JP2024080696A - Solid preparation for cleaning - Google Patents

Abstract

To provide a solid preparation for cleaning.SOLUTION: A solid preparation for cleaning is prepared, intended for cleaning oral appliances such as dentures or dental orthodontic retainers, wherein the solid preparation contains (A) at least one selected from the group consisting of dichloroisocyanuric acid salt, quaternary ammonium salt, isopropylmethylphenol, fluoride, thymol, hinokitiol, cetylpyridinium chloride, benzethonium chloride, chlorhexidine acetate, chlorhexidine gluconate, sodium monofluorophosphate, triclosan, lysozyme chloride, and chlorhexidine hydrochloride, (B) oxygen-based bleaching agent, and (C) foamer.SELECTED DRAWING: None

Description

The present invention relates to a solid preparation for cleaning. More specifically, the present invention relates to a solid preparation for cleaning oral cavity-wearable related instruments including dentures, orthodontic retainers, sports mouthpieces, and containers for these items.

Oral care is important for improving quality of life and is also useful for preventing systemic diseases such as cardiovascular disease and diabetes, which are believed to be related to periodontal disease.

For people who wear dentures or removable retainers after orthodontic treatment, keeping the dentures and appliances clean leads to maintaining a clean mouth and good overall health. Keeping dentures and appliances in an unclean state can have a negative effect on the remaining teeth and periodontal tissues that come into contact with the appliances, and can cause dental caries and periodontal disease.

Stains on dentures and retainers include food residue, denture pellicle (derived from saliva), denture plaque, tartar deposits, and discoloration. In response to this, for example, denture care compositions that include agents to prevent adhesion of food residue (Patent Document 1) and cleansers that act on biofilms have been proposed (Patent Document 2).

JP 2018-104345 A JP 2021-104937 A

Although there are cleaning agents that remove or prevent stains from adhering to dentures and retainers, it cannot be said that there have been sufficient proposals for cleaning agents that act effectively on bacterial flora.

The present invention aims to provide a solid preparation for cleaning that has excellent bactericidal properties for intraoral instruments.

As a result of extensive research to solve this problem, the inventors discovered that by incorporating a specific concentration of a bactericidal component and making it into a foamable solid preparation, it is possible to prepare a cleanser that exhibits excellent bactericidal effect while also being safe enough for cleaning instruments worn in the oral cavity, and thus completed the present invention.

That is, the present invention provides the following solid preparations for cleaning.
Item 1.
A solid preparation for cleaning oral cavity-worn appliances, comprising (A) at least one selected from the group consisting of dichloroisocyanurate, a quaternary ammonium salt, isopropylmethylphenol, fluoride, thymol, hinokitiol, chlorhexidine acetate, chlorhexidine gluconate, sodium monofluorophosphate, triclosan, lysozyme chloride, and chlorhexidine hydrochloride, (B) an oxygen-based bleaching agent, and (C) a foaming agent.
Item 2.
Item 2. The solid preparation for cleaning according to Item 1, which is a tablet.
Item 3.
Item 3. The solid preparation for cleaning according to Item 1 or 2, wherein the component (A) is a dichloroisocyanurate or a quaternary ammonium salt.
Item 4.
Item 4. The solid preparation for cleaning according to any one of Items 1 to 3, wherein the component (B) is at least one selected from the group consisting of hydrogen persulfates, persulfates, percarbonates, and perborates.
Item 5.
Item 5. The solid preparation for cleaning according to any one of Items 1 to 4, wherein the component (C) is a combination of a carbonate or a bicarbonate and succinic acid, sulfamic acid, or citric acid.

The present invention provides a solid preparation for cleaning intraoral instruments that has both bactericidal effect and safety.

In this specification, the term "salt" refers to alkali metal salts such as lithium salts, sodium salts, and potassium salts; alkaline earth metal salts such as barium salts; ammonium salts; and hydrates thereof.

In this specification, examples of control bacteria for sterilization, disinfection, and eradication include, but are not limited to, Candida albicans (a fungus normally present in the oral cavity), Streptococcus mutans (a gram-positive cocci that are one of the bacteria that cause dental caries), and Porphyromonas gingivalis (a gram-negative rod-shaped bacillus that is involved in periodontal disease).

