CN109152722B - Oral composition - Google Patents

Abstract

An oral composition comprising (A) tocopherol or a derivative thereof, (B) xanthan gum and carrageenan, (C) 1 or 2 or more anionic surfactants selected from acylamino acids, acyltaurines and salts thereof, wherein the content of component (B) is 1.2 to 3% by mass and the content of component (C) is 0.1 to 3% by mass.

Description

Oral composition

Technical Field

The present invention relates to an oral composition having excellent retention in the oral cavity of tocopherol or a derivative thereof.

Background

Although tocopherol or a derivative thereof (vitamin E) is considered to be a component having a prophylactic and therapeutic effect on gingivitis and periodontitis, and is excellent in retention in the oral cavity, it is considered to be useful in terms of the effect, it is difficult for tocopherol or a derivative thereof, which is an oil-soluble component and has a problem in stability, to be sufficiently and satisfactorily retained in the oral cavity where saliva is often secreted.

Patent document 1 (japanese patent No. 5682235) proposes: the present inventors have further studied on the improvement of the oral retention of vitamin E, and particularly, have room for improvement in the oral retention of vitamin E when the amount of vitamin E to be mixed is large.

Further, patent document 2 (japanese patent publication No. 7-88292) discloses that the stability of tocopherol or a derivative thereof in an oral composition is improved: in the presence of an alkyl sulfate, the storage stability of tocopherol or a derivative thereof is improved by a specific amino acid, and patent document 3 (japanese patent No. 4496429) discloses: in a dentifrice composition containing vitamin E or a derivative thereof and an anionic surfactant, the stability of vitamin E or a derivative thereof in a container is maintained by a specific nonionic surfactant mixture, and patent document 4 (japanese patent laid-open No. 2015-110664) discloses: although the storage stability of ascorbic acid phosphate ester or a salt thereof and vitamin E or a derivative thereof is improved by a specific nonionic surfactant, no study has been made on the retention property in the oral cavity of tocopherol or a derivative thereof.

Documents of the prior art

Patent document

[ patent document 1] Japanese patent No. 5682235

[ patent document 2 ] Japanese patent publication No. Hei 7-88292

[ patent document 3 ] Japanese patent No. 4496429

[ patent document 4 ] Japanese patent laid-open No. 2015-110664

Disclosure of Invention

Problems to be solved by the invention

Therefore, there is a problem in oral compositions that the retention in the oral cavity of tocopherol or a derivative thereof is improved.

The present invention has been made in view of the above circumstances, and an object thereof is to provide an oral composition which is excellent in retention in the oral cavity of tocopherol or a derivative thereof, and is excellent in extrudability of a preparation from a container and also in usability (stringiness).

Means for solving the problems

The present inventors have conducted intensive studies to achieve the above object, and as a result, have recognized that: in the oral composition containing tocopherol or a derivative thereof, by mixing a specific amount of both xanthan gum and carrageenan and a specific anionic surfactant, the oral retention of tocopherol or a derivative thereof in the oral cavity is improved, and the preparation is excellent in extrudability from a container and good in usability. Namely, according to the present invention, it was found that: the present invention has been completed by finding that an oral composition containing (a) tocopherol or a derivative thereof, (B) xanthan gum and carrageenan, (C) 1 or 2 or more anionic surfactants selected from acylamino acids, acyltaurines and salts thereof, (B) 1.2 to 3% by mass of the component, and (C) 0.1 to 3% by mass of the component has excellent retention of the component (a) in the oral cavity, has appropriate hardness, can be smoothly extruded from a container, has excellent extrudability, and has good paste fracture (stringiness) when placed on a toothbrush, and can be used favorably.

Further, in the present invention, when the components (B) and (C) are combined with the component (A), the retention in the oral cavity of the component (A) is significantly improved by a combination system of the components (B) and (C), and a significant action effect which cannot be achieved by adding an inappropriate binder or an inappropriate anionic surfactant is obtained. In this case, when xanthan gum or carrageenan is used alone, the retention in the oral cavity of the component (a) cannot be satisfactorily improved, and further, when xanthan gum is used alone, the kneading property (stringiness) when placed in a toothbrush is poor, and the usability is also poor, and when xanthan gum and carrageenan are used in combination, there arises a problem that the extrudability of the preparation from a container becomes hard after storage, and that does not occur when xanthan gum or carrageenan is used alone. On the other hand, by using the component (C) in combination with the component (B), the oral retention of the component (a) can be increased without causing the problems relating to the use such as the extrusion property and the stringiness, and thus, an excellent oral retention property can be imparted in which a large amount of the component (a) remains even when the gum model is washed with water for a plurality of times as shown in examples described later.

