation are sufficient, and there is room for improvement. was there. Therefore, a composition for oral cavity with a good feeling of use that exhibits a high effect of suppressing adhesion of tongue coating is desired.
• Patent Document 4 International Publication No. 2005/049050 pamphlet
• Patent Document 5 Japanese Patent Laid-Open No. 2009-274967 discloses that an oral spray composition in which an organic acid such as citric acid or a salt thereof and glycerin are used in combination with polyglutamate is effective in improving dry feeling in the mouth. Has been proposed.
• the present invention has been made in view of the above circumstances, and an object of the present invention is to provide a liquid or liquid oral composition and tongue coating adhesion inhibitor that exhibits a high effect of suppressing tongue coating adhesion and has a good usability.
• the present inventors have found that (A) a glycerin fatty acid ester having 8 to 14 carbon atoms in a fatty acid and (B) a polyglutamate are combined with (B) component / ( By combining and blending the component (A) in a mass ratio of 0.1 to 150, a liquid or liquid preparation having an excellent effect of suppressing adhesion of tongue coating can be obtained. Thus, the present inventors have found that it has low irritation and good usability, and has made the present invention.
• the present inventors surprisingly that the specific glycerin fatty acid ester of the component (A) has an effect of suppressing tongue coating adhesion, and the polyglutamate of the component (B) is appropriately combined with the component (A).
• synergistic increase in tongue coating adhesion suppression effect excellent tongue coating adhesion suppression effect is exhibited, taste reduction and irritation caused by component (A) are eliminated, taste is good and low irritation to oral mucosa is good It has been found that it can be suitably applied to the tongue surface.
• polyglutamate has an effect of promoting salivary secretion, but by using polyglutamate together with a specific glycerin fatty acid ester, for example, spraying or dripping into the oral cavity, or washing the oral cavity is performed. It is a new finding of the inventors of the present application that by applying to the surface of the tongue by mouthing, an excellent effect of suppressing adhesion of tongue coating while maintaining a good feeling of use.
• the present invention provides the following.
• [1] Fatty acid ester having 8 to 14 carbon atoms of fatty acid and (B) polyglutamate, and (B) component / (A) component is in the range of 0.1 to 150 as mass ratio A liquid or liquid oral composition characterized by the above.
• [2] (A) Fatty acid consisting of glycerin fatty acid ester having 8 to 14 carbon atoms and (B) polyglutamate, wherein (B) component / (A) component has a mass ratio in the range of 0.1 to 150. Tongue adhesion inhibitor.
• a liquid or liquid oral composition and a tongue coating adhesion inhibitor that have a high effect of suppressing tongue coating adhesion and that have a good taste and low irritation to the oral mucosa and have a good feeling of use.
• the present invention comprises (A) a glycerin fatty acid ester having 8 to 14 carbon atoms in a fatty acid and (B) a polyglutamate in combination of the (B) component and the (A) component in an appropriate ratio. It is characterized by.
• the component (A) is a glycerin fatty acid ester having 8 to 14 carbon atoms, preferably 8 to 11 carbon atoms. Those having less than 8 carbon atoms are difficult to obtain, and those having more than 14 carbon atoms are insufficient in the effect of suppressing adhesion of tongue coating.
• glycerin fatty acid esters examples include glyceryl caprylate, glyceryl caprate, glyceryl undecylenate, glyceryl laurate and the like. More preferred.
• the blending amount of the glycerin fatty acid ester as the component (A) is 0.01 to 2% (mass%, the same applies hereinafter) of the whole composition from the viewpoint of keeping the mouth clean (inhibition of tongue coating), 1 to 1% is preferable. If it is less than 0.01%, the adhesion inhibitory effect of tongue coating may not be sufficiently exhibited, and if it exceeds 2%, an unpleasant taste may remain after use, and oral mucosal irritation may become strong.
• a sodium or potassium salt of polyglutamic acid is preferably used.
• ⁇ or ⁇ -polyglutamic acid that is chemically synthesized, or sodium or potassium salt of natural ⁇ or ⁇ -polyglutamic acid obtained as a fermentation product from various strains is preferred, and natural polyglutamate is particularly preferred.
• ⁇ -polyglutamate having high productivity as a raw material is more preferable.
• the viscosity of the polyglutamate is not particularly limited, but the viscosity (25 ° C.) of a 4% aqueous solution by a measurement method using a B-type viscometer described later is in the range of 10 to 200 mPa ⁇ s, particularly 30 to 150 mPa ⁇ s. It is preferable. If it is less than 10 mPa ⁇ s, sufficient saliva secretion may not occur and the tongue coating removal effect may not be sufficiently exhibited. In addition, unpleasant taste and oral mucosal irritation may not be sufficiently reduced or suppressed. When it exceeds 200 mPa ⁇ s, the viscosity of the preparation becomes high, the dispersibility in the mouth is deteriorated, and a sufficient effect may not be exhibited.
