WO2018105256A1

WO2018105256A1 - Gel-like oral composition

Info

Publication number: WO2018105256A1
Application number: PCT/JP2017/038277
Authority: WO
Inventors: 慧理橋口; 祐輔吉田
Original assignee: ライオン株式会社
Priority date: 2016-12-09
Filing date: 2017-10-24
Publication date: 2018-06-14

Abstract

A gel-like oral composition containing no polishing agent, said composition being characterized by comprising 0.1 to 3% by mass of (A) an ascorbic acid ester or a salt thereof, 0.1 to 3% by mass of (B) ortho-phosphoric acid or a salt thereof, 0.7 to 2% by mass of (C) xanthane gum, 0.1 to 1% by mass of (D) polyacrylic acid or a salt thereof and 0.1 to 10% by mass of (E) thickening silica, wherein the (C)/(D) ratio is 1.0 to 10 by mass. According to the present invention, a gel-like oral composition containing no polishing agent can be provided, which does not undergo preparation discoloration caused by the ascorbic acid ester or the salt thereof over time, and which has good preparation properties.

Description

Gel oral composition

The present invention relates to a gel-free composition for oral cavity containing no abrasives, in which discoloration of a preparation due to ascorbic acid ester or a salt thereof is suppressed even over time and the preparation characteristics are good.

Ascorbic acid plays an important role in the expression of enzyme activity in the living body and is known to have various physiological activities. In particular, ascorbic acid acts as a coenzyme for prolyl and dil hydroxylase and is essential for collagen synthesis. Has been. For this reason, ascorbic acid is useful for the prevention or treatment of periodontal diseases such as gingivitis and periodontitis associated with collagen destruction. Conventionally, various ascorbic acid derivatives have been developed and used in oral compositions. In particular, ascorbic acid esters such as ascorbic acid phosphates or salts thereof have attracted attention.

However, oral preparations containing ascorbic acid esters or salts thereof have a problem of causing discoloration over time. The degree of the preparation discoloration varies depending on the preparation form, dosage form, and compounding components, and does not necessarily match the degree of decrease in the residual rate of ascorbic acid esters.

On the other hand, an oral composition such as a toothpaste generally contains an abrasive to remove dirt such as plaque, and the use of this abrasive may invade a weak gum surface. In particular, there is a concern about its use in high-risk individuals who have developed gingivitis and periodontitis. For this reason, a gel-like composition for oral cavity containing an ascorbic acid ester or a salt thereof and not containing an abrasive is desirable for safe use even for persons with high risk of periodontal disease.

Patent Documents 1 to 4 propose techniques for stabilizing ascorbic acid esters or salts thereof using orthophosphoric acid or salts thereof. Patent Document 1 discloses that coloring immediately after preparation of a liquid oral composition containing an ascorbic acid ester or a salt thereof and a cationic bactericide is suppressed by orthophosphoric acid or a salt thereof. Is described as containing no abrasive. In Patent Literature 2, ascorbic acid phosphate or a salt thereof is stabilized in a liquid oral composition not containing an abrasive by a combined system of an orthophosphate and an organic acid or a salt thereof. It is a suppression of the decrease, and it is described that the degree of decrease in the residual rate does not necessarily coincide with the intensity of coloring of the preparation.

JP 2013-256466 A JP 2012-131755 A JP 2004-26658 A International Publication No. 2013/094312

However, according to the conventional technology, in a gel-like oral composition that does not contain an abrasive, it is possible to suppress formulation discoloration due to ascorbic acid esters or salts thereof over time while maintaining good gel properties and maintaining formulation characteristics. was difficult.

The present invention has been made in view of the above circumstances, and provides a gel-like composition for an oral cavity that does not contain an abrasive and can be prevented from being discolored by ascorbic acid ester or a salt thereof over time and has good formulation characteristics. Objective.

As a result of intensive studies to achieve the above-mentioned object, the present inventors have obtained a gel-like composition for oral cavity containing no abrasive, ascorbic acid ester or a salt thereof, orthophosphoric acid or a salt thereof, xanthan gum and a polyacrylic acid. Or by combining the salt and thickening silica in combination, the discoloration of the preparation due to ascorbic acid ester or its salt can be suppressed over time, and the gel properties can be kept good and the preparation characteristics can be maintained. I found out. That is, according to the present invention, (A) ascorbic acid ester or a salt thereof, (B) orthophosphoric acid or a salt thereof, (C) xanthan gum, (D) polyacrylic acid Alternatively, the salt thereof and (E) thickening silica are respectively blended in specific amounts, and (C) / (D) is 1.0 to 10 as a mass ratio, so that the discoloration of the preparation due to the component (A) It was found that a gel-like composition for oral cavity was obtained, and the formulation characteristics were good in retention with time, liquid separation stability and spinnability.

