JPH10167943A - Preparation for oral cavity - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a preparation for oral cavities, capable of directly administering a specific liquid composition into the oral cavities in a foamy state and good in suability by charging the composition into a specified container. SOLUTION: This preparation for oral cavities is obtained by charging a liquid oral cavity composition containing (A) 0.1-2wt.% of a surfactant preferably comprising a phosphate monoester e.g. a compound of the formula [R<1> is a (fluorinated) 6-20C linear or branched alkyl, alkenyl; one of X<1> , X<2> is a basic amino acid residue, and the other is H, an alkali metal, ammonium, etc.; (n) is 0-4]} and, if necessary, (B) a defoaming agent preferably a silicone defoaming agent, an antifungal agent, an antibacterial agent, a vehicle for oral cavities, etc., into a container equipped with a foam-generating mechanism and enabling to directly administer the composition into the oral cavities in a foam state through the mechanism. The extrusion port of the container preferably comprises a nozzle having an inner diameter of 1-7mm, an outer diameter of 2-10mm and a length of 5-60mm.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral preparation,
More specifically, the present invention relates to an oral preparation having good usability, in which an oral composition can be directly foamed from a container and charged.

[0002]

2. Description of the Related Art Among oral compositions, a mouthwash is used by rinsing the inside of an oral cavity without using a toothbrush, rinsing the inside of the oral cavity, and then using the mouthwash. Mouthwashes have a function of purifying the mouth and preventing bad breath, and those containing medicinal ingredients are also effective in preventing tooth decay and periodontal disease. Mouthwashes include a stock solution type, a concentrated type, and a powder type. Currently, the stock solution type is widely used.

[0003] Undiluted type mouthwashes are less troublesome to use than other types of mouthwashes, but the amount of use must be checked visually. When the cap of the container must be used after pouring it into the cap of the container, there is a trouble such that the cap must be washed after use in order to prevent the liquid from dripping to the outside of the container. In addition, since the mouthwash contains components that are strongly irritating in its function, if it is kept in the mouth for a predetermined period of time, it will be painful, and even though a refreshing feeling can be obtained, it is effective after use It is not satisfactory enough in terms of feeling. Furthermore, in order to sufficiently wash the inside of the mouth with a mouthwash, rinsing in the mouth is required strongly and for a predetermined time, which is not satisfactory in terms of usability.

[0004]

SUMMARY OF THE INVENTION Accordingly, it is an object of the present invention to provide an oral preparation which has no troublesome use and has reduced irritation in the oral cavity.

[0005]

In view of such circumstances,
As a result of intensive studies, the present inventors filled a liquid oral composition containing a surfactant for foam generation into a container equipped with a foam generating mechanism, and foamed the liquid oral composition at the time of use. It is discharged from the container as a shape, and it is directly injected into the oral cavity, so there is no need to use cups and caps of the container, so there is no need to use it, and from the moment when it is injected into the oral cavity Since the foamy oral composition spreads throughout the oral cavity, it acts on the upper teeth (especially the posterior teeth) which are difficult to reach when rinsing the oral cavity with the ordinary liquid oral composition, and also has a smooth mouth feel. The present inventors have found that the stimulus in the oral cavity is also reduced calmly, and have completed the present invention.

[0006] That is, the present invention provides a container for directly charging a liquid oral composition containing a surfactant into the oral cavity from a discharge port through a foaming mechanism. It is intended to provide an oral preparation characterized by being filled into a mouth.

[0007]

DESCRIPTION OF THE PREFERRED EMBODIMENTS The surfactant to be added to the liquid oral composition according to the present invention plays a role as a foam generating agent. For example, phosphates, sodium alkyl sulfate, alkyl benzene sulfonic acid sodium,
Sodium N-acyl sarcosinate, N-acyl glutamate, polyoxyethylene hydrogenated castor oil, polyoxyethylene polyoxypropylene block copolymer (pluronic type), sucrose fatty acid ester, alkyl glycosides, sorbitan fatty acid ester, polyoxyethylene Examples include sorbitan fatty acid esters, alkyldimethylamine oxides, carbobetaines, hydroxycarbobetaines, phosphobetaines, hydroxyphosphobetaines, sulfobetaines, hydroxysulfobetaines and the like. Of these, phosphate esters are not only excellent in surface activity, but also less irritating and form a film on the tooth surface,
It is preferred from the viewpoint of improving the acid resistance of the teeth, and is excellent in the effects of suppressing plaque formation and preventing dental caries, and phosphoric acid monoesters are particularly preferred.

