JP2001131042A - Oral composition - Google Patents

Abstract

PROBLEM TO BE SOLVED: To obtain a composition for oral use excellent in stain removing effect. SOLUTION: This composition for oral use contains 0.1-50 mass % of at least one species selected from a group consisting of hydroxyapatite, fluoroapatite, apatite carbonate, calcium tertiary phosphate and calcium octavus phosphate, 0.1-30 mass % of at least one species of polyethylene having 200-20,000 average molecular weight and 0.01-3 mass % of at least one species of polypyrrolidone having 10,000-360,000 average molecular weight.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to an oral composition having an excellent stain removing effect.

[0002]

2. Description of the Related Art It has been conventionally known that a dentifrice composition is blended with polyethylene glycol or polyvinylpyrrolidone having a dissolving effect on stains to enhance the effect of removing stains on tooth surfaces. Here, the stain refers to pigment deposits attached to the teeth, and is generally accumulated by smoking or ingesting favorite items such as coffee, black tea, and Japanese tea. However, simply mixing the two types of polyethylene glycol and polyvinylpyrrolidone does not provide a sufficient stain removal effect. Although various oral compositions having a stain removing effect have been proposed, no oral compositions having a sufficient effect have yet been found.
Therefore, an oral composition having an excellent stain removing effect is desired.

[0003]

SUMMARY OF THE INVENTION An object of the present invention is to provide an oral composition having an excellent stain removing effect.

[0004]

Means for Solving the Problems The present inventors have conducted intensive studies to solve the above-mentioned problems, and as a result, have found that at least one selected from the group consisting of apatites and an average molecular weight of 20
It has been found that an excellent stain removal effect can be imparted by blending polyethylene glycol of 0 to 20,000 with polyvinylpyrrolidone having an average molecular weight of 10,000 to 360,000. Accordingly, the present invention provides at least one selected from the group consisting of hydroxyapatite, fluorapatite, carbonate apatite, tribasic calcium phosphate, calcium tetraphosphate and calcium octaphosphate.
0.1 to 50% by weight, at least one kind of polyethylene glycol having an average molecular weight of 200 to 20,000 is 0.1 to 30% by weight, and at least one kind of polyvinylpyrrolidone having an average molecular weight of 10,000 to 360,000 is 0.001 to 3% by mass
The present invention relates to an oral composition characterized by containing the composition.

[0005]

BEST MODE FOR CARRYING OUT THE INVENTION The oral composition referred to in the present specification includes dentifrices such as toothpaste and liquid dentifrice, troches, creams, ointments, attachments, mouthwash,
Including mouthwash, mouthwash, chewing gum or gargle. The apatite used in the present invention means hydroxyapatite, fluoroapatite, carbonate apatite, tribasic calcium phosphate, quaternary calcium phosphate and calcium octaphosphate. In the present specification, hydroxyapatite, fluoroapatite, carbonate apatite, tribasic calcium phosphate, calcium tetraphosphate and calcium octaphosphate are collectively referred to as apatites. Each is represented by the following chemical formula. Hydroxyapatite: Ca ₁₀ (PO ₄ ) ₆ (OH) ₂ Fluoroapatite: Ca ₁₀ (PO ₄ ) ₆ F ₂ Carbonate apatite: CO ₃ Ap Calcium phosphate tribasic: Ca ₃ (PO ₄ ) ₂ Quaternary calcium phosphate: Ca ₄ O (PO _{4) 2} eighth _{calcium: Ca 8 (PO 4) 6} · 5H 2 O among these, hydroxyapatite and tricalcium phosphate are preferably used.

[0006] These apatites are the main components (inorganic components) of teeth and bones, and are highly safe materials with excellent biocompatibility. For this reason, hydroxyapatite, tribasic calcium phosphate, and the like are used as biomaterials in artificial joints, artificial roots, and the like. Also, hydroxyapatite is known to replace calcium ions, phosphate ions, and hydroxide ions with various trace elements, and those in which hydroxide ions are replaced with fluorine ions become fluoroapatite, When carbonate ions are taken into the crystal, it becomes carbonate apatite. Synthetic products are generally used for apatite, and such commercially available synthetic products can also be used in the present invention. These are not particularly limited, but are supplied in the form of a white aqueous suspension or powder, and have an average particle size of 1 to 70 μm.