More specifically, when an ascorbic acid ester or a salt thereof is added to a gel-like composition for oral cavity which does not contain an abrasive, and orthophosphoric acid salt or hydrogen salt is added as a discoloration inhibitor of the preparation, the gel properties are improved. There arises a problem that it becomes worse and it becomes impossible to maintain the shape retention property well. On the other hand, in the present invention, (C), (D), and (E) components are used in combination with (B) component, and the above four components are combined and blended, so that the mass of (C) / (D) The ratio is within a specific range, and as described above, without causing deterioration of gel properties, the (B) component suppresses the discoloration of the preparation due to the (A) component even over time, gives an excellent discoloration inhibiting effect, and at the same time is good Special formulation characteristics, specifically shape retention that keeps the shape of the toothbrush without changing or dripping when it is pushed out of the container even after storage, liquid separation that suppresses the occurrence of liquid separation after storage Provides stability and low stringing when discharged from the container, and provides excellent properties for use.

In the gel oral composition that does not contain an abrasive, the concealing effect of a white powder that is common as an abrasive cannot be expected, and the problem of the discoloration of the preparation due to ascorbic acid ester or its salt is solved compared to the abrasive-containing preparation. Not only will it be a strict level, but there will also be a problem with gel properties, for example, a problem with the formulation characteristics as compared to a toothpaste containing an abrasive. However, according to the present invention, in the gel-like composition for oral cavity that does not contain an abrasive, the components (A), (B), (C), (D), (E) are contained in a specific amount and (C) / ( The combination of the mass ratios of D) within a specific range gives an excellent discoloration suppressing effect and formulation characteristics, so that a simple addition of orthophosphoric acid salt or hydrogen salt, or the addition of an inappropriate binder is added. In this case, there is a remarkable effect that cannot be achieved.

Accordingly, the present invention provides the following gel oral composition.
[I]
A gel-like composition for oral cavity containing no abrasive,
(A) Ascorbic acid ester or salt thereof 0.1 to 3% by mass,
(B) orthophosphoric acid or a salt thereof 0.1 to 3% by mass,
(C) xanthan gum 0.7-2% by mass,
(D) Polyacrylic acid or a salt thereof 0.1 to 1% by mass
And (E) thickening silica 0.1 to 10% by mass
A gel-like composition for oral cavity, wherein (C) / (D) is 1.0 to 10 in terms of mass ratio.
[II]
(B) The gel-like composition for oral cavity of [I] whose orthophosphoric acid or its salt is 1 type (s) or 2 or more types chosen from orthophosphoric acid, its normal salt, and a hydrogen salt.
[III]
(B) The gel oral composition according to [II], wherein the orthophosphoric acid or a salt thereof is hydrogen phosphate.
[IV]
Further, (F) polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 10 to 60 moles and an alkyl group having 14 to 18 carbon atoms and an average addition mole number of ethylene oxide of 5 to 10 moles The gel oral composition according to any one of [I] to [III], containing 0.1 to 4% by mass of one or more nonionic surfactants selected from polyoxyethylene alkyl ethers.
[V]
(G) The gel oral composition according to any one of [I] to [IV], further containing 0.1 to 2% by mass of alginic acid or a salt thereof.
[VI]
The gel oral composition according to any one of [I] to [V], which is a gel dentifrice.

According to the present invention, discoloration of the preparation due to ascorbic acid ester or a salt thereof is suppressed even with time, excellent appearance stability, and preparation characteristics (time retention, liquid separation stability, spinnability) are also good. In addition, a gel-like composition for oral cavity containing no abrasive containing ascorbic acid ester or a salt thereof can be provided. The gel composition for oral cavity of the present invention is also suitable for use by persons with high risk of periodontal disease, and can be effectively used widely for the prevention or suppression of periodontal disease.

The present invention will be described in further detail below. The gel composition for oral cavity of the present invention does not contain an abrasive, (A) ascorbic acid ester or salt thereof, (B) orthophosphoric acid or salt thereof, (C) xanthan gum, (D) polyacrylic acid or salt thereof. And (E) thickening silica.
Here, the gel-like composition for oral cavity according to the present invention is an composition for oral cavity having a time-retaining property that does not sag from the toothbrush when placed on a toothbrush, although it contains no abrasive.