[0008] Examples of the phosphoric acid monoesters include those represented by the following general formula (1) or (2).

[0009]

Embedded image

[In the formula, R ¹ represents a linear or branched alkyl or alkenyl group having 6 to 20 carbon atoms which may be substituted by a fluorine atom, and ^one of X ¹ and X ² represents a basic amino acid residue. A hydrogen atom, an alkali metal atom,
Represents an ammonium, alkylamine, alkanolamine or basic amino acid residue, and n represents a number from 0 to 4]

In the phosphoric acid monoester (1), R ¹
Having 6 to 6 carbon atoms which may be substituted by a fluorine atom
20 linear or branched alkyl or alkenyl groups include hexyl, octyl, decyl, dodecyl, tetradecyl, hexadecyl, octadecyl, eicosyl, 2-ethylhexyl, dodecenyl, oleyl, Elaidyl groups and the like. Among these R ¹ , an alkyl group having 8 to 20 carbon atoms, particularly preferably 10 to 20 carbon atoms, more preferably 12 to 16 carbon atoms, and further preferably 14 carbon atoms is preferable. These alkyl groups and alkenyl groups may have a single chain length or a mixture of a plurality of alkyl groups having different chain lengths.

The basic amino acids include, but are not limited to, naturally occurring arginine, lysine, and histidine, but are not limited thereto, and have a carboxyl group and an amino group in the molecule, are water-soluble, and have a pH of aqueous solution. Should be 7 or more. Of these, arginine is particularly preferred.

[0013]

Embedded image

Wherein R ² represents a linear or branched alkyl or alkenyl group having 8 to 30 carbon atoms, and X ³ and X ^3
4 is the same or different, a hydrogen atom, an alkali metal atom,
Represents an alkylammonium group, a hydroxy-substituted alkylammonium group or a basic amino acid residue]

In the general formula (2), R ² has 8 to ² carbon atoms.
0, especially 10-20, more preferably 12-16, and even 14 alkyl groups are preferred. Specific examples include a decyl group, a dodecyl group, a tetradecyl group, and a hexadecyl group. X ³ and X ⁴ are preferably partially neutralized products,
It is desirable that the degree of neutralization is 0.8 to 2.0, particularly 1.0 to 1.8. Specific examples thereof include monopotassium monodecyl phosphate, 1.2 sodium monododecyl phosphate, 1.3 potassium monotetradecyl phosphate, 1.5 triethanolamine monotetradecyl phosphate, monoarginine monotetradecyl phosphate, Monotetradecyl phosphate 1.3
Arginine, 1.2 sodium monohexadecyl phosphate, and the like.

The amount of the surfactant is preferably 0.01 to 2% by weight (hereinafter simply referred to as "%") in the liquid oral composition from the viewpoint of foaming and the like, and is preferably 0.02 to 2%. 1%
Is particularly preferred.

In the present invention, an antifoaming agent can be blended to adjust the foam quality of the liquid oral composition.
Examples of the antifoaming agent include silicones, alcohols, glycols, mineral oil, and polyoxyalkylene compounds, and silicones are particularly preferable. As the silicones, any shape such as an oil, a dissolved and dissolved, an emulsion, and an oil compound can be used.

The silicones have a viscosity of 10 to 10
Dimethyl polysiloxane and methyl phenyl polysiloxane having a molecular weight of 000 cs, particularly 100 to 5,000 cs; silicone resins, polyether-modified silicones and the like are preferable.
A high polymerization degree dimethylpolysiloxane having a 0% solution concentration of 1,000 to 10,000 cs can also be used.

