JPH11116450A - Composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain the subject composition capable of improving retentivity of an antimicrobial agent in the oral cavity, and inhibiting the adhesion and the proliferation of microorganisms on the surface of a tooth by including a non-cationic antimicrobial agent, a cationic polymer, and a specific surface active agent. SOLUTION: The objective composition comprises (A) 0.0001-5 wt.% non- cationic antimicrobial agent [e.g. triclosan (2,4,4'-trichloro-2'-hydroxydiphenyl ether)], (B) 0.0001-5 wt.% cationic polymer (e.g. dimethyldiallylammonium- contaning polymer) and (C) 0.01-5 wt.% polyoxyethylene-polyoxypropylene block copolymer type surface active agent having >=70 deg.C clouding point [e.g. polyoxyethylene(200)-polyoxypropylene glycol(70)]. The composition is used for a dentifrice, a liquid dentifrice, a mouth rinsing agent, a mouthwash, a chewing gum or the like, and especially preferably used in a liquid form.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a composition for the oral cavity which has an excellent effect of inhibiting the adhesion and growth of microorganisms in the oral cavity to the tooth surface and can effectively inhibit plaque formation.

[0002]

2. Description of the Related Art Conventionally, a technique for preventing dental caries and periodontal diseases, which are two major diseases of dentistry, by adding an antibacterial agent to an oral composition such as a dentifrice. Research into development has led to several oral compositions to which antimicrobial agents have been added. Antibacterial agents are known to reduce the total number of bacteria in the oral cavity due to their effects and suppress plaque formation that causes disease, but the antibacterial effect in the oral cavity may be a temporary effect In many cases, sustainability of the antibacterial effect in the oral cavity is required. To address this problem, several studies have been made to improve the retention of antibacterial agents by adding a polymer compound (JP-A-6-192060, JP-A-7-267840, etc.). But,
In order to keep the physical properties of the composition stable and to provide an oral cleansing effect at the time of use, it is necessary to add a surfactant, and when these surfactants are added, the action of the antibacterial agent is remarkable. It is also known that the antibacterial agent is reduced. Therefore, it has been desired to develop an oral composition having an excellent antibacterial agent retention property in the oral cavity and exhibiting a high antibacterial effect even when a surfactant is added.

[0003] The present invention has been made in view of the above circumstances,
Improves the retention of antibacterial agents in the oral cavity, suppresses microbial adhesion and growth on the tooth surface, and effectively reduces plaque formation, which is an important factor in oral diseases, in a system containing a surfactant It is an object of the present invention to provide a composition for oral cavity that inhibits bleeding.

[0004]

Means for Solving the Problems and Embodiments of the Invention As a result of intensive studies to achieve the above object, the present inventor has found that a cationic polymer and a cloud point having a cloud point of 70 ° C. or more are added to a non-cationic germicide. By combining a polyoxyethylene polyoxypropylene block copolymer type surfactant in combination, the bactericidal activity is maintained, the retention on the tooth surface is increased, and the adhesion of microorganisms and the growth of bacteria on the tooth surface are suppressed. Exhibits the effect of preventing plaque formation, which is an important factor for oral diseases, and maintains the solubilized state of the composition stably, effective in preventing oral diseases (prevention of dental caries and periodontal disease) The present inventors have found that a suitable oral composition can be obtained, and have accomplished the present invention.

Hereinafter, the present invention will be described in more detail. The oral composition of the present invention comprises a non-cationic bactericide, a cationic polymer, and a polyoxyethylene polyoxypropylene block copolymer having a cloud point of 70 ° C. or more. A surfactant containing a polyoxyethylene polyoxypropylene block copolymer type surfactant having a cloud point of 70 ° C. or more, while controlling the adhesion of microorganisms to the tooth surface and the growth of bacteria. It is characterized in that the separation and precipitation of the non-cationic germicide are suppressed, and the solubilized properties of the composition are kept stable.

Here, examples of the non-cationic bactericide include halogenated diphenyl ether, halogenated salicylanilide, halogenated carbanilide, organic acid esters, phenolic compounds, hinokitiol, and mixtures thereof. Of these, halogenated diphenyl ethers and phenol compounds are preferred, and triclosan (2,4,4'-trichloro-2'-hydroxydiphenyl ether) is most preferred as the halogenated diphenyl ether. As the phenol compound, phenol, thymol, eugenol, hexylresorcinol and 2,2-methylenebis (4-chloro-6-bromophenol) are preferred.