(A) Ascorbic acid ester or a salt thereof can be used ascorbic acid phosphoric acid ester or a salt thereof having an effect of preventing or ameliorating periodontal disease and suitable for oral use. Ascorbic acid phosphoric acid ester and its salt Salts may be used. As said salt, ascorbic acid phosphate magnesium and ascorbic acid sodium phosphate are preferable, and ascorbic acid phosphate magnesium is especially preferable.
Examples of ascorbic acid phosphate esters include those in which one or more of the hydroxyl groups at positions 2, 3, 5, and 6 of ascorbic acid are esters of compounds such as phosphoric acid and polyphosphoric acid. Acid-2-phosphate ester, ascorbic acid-3-phosphate ester, ascorbic acid-6-phosphate ester, ascorbic acid-2-polyphosphate ester, and the like. These salts include sodium salt and potassium salt. , Alkali metal salts such as calcium salts and magnesium salts, and alkaline earth metal salts. 1 type (s) or 2 or more types chosen from these can be used as (A) ascorbic acid ester or its salt. In particular, from the viewpoint of the stability of the composition, a derivative in which the hydroxyl group at the 2-position or 3-position of ascorbic acid is converted to a phosphate ester is preferable, and a magnesium salt or sodium salt of ascorbyl 2-phosphate ester is more preferable. Particularly preferred is a magnesium salt.

(A) The blending amount of ascorbic acid ester or a salt thereof is 0.1 to 3% (mass%, hereinafter the same) of the whole composition, preferably 0.2 to 2%. As the amount is increased, the effect of preventing or ameliorating periodontal disease is sufficiently exhibited, but when it is 3% or less, the shape retention property with time is excellent.

(B) Orthophosphoric acid or a salt thereof is a discoloration inhibitor, and one or more selected from orthophosphoric acid, orthophosphoric orthophosphate and orthophosphoric hydrogen salt can be used.
Specific examples of orthophosphates include orthophosphates such as sodium phosphate, potassium phosphate, and ammonium phosphate, disodium monohydrogen phosphate, monosodium dihydrogen phosphate, monopotassium dihydrogen phosphate, monohydrogen phosphate Examples thereof include hydrogen salts such as dipotassium, and these may be hydrates. These can be used individually by 1 type or in mixture of 2 or more types from the point of effect expression.
(B) As orthophosphoric acid or a salt thereof, a hydrogen salt of orthophosphoric acid, particularly sodium dihydrogen phosphate is particularly preferred from the viewpoint of the effect of suppressing discoloration of the preparation.

(B) The blending amount of orthophosphoric acid or a salt thereof is 0.1 to 3%, preferably 0.2 to 2% of the entire composition. If the blending amount is less than 0.1%, the discoloration suppressing effect of the preparation is inferior, and if it exceeds 3%, the shape retention property of the preparation is inferior.

In the present invention, (B) orthophosphoric acid or a salt thereof, (C) xanthan gum, (D) polyacrylic acid or a salt thereof, and (E) a thickening silica are used in combination, and (A) component-containing preparation In addition to being excellent in discoloration-inhibiting effect, the formulation properties are all excellent in temporal retention, liquid separation stability, and stringiness. If any of the components (C), (D), and (E) is lacked, the gel physical properties are deteriorated. If the component (C) is absent, the liquid separation stability is inferior. If the component (D) is absent, the spinnability is inferior. If the component (E) is absent, the shape retention with time is inferior.

(C) The xanthan gum may be any as long as it is usually used in oral compositions, but the viscosity at 25 ° C. of a 1% xanthan gum 1% aqueous solution containing 1% potassium chloride is 600 to 2,000 mPa · s. Those of 1,000 to 2,000 mPa · s are preferred. The thixotropic index (apparent viscosity at 5 rpm (η1) / apparent viscosity at 50 rpm (η2)) is preferably 4 to 6.
The above viscosity is a value measured by a Brookfield type rotational viscometer (rotor No. 3, rotation speed 60 rpm, measurement time 30 seconds), and thixotropic index is a B type viscometer (Toki Sangyo ( This is a value measured by VISCOMETER TVB-10, H2 rotor, measurement time 3 minutes) (manufactured by Co., Ltd.) (the same applies hereinafter).
As such xanthan gum, commercially available products such as Monato Gum DA and GS manufactured by DSP Gokyo Food & Chemicals Co., Ltd. can be used.