[Solid preparation for cleaning]
The solid preparation for cleaning of the present invention contains (A) at least one selected from the group consisting of dichloroisocyanurate, quaternary ammonium salt, isopropylmethylphenol, fluoride, thymol, hinokitiol, and chlorhexidine hydrochloride, (B) an oxygen-based bleaching agent, and (C) a foaming agent, and is intended for cleaning intraoral appliances such as dentures or orthodontic retainers.

(Component (A))
The solid preparation for cleaning of the present invention contains (A) at least one selected from the group consisting of dichloroisocyanurate, quaternary ammonium salt, isopropylmethylphenol, fluoride, thymol, hinokitiol, chlorhexidine acetate, chlorhexidine gluconate, sodium monofluorophosphate, triclosan, lysozyme chloride, and chlorhexidine hydrochloride. Examples of the quaternary ammonium salt include cetylpyridinium chloride, benzalkonium chloride, and benzethonium chloride.
As the component (A), two or more of these may be used in combination. Although not limited thereto, among these, dichloroisocyanurate or quaternary ammonium salt is preferred, and dichloroisocyanurate, cetylpyridinium chloride, benzethonium chloride or benzalkonium chloride is more preferred.

The content of component (A) relative to the total amount of the solid preparation for cleaning of the present invention may vary depending on the mass per unit of the solid preparation for cleaning, but from the viewpoint of exerting the effects of the present invention, it is preferably 0.1% by mass or more and 20% by mass or less, more preferably 0.2% by mass or more and 10% by mass or less, and even more preferably 0.3% by mass or more and 8% by mass or less.

The solid preparation for cleaning of the present invention is preferably used by dissolving it in water, and the content of component (A) during use is preferably 0.001 w/v% or more and 1 w/v% or less, more preferably 0.01 w/v% or more and 0.5 w/v% or less, and even more preferably 0.1 w/v% or more and 0.2 w/v% or less, from the viewpoint of exerting the effects of the present invention.

(B) Oxygen bleach
The solid preparation for cleaning of the present invention contains an oxygen bleaching agent, such as hydrogen persulfate, persulfate, percarbonate, or perborate.

Examples of hydrogen persulfates include sodium hydrogen persulfate, potassium hydrogen persulfate, lithium hydrogen persulfate, barium hydrogen persulfate, potassium monohydrogen persulfate double salt, and ammonium hydrogen persulfate.

Examples of persulfates include sodium persulfate, potassium persulfate, and ammonium persulfate.

Examples of perborates include sodium perborate, potassium perborate, ammonium perborate, and sodium perborate monohydrate.

Examples of percarbonates include sodium percarbonate, potassium percarbonate, and ammonium percarbonate.

As the oxygen bleaching agent, at least one of these may be used, or two or more of them may be used in combination.
As the oxygen bleaching agent, an alkali metal salt of hydrogen persulfate or a double salt of potassium hydrogen persulfate, potassium hydrogen sulfate, and potassium sulfate is preferred.

The content of component (B) relative to the total amount of the solid cleaning preparation of the present invention may vary depending on the mass per unit of the solid cleaning preparation, but from the viewpoint of exerting the effects of the present invention, it is preferably from 2% by mass to 50% by mass, more preferably from 3% by mass to 45% by mass, and even more preferably from 4% by mass to 40% by mass.

The solid preparation for cleaning of the present invention is preferably used by dissolving it in water, and the content of component (A) during use is preferably 0.006 w/v% or more and 7 w/v% or less, more preferably 0.02 w/v% or more and 3 w/v% or less, and even more preferably 0.025 w/v% or more and 1.3 w/v% or less, from the viewpoint of exerting the effects of the present invention.

In the solid preparation for cleaning of the present invention, the ratio of component (B) to component (A) is preferably 0.1 parts by mass or more and 500 parts by mass or less, more preferably 0.3 parts by mass or more and 225 parts by mass or less, and even more preferably 0.5 parts by mass or more and 133 parts by mass or less, of component (B) per 1 part by mass of component (A).

((C) Foaming Agent)
The solid preparation for cleaning of the present invention contains a foaming agent. Examples of the foaming agent include a combination of a carbonate and/or a bicarbonate with an acid.

Examples of carbonates and/or hydrogen carbonates include sodium carbonate, potassium carbonate, sodium hydrogen carbonate, potassium hydrogen carbonate, and sodium sesquicarbonate.
At least one of these may be used, or two or more of them may be used in combination.
As the carbonate and/or hydrogen carbonate, sodium carbonate or sodium hydrogen carbonate is preferred.