When these silicones are used, the amount thereof to be used is preferably 1/50 to 5, especially 1/20 to 2 by weight relative to the surfactant, and the foam quality of the liquid oral composition is It is preferable from the point of view.

The liquid oral composition according to the present invention preferably contains a bactericide or an antibacterial agent in order to prevent tooth decay and periodontal disease. In the present invention, for example, the following general formula (3), which has a fast-acting bactericidal activity and a continuous antibacterial activity against oral bacteria, has a good taste, and does not decrease the bactericidal activity even when used in combination with a surfactant. ) Or (9).

[0021]

Embedded image

Wherein A ^{m +} represents a nitrogen-containing antibacterial cation, and a counter anion X ⁻ represents a straight-chain or branched-chain monoalkyl phosphate ion, monoalkenyl phosphate ion or monoalkyl phosphone having 8 to 20 carbon atoms. Represents an acid ion or a monoalkenyl phosphonate ion, and m represents the valence of the cation A]

Examples of the antibacterial compound (3) include compounds represented by the following general formulas (4) to (6).

[0024]

Embedded image

[Wherein at least one of R ³ , R ⁴ and R ⁵ represents a linear or branched alkyl or alkenyl group having 8 to 30 carbon atoms, and the rest is a methyl group, an ethyl group, a benzyl group,

[0026]

Embedded image

And R ⁶ represents —CH ₃ , —CH ₂ CH ₃ or —CH ₂ CH ₂ O
H, and the counter anion X ^5- represents a linear or branched monoalkyl phosphate ion, monoalkenyl phosphate ion, monoalkyl phosphonate ion or monoalkenyl phosphonate ion having 8 to 20 carbon atoms.]

In the general formula (4), at least one of R ³ , R ⁴ and R ⁵ is a linear or branched alkyl group having 8 to 14 carbon atoms, for example, 2-ethylhexyl, decyl, dodecyl or tetradecyl. And the remainder is a methyl group and / or
Or a compound which is a benzyl group is preferable.

[0029]

Embedded image

[Wherein, R ⁷ represents a linear or branched alkyl group having 10 to 20 carbon atoms, and X ^6- and X ⁷ are the same or different and each represent a linear or branched alkyl group having 8 to 20 carbon atoms. A monoalkyl phosphate ion, a monoalkenyl phosphate ion, a monoalkyl phosphonate ion or a monoalkenyl phosphonate ion]

The linear or branched alkyl group having 10 to 20 carbon atoms represented by R ⁷ in the general formula (5) includes:
For example, decyl group, dodecyl group, tetradecyl group, hexadecyl group, octadecyl group, eicosyl group and the like can be mentioned.

In addition, monoalkyl phosphate ions, monoalkenyl phosphate ions, and monoalkyl phosphonates which are counter anions (X ⁻ , X ^{5 −} , X ^6- or X ⁷ ) in the general formulas (3) to (6) Examples of the ion or monoalkenyl phosphonate ion include those represented by the following general formulas (7) and (8).

[0033]

Embedded image

[In the formula, R ⁸ represents a linear or branched alkyl or alkenyl group having ⁸ to 20 carbon atoms, and R ⁹ represents a hydrogen atom, an alkali metal atom, an alkyl ammonium group, a hydroxy-substituted alkyl ammonium group or a base. Shows amino acid residues)

[0035]

Embedded image

[In the formula, R ¹⁰ represents a linear or branched alkyl or alkenyl group having 8 to 20 carbon atoms, and R ¹¹ represents a hydrogen atom, an alkali metal atom, an alkyl ammonium group, a hydroxy-substituted alkyl ammonium group or a base. Shows amino acid residues)

In the general formula (7) or (8), R ⁸ and R ^{10 each} have 10 to 20 carbon atoms, particularly 12 to 16 carbon atoms,
The alkyl group is preferably a dodecyl group, a tetradecyl group, a hexadecyl group or the like. R ⁹ and R ¹¹ are usually a hydrogen atom, but may be partially substituted with an alkali metal atom such as potassium or sodium, an alkyl ammonium, a hydroxy-substituted alkyl ammonium or a basic amino acid.