(C) The amount of xanthan gum blended is 0.7 to 2%, preferably 0.8 to 1.5% of the entire composition. If the blending amount is less than 0.7%, the liquid separation stability is inferior, and if it exceeds 2%, the discoloration suppressing effect of the preparation is lowered.

(D) As polyacrylic acid or a salt thereof, sodium polyacrylate can be used.
Any sodium polyacrylate may be used as long as it is usually used in oral compositions, but the viscosity of a 0.5% aqueous solution at 25 ° C. is 5,000 to 15,000 mPa · s, particularly 7,000 to The thing of 10,000 mPa * s is preferable. The thixotropic index (apparent viscosity at 5 rpm (η1) / apparent viscosity at 50 rpm (η2)) is preferably 4 to 6.
In addition, the said viscosity is the value measured with the Brookfield type rotational viscometer (rotor No. 5, rotation speed 20rpm, measurement time 2 minutes), and a thixotropic index is the same method as (C) xanthan gum. It is a measured value (the same applies hereinafter).
As such sodium polyacrylate, commercially available products such as Rheojic 260H manufactured by Toagosei Co., Ltd. can be used.

(D) The blending amount of polyacrylic acid or a salt thereof is 0.1 to 1%, preferably 0.2 to 0.8% of the whole composition. When the blending amount is less than 0.1%, the spinnability is inferior, and when it exceeds 1%, the discoloration suppressing effect of the preparation is lowered.

In the present invention, (C) / (D) indicating the blending ratio of the component (C) and the component (D) is 1.0 to 10, preferably 1.5 to 8, as a mass ratio. If it is less than 1.0 or exceeds 10, shape retention properties with time are inferior.

(E) Although the thickening silica is not particularly limited, precipitated silica having a BET specific surface area of 300 to 450 m ² / g, particularly 350 to 450 m ² / g is preferable. When the BET specific surface area is within the above range, the retention with time is particularly excellent after low-temperature storage, and when it is less than 300 m ² / g, sufficient retention with time may not be obtained. Those exceeding 450 m ² / g are difficult to obtain as commercial products.
The BET specific surface area is a value measured at 25 ° C. using a specific surface area measuring device (manufactured by Nikkiso Co., Ltd., automatic specific surface area meter, BET multipoint method, measurement gas; nitrogen).
Examples of such thickening silica include DSL. Commercial products such as CARPLEX # 67 manufactured by Japan Corporation may be used.

(E) The blending amount of the thickening silica is 0.1 to 10%, preferably 0.5 to 7% of the whole composition. When the blending amount is less than 0.1%, the shape retention property with time is inferior, and when it exceeds 10%, the discoloration suppressing effect of the preparation is lowered.

The composition of the present invention further comprises, as a surfactant, (F) polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 10 to 60 moles, an alkyl group having 14 to 18 carbon atoms and an average of ethylene oxide It is preferable to add one or more nonionic surfactants selected from polyoxyethylene alkyl ethers having an addition mole number of 5 to 10 moles, in combination with polyoxyethylene hydrogenated castor oil and polyoxyethylene alkyl ether May be. (F) By mix | blending component, intraoral irritation can also be fully suppressed.
The nonionic surfactant (F) is a polyoxyethylene hydrogenated castor oil having an average added mole number of ethylene oxide of 10 to 20, especially from the viewpoint of no irritation in the oral cavity, and the carbon number of the alkyl group is the above-mentioned. Polyoxyethylene alkyl ethers having an average addition mole number of ethylene oxide within the range of 5 to 10 moles are preferred.

The blending amount of the nonionic surfactant as the component (F) is preferably 0.1 to 4%, more preferably 0.1 to 3% of the entire composition. When the blending amount is within the above range, the absence of oral irritation is more excellent, and the discoloration of the preparation can be sufficiently suppressed. When it exceeds 4%, the discoloration suppressing effect of the preparation may be lowered.

In the present invention, it is preferable to further blend (G) alginic acid or a salt thereof. When (G) alginic acid or a salt thereof is added in addition to the components (C), (D), and (E), the smoothness of the skin surface of the preparation is also improved.
Sodium alginate has a viscosity of 2% aqueous solution at 25 ° C. (Brookfield type rotational viscometer, rotor No. 3, rotation speed 12 rpm, measurement time 3 minutes) of 1,000 to 4,000 mPa · s, particularly 2,000 to What is 4,000 mPa * s is good.
(G) When alginic acid or a salt thereof is blended, the blending amount is preferably 0.1 to 2%, more preferably 0.5 to 1.5% of the entire composition.