Accordingly, the present invention provides an oral composition characterized by containing

(A) A tocopherol or a derivative thereof, or a pharmaceutically acceptable salt thereof,

(B) the xanthan gum and the carrageenan are mixed to prepare the emulsion,

(C) 1 or 2 or more anionic surfactants selected from acylamino acids, acyltaurines and salts thereof, wherein the content of the component (B) is 1.2-3% by mass, and the content of the component (C) is 0.1-3% by mass.

Effects of the invention

The present invention provides an oral composition which is excellent in retention in the oral cavity of tocopherol or a derivative thereof, and which is excellent in extrudability of the preparation from a container and also excellent in usability such as stringiness. Further, even in the oral cavity where saliva is often secreted, the component (a) is satisfactorily retained, and an improvement in the effects of preventing and treating gingivitis and periodontitis can be expected, and therefore, the component (a) is suitable for preventing or inhibiting periodontal diseases.

Detailed Description

The present invention will be described in further detail below. The oral composition of the present invention contains (a) tocopherol or a derivative thereof, (B) xanthan gum and carrageenan, and (C) an anionic surfactant selected from an acylamino acid, an acyltaurine and a salt thereof as essential ingredients.

(A) Tocopherol or its derivatives have blood circulation promoting effect, and are used for preventing or inhibiting gingivitis and periodontitis.

Examples of the tocopherol or a derivative thereof include d- α -tocopherol, dl- α -tocopherol, β -tocopherol, γ -tocopherol, δ -tocopherol, and esters thereof with organic acids such as acetic acid, nicotinic acid, succinic acid, and linolenic acid, and salts thereof. Specific examples of such tocopherol derivatives include d- α -tocopheryl acetate, dl- α -tocopheryl acetate, d- α -tocopheryl nicotinate, dl- α -tocopheryl nicotinate, d- α -tocopheryl succinate, dl- α -tocopheryl succinate, d- α -tocopheryl linolenate, dl- α -tocopheryl linolenate, and calcium tocopheryl succinate. Among them, from the viewpoint of good appearance (color tone) of the preparation, dl- α -tocopherol acetate, and dl- α -tocopherol nicotinate are preferable, and dl- α -tocopherol acetate is particularly preferable.

As the tocopherol or a derivative thereof, a product conforming to the standard of old cosmetic raw materials (cosmetic standards) or the standards 2006 of raw materials for pharmaceuticals for external use can be used, and commercially available products such as those manufactured by DSM Nutrition Japan, manufactured by sanitary food chemical co.

(A) The amount of the component (b) is 0.1% by mass or more, preferably 0.1 to 2%, more preferably 0.2 to 2%, still more preferably 0.3 to 1.5%, particularly preferably 0.5 to 1.5% of the total composition. When the amount is too large, the medicinal effect is effectively exhibited, and when the amount is too large, problems may occur in the physical properties of the preparation.

(B) The component (A) is a mixture of xanthan gum and carrageenan, and the oral retention of the component (A) is improved by combining both components. When xanthan gum or carrageenan is used alone, the retention in the oral cavity is poor.

As the xanthan gum, any xanthan gum may be used as long as it is generally used in a dentifrice composition, but the viscosity of xanthan gum is preferably: the 1% aqueous solution of xanthan gum containing 1% potassium chloride has a viscosity of 600 to 2,000 mPas, and particularly preferably 1,000 to 2,000 mPas.

The viscosity is measured using a brookfield type rotational viscometer with a spindle 3 at 60rpm and 25 ℃ for 30 seconds.

Examples of the xanthan gum include commercially available products such as Novazan (manufactured by ADM far east), MONATGUM DA (manufactured by CP Kelco), KELZAN T, KELDENT, and ECOGUM (manufactured by Dainippon pharmaceutical Co., Ltd.).

