JP2001302478A - Liquid composition for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide a uniform and transparent composition containing an oil-soluble component and having a small amount of a surfactant. SOLUTION: This transparent liquid composition for oral cavity is characterized by containing water, an oil-soluble component and a nonionic surfactant and having (1,000:1)-(1:1) weight ratio of blending ratio of the oil soluble component to the nonionic surfactant.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a liquid composition for oral cavity.

[0002]

2. Description of the Related Art In many cases, an oil-soluble component such as an oil-soluble flavor, an oil-soluble medicinal component and the like is blended in an oral liquid composition. When an oil-soluble component is blended, a transparent composition is required to increase the commercial value, but a large amount of the interface is usually larger than the amount of the oil-soluble component in order to solubilize and make the composition transparent. An activator is used. Surfactants themselves have a peculiar odor, and when blended in a composition, there are problems such as deterioration of perfume standing and inhibition of action of medicinal ingredients. More specifically, an oral composition containing a cationic fungicide for the purpose of preventing dental caries and periodontal disease has a problem that the activity of the cationic fungicide is lost by the surfactant. For example, Japanese Patent Application Laid-Open No. 4-202121 proposes a technique for sufficiently exhibiting the effect of a cationic bactericide by blending polyoxyethylene polyoxypropylene glycol which is a nonionic surfactant. Since the surfactant has a low solubilizing power of the oil-soluble component, if the amount is such that transparency can be obtained, the perfume will not stand well.

[0003] However, if the amount of the surfactant is reduced, the solubilizing power of the oil-soluble component is reduced, and the transparency is poor. As a technique for reducing the amount of the surfactant, for example, JP-A-61-268614 and JP-A-7-101842 disclose an oral composition using a fragrance as a hydrophilic fragrance (water-soluble fragrance). However, the above-mentioned disadvantages when an oil-soluble component is blended are not solved.

[0004]

An object of the present invention is to provide a transparent oral liquid composition which does not have the above-mentioned disadvantages.

[0005]

Means for Solving the Problems The present inventors have found that a uniform and transparent composition can be obtained even for an oral composition containing an oil-soluble component and having a small amount of a surfactant. The present invention has been completed.

That is, the present invention provides the inventions described in the following items.

Item 1 contains water, an oil-soluble component and a nonionic surfactant, and is characterized in that the weight ratio of the oil-soluble component to the nonionic surfactant is from 1000: 1 to 1: 1. Transparent oral liquid composition.

Item 2 The oral liquid composition according to Item 1, wherein the weight ratio of the amounts of the oil-soluble component and the nonionic surfactant is from 100: 1 to 1: 1.

Item 3 The oral liquid composition according to Item 1, wherein the amount of the nonionic surfactant is 0.0001 to 0.1% by weight.

Item 4 The oral liquid composition according to Item 3, wherein the amount of the nonionic surfactant is 0.005 to 0.05% by weight.

Item 5. The oral composition according to Item 1, which contains a cationic bactericide.

Item 6 The oral liquid composition according to item 5, wherein the cationic bactericide is at least one selected from the group consisting of quaternary ammonium compounds and biguanide compounds.

Item 7 The oral liquid composition according to Item 5, wherein the cationic bactericide is at least one selected from the group consisting of cetylpyridinium chloride, stearyldimethylbenzylammonium chloride and chlorhexidine salt.

Item 8: Item 1 containing malic acid and its salt
A liquid composition for oral cavity according to item 1.

[0015]

DETAILED DESCRIPTION OF THE INVENTION The oral liquid composition of the present invention contains an oil-soluble component and a nonionic surfactant, and the ratio of the oil-soluble component to the nonionic surfactant is 1000: 1 to 1: 1. This is a transparent and uniform liquid composition for oral cavity.

In the present invention, "transparent" means that the composition has a transmittance of about 70% or more, preferably about 80% or more. The transmittance can be measured using a spectrophotometer at a measurement wavelength in the visible light region.

The nonionic surfactant used in the oral composition of the present invention is not particularly limited, and can be appropriately selected according to the type of the oil-soluble component.