In the oral composition of the present invention, the content of at least one selected from the group consisting of hydroxyapatite, fluoroapatite, carbonate apatite, tricalcium phosphate, calcium quaternary phosphate and calcium octaphosphate is 0.1 to 5 based on total mass
0 mass% is appropriate, and preferably 1 to 30 mass%. If this amount is less than 0.1% by mass, the desired effect of the present invention cannot be sufficiently obtained, while if it exceeds 50% by mass, no improvement in the effect is observed.

The polyethylene glycol used in the present invention is a polymer obtained by adding ethylene oxide to water or ethylene glycol, and is represented by H (OCH ₂ CH ₂ ) nOH. Depending on the amount of ethylene oxide added, polymers of various molecular weights from liquid low molecular weight to solid high molecular weight can be formed, and the products are mixed with various degrees of polymerization. Polyethylene glycols are classified according to their average molecular weight. In the present invention, the average molecular weight is 200 to 200.0.
One or more polyethylene glycols can be used. That is, two or more compounds having different average molecular weights may be used. Those having an average molecular weight of less than 200 do not exhibit the expected effects, while those having an average molecular weight of more than 20,000 make it difficult to incorporate them in a dosage form.

Such polyethylene glycol is widely and generally used in pharmaceuticals, cosmetics, fibers, rubbers, adhesives, metals, ceramics, petroleum, printing, inks, and the like. Commercially available products used in the above can be used. The content of one or more polyethylene glycols in the oral composition of the present invention is 0.1 to 3 with respect to the total mass of the oral composition.
0% by mass, preferably 0.5 to 10% by mass. If this amount is less than 0.1% by mass, the expected effect is not exhibited. On the other hand, if it exceeds 30% by mass, an effect commensurate with the content cannot be obtained and the usability may be impaired.

[0010] Polyvinylpyrrolidone is a kind of synthetic compound obtained by a high-pressure synthesis Reppe reaction of acetylene, and is a linear polymer of vinylpyrrolidone. In addition, the molecular weight of this product is 100,000 depending on the amount of catalyst for polymerization reaction, temperature, time and the like.
It exists up to about 0-700,000. In the present invention, one or more kinds of polyvinylpyrrolidone having an average molecular weight of 10,000 to 360,000 can be used. That is, two or more compounds having different average molecular weights may be used. Those having an average molecular weight of more than 360,000 are difficult to mix in a dosage form.

[0011] Such polyvinylpyrrolidone is widely and generally used in pharmaceuticals and cosmetics, as well as in the textile, paper industry, printing, ink industry, protective coatings, beverage fining agents, adhesives, agricultural chemistry, plastic industry, and the like. In the present invention, commercially available products used for these can be used. The content of one or more polyvinylpyrrolidone in the oral composition of the present invention is 0.01 to 3% by mass, preferably 0.03% by mass, based on the total mass of the oral composition.
0.05 to 1% by mass. If the amount is less than 0.01% by mass, the expected effect is not exhibited, while if it exceeds 3% by mass, the effect corresponding to the content cannot be obtained and the usability may be impaired.

In the oral composition of the present invention, the ratio of the total mass of polyethylene glycol to the total mass of polyvinyl pyrrolidone to be blended can be used in a wide range of from 1:30 to 3,000: 1, and more preferably from 1:30 to 3,000: 1. 30-1,000: 1,
Preferably 1: 30-300: 1, more preferably 1: 1.
The range is 30 to 200: 1.

The oral composition of the present invention may contain, in addition to the above components, the following components, if necessary, within the usual range of use, depending on the type of the composition. <Abrasives> Silica gel, precipitated silica, igneous silica,
Silica-based abrasives such as hydrous silicic acid, silicic anhydride, zeolite, aluminosilicate, zirconosilicate, dibasic calcium phosphate dihydrate, dibasic calcium phosphate anhydrate, calcium pyrophosphate, tertiary magnesium phosphate,
Aluminum hydroxide, alumina, light calcium carbonate,
Examples thereof include heavy calcium carbonate, magnesium carbonate, zirconium silicate, and a synthetic resin-based abrasive, and one or more of these can be used in combination.
The compounding amount of the above-mentioned abrasive is preferably 3 to 60% by mass, more preferably 10 to 45% by mass, based on the whole composition.