On the other hand, examples of the cationic polymer include a dimethyldiallylammonium chloride-containing polymer (a homopolymer of dimethyldiallylammonium chloride, a dimethyldiallylammonium chloride and a polymerizable monomer having at least one or more ethylenically unsaturated hydrocarbons). Cationized cellulose, cationized polyvinylpyrrolidone, cationized polyamide, cationized polymethacrylate, cationized polyacrylamide, cationized methacrylate and acrylamide copolymer, cationized methacrylate and methacrylate copolymer, polyethyleneimide, cationized starch Cationized amylose, cationized guar gum, cationized roast bee gum, cationized agar, and the like. These cationic polymers may be used alone or as a mixture of two or more.

The dimethyldiallylammonium-containing polymer is a homopolymer obtained by polymerizing dimethyldiallylammonium chloride represented by the following structural formula (1) or an ethylenically unsaturated polymer represented by the following structural formula (2). A copolymer obtained by copolymerizing at least one kind of polymerizable monomer having a hydrocarbon group is effective.

[0009]

Embedded image (However, in the formula, R ₁ represents a COOH group or a CONH ₂ group.
R ₂ is a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms such as a methyl group. )

As the polymerizable monomer having an ethylenically unsaturated hydrocarbon group of the above formula (2), for example, acrylic acid, methacrylic acid, acrylamide and the like are suitable.

As such a dimethyldiallylammonium chloride-containing polymer, specifically, a mercoat (trade name) manufactured by Calgon can be suitably used. For example, Mercoat 100 which is a homopolymer of dimethyldiallylammonium chloride, dimethyldiallylammonium chloride, Mercoat 280, which is a copolymer of acrylic acid, Mercoat 550, which is a copolymer of dimethyldiallylammonium chloride and acrylamide, and Mercoat 3330, which is a three-component copolymer of dimethyldiallylammonium chloride, acrylic acid, and acrylamide (the following structural formula) reference).

[0012]

Embedded image

As the cationized cellulose, those having a degree of cationization of 0.01 to 1 and a viscosity of 100 to 3000 centipoise are preferable. Specifically, Leogard MGP, Leogard HLP and Leogard GP manufactured by Lion Corporation.
S, Leogard KGP, Leogard G, Leogard G
P, Leogard MLP, Polymer JR-125, Polymer JR- manufactured by Union Carbide Corporation
400, polymer JR-30M, cell coat H-100, cell coat L-200 manufactured by Kanebo NSC
Etc. can be used.

As the cationized polyvinylpyrrolidone, G.P. A. GA Corporation's GAFQUAT 74
3. GAFQUAT 745, Hymoloc Q-101 manufactured by Kyoritsu Organic Co., Ltd. as cationized polyamide, and Sumifloc FC-A and Sumifloc FC-B manufactured by Sumitomo Chemical Co., Ltd. as cationized polymethacrylate are cationized polyacrylamide. As Sanfloc C-450, Sanfloc C-454 manufactured by Sanyo Chemical Industries,
Hymoloc M-966 manufactured by Kyoritsu Organic Co., Ltd., Sumifloc FC-L manufactured by Sumitomo Chemical Co., Ltd., and Hymoloc MP-373 manufactured by Kyoritsu Organic Co., Ltd., and Sumifloc manufactured by Sumitomo Chemical Co., Ltd. as copolymers of cationized methacrylate and acrylamide. FC-373, Sumifloc FC-200,
Sumifloc FC-C may be used as a copolymer of cationized methacrylate and methacrylate. Sumifloc FC-E manufactured by Sumitomo Chemical Co., Ltd. may be used. As polyethyleneimide, Epomin P-1000 manufactured by Nippon Shokubai Chemical Co., Ltd. may be used.

The polyoxyethylene polyoxy according to the present invention
Cypropylene block copolymer type surfactants include the following general
Formula HO (C_TwoH_FourO)_a− (C_ThreeH₆O )_b− (C_TwoH_FourO)_cH (where a, b, and c are arbitrary integers)
Among them, those having a cloud point of 70 ° C. or more, more preferably
100 ° C or higher. If the cloud point is less than 70 ° C, the interface
Reduced water solubility as active agent, oral composition of the present invention
Can not be dissolved. Among them, polyoxyethylene (200)
Polyoxypropylene glycol (70), polyoxy
Ethylene (300) polyoxypropylene glycol
(55), polyoxyethylene (200) polyoxyp
Propylene glycol (40), polyoxyethylene (1
50) Polyoxypropylene glycol (35), poly
Oxyethylene (160) polyoxypropylene glyco
(30), polyoxyethylene (20) polyoxy
High effect is obtained with propylene glycol (20)
These are used as pluronic surfactants by Asahi Denka
Pluronic F-108, Pluronic F-1
27, Pluronic F-88, Pluronic F-87,
Traders such as Pluronic F-68 and Pluronic L-44
It is marketed under the product name.