The following nonionic surfactants are preferably used.

A polyoxyethylene polyoxypropylene block copolymer type nonionic surfactant, for example, polyoxyethylene polyoxypropylene glycol having a degree of polymerization of ethylene oxide of about 4 to 260 and a degree of polymerization of propylene oxide of about 10 to 80; More specifically, polyoxyethylene (150) polyoxypropylene (30) glycol and the like can be mentioned.

Saccharide fatty acid esters, such as sucrose fatty acid esters, maltose fatty acid esters, and lactose fatty acid esters, in which the fatty acid has about 8 to 20 carbon atoms; for example, sucrose stearate, maltose laurate, lactose myristate, etc. Is mentioned.

Fatty acid alkanolamides having about 8 to 20 carbon atoms in fatty acids; for example, lauric acid monoethanolamide, coconut oil fatty acid diethanolamide and the like.

Polyoxyethylene hydrogenated castor oil having a degree of polymerization of ethylene oxide of about 5 to 120; for example, polyoxyethylene (60) hydrogenated castor oil, polyoxyethylene (1
0) Hardened castor oil and the like.

Polyoxyethylene fatty acid esters having a degree of polymerization of ethylene oxide of about 5 to 200 and a fatty acid having about 8 to 20 carbon atoms; for example, polyoxyethylene (20) monooleate, polyoxyethylene (2) monostearate And the like.

Sorbitan fatty acid esters having about 8 to 20 carbon atoms of fatty acids; for example, sorbitan stearate, sorbitan monoisostearate, sorbitan monopalmitate and the like.

Fatty acid monoglycerides in which the fatty acid has about 8 to 20 carbon atoms; for example, oleic acid monoglyceride, monostearic acid glyceride, lauric acid glyceride and the like.

Polyoxyethylene alkyl ether having a polymerization degree of ethylene oxide of about 2 to 20 and an alkyl group of about 8 to 20 carbon atoms; for example, polyoxyethylene (15) lauryl ether, polyoxyethylene (10) myristyl Ether and the like.

These surfactants may be used alone or in combination of two or more. HL if used together
It is preferable to use those having a B value of 10 or more and those having a B value of less than 10.

The amount of the nonionic surfactant is not particularly limited as long as the desired effect of the present invention can be obtained, but is usually about 0.000 to the total amount of the composition.
About 1 to 0.1% by weight, preferably 0.005 to 0.0
It is about 5% by weight.

The oil-soluble component is not particularly limited as long as it is an oil-soluble component usually blended in a liquid composition for oral cavity. Examples of the oil-soluble component include oil-soluble flavors, oil-soluble active ingredients and Medicinal ingredients and the like.

Examples of oil-soluble flavors include menthol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, diatom oil, perilla oil, winter green oil, clove oil, eucalyptus oil, pimento oil, Anethole, eugenol, plum oil and the like are exemplified. These can be used alone or in combination of two or more.

The oil-soluble active ingredient or medicinal ingredient includes:
There is no particular limitation, and it can be appropriately selected according to the intended use from the medicinal components usually contained in the oral composition. Examples thereof include vitamin Es such as dl-α-tocopherol acetate, tocopherol succinate, and tocopherol nicotinate; and oil-soluble bactericides such as triclosan and isopropylmethylphenol.

The oil-soluble component used in the present invention is preferably a liquid (including an oil or paste) at room temperature, but a solid or powdery oil-soluble component at room temperature may be used. When a solid or powdery oil-soluble component is used at room temperature, it is usually used by heating it into a liquid state or by dissolving it in another oil-soluble component that is liquid at room temperature. Such components include triclosan, ρ-methoxycinnamic aldehyde, tranexamic acid, dihydrocholesterol,
Glycyrrhetinic acid, glycerophosphate, chlorophyll and the like.

The amount of the oil-soluble component is not particularly limited as long as the desired effect of the present invention can be obtained, but is usually 0.01 to 5.0 with respect to the total amount of the composition.
% By weight, preferably about 0.1 to 0.5% by weight.