• Viscosity Measurement Method Take 96 g of water in a 200 mL beaker and add 4.0 g of ⁇ -polyglutamate to the solution while stirring with a stirrer to completely dissolve it. Next, after leaving still in a 25 degreeC thermostat for 1 hour, the viscosity after 1 minute is measured correctly using a BL type
• BL type viscometer Tokyo Keiki B type viscometer Model BL Rotor: No. 2 Number of revolutions: 60 rpm Measurement temperature: 25 ° C
• the blending amount of the polyglutamate component (B) is preferably 0.05 to 5%, particularly preferably 0.1 to 2% of the total composition. If it is less than 0.05%, the unpleasant taste and oral mucosal irritation of glycerin fatty acid ester may not be suppressed, or the secretion of saliva is not sufficiently promoted, so that the effect of suppressing adhesion of tongue coating may not be satisfactorily exhibited. When it exceeds 5%, the viscosity of the preparation becomes high, the preparation becomes difficult to spread throughout the mouth, and the tongue moss adhesion inhibitory effect may not be sufficiently exhibited.
• the blending ratio of the component (B) to the component (A) is (B) / (A) as a mass ratio of 0.1 to 150, preferably 0.2 to 15. Even if the blending amounts of component (A) and component (B) are within the above ranges, if the ratio (B) / (A) is less than 0.1, the unpleasant taste and oral mucosal irritation are sufficiently reduced. It cannot be suppressed. When it exceeds 150, the viscosity of the preparation becomes high, dispersibility in the mouth is deteriorated, and sufficient effects are not exhibited.
• the oral composition of the present invention is liquid or liquid in form.
• the liquid oral composition is a transparent or translucent preparation in which the blending components are solubilized, and solid components that are not solubilized such as abrasives are not usually blended, such as wetting agents, surfactants, A solvent, and if necessary, a sweetener, a fragrance, an active ingredient and the like are blended.
• the liquid oral composition is a gel-like preparation having low shape retention and fluidity, and a solid component such as an abrasive may be dispersed without being solubilized.
• a polishing agent, a wetting agent, a thickening agent, a surfactant, a solvent, and a sweetener, a fragrance, an active ingredient, and the like are blended if necessary.
• the composition of the present invention is preferably used so that it can be directly applied to the tongue surface by spraying, dripping, or rinsing the oral cavity in the oral cavity, particularly the tongue surface. You may brush with a toothbrush.
• the dosage form is preferably a dosage form suitable for such use, specifically, mouthwash such as mouthwash, dentifrice such as liquid dentifrice, liquid dentifrice, spray, dripping agent, capsule, etc. Among them, it is particularly preferable to use it as a spray agent or a dripping agent from the viewpoint of portability where an appropriate amount can be freely used anytime and anywhere.
• composition of the present invention other known components other than the above components (A) and (B) can be blended as necessary, as long as the effects of the present invention are not hindered depending on the form and dosage form.
• a component and water can be mixed and prepared by a conventional method.
• abrasives usually used for oral compositions can be used.
• silica-based abrasives such as precipitated silica and aluminosilicate, dicalcium phosphate dihydrate and hydrates, calcium phosphate compounds such as primary calcium phosphate, tertiary calcium phosphate, and calcium pyrophosphate, calcium carbonate,
• calcium hydroxide, aluminum hydroxide salt and the like can be blended (the blending amount is usually 0 to 50%, particularly 10 to 50%).
• an anionic surfactant As the surfactant, an anionic surfactant, a nonionic surfactant, and an amphoteric surfactant can be blended.
• the anionic surfactant include sodium alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, and N-acyl sarcosine sodium such as N-lauroyl sarcosine sodium and N-myristoyl sarcosine sodium.
• Nonionic surfactants include polyoxyethylene hydrogenated castor oil, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, sugar alcohol fatty acid esters such as sucrose fatty acid ester, polyoxyethylene glycerin fatty acid ester, polyethylene glycol fatty acid ester, etc.
• Examples of the cationic surfactant include alkyl ammonium and alkyl benzyl ammonium salts.
• amphoteric surfactants include betaine acetate type amphoteric surfactants and imidazoline type amphoteric surfactants. The blending amount of these surfactants can be 0 to 10%, particularly 0.1 to 5.0%.
• thickener examples include xanthan gum, carrageenan, hydroxyethyl cellulose, sodium alginate, polyvinyl alcohol, sodium carboxymethyl cellulose and the like (the amount is usually 0 to 5%, particularly 0.5 to 3%).
• wetting agent examples include sugar alcohols such as sorbitol, malt, and lactit, and polyhydric alcohols such as glycerin, ethylene glycol, polyethylene glycol, propylene glycol, and 1,3-butylene glycol (the amount is usually 2 to 70%). ).
• sugar alcohols such as sorbitol, malt, and lactit
• polyhydric alcohols such as glycerin, ethylene glycol, polyethylene glycol, propylene glycol, and 1,3-butylene glycol (the amount is usually 2 to 70%).
• water is usually used, and its content can be 20% or more.
• alcohols such as lower monohydric alcohols having 2 to 4 carbon atoms such as ethanol, isopropanol, butanol, and propanol can be blended, and the blending amount can be 0 to 20%.