Examples of the acid include organic acids and phosphoric acids, and more specifically, examples of the acid include citric acid, succinic acid, sulfamic acid, malic acid, gluconic acid, tartaric acid, maleic acid, sorbic acid, phytic acid, and phosphoric acid.
At least one of these may be used, or two or more of them may be used in combination.
The acid is preferably, but not limited to, for example, citric acid, succinic acid, or sulfamic acid.

The ratio of carbonate and/or bicarbonate to acid is not particularly limited, but is preferably 0.3 parts by mass to 4 parts by mass of acid per 1 part by mass of carbonate and/or bicarbonate, more preferably 0.4 parts by mass to 3.5 parts by mass, and even more preferably 0.5 parts by mass to 3 parts by mass.

From the viewpoint of exerting the effects of the present invention, the content of the foaming agent relative to the total amount of the solid preparation for cleaning of the present invention is preferably 30% by mass or more and 95% by mass or less, more preferably 40% by mass or more and 94% by mass or less, and even more preferably 50% by mass or more and 92% by mass or less.

(Other ingredients)
In addition to the above-mentioned components (A), (B), and (C), the solid preparation for cleaning of the present invention may contain optional components as appropriate, so long as the optional components do not impair the effects of the present invention. The optional components may be surfactants, binders, enzymes, flow improvers, stabilizers, deodorants, rust inhibitors, fragrances, and/or colorants.

As the surfactant, any of anionic surfactants, nonionic surfactants, and amphoteric surfactants can be used, but anionic surfactants are particularly preferred.

Examples of such anionic surfactants include alkylbenzenesulfonates, olefinsulfonates, alkylsulfoacetates, alkyl sulfates, and alkanesulfonates, etc. Among these, alkyl sulfates or olefinsulfonates having an alkyl group with 8 to 16 carbon atoms are particularly preferred, sulfates or olefinsulfonates having a lauryl group or a myristyl group are more preferred, and sodium lauryl sulfate or sodium olefinsulfonate is even more preferred.
At least one of these may be used, or two or more of them may be used in combination.

Examples of nonionic surfactants include sorbitan fatty acid esters, propylene glycol fatty acid esters, hydrogenated castor oil derivatives, polyoxyethylene sorbitan fatty acid esters, glycerin derivatives, polyoxyalkylene alkyl ethers, etc.

Examples of amphoteric surfactants include alkyl betaines, fatty acid amidopropyl betaines, alkyl imidazoles, lauroyl glutamate salts, and amine oxides.

Examples of the binder include polyvinylpyrrolidone, polyoxyethylene, polyethylene glycol, carbowax, sodium carboxymethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, cellulose, etc. These binders may be used alone or in combination of two or more.
At least one of these may be used, or two or more of them may be used in combination.
The binder is not limited, but for example, polyethylene glycol or a cellulose derivative having a molecular weight of about 1000 to 10,000 is preferable.

Examples of enzymes include protease, alcalase, amylase, lipase, dextranase, mutanase, glucanase, etc. These enzymes may be used alone or in combination of two or more. Among these, proteases such as papain are preferred.

Examples of flow improvers (lubricants) include talc powder, magnesium stearate, magnesium oxide, talc, finely powdered anhydrous silicic acid, etc.

Preferred rust inhibitors include sodium salts of aromatic carboxylates, chromates, molybdates, tungstates, nitrites, polymeric phosphates, zinc salts, mercaptone benzothiazoles, benzotriazoles, alkanolamines, fatty acid salts, alkylamine ethylene oxide adducts, alkyl phosphate ester salts, petroleum sulfonates, diisopropylamine nitrite, and dicyclohexylammonium nitrite, with nitrites and sodium salts of aromatic carboxylates being particularly preferred.

(pH)
From the viewpoint of the stability or safety of the components, the solid preparation for cleaning of the present invention preferably gives a solution with a pH of 1 to 9, and more preferably a solution with a pH of 1.5 to 8.5, when, for example, 3 g of the preparation is dissolved in 150 ml of water and measured at 20° C. The pH can be measured at 20° C. using a commercially available pH meter (e.g., F-52 (registered trademark) model, manufactured by Horiba, Ltd.).

(Use, etc.)
The solid preparation for cleaning of the present invention is a solid preparation for cleaning related instruments worn in the oral cavity. Here, the related instruments worn in the oral cavity refer to dentures, orthodontic retainers, sports mouthpieces, and containers for these instruments.