In the composition of the present invention, the mixing ratio of the oil-soluble component and the nonionic surfactant is 1000: 1 by weight.
About 1: 1 and preferably about 100: 1 to 1: 1. It is preferable if it is in the above range, since the transparency is excellent and the effect of the oil-soluble component is not hindered.

The oral composition of the present invention may further contain, according to the form of the composition, commonly used components as long as the effects of the present invention are not impaired.

For example, a water-soluble bactericide, which is usually contained in an oral composition, can be added. Preferred examples of the bactericide include cationic surfactants such as quaternary ammonium compounds and biguanide compounds. More specifically, quaternary ammonium salts include cetylpyridinium chloride and stearyldimethylbenzylammonium chloride, and biguanide compounds include chlorhexidine salts such as chlorhexidine hydrochloride and chlorhexidine gluconate.

When a water-soluble bactericide is added, it is added in an amount of about 0.001 to 10% by weight, preferably about 0.01 to 1% by weight, based on the total amount of the composition. Within such a range, a sufficient bactericidal effect is exhibited, and there is no possibility of causing a problem of tooth coloring.

The oral composition of the present invention comprises, as active ingredients other than a bactericide, or other active ingredients, enzymes such as dextranase, amylase, protease, mutanase, lysozyme, and lytic enzyme (Litech enzyme); Alkali metal monofluorophosphates such as sodium and potassium monofluorophosphate; fluorides such as sodium fluoride and stannous fluoride; epsilon aminocaproic acid, aluminum chlorohydroxyl allantoin, glycyrrhizin salts, sodium chloride, caropeptide, etc. Or in combination of two or more. When these water-soluble active ingredients or medicinal ingredients are compounded, the total amount of the composition is 0.00
It can be blended at a ratio of about 1 to 10% by weight, preferably about 0.01 to 1% by weight.

The composition of the present invention may contain a sweetener such as saccharin sodium, acesulfame potassium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartin, thaumatin, asparatyl phenylalanyl methyl ester and the like. You. When a sweetener is added, it can be added at a rate of about 0.01 to 1% by weight, preferably about 0.05 to 0.5% by weight, based on the total amount of the composition.

The composition of the present invention contains malic acid and its salts (eg, sodium salt and potassium salt) in an amount of about 0.0001 to 1% by weight, preferably 0.1 to 1% by weight, based on the total weight of the composition.
It can be blended at a ratio of about 001 to 0.5% by weight. It is preferable to mix malic acid and a salt thereof because the low-temperature stability of the composition is improved.

The oral composition of the present invention further includes alkali metal alginate such as cationized hydroxyethyl cellulose and sodium alginate; gums such as propylene glycol alginate, xanthan gum, tragacanth gum, karaya gum, arabia gum, and carrageenan; polyvinyl alcohol; One or more kinds of binders such as sodium polyacrylate, carboxyvinyl polymer, and polyvinylpyrrolidone can be blended. The blending amount when these are blended is usually
It is about 0.001 to 0.1% by weight.

Further, as humectants, sorbitol, glycerin, ethylene glycol, propylene glycol,
1,3-butylene glycol, hexylene glycol,
Polyethylene glycol, polypropylene glycol,
Xylit, maltit, lactit and the like can be used alone or in combination of two or more. The compounding amount of these compounds is usually about 5 to 30% by weight based on the total amount of the composition. In addition to the above, the composition of the present invention further comprises an N-long-chain acyl basic amino acid lower alkyl ester. Alternatively, a salt thereof can be blended. The basic amino acid moiety is particularly preferably ornithine, lysine, or arginine, which may be any of an optically active form and a racemic form. An acyl group is a saturated or unsaturated natural or synthetic fatty acid residue having 8 to 22 carbon atoms, for example,
Examples thereof include a single fatty acid residue such as a lauroyl group, a myristyl group, a palmitoyl group, and a stearoyl group, and may be a natural mixed fatty acid residue such as a coconut oil fatty acid residue and a bovine oil fatty acid residue. Examples of the lower alkyl ester include a methyl ester, an ethyl ester, and a propyl ester. Salts of these lower alkyl esters of N-long chain acyl basic amino acids include inorganic salts such as hydrochloride and sulfate; glutamate, pyroglutamate, acetate, tartrate, citrate, fatty acid salt, Organic acid salts such as acidic amino acid salts are exemplified. In particular, glutamate,
Pyroglutamate, acetate and citrate are preferred. As the N-long-chain acyl basic amino acid lower alkyl ester or a salt thereof, specifically, N-cocoyl-L-
Arginine ethyl ester / pyrrolidone carboxylate (CA
E) and N-lauryl-L-arginine ethyl ester / pyrrolidone carboxylate.