The antibacterial compound (9) is represented by the following formula.

[0039]

Embedded image

[In the formula, A ^{m +} represents a nitrogen-containing antibacterial cation, the counter anion Y ⁻ represents a halogen ion or a gluconate ion, and m represents the valence of the cation A.]

Examples of the antibacterial compound (9) include compounds represented by the following general formulas (10), (11) and (12).

[0042]

Embedded image

[Wherein, the counter anions Y ^1- and Y ^2- each represent a halogen ion, Y ³ represents a halogen atom or a gluconic acid residue, and R ³ , R ⁴ , R ⁵ , R ⁶ and R ⁷ Is the same as above)

The antibacterial compound (3) or (9) is
0.001 to 20%, especially 0.1 to 20% in the oral composition of the present invention.
It is preferred that the content be in the range of 01 to 1%. The blending amount is 0.
If it is less than 001%, the bactericidal activity is weak, and if it is more than 20%, the formulation becomes unstable, and both are not preferred.

When the antibacterial compound (3) or (9) is blended with the liquid oral composition of the present invention, the surfactant represented by the formula (2) may be used as a surfactant. Is preferred from the viewpoint of persistence.

The compounding ratio of the antibacterial compound (3) or (9) and the surfactant varies depending on the kind of the antibacterial cation (A ^{m +} ), but the molar ratio is (A ^{m +} ) / (C) = 1/2. 1/10
An amount that satisfies 0, particularly (A ^{m +} ) / (C) = 1/2 to 1/50 is preferable. To describe in detail for each antibacterial compound, in the case of the antibacterial compound of the general formula (4) or (10), (A ^{m +} ) /
(C) = 1/2 to 1/100, preferably 1/2 to 1/100
In the case of the antibacterial compound of the general formula (5) or (11), (A ^{m +} ) / (C) = 1/2 to 1/20, preferably 1/2 to 1/10; (6) or (12)
1/2 to 1/50, preferably 1
/ 2 to 1/20.

The liquid oral composition according to the present invention contains, in addition to the above-mentioned components, an oral vehicle which is usually used within a range not to impair the effects of the present invention, and forms a mouthwash, liquid dentifrice and the like. can do.

[0048] Such oral vehicles include fragrances,
Examples include sweeteners, preservatives, pigments, water, water-soluble fluorides, and other active ingredients.

Examples of the humectant include polyethylene glycol, propylene glycol, sorbitol, glycerin, maltitol, xylitol and the like. Of these, glycene, sorbitol and the like are preferred. Natural flavors such as spearmint oil, peppermint oil, winter green oil, sassafras oil, clove oil, sage oil, eucalyptus oil, mayonnaise oil, cinnamon oil, thyme oil, lemon oil and orange oil; and l-menthol, anethole , Carvone, eugenol, thymol, methyl salicylate and the like. Examples of the sweetener include saccharin, saccharin sodium, stevioside, neohesperidyl dihydrochalcone, berraltin, p-methoxycinnamic aldehyde, glycyrrhizinate, aspartame (aspartylphenylalanine methyl ester) and the like. Preservatives include benzoic acid, sodium benzoate, parahydroxybenzoate and the like. Examples of the water-soluble fluoride include sodium fluoride and sodium monofluorophosphate. Other active ingredients include chlorophyll compounds, sodium chloride, vitamin C, vitamin E, nicotinic acid ester, allantoinchlorohydroxyaluminum, azulene, lysozyme chloride, hinokitiol, β-glycyrrhetinic acid, dipotassium glycyrrhizinate, protease, crude drug extracts, etc. Is mentioned.

Among these oral vehicles, the liquid oral composition basically contains 1 to 30% of a wetting agent,
Preferably, it contains 50 to 96% of alcohol and water. Here, the ratio of water: alcohol is 1: 1 to 2 by weight.
00: 1, particularly preferably 5: 1 to 100: 1. In addition, it is preferable to mix | blend 1-20% of alcohol in the whole composition. It is preferable that the flavor and the sweetener are combined in a total amount of 0.01 to 5%. Further, the liquid oral composition of the present invention
The pH is preferably in the range from 5 to 9.5, in particular from 6 to 8.