The carrageenan includes kappa carrageenan, iota carrageenan and lambda carrageenan, and 1 or 2 or more species of carrageenan can be used, and iota carrageenan can be suitably used. Examples of iota-carrageenan include GENUVISCO manufactured by CP Kelco corporation, and the like.

(B) The amount of the component (a) is 1.2% or more, particularly preferably 1.2 to 3%, more preferably 1.4 to 2.5% in total based on the total composition. When the amount is larger, the intraoral retention of component (A) becomes higher, and when it is less than 1.2%, the intraoral retention is poor. The more the amount to be mixed, the higher the retention in the oral cavity, but from the viewpoint of maintaining the extrusion property of the preparation well, it is preferably 3% or less.

Further, within the above total amount, the amount of xanthan gum is preferably 0.6 to 2.8%, more preferably 0.9 to 2.1% of the total composition, and the amount of carrageenan is preferably 0.2 to 2.4%, more preferably 0.4 to 1.6% of the total composition.

Further, the xanthan gum/carrageenan in the mass ratio of the xanthan gum and the carrageenan is preferably 0.5 to 5, more preferably 1 to 3. When the amount is within this range, the oral retention of component (A) is more excellent, and the stringiness is further improved. If the amount is less than 0.5, the retention in the oral cavity may not be sufficiently improved, and if it exceeds 5, the stringiness may be increased.

(C) The anionic surfactant of component (A) is 1 or more than 2 selected from acylamino acid, acyltaurine and their salts.

The acylamino acid is preferably an amino acid having an acyl group with 8 to 20 carbon atoms, particularly preferably 12 to 16 carbon atoms, and examples of the amino acid residue include glutamic acid, aspartic acid, glycine, sarcosine, alanine, methionine, phenylalanine, leucine, and isoleucine. Examples of the salt include alkali metal salts such as sodium salt and potassium salt, alkaline earth metal salts, and organic amine salts.

The acyl amino acid and its salt are preferably acyl glutamate, acyl aspartate, or acyl glycinate having the above-mentioned carbon number as the acyl group, particularly preferably acyl glutamate, and particularly preferably sodium lauroyl glutamate, which are less odorous (bitter taste) than other compounds having an amino acid residue, and are preferable.

Examples of the acylamino acid salts include acyl glutamates such as sodium N-lauroyl-L-glutamate, sodium N-myristoyl-L-glutamate and potassium N-cocoyl fatty acid acyl-L-glutamate; acyl aspartate such as sodium N-lauroyl-L-aspartate; acyl glycinates such as potassium N-cocoyl fatty acid acyl glycinate; and the like.

As acylamino acids and salts thereof, there can be used, specifically, Aminosouct ALMS-P1 (sodium N-lauroyl-L-glutamate, Asahi Kasei Chemicals), AMISOFT LS-11 (sodium N-lauroyl-L-glutamate, Kyoshiki Kasei Chemicals), AMINOSURFACT AMMS-P1 (sodium N-myristoyl-L-glutamate, Asahi Kasei Chemicals), AMISOFT MS-11 (sodium N-myristoyl-L-glutamate, Kyoshiki Kasei Chemicals CO., INC.), INOFOAMER FLDS-L (sodium N-lauroyl-L-aspartate, Asahi Kasei Chemicals), AMILITE GCK-12K (potassium N-cocoyl fatty acid glycinate, gourmet health products co., ltd.) and the like.

The acyl taurine is preferably a C8-20 acyl group, particularly preferably a C12-16 acyl group, and the taurine residue is taurine, methyltaurine or the like. Examples of the salt include alkali metal salts such as sodium salt and potassium salt.

Specific examples of the acyl taurates include sodium cocoyl methyl taurate, potassium cocoyl methyl taurate, sodium lauroyl methyl taurate, sodium stearyl methyl taurate, sodium myristoyl methyl taurate, sodium oleoyl methyl taurate, sodium palmitoyl methyl taurate, and sodium cocoyl taurate.

Among them, acyl methyltaurate is preferable, and sodium lauroyl methyltaurate is particularly preferable.