When the N-long-chain acyl basic amino acid lower alkyl ester or a salt thereof is compounded, the compounding amount thereof is about 0.005 to 5% by weight, especially 0.01 to 5% by weight based on the whole oral liquid preparation.
About 1% by weight is preferred.

When an N-long-chain acyl basic amino acid lower alkyl ester or a salt thereof is blended with a cationic fungicide, the effect of adsorbing the fungicide to the tooth surface is enhanced. Therefore, when a cationic bactericide is blended, it is preferred to blend it with an N-long-chain acyl basic amino acid lower alkyl ester or a salt thereof. Cationic fungicide and N
When the lower alkyl ester of a long-chain acyl basic amino acid or a salt thereof is simultaneously added, the amount thereof is preferably about 1/5 or more by weight based on the cationic bactericide. The upper limit of the weight ratio in this case is not particularly limited,
Usually, it is about 10 times.

In the composition of the present invention, for example, a composition which is made cloudy by previously mixing water, an oil-soluble component and a surfactant and, if necessary, other components is further mixed under pressure under specific conditions. Can be obtained by:

The method of preliminarily mixing (“preliminary mixing”) is not particularly limited, but can be performed using a commonly used high-speed stirrer, ultrasonic homogenizer, or the like. The premixing conditions are not particularly limited, and the premixing may be performed under pressure or under atmospheric pressure. The oil-soluble component in the form of solid or powder at room temperature may be preliminarily mixed by heating it to a liquid state or dissolving it in another oil-soluble component in a liquid state at room temperature.

When premixing is performed using a high-speed stirrer,
For example, at about 1,000 to 20,000 rpm,
The mixture can be stirred for about 60 minutes.

When premixing is carried out using an ultrasonic homogenizer, each component is supplied to an ultrasonic irradiation chamber at a constant flow rate, irradiated with ultrasonic waves at an oscillation frequency of about 20 kHz, and dispersed to produce a cloudy mixture. A liquid can be obtained.

The degree of the pre-mixing is not particularly limited, but as the components are more finely dispersed in the obtained turbid mixture, the transparency is increased by mixing under pressure described later. An excellent transparent liquid composition is obtained.

The cloudy liquid mixture obtained by the premixing is further mixed under pressure to be transparent. Mixing under pressure is performed, for example, by using a high-pressure homogenizer,
It can be performed using a fluid mixing device (Ramond mixer) as disclosed in JP-A-39173, a device for passing through a microporous membrane as disclosed in JP-B-8-2416, or the like. .

In the present invention, the conditions in the case of using a high-pressure homogenizer to make the cloudy mixture transparent are not particularly limited as long as a transparent composition can be obtained. It can be set appropriately according to the type of the soluble component and the like.

For example, at a pressure of about 10 to 200 MPa, preferably about 50 to 150 MPa, it is desirable that the mixture is circulated 2 to 5 times at room temperature or while heating as needed, and mixed as needed. .

In the case of using a ramond mixer, for example, using an apparatus disclosed in Japanese Patent Publication No. 59-39173, at a pressure of about 0.1 to 10 MPa, while heating at room temperature or as needed. Can be mixed. Moreover, you may circulate and mix 2 to 5 times as needed.