The container for filling the liquid oral composition has a foam generating mechanism, and has a structure in which the foamed liquid oral composition is directly introduced into the oral cavity via the mechanism. The container body is flexible, and the discharge port is a nozzle, and the liquid is generated when the container body is pressed and deformed to pressurize the inside of the container. It is preferable from the viewpoint of usability that the composition has a structure in which the composition for oral cavity is ejected in the form of foam.

The discharge nozzle of the container has an inner diameter of 1 to 7 mm and an outer diameter of 2 to 10 in order to ensure that the discharged foamy composition is properly injected into the oral cavity and is not directly discharged to the throat.
mm and a length of 5 to 60 mm are preferable, but an inner diameter of 1 to 5 mm, an outer diameter of 2 to 8 mm, and a length of 5 to 40 mm are more preferable. Further, it is preferable that the discharge nozzle is directed upward by about -5 to 20 degrees, particularly 0 to 15 degrees above the horizontal direction. The diameter of the suction tube is preferably 1 to 3.5 mm, and 1.5 to 2.
5 mm is more preferred. In addition, since the size of the container is to be directly injected into the oral cavity from the container, a capacity of 5
About 0 to 400 ml is preferable. Further, as the foam generation mechanism, a mechanism is preferable in which when the inside of the container is pressurized by pressing and deforming the container body, the composition is mixed with air and generates bubbles through a net provided inside.

[0053]

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

Embodiment 1 FIG. 1 is a schematic view showing an example of a container provided with a foam generating mechanism used in the present invention. The foam discharge container includes a base cap 1 attached to a flexible container main body 2 and a base cap 1
And an overcap 30 which is slidably fitted between an open position and a closed position.

A mixer 16, a net holder 17 to which a foam homogenizing net 18 is welded, and a pipe 19 are assembled and integrated into the base cap 1 by press-fitting or the like. The base cap 1 is made of polypropylene (PP) and the mixer 16
Is high-density polyethylene (HDPE), net holder 1
7 is chain low density polyethylene (LLDPE), net 1
8 is polyethylene terephthalate (PET), pipe 1
9 was molded from polypropylene (PP). Also,
The nozzle 31 is integrated with the base cap 1 by press-fitting or the like. Nozzle 31 is polypropylene (PP)
Molded.

The base cap 1 is connected to the oral composition introduction passage 2 extending to the bottom in the container body 2 by a pipe 19.
1 is formed, an air introduction passage 20 communicating with the upper space in the container body 2 is formed by the mixer 16, and a liquid introduction passage 31 and a downstream side of the air introduction passage 20 are communicated by the mixer 16 and the net holder 17. The gas-liquid mixing chamber 22 is formed, and a bubble outflow passage 23 communicating with the downstream side of the gas-liquid mixing chamber 22 via the net 18 by the inner diameter portion of the mixer mounting cylinder 10 is formed. The base cap 1 closes the upper end of the foam outflow passage 23 with the plug 13, and opens the foam outflow passage 23 on the side of the plug 13.

Therefore, in the foam discharging container, when the inside of the container main body 2 is pressurized and deformed at the time of discharging the foam to pressurize the inside of the container main body 2, the solution in the container is discharged from the pipe 19 through the composition introduction passage 2 for the oral cavity.
1 and is sent to the gas-liquid mixing chamber 22, and the air in the container passes through the air introduction passage 20 of the mixer 16 and the gas-liquid mixing chamber 22.
Sent to. Then, in the gas-liquid mixing chamber 22, the liquid introduced from the liquid introduction passage 21 and the air sent from the air introduction passage 20 are mixed and foamed, and the foam is homogenized by the net 18 and the foam outflow passage 23 And further flows through the bubble discharge passage 29 and is discharged from the nozzle 31. At this time, the container body 2 is pressed and the air in the container is discharged and deformed, but the deformation of the container body 2 is released and restored by taking in the outside air from the air return passage immediately after the discharge of the foam. In FIG. 1, 3 is an opening, 4 is a discharge port, 5 is a nozzle cap, 6 is a sealing portion, 7 is a cover portion, 7a is a lower end portion,
8 and 9 are fitting cylinders, 11 is a cylinder, 12 is a cap slide guide cylinder, 14 is a step, 15 is a mouth, 24 and 2
5 is a projection, 26 is a skirt, 27 is a cylinder, and 28 is a slide guide cylinder.