As the component (C), 1 kind selected from acylamino acids, acyltaurines and salts thereof may be used alone, or 2 or more kinds may be used in combination, and from the viewpoint of extrudability, acyl taurates are particularly preferable.

(C) The amount of the component (B) is 0.1 to 3%, preferably 0.3 to 1.5% of the total composition. If the amount to be mixed is less than 0.1%, the retention in the oral cavity of component (A) is not sufficiently improved, and the preparation is difficult to be extruded from the container after storage, resulting in poor extrudability. When the amount is larger, the retention in the oral cavity and the extrusion property are improved, but when it exceeds 3%, bitterness and irritation are generated, or the stability of the component (A) is lowered.

The ratio (B)/(C) of the components (B) and (C) is preferably 0.5 to 10, more preferably 1 to 8, and particularly preferably 1.2 to 6 in terms of mass ratio. When the amount is within this range, the oral retention property is more excellent, and the extrudability and the drawability are further improved.

In addition, an anionic surfactant other than the component (C) may be mixed within a range not interfering with the effects of the present invention, but is preferably 50% or less, preferably 20% or less of the total amount of anionic surfactants.

The oral composition of the present invention can be prepared in the form of liquid, gel, paste, etc. into dentifrice such as toothpaste, liquid dentifrice, and emollient dentifrice; a dosage form such as a mouthwash, but a dentifrice is particularly preferable. In this case, the composition may be prepared by a usual method by mixing other known components as necessary in addition to the above components according to the purpose and formulation of the composition. For example, in the case of a dentifrice, an abrasive, a binder, a thickener, a surfactant, a sweetener, a coloring agent, a preservative, a pH adjuster, a flavor, an active ingredient, and the like can be mentioned.

Examples of the polishing agent include silica-based polishing agents such as precipitated silica, aluminum silicate, and zirconium silicate; calcium phosphate compounds such as calcium hydrogen phosphate dihydrate and anhydrous compounds, calcium phosphate, and tricalcium phosphate; calcium carbonate, calcium hydroxide, aluminum hydroxide, and the like. The amount of the polishing agent to be mixed is usually 2 to 40%, preferably 10% or less, more preferably 5% or less, and may not be mixed (0%).

In the oral composition, it is preferable to reduce the number of rinsing with water after use in order to retain the medicinal component in the oral cavity, and in the present invention, the amount of the abrasive such as a water-insoluble powder, particularly a silica-based abrasive, is preferably small in view of easiness of rinsing. The composition of the invention is further preferably a dentifrice of gel-based composition, in particular aqueous gel-based composition, free of abrasives (0% abrasive content).

As the binder, a binder other than xanthan gum and carrageenan may be mixed within a range not interfering with the effect of the present invention. Specifically, thickening silica such as gelling silica as an inorganic binder; cellulose derivatives such as sodium carboxymethylcellulose, methylcellulose and hydroxymethylcellulose as organic binders; alginic acid derivatives such as sodium alginate; sodium polyacrylate and the like are particularly preferably used as an inorganic binder such as thickening silica in view of retention feeling, appearance (moldability) and extrudability.

The amount of these binders is preferably 0.5 to 10%, particularly preferably 1 to 8%.

In view of the retention in the oral cavity and the extrudability of the component (a), the amount of the organic binder other than the component (B) is preferably 0.2% or less, particularly preferably 0.1% or less, and is preferably not mixed (0%).

Examples of the thickener include sugar alcohols such as sorbitol and xylitol; polyhydric alcohols such as glycerin and propylene glycol. The amount to be mixed is usually 5 to 50%, particularly preferably 20 to 45%.

The surfactant may be a mixture of a sugar fatty acid ester such as sucrose fatty acid ester as a nonionic surfactant, in addition to the anionic surfactant; polyoxyethylene fatty acid esters such as sugar alcohol fatty acid esters, sorbitan fatty acid esters, glycerin fatty acid esters, polyglycerin fatty acid esters, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene hydrogenated castor oil; polyoxyethylene higher alcohol ethers such as polyoxyethylene lauryl ether, and the like.

In addition, a cationic surfactant such as an alkylammonium surfactant such as distearylmethylammonium chloride; betaine type, acetic acid betaine type, imidazoline type, and other amphoteric surfactants.