• sweetening agents xylitol, maltitol, saccharin, sodium saccharin, stevioside, aspartame and the like can be blended.
• a colorant a highly safe water-soluble pigment such as Blue No. 1, Green No. 3, Yellow No. 4, Red No. 105, and the like can be added.
• citric acid, malic acid, tartaric acid, succinic acid and salts thereof, phosphoric acid, phosphates (sodium dihydrogen phosphate, disodium hydrogen phosphate, trisodium phosphate, etc.), carbonates, Bicarbonate and the like can be added.
• the pH of the composition is preferably 3 to 10, particularly 5 to 8.
• Perfumes include natural oils such as peppermint oil, spearmint oil, eucalyptus oil, wintergreen oil, clove oil, thyme oil, sage oil, cardamom oil, rosemary oil, marjoram oil, lemon oil, nutmeg oil, lavender oil, paracres oil, etc.
• active ingredients include cationic fungicides such as cetylpyridinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, benzalkonium chloride and benzethonium chloride, nonionic fungicides such as isopropylmethylphenol, tranexamic acid, epsilon-aminocaproic acid, etc.
• cationic fungicides such as cetylpyridinium chloride, chlorhexidine hydrochloride, chlorhexidine gluconate, benzalkonium chloride and benzethonium chloride
• nonionic fungicides such as isopropylmethylphenol, tranexamic acid, epsilon-aminocaproic acid, etc.
• Anti-inflammatory agents enzymes such as dextranase and mutanase, fluorides such as sodium fluoride, sodium monofluorophosphate, stannous fluoride, vitamin C such as ascorbic acid, dihydrocholesterol, glycyrrhetin salts, glycyrrhetinic acids , Hydrocholesterol, chlorophyll, copper chlorophyllin sodium, thyme, hornon, clove, hamamelis and other plant extracts, copper gluconate, caropeptide, sodium polyphosphate, water-soluble inorganic phosphate Compounds, polyvinylpyrrolidone, anti-tartar agents, anti-plaque agents, potassium nitrate, may be added to aluminum lactate and the like. In addition amount of these active ingredients can be made into the range which does not prevent the effect of this invention.
• a known container suitable for storing the oral composition can be used.
• the material include polyethylene, polypropylene, polyethylene terephthalate, polyacetal and the like, and a container corresponding to the dosage form is used.
• a spray agent if it is a container which has a structure which can spray a medicine, it will not be restricted in particular. Specifically, it is equipped with a container body such as a plastic bottle that contains the contents and a spray part having a spray mechanism such as a pump dispenser, and presses the pressing part of the spray part that is mounted in close contact with the upper opening of the container body What is sprayed by doing, or the container sprayed by pushing the container main body which stores the contents etc. can be used.
• a dripping agent will not be restrict
• the tongue coating adhesion inhibitor which is the range can be provided. In this case, the details of the blending components, blending amounts, ratios, and the like are the same as described above.
• compositions for oral cavity having the compositions shown in Tables 1 to 4 were prepared by the following method and evaluated as follows. The results are also shown in Tables 1 to 4.
• the average score of each evaluation was calculated and judged according to the following criteria. ⁇ 6 points or more ⁇ 4.5 points or more and less than 6 points ⁇ 3.5 points or more and less than 4.5 points ⁇ less than 3.5 points
• Example 19 to 31 Oral compositions having the compositions shown in Tables 5 to 7 were prepared by the same production method as described above. Examples 19 to 23 were filled in the same spray container as described above, and Examples 24 to 28 were filled in a dropping agent container (manufactured by Nissei Plastic Industry Co., Ltd., Essence Series DE20, material: polyethylene, 20 mL). Examples 29 to 31 were filled in a mouthwash container (manufactured by Yoshino Kogyosho, manufactured by polyethylene terephthalate, 250 mL) and evaluated by the above evaluation method.
• a dropping agent container manufactured by Nissei Plastic Industry Co., Ltd., Essence Series DE20, material: polyethylene, 20 mL
• Examples 29 to 31 were filled in a mouthwash container (manufactured by Yoshino Kogyosho, manufactured by polyethylene terephthalate, 250 mL) and evaluated by the above evaluation method.
• Glyceryl caprylate manufactured by Taiyo Kagaku Co., Ltd.
• trade name Sunsoft 700P-2 Glyceryl caprate: manufactured by Taiyo Chemical Co., Ltd.
• Sunsoft 760 Glyceryl undecylenate: Nikko Chemicals, trade name NIKKOL MGU
• Glyceryl laurate manufactured by Taiyo Kagaku Co., Ltd.
• Sunsoft 750 Glyceryl palmitate: Nippon Emulsion Co., Ltd., trade name GMS-P Sodium polyglutamate: manufactured by Meiji Food Materia Co., Ltd., trade name: Meiji polyglutamate, viscosity as shown in the table.
• Potassium polyglutamate manufactured by Meiji Food Materia Co., Ltd., viscosity is as described in the table.
• Sodium pyrophosphate manufactured by Taihei Chemical Industry Co., Ltd. Further, as perfumes A to F, those shown in Tables 8 to 14 were used.

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