The nozzle 31 has an inner diameter of 1 to 7 mm, an outer diameter of 2 to 10 mm, and a length of 5 to 60 mm in order to reliably and easily introduce the foamed oral composition into the oral cavity. Preferably, the angle between the nozzle and the cap 1 (θ)
Is preferably set to 85 to 110 degrees. In terms of usability, the nozzle 31 has an inner diameter of 1 to 5 mm, an outer diameter of 2 to 8 mm, and a length of 5 mm.
It is particularly preferable to set the angle (?) To 90 to 105 degrees. In addition, in the container shown in FIG. 1, the discharge port may be provided not on the side surface of the container but on the top.

Examples 2-3 A liquid oral composition was prepared according to the following formulation, and
In the foam discharge container shown in (1), a container body 2 (capacity 250 ml) made of PET, inner diameter 2.5 mm, outer diameter 6 mm, length 2
The container was equipped with a nozzle 3 having 0 mm and an angle (θ) of 90 degrees.

[0060]

[Table 1]

Test Example 1 The liquid oral cavity composition of Example 2 was filled in the container shown in FIG. 1 and foamed directly into the oral cavity, and the container net 18 shown in FIG. The removed container was filled with the composition, and the liquid was directly injected into the oral cavity as it was, and the usability was evaluated by men and women in their 20s and 30s.
The results are shown in the following table.

[0062]

[Table 2]

In the case of a foamed product, even if it is put into the mouth by increasing the pressure on the container, the contact with the oral cavity wall and throat is gentle, so that the pressure on the container is easy to use and easy to use. The irritation is felt small, and a refreshing feeling after use is sufficiently obtained. On the other hand, in the case of a liquid, when the pressure on the container is large, the composition is injected into the back of the throat, and the contact is severe, so that the composition is choppy.

[0064]

The oral preparation of the present invention has excellent advantages such as good usability since the oral composition can be directly foamed from a container and put into a foam.

[Brief description of the drawings]

FIG. 1 is a schematic view showing an example of a discharge container used in the present invention.

[Explanation of symbols]

 DESCRIPTION OF SYMBOLS 1 Base cap 2 Container main body 3 Opening 4 Discharge port 5 Nozzle cap 6 Sealing part 7 Cover part 7a Lower end part 8 Fitting cylinder part 9 Fitting cylinder part 10 Mixer attachment cylinder part 11 Tube part 12 Cap slide guide cylinder part DESCRIPTION OF SYMBOLS 13 Plug 14 Step part 15 Mouth 16 Mixer 17 Net holder 18 Net 19 Pipe 20 Air intake hole 21 Oral composition introduction passage 22 Gas-liquid mixing chamber 23 Bubble outflow passage 24 Projection 25 Projection 26 Skirt 27 Tube 28 Slide guide cylinder 29 Bubble discharge passage 30 Overcap 31 Nozzle

Claims (4)

[Claims] Claims: 1. A liquid oral composition containing a surfactant is filled in a container that is directly injected into the oral cavity from a discharge port through a foaming mechanism, the liquid oral composition being foamed. An oral preparation characterized by the following. 2. The oral preparation according to claim 1, wherein the liquid oral composition further contains an antifoaming agent. 3. The oral agent according to claim 1, wherein the surfactant is a phosphoric acid monoester. 4. The discharge port has an inner diameter of 1 to 7 mm and an outer diameter of 2 to 10
The oral agent according to any one of claims 1 to 3, which is a nozzle having a length of 5 to 60 mm in mm.