<Wetting agent> One or more kinds of polyhydric alcohols such as glycerin, concentrated glycerin, diglycerin, sorbitol, maltitol, dipropylene glycol, propylene glycol, 1,3-butylene glycol and xylitol are used. can do. <Binder> carrageenan (ι, λ, κ), alginic acid,
Alginate such as sodium alginate, propylene glycol alginate, sodium alginate containing calcium, potassium alginate, calcium alginate, ammonium alginate and derivatives thereof, xanthan gum, guar gum, gelatin, agar, sodium carboxymethyl cellulose, hydroxyethyl cellulose, sodium polyacrylate, etc. These may be used alone or in combination of two or more.

<Effervescent agent> N-acyl amino acid salts such as sodium lauryl sulfate, sodium lauroyl sarcosine, sodium alkyl sulfosuccinate, sodium coconut fatty acid monoglycerin sulfonate, sodium α-olefin sulfonate, N-acyl glutamate, Alkyl
-N-carboxymethyl-N-hydroxyethylimidazolinium betaine, maltitol fatty acid ester, sucrose fatty acid ester, polyglycerin fatty acid ester, fatty acid diethanolamide, polyoxyethylene sorbitan monostearate, polyoxyethylene hydrogenated castor oil, poly Oxyethylene fatty acid esters and the like can be mentioned, and one or more of these can be used in combination.

<Sweetening agents> Saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde, neohesperidyl dihydrochalcone, perillartin and the like. <Preservatives> Parabens such as methylparaben, ethylparaben, propylparaben, and butylparaben, sodium benzoate, phenoxyethanol, and alkyldiaminoethylglycine hydrochloride.

<Fragrance ingredients> l-menthol, anethole,
One or more of menthone, cineole, limonene, carvone, methyl salicylate, ethyl butyrate, eugenol, thymol, cinamic aldehyde, trans-2-hexenal and the like can be used in combination. These components may be compounded individually,
Essential oils containing these may be blended. Further, in addition to the above flavor components, aliphatic alcohols and esters thereof, terpene hydrocarbons, phenol ethers, aldehydes,
Perfume components such as ketones and lactones, and essential oils may be blended as long as the effects of the present invention are not impaired. The amount of the above fragrance is
The content is preferably set to 0.02 to 2% by mass based on the whole composition.

<Active ingredient> Lysozyme chloride, monofluorophosphate, sodium fluoride, potassium fluoride,
Sodium monofluorophosphate, hinokitiol, ascorbic acid, chlorhexidine salts, triclosan, isopropylmethylphenol, cetylpyridinium chloride, benzalkonium chloride, benzethonium chloride, bisabolol, tocopherol acetate, ε-aminocaproic acid, tranexamic acid, aluminum hydroxyl allantoin, lactic acid Aluminum, dihydrocholesterol,
One or more of glycyrrhetinic acid, glycyrrhizinates, copper chlorophyllin salts, sodium chloride, guaiazulene sulfonate, dextranase, zeolite, pyridoxine hydrochloride and the like can be blended.

<Others> Pigments such as Blue No. 1, pigments such as titanium oxide, antioxidants such as dibutylhydroxytoluene, chelating agents such as edetate, tea extract, tea distillation, propolis extract, sodium glutamate, etc. Agents and the like. The oral composition of the present invention can be produced according to a conventional method, and the production method is not particularly limited. The obtained oral composition such as toothpaste can be used after being filled in an aluminum tube, a laminate tube, a glass deposition tube, a plastic tube, a plastic bottle, an aerosol container, or the like.

[0020]

The oral composition of the present invention has an excellent stain removing effect.

[0021]

EXAMPLES The present invention will be described in detail below with reference to experimental examples and examples, but the present invention is not limited to the following examples. Various toothpastes were prepared by the usual method using the compositions (unit: mass%) shown in Tables 1 to 3, and subjected to the following tests. In the composition, polyvinylpyrrolidone K30 has a degree of polymerization of about 40,000, and polyvinylpyrrolidone K90 has a degree of polymerization of about 360,000. <Stain removal test 1> A dentifrice dispersion obtained by adding 25 g of ion-exchanged water to 10 g of the above-mentioned various toothpastes and uniformly dispersing the same was used for the test. In the center of an acrylic case with an inner diameter of 15 x 7 x 7 cm, a human extracted tooth (maxillary anterior tooth) with tar extracted from tobacco applied on the entire front surface is fixed with the tar applied surface facing up, and the dentifrice is dispersed there. 30 g of the liquid was poured. Normally, the above-mentioned acrylic case was fixed to an abrasive tester for dentifrice equipped with a commercially available toothbrush, and the weight of brushing was 200 g and the number of times of brushing was 10
Artificial brushing was performed with 0 stroke and a stroke width of 10 cm. After the brushing was completed, a human extracted tooth from which the dentifrice dispersion was washed away with running water was used as a test sample. The test samples were subjected to visual sensory evaluation of stain removal based on the following evaluation criteria.