When the turbid mixture is mixed using a microporous membrane, the turbid mixture obtained by the premix is subjected to a pressure at which a transparent composition is obtained, usually a pressure of about 0.3 to 20 MPa. While passing through the microporous membrane. If necessary, the mixture can be circulated 2 to 5 times and passed through the microporous membrane to mix. The microporous membrane may be inorganic or organic as long as it has a uniform pore size. For example, Japanese Patent Publication No. 62-256
No. 18 disclosed in Japanese _{CaO-B 2 O 3 -SiO 2} -A
l ₂ O ₃ based porous glass, Sho 61-40841 Patent Publication and US Patent No. 4,657,875 Pat disclosed in the _{CaO-B 2 O 3 -SiO 2} -Al 2 O 3 -Na 2 O-based porous glass and _{CaO-B 2 O 3 -SiO 2} -Al 2 O 3 -N
a ₂ O-MgO-based porous glass and the like can be used as-coated film to the glass porous membrane material.

Here, the “uniform pore diameter” is defined in Japanese Patent Publication No.
As disclosed in Japanese Patent No. 2416, the pore diameter of the microporous membrane body is defined as the pore diameter (φ10) when the pore volume occupies 10% of the whole in the relative cumulative pore distribution curve,
Pore diameter when the pore volume occupies 90% of the whole (φ90)
Is in the range of about 1 to 1.5.

The average pore size of the microporous membrane used for the transparency of the cloudy mixed solution can be appropriately selected according to the transparency to be obtained, and is usually about 1 μm or less, preferably about 0.8 μm or less. More preferably, it is about 0.5 μm or less.

The thickness of the microporous membrane is not particularly limited, but is usually about 0.4 to 2 mm.

Among these exemplified production methods, the method for producing the transparent liquid composition of the present invention is preferably a method in which pressure mixing is performed using a microporous membrane.

The process for producing the composition of the present invention comprises water, an oil-soluble component and a nonionic surfactant, wherein the ratio of the oil-soluble component to the nonionic surfactant is from 1000: 1 to 1: 1; Any method may be used as long as a transparent and uniform composition can be obtained, and it is not limited to the above-described production methods and conditions.

The oral composition of the present invention can be in the form of a liquid such as liquid dentifrice, mouthwash, mouthwash, dental rinse, mouthwash, mouthwash (gargle) and the like.

[0061]

According to the present invention, a transparent composition containing water, an oil-soluble component and a surfactant and having a low surfactant content can be obtained.

[0062]

The present invention will be described in more detail with reference to the following examples, but the present invention is not limited to these examples. In Examples,% is% by weight unless otherwise specified.

Examples 1 to 4 and Comparative Examples 1 to 3 Liquid dentifrices were prepared according to the formulations shown in Table 1 according to a conventional method (the numerical values of each component in the table indicate the amount (%)). The resulting liquid dentifrice was evaluated for flavor, effectiveness of the fungicide and transparency.

Each component was uniformly dissolved and mixed using a high-speed stirrer (15,000 rpm for 15 minutes). The obtained cloudy mixed solution was passed through a microporous membrane having a uniform pore size of 0.1 μm while applying pressure (1.0 MPa).

With respect to the flavor, five panelists were allowed to use the liquid dentifrice for one minute, and the sensory evaluation was carried out on a five-point scale according to the following evaluation criteria.

-: Very bad flavor-: Bad flavor ±: Normal flavor +: Good flavor ++: Very good flavor

The effectiveness of the bactericide was measured by measuring the amount of stagnation in hydroxyapatite (hereinafter referred to as HA) as a tooth surface model.
The ratio (%) when it was set to 0% was obtained, and expressed in five stages according to the following evaluation criteria.

-: Retention amount of fungicide in HA is less than 40%-: Retention amount of fungicide in HA is less than 40% and less than 60% ±: Retention amount of fungicide in HA is 60% or more , Less than 80% +: The amount of germicide retained in HA is 80% or more and less than 100% ++: The amount of bactericide retained in HA is 100% or more.

The transmittance was measured using a spectrophotometer, and evaluated in five steps according to the following evaluation criteria.