The amount of the non-cationic bactericide to be added to the oral composition of the present invention is preferably 0.0001 to 5% by weight, particularly preferably 0.001 to 1% by weight, and more preferably 0.001 to 1% by weight of the whole composition.
If the amount is less than 01% by weight, a sufficient effect may not be obtained. Also,
The amount of the cationic polymer to be added is 0.1% of the whole composition.
0001 to 5% by weight, particularly 0.001 to 1% by weight is preferable, and if less than 0.0001% by weight, a sufficient effect may not be obtained. It will be difficult. The blending amount of the polyoxyethylene polyoxypropylene block copolymer type surfactant is preferably 0.01 to 5% by weight, particularly 0.02 to 3% by weight of the whole composition, and if less than 0.01% by weight, the dissolving power is reduced. Is insufficient, and it is difficult to uniformly mix the composition, and if it exceeds 5% by weight, the viscosity increases, and it becomes difficult to uniformly mix the composition.

The proportion of the cationic polymer and the non-cationic bactericide is appropriately selected, and the total amount of the cationic polymer is 0.5 to 9 per 100 parts by weight.
It is preferred to use 9.5 parts by weight, especially 5 to 95 parts by weight, 99.5 to 0.5 parts by weight, especially 95 to 5 parts by weight of the non-cationic fungicide.

The oral composition of the present invention may contain, in addition to the above-mentioned components, appropriate optional components according to the dosage form. Specifically, dentifrices such as toothpastes include crystalline silica, amorphous silica, aluminosilicate, zirconosilicate, other silica-based abrasives, aluminum oxide, aluminum hydroxide, and insoluble sodium metaphosphate as abrasives. , Insoluble potassium metaphosphate, titanium oxide, dibasic calcium phosphate dihydrate, dibasic calcium phosphate anhydrous, heavy calcium carbonate, light calcium carbonate, etc. (usually 3 to 99% by weight), carboxymethylcellulose as a binder Cellulose derivatives such as sodium, methylcellulose, hydroxymethylcellulose, carboxymethylhydroxymethylcellulose, synthetic binders such as polyvinyl alcohol and polyvinylpyrrolidone, and inorganic binders such as gelling silica, gelling aluminum silica, veganth and laponite. (Usually 0.5 to 10% by weight), sorbit, glycerin, ethylene glycol, propylene glycol, 1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltite, lactit, etc. 50% by weight).

Examples of the surfactant include nonionic surfactants such as sucrose fatty acid ester, polyoxyethylene hydrogenated castor oil, polyglycerin fatty acid ester, alkyl glycosides, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, and alkyldimethylamine oxide. Activators, betaine acetate-type amphoteric surfactants such as betaine alkyldimethylaminoacetate and fatty acid amidopropyldimethylaminoacetate, and imidazoline-type amphoteric surfactants such as N-fatty acid acyl-N-carboxymethyl-N-hydroxyethylethylenediamine salt ,
Anionic surfactants such as sodium lauryl sulfate, sodium dodecylbenzenesulfonate, and sodium lauryl sulfoacetate can be added in a range that does not impair the effects of the present invention (usually in an amount of 0.01 to 5% by weight).

Further, optional components include, for example, saccharin sodium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, thaumatin, asparatyl phenylalanine methyl ester,
p-methoxycinnamic aldehyde, sucrose, fructose,
Sweeteners such as sodium sakuramate, spearmint oil,
Peppermint oil, wintergreen oil, sassafras oil, clove oil, eucalyptus oil, sage oil, mayonnaise oil,
Flavors such as thyme oil, lemon oil, orange oil, l-menthol, carvone, anethole, methyl salicylate, etc., enzymes such as epsilon aminocaproic acid, tranexamic acid, dextranase, amylase, protease, mutanase, lysozyme, lytic enzyme, and litech enzyme. Chlorohexidine salts, cholestanol, glycyrrhetin salts, glycyrrhetinic acid, chlorophyll, caropeptides, vitamins, azulene, lysozyme chloride, anti-calculus agents, anti-plaque agents, potassium nitrate, aluminum lactate and the like. In addition, the addition amount of these optional components can be a usual amount as long as the effects of the present invention are not impaired.

The oral composition of the present invention includes a dentifrice,
Liquid dentifrice, mouthwash, mouthwash, chewing gum and the like, preferably dentifrice, liquid dentifrice, mouthwash, mouthwash, especially the composition of the present invention has a stable solubilization property It is characterized in that it is kept, and it is more preferable to use it in a liquid form such as a liquid dentifrice, mouthwash, mouthwash and the like.

[0022]

EFFECT OF THE INVENTION The oral composition of the present invention is excellent in the effect of inhibiting the adhesion of microorganisms to the tooth surface and the growth of bacteria, can effectively inhibit the formation of plaque, and is effective in preventing oral diseases. Can be used.