The amount of these surfactants to be mixed is usually 0.01 to 10%, particularly 0.1 to 5%.

Examples of the sweetener include saccharin sodium. Examples of the colorant include blue No. 1, yellow No. 4, and titanium dioxide.

Examples of the preservatives include parabens such as methyl paraben; benzoic acid such as sodium benzoate or a salt thereof; and the like.

Further, a pH adjuster may be added, and examples thereof include hydroxides, bicarbonates, carbonates, sulfates and the like of alkali metals such as sodium hydroxide.

As the flavor, the following known flavor raw materials used in the oral composition can be used in combination: natural flavors such as peppermint oil (peppermint oil), spearmint oil, anise oil, eucalyptus oil, wintergreen oil, cinnamon oil, clove oil, senecio oil, sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, lime oil (lime oil), lavender oil, rosemary oil, myrcia oil (laurel oil), chamomile oil (chamomile oil), caraway oil (caraway oil), marjoram oil (marjoram oil), bay leaf oil, lemongrass oil, oregano oil, pine needle oil, orange flower oil, rose oil, jasmine oil, grapefruit oil, lime oil, grapefruit oil, iris extract, peppermint oil, rose oil, orange flower oil, and the like; and a perfume obtained by processing (removing pre-fraction, removing post-fraction, fractionating, liquid-liquid extracting, refining, powdering, etc.) these natural perfumes; and also monotropic flavors such as menthol, carvone, anethole, eucalyptol, methyl salicylate, cinnamaldehyde, eugenol, 3-l-menthoxypropane-1, 2-diol, thymol, linalool, linalyl acetate, limonene, menthone, menthyl acetate, N-substituted-p-menthane-3-carboxamide, pinene, octanal, citral, pulegone (pulegone), carvonyl acetate, anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexylpropionate, methyl anthranilate, ethyl methylphenylglycerol, vanillin, undecalactone, hexanal, butanol, isoamyl alcohol, hexenol, dimethyl sulfide, methyl cyclopentenolone, furfural, trimethylpyrazine, ethyl lactate, ethyl thioacetate; and blending flavors such as strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, butter flavor, milk flavor, fruit mix flavor, tropical fruit flavor, and the like, but not limited to the flavors described in the examples.

The amount of the fragrance raw material to be mixed is not particularly limited, and the fragrance raw material is preferably used in an amount of 0.000001 to 1% in the composition. In addition, as the perfume for giving fragrance using the perfume raw material, 0.1 to 2% is preferably used in the composition.

As the active ingredient, other active ingredients may be mixed in addition to the component (a), and specific examples thereof include nonionic bactericides such as isopropyl methylphenol; cationic bactericides such as cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, and the like; an anti-inflammatory agent; enzymes such as dextranase; fluorides such as sodium fluoride and sodium monofluorophosphate; vitamins; anticalculus agent, etc. In addition, an effective amount of the above-mentioned active ingredient may be mixed within a range not to impair the effects of the present invention.

[ examples ] A method for producing a compound

The present invention will be described in more detail below with reference to examples, comparative examples and formulation examples, but the present invention is not limited to the following examples. Unless otherwise specified, the% in the following examples represents mass%.

[ examples and comparative examples ]

Dentifrice compositions having compositions shown in tables 1 to 3 were produced by the following methods and evaluated by the following methods. The results are also shown in the table.

The manufacturing method comprises the following steps: mixing the water-soluble component with purified water, adding the component (B) dispersed in propylene glycol, mixing, sequentially adding the perfume, the component (A) and the component (C), defoaming, and mixing.

The xanthan gum used was a 1% aqueous solution of xanthan gum containing 1% potassium chloride and having a viscosity (brookfield type rotational viscometer, No. 3 spindle, 60rpm, 25 ℃ C., measurement time 30 seconds) of about 1,500 mPas, and the carrageenan was iota-carrageenan.

< method for evaluating intraoral Retention >

40. mu.L of a dentifrice diluent obtained by diluting a dentifrice composition 3 times with water was placed in a hamster cheek pouch (3-week-old male, Syria, manufactured by SLC, Japan) whose diameter was knocked out to 10 mm. After standing for 3 minutes, the mixture was washed with water 7 times, extracted with 1mL of ethanol, and the tocopherol or its derivative as an oil-soluble component was quantified by liquid chromatography in the following manner.