-: Transmittance is less than 60%-: Transmittance is 60% or more and less than 70% ±: Transmittance is 70% or more and less than 80% +: Transmittance is 80% or more and less than 90% ++: Transmittance is 90% or more.

Table 1 shows the results.

[0072]

[Table 1]

The compositions of Examples 1 to 4 and Comparative Examples 1 and 2 whose transparency immediately after production was + or ++ were evaluated for transparency even after being left at 55 ° C. for 2 weeks. However, the result was similar to that immediately after the production.

Comparative Examples 1 to 3 in which the mixing ratio of the fragrance and the surfactant is out of the range (1000: 1 to 1: 1) of the present invention.
Did not provide a composition with excellent transparency, flavor and fungicide efficacy. On the other hand, in Examples 1 to 4 in which the mixing ratio of the fragrance and the surfactant was within the range of the present invention, a composition excellent in all of the transparency, the flavor and the effectiveness of the bactericide was obtained.

Hereinafter, formulation examples of the oral composition of the present invention will be shown.

Formulation Example 1 The following components dissolved uniformly were mixed using a high-speed stirrer (15,000 rpm for 15 minutes). The obtained cloudy mixed solution was passed through a microporous membrane having a uniform pore size of 0.4 μm while applying pressure (1.0 MPa) to prepare a mouthwash. Ingredient name Blended amount (%) Concentrated glycerin 20 POE (60) hydrogenated castor oil 0.01 Saccharin sodium 0.1 Cetylpyridinium chloride 0.1 Sodium malate 0.05 Tocopherol acetate 0.02 N-cocoyl-L-alkidinine ethyl ester Hydrolitonic acid carbonate 0.15 Fragrance 0.2 Purified water Remainder Total 100 The obtained mouthwash was evaluated according to the same criteria as in the example. The flavor, the effectiveness of the fungicide, the transparency and its daily stability were evaluated. Both were excellent.

Formulation Example 2 The following components uniformly dissolved were mixed using a high-speed stirrer (at 10,000 rpm for 10 minutes). The obtained cloudy mixed solution was passed through a microporous membrane having a uniform pore size of 0.1 μm while applying pressure (0.5 MPa) to produce a liquid dentifrice. Component name Content (%) Concentrated glycerin 20 POE (20) sorbitan fatty acid ester 0.005 Sodium saccharin 0.1 Chlorhexidine gluconate 0.1 Sodium malate 0.05 Carrageenan 0.01 Tocopherol acetate 0.1 Fragrance 0.1 Purification Water Remainder Total 100 When the obtained liquid dentifrice was evaluated according to the same criteria as in the above example, it was found to be excellent in all of the flavor, the effectiveness of the fungicide, the transparency, and the stability over time.

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Claims (8)

[Claims] 1. A composition comprising water, an oil-soluble component and a nonionic surfactant, wherein the weight ratio of the oil-soluble component to the nonionic surfactant is from 1000: 1 to 1: 1. Transparent oral liquid composition. 2. The oral liquid composition according to claim 1, wherein the weight ratio of the amounts of the oil-soluble component and the nonionic surfactant is from 100: 1 to 1: 1. 3. The compounding amount of the nonionic surfactant is 0.0
The oral liquid composition according to claim 1, wherein the amount is from 001 to 0.1% by weight. 4. The compounding amount of the nonionic surfactant is 0.0
The oral liquid composition according to claim 3, wherein the amount is from 0.05 to 0.05% by weight. 5. The oral composition according to claim 1, further comprising a cationic bactericide. 6. The oral liquid composition according to claim 5, wherein the cationic bactericide is at least one selected from the group consisting of quaternary ammonium compounds and biguanide compounds. 7. The liquid composition for oral cavity according to claim 5, wherein the cationic bactericide is at least one selected from the group consisting of cetylpyridinium chloride, stearyldimethylbenzylammonium chloride and chlorhexidine salt. 8. The composition according to claim 1, which contains malic acid and a salt thereof.
A liquid composition for oral cavity according to item 1.