[0023]

EXAMPLES Hereinafter, the present invention will be described in detail with reference to experimental examples and examples, but the present invention is not limited to the following examples.

[Experimental Example] As an experiment for inhibiting plaque formation on the tooth surface by microorganisms, the components shown in Table 1 were evaluated for the effect of inhibiting the growth of Streptococcus mutans 10449 on a saliva-coated hydroxyapatite plate by the following method. In addition, the solubilization properties of the composition were evaluated as follows: the samples shown in Table 1 were prepared and then allowed to stand at 37 ° C. for 24 hours. Table 1 shows the results
Shown in

(1) A hydroxyapatite piece (manufactured by Asahi Optical Co., Ltd.) was used as a tooth model.
C. for 2 hours. (2) After being immersed in the sample shown in Table 1 for 30 minutes, it was washed with distilled water. (3) The cells were cultured for 12 hours in a liquid medium (Brain Heart Infusion) containing Streptococcus mutans. (4) After washing with distilled water, the cells were stained with fuchsin, and the cell adhesion area was calculated by image analysis. (5) The bacterial growth inhibition rate relative to the control was determined by calculation according to the following equation.

[0026]

(Equation 1)

[0027]

[Table 1] (However, cloud point of surfactant is measured with 1% aqueous solution)

From the results in Table 1, it can be seen that the combination of a non-cationic germicide, a cationic polymer, and a polyoxyethylene polyoxypropylene block copolymer type surfactant having a cloud point of 70 ° C. or more can be used in combination. It was confirmed that an oral composition having excellent solubilized properties, suppressing plaque formation, and effective in preventing oral diseases (prevention of dental caries and periodontal disease) was obtained.

Example 1 Toothpaste Aluminum hydroxide 45% by weight Sorbit 30 Sodium lauryl sulfate 0.5 Polyoxyethylene (60) hydrogenated castor oil 0.5 Saccharin sodium 0.1 Propylene glycol 5 Fragrance 1.3 Leogard MGP 0 .03 Triclosan 0.03 Pluronic F-108 1.5 Water Balance 100.0% by weight

Example 2 Toothpaste Dibasic calcium phosphate dihydrate 40% by weight Sorbit 30 Sodium saccharin 0.1 Propylene glycol 5 Polyoxyethylene (60) hydrogenated castor oil 1.5 Sodium monofluorophosphate 0.05 Hydroxymethylcellulose 0.3 Fragrance 1.3 Leogard GPS 0.05 Triclosan 0.05 Pluronic F-127 2 Water Balance 100.0% by weight

Example 3 Liquid Toothpaste Silica 18% by Weight Sorbit 55 Glycerin 18 Decaglycerin Monolaurate 1 Saccharin Sodium 0.15 Sodium Lauryl Sulfate 0.5 Propylene Glycol 2 Fragrance 1.5 Sodium Fluoride 0.1 Polyoxyethylene Glycol # 4000 0.5 Mercoat 280 0.1 Triclosan 0.1 Pluronic F-87 2.5 Water Balance 100.0% by weight

Example 4 Mouthwash Denatured ethanol 1.6% by weight Citric acid 0.01 Trisodium citrate 0.3 Sodium saccharin 0.1 Fragrance 0.5 Glycerin 7 Xylit 2 Leogard MGP 0.03 Triclosan 0. 03 Pluronic F-108 1 Water balance 100.0% by weight

Example 5 Mouthwash Ethanol 5% by weight Sodium saccharin 0.05 Chlorohexidine gluconate 0.01 Sodium lauryl sulfate 0.5 Dye 0.01 Sodium benzoate 0.05 Antioxidant 0.01 Perfume 0 3 Xylit 5 Polyoxyethylene (60) hydrogenated castor oil 0.5 Sodium monofluorophosphate 0.05 Leogard HLP 0.02 Triclosan 0.03 Pluronic F-127 1.5 Water Balance 100.0% by weight

Example 6 Mouthwash Denatured ethanol 5% by weight Fragrance 0.5 Glycerin 5 Xylit 5 Citric acid 0.01 Trisodium citrate 0.3 Leogard MGP 0.1 Hinokitiol 0.1 Pluronic F-108 1 Water balance 100.0% by weight

Example 7 Mouthwash 90% ethanol 20% by weight Fragrance 1.5 Sodium monofluorophosphate 0.05 Mercoat 100 0.02 Triclosan 0.02 Pluronic F-108 0.5 Water Balance 100.0 weight%

Claims (1)

[Claims] 1. An oral composition comprising a non-cationic bactericide, a cationic polymer, and a polyoxyethylene polyoxypropylene block copolymer type surfactant having a cloud point of 70 ° C. or higher.