The measurement conditions were: the measurement was carried out by an absolute calibration curve method under ultraviolet absorbance (measurement wavelength: 284nm) using a column packed with a 5 μm octadecylsilylated silica gel for liquid chromatograph and a stainless steel tube having an inner diameter of 4.6mm and a length of 15cm and methanol as a mobile phase at a column temperature of 25 ℃ and a flow rate of 1.0 mL/min.

The oral retention of tocopherol or a derivative thereof was averaged over 3 times, and the ratio of the remaining amount to the initial amount (the amount of tocopherol or a derivative thereof contained in 40. mu.L of the initially treated 3-fold diluted solution) was calculated and evaluated according to the following criteria.

Evaluation criteria

Very good: retention of over 30%

O: the retention is more than 20 percent and less than 30 percent

And (delta): the retention is more than 10 percent and less than 20 percent

X: the retention is less than 10 percent

< method for evaluating extrudability >

After 3 pieces of each composition were stored at-5 ℃ for 1 month in a laminated tube container having an aperture of 8mm filled with 50g of the dentifrice composition, the dentifrice composition was extruded, and the degree of extrusion hardness was evaluated on the following 4 scales.

Evaluation criteria

Very good: smooth extrusion dentifrice compositions

O: slightly harder, but extrusion dentifrice compositions do not have problems

And (delta): hard, so that the dentifrice composition is somewhat difficult to extrude

X: hard, so that the dentifrice composition is difficult to extrude

< method for evaluating drawability >

The dentifrice composition was filled into a laminated tube container having an aperture of 8mm, and after about 1g was placed on a toothbrush through the tube, a test of the kneadability (stringiness) was conducted in the upward direction while pulling the tube away from the toothbrush. Stringiness is a property in which the dentifrice composition is drawn into a stringiness when taken out of a tube, and the length thereof is measured. Evaluation was performed according to the following criteria.

Evaluation criteria

Very good: the wire drawability is less than 0.5cm, and the kneading and cutting performance is good

O: the drawability of 0.5cm or more and less than 1cm was observed, and no problem was found in use

And (delta): the drawability of 1cm or more and less than 1.5cm was observed, and there was a slight problem in use

X: the drawability of 1.5cm or more is observed, and there is a problem in use

[ TABLE 1]

[ TABLE 2 ]

[ TABLE 3 ]

[ prescription example 1] toothpaste

Xanthan/carrageenan ratio: 3 (B)/(C): 2

Claims (10)

1. An oral composition comprising

(A) A tocopherol or a derivative thereof, or a pharmaceutically acceptable salt thereof,

(B) the xanthan gum and the carrageenan are mixed to prepare the emulsion,

(C) 1 or 2 or more anionic surfactants selected from acyl taurines having an acyl group with 8 to 20 carbon atoms and salts thereof,

(B) the content of the component (C) is 0.1-3% by mass, and the content of the component (C) is 1.2-3% by mass.

2. The oral composition according to claim 1, wherein the content mass ratio of xanthan gum and carrageenan represented by xanthan gum/carrageenan is 0.5 to 5.

3. The oral composition according to claim 1 or 2, wherein the xanthan gum is contained in an amount of 0.6 to 2.8% by mass, and the carrageenan is contained in an amount of 0.2 to 2.4% by mass.

4. The oral composition according to claim 1 or 2, wherein the component (C) is 1 or 2 or more anionic surfactants selected from acyl taurates and acyl methyltaurates having 8 to 20 carbon atoms in the acyl group.

5. The oral composition according to claim 1 or 2, wherein the content mass ratio of the component (B) to the component (C) represented by (B)/(C) is 0.5 to 10.

6. The oral composition according to claim 1 or 2, wherein the content of the component (A) is 0.1 to 2% by mass.

7. The oral composition according to claim 1 or 2, wherein the composition further comprises an abrasive 10 mass%.

8. The oral composition of claim 1 or 2, wherein the composition is free of abrasives.

9. The oral composition according to claim 1 or 2, wherein the composition further contains 0.5 to 10% by mass of an inorganic binder.

10. The oral composition according to claim 1 or 2 which is a dentifrice.