The solid preparation for cleaning of the present invention is dissolved in a solvent such as water, and the resulting solution is used for immersing the intraoral appliance.

The solid preparation for cleaning of the present invention may be provided in the form of, but is not limited to, a tablet or granule. Preferably, it is a tablet. There is no particular limitation on the shape, mass, hardness, etc. of the tablet.

The solid preparation for cleaning of the present invention may preferably have a shape, but is not limited to, a sphere, a cylinder, an oval sphere, a polygonal prism, etc.

The mass of the solid preparation for cleaning of the present invention per tablet is not limited, but is preferably, for example, about 0.5 to 20 g, more preferably about 1 to 10 g, and even more preferably about 1 to 5 g.

Although not limited, the diameter of each tablet of the solid preparation for cleaning of the present invention is preferably about 100 to 400 mm, and more preferably 150 to 300 mm.

The solid preparation for cleaning of the present invention preferably has a hardness of, but is not limited to, about 45N or more, preferably about 35 to 130N, more preferably about 40 to 125N, and even more preferably about 45 to 120N.

The solid preparation for cleaning of the present invention can be used about once or twice a day, or about once every 2 to 7 days.

Specific examples of how the solid preparation for cleaning of the present invention can be used include, but are not limited to, a typical procedure in which, for example, a tablet is dissolved in about 50 to 300 mL of water, preferably about 100 to 200 mL of water, and more preferably about 150 mL of water, while a control oral cavity-wearable device is immersed in the solution, and the solution is left to stand for about 3 minutes to overnight, after which the oral cavity-wearable device is thoroughly washed with water.

Next, the present invention will be specifically described using examples, but the present invention is not limited to the following examples. Note that the unit of each component amount in the table is mass % unless otherwise specified in the table.

Tablets of the examples and comparative examples having the compositions shown in Table 1 were prepared. Specifically, each component in the table was weighed, and the weighed components were mixed by manual stirring. The resulting raw material mixture was tableted using a mold with a diameter of 250 mm to produce solid preparations for cleaning dentures weighing 2.7 g per tablet.

[1] Bactericidal Efficacy Evaluation Test The bactericidal efficacy of these tablets was evaluated.

The bactericidal efficacy was evaluated as follows:

(Target bacteria)
Candida albicans

(Culture medium used for bacterial culture)
GP agar medium (glucose peptone agar medium) supplemented with lecithin and polysorbate 80 was used.

(Method of preparing bacteria-adherent dentures)
Tablets of the Examples and Comparative Examples shown in Table 1 were dissolved in 150 mL of water. Then, a liquid of the target bacteria was added to the test specimen so that the concentration was about 10 ⁵ to 10 ⁶ cfu/mL, and the mixture was thoroughly mixed. The test specimen was then stored at 25°C, and the viable cell count in the test liquid was measured after 10 hours.

The amount of bacteria after the action was divided by the amount of bacteria before the action to calculate the reduction in bacteria.
Viable bacteria count reduced to 1/100 or less: ◎
Viable bacteria count is 1/10 or less, over 1/100: ○
The number of viable bacteria does not decrease to 1/10 or less: ×
It was rated as follows:

As a result of the evaluation test, the compositions of the examples showed a higher bactericidal effect than the compositions of the comparative examples.

Claims (5)

A solid preparation for cleaning an intraoral appliance, comprising (A) at least one selected from the group consisting of dichloroisocyanurate, quaternary ammonium salt, isopropylmethylphenol, fluoride, thymol, hinokitiol, chlorhexidine acetate, chlorhexidine gluconate, sodium monofluorophosphate, triclosan, lysozyme chloride, and chlorhexidine hydrochloride, (B) an oxygen bleaching agent, and (C) a foaming agent. The solid preparation for cleaning according to claim 1, which is a tablet. The solid preparation for cleaning according to claim 1, wherein the component (A) is a dichloroisocyanurate or a quaternary ammonium salt. The solid preparation for cleaning according to claim 1, wherein the component (B) is at least one selected from the group consisting of hydrogen persulfates, persulfates, percarbonates, and perborates. 2. The solid preparation for cleaning according to claim 1, wherein the component (C) is a combination of a carbonate or a bicarbonate and succinic acid, sulfamic acid, or citric acid.