"Evaluation Criteria" Stain removal degree ◎: Stain is completely removed.・: Most stains are removed. △ ・ ・ ・ ・ ・ Stain was slightly removed. ×: No stain was removed at all. The results of the stain removal test 1 are also shown in Tables 1 to 3.

[0023]

[Table 1]

[0024]

[Table 2]

[0025]

[Table 3]

<Stain Removal Test 2> (1) Ten male subjects habitually smoke 20 or more cigarettes a day with a tar content of 10 mg or more. Five of the ten subjects used the dentifrice of Example 1 and the remaining five used the dentifrice of Comparative Example 1 for two days a week for one week.
Normal brushing was performed for about 3 minutes. After the use test for one week, a questionnaire describing the following evaluation criteria was given to each subject. After a one-month blank, the same use test was performed again, and the same questionnaire was performed. 1
The group using the dentifrice of Example 1 in the second use test uses the dentifrice of Comparative Example 1, and the group using the dentifrice of Comparative Example 1 in the first use test uses the dentifrice of Example 1. It was decided to. (2) The dentifrice of Example 3 and the dentifrice of Comparative Example 3 were tested in the same procedure as in the above test (1).

The evaluation of each dentifrice was based on the results of a questionnaire, the average value of 10 persons was determined, and the evaluation was performed in the following four stages. 4 <◎ ≦ 3 3 <○ ≦ 2 2 <△ ≦ 1 1 <× ≦ 0 “Evaluation criteria” Stain removal degree 4... Stain is completely removed. 3. Stain is almost completely removed. 2. Slight stain has been removed. 1... No stain is removed at all. The results were ○ for the toothpaste of Example 1, Δ for the toothpaste of Comparative Example 1, ◎ for the dentifrice of Example 3, and X for the dentifrice of Comparative Example 3.

From the above experimental results, it was found that the toothpaste according to the present invention was excellent in the stain removing effect. In addition, when the above-described experiments were performed on Examples 9 to 24 described below, all the same results were obtained. Less than,
The composition of the toothpastes of Examples 9 to 24 is shown. The unit of the compounding amount is mass%.

[0029]

Embodiment 9

[0030]

Embodiment 10

[0031]

Embodiment 11

[0032]

Embodiment 12

[0033]

Embodiment 13

[0034]

Embodiment 14

[0035]

Embodiment 15

[0036]

Embodiment 16

[0037]

Embodiment 17

[0038]

Embodiment 18

[0039]

Embodiment 19

[0040]

Embodiment 20

[0041]

Embodiment 21

[0042]

Embodiment 22

[0043]

Embodiment 23

[0044]

Embodiment 24

──────────────────────────────────────────────────の Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 7/28 A61K 7/28 (72) Inventor Yoshikazu Ishii 2-216-3 Minami-Osawa, Hachioji-shi, Tokyo Mitsuwa Crest 206 F-term (reference) 4C083 AA112 AB222 AB291 AB292 AB321 AB322 AB372 AB472 AC122 AC132 AC312 AC432 AC472 AC482 AC582 AC622 AC662 AC692 AC712 AC742 AC782 AC792 AC842 AC862 AD041 AD042 AD071 AD072 AD212 AD272 AD352 AD472 AD532 AD662 CC41 DD22 EE

Claims (1)

[Claims] 1. At least one member selected from the group consisting of hydroxyapatite, fluoroapatite, carbonate apatite, tribasic calcium phosphate, quaternary calcium phosphate and calcium octaphosphate, in an amount of 0.1 to 50% by mass and an average molecular weight of 200 to 20,000. 0.1 to 30% by mass of polyethylene glycol having an average molecular weight of 10,
An oral composition comprising 0.01 to 3% by mass of at least one kind of polyvinylpyrrolidone of 000 to 360,000.