The gel oral composition of the present invention is not particularly limited in dosage form, but is particularly suitable as a gel dentifrice. In addition to the above-mentioned components, the composition of the present invention contains known additive components (pharmacologically acceptable carriers) that can be used in oral compositions within a range that does not impair the effects of the present invention. It can be blended depending on the type. Specifically, binders other than the components (C), (D), (E) and (G), surfactants other than the component (F), thickeners, pigments, sweeteners, fragrances, (B ), A pH adjuster other than the component, and an active ingredient other than the component (A). Although the specific example of an additional component is shown below, the component which can be mix | blended with the composition for oral cavity of this invention is not restrict | limited to these.

Examples of the binder include cellulose binders such as sodium carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, hydroxypropylmethylcellulose, hydroxymethylethylcellulose, methylcellulose, and cationized cellulose, carrageenan, guar gum, montmorillonite, and gelatin. These binders do not need to be blended, but the amount added when blended is preferably 0.1 to 2%.
In the gel oral composition of the present invention, the total amount of the binder is preferably 0.9% or more, particularly 1.5% or more, more preferably 5% or less of the whole composition. In particular, it is 3.8% or less. In the present invention, the components (C), (D), (E), and further the component (G) also act as a binder, so that (C) within a range satisfying the total blending amount of the binder. , (D), (E) component, and further, (G) component are particularly preferable from the viewpoint of effect expression.

Examples of the surfactant include an anionic surfactant, a cationic surfactant, and an amphoteric surfactant.
Examples of the anionic surfactant include alkyl sulfates such as sodium lauryl sulfate and sodium myristyl sulfate, sodium dodecylbenzene sulfonate, hydrogenated coconut fatty acid monoglyceride sodium monosulfate, sodium lauryl sulfoacetate, sodium α-olefin sulfonate, and the like. . Examples of the cationic surfactant include distearylmethylammonium chloride and stearyldimethylbenzylammonium chloride. Examples of the zwitterionic surfactant include 2-alkyl-N-carboxymethyl-N-hydroxyethylimidazolium betaine and N-lauryl. N-alkyldiaminoethylglycine such as diaminoethylglycine and N-myristyldiaminoethylglycine, N-alkyl-1-hydroxyethylimidazoline betaine sodium and the like.
The amount of these surfactants is usually 0.6 to 7%, particularly 1.1 to 5%.

Examples of the thickener include propylene glycol, pentylene glycol, hexylene glycol, octylene glycol, polyethylene glycol having an average molecular weight of 200 to 6,000 (average molecular weight described in Quasi-drug Raw Material Standard 2006), ethylene glycol, 1, Examples thereof include polyhydric alcohols such as 3-butylene glycol and glycerin, reduced starch saccharified products, sugar alcohols such as sorbitol, xylitol and erythritol. The blending amount of the thickener is usually 30 to 60%, particularly 40 to 50%.

As dyes, legal dyes such as Blue No. 1, Yellow No. 4 and Green No. 3, natural dyes such as caramel, titanium oxide, etc. Sweeteners include saccharin sodium, aspartame, stevioside, stevia extract, paramethoxycinnamic aldehyde , Neohesperidyl dihydrochalcone, perilartin and the like.

As the fragrance, those generally used as oral fragrances can be used. For example, menthol, anethole, carvone, eugenol, limonene, n-decyl alcohol, citronellol, α-terpineol, citronellyl acetate, cineol, linalool, ethyl linalool, vanillin , Thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, pimento oil, cinnamon oil, perilla oil, winter green oil, clove oil, eucalyptus oil and the like. The blending amount of the fragrance is a normal amount, and it is preferable to use 0.000001 to 2%.

Active ingredients include enzymes such as dextranase, amylase, protease and mutanase, alkali metal monofluorophosphates such as sodium monofluorophosphate, fluorides such as sodium fluoride and stannous fluoride, tranexamic acid, epsilon -Aminocaproic acid, allantoin, aluminum chlorohydroxy allantoin, azulene, glycyrrhizinate, glycyrrhetinic acid, sodium chloride, anti-inflammatory agents such as vitamins other than component (A), cetylpyridinium chloride, benzalkonium chloride, triclosan, hinokitiol, Examples include bactericides such as lysozyme chloride, anticalculus agents such as polyphosphates, tobacco spider removers such as polyvinylpyrrolidone, and amino acids such as glycine and proline. These can be blended in an effective amount as long as the effects of the present invention are not hindered.

The pH (25 ° C.) of the composition is preferably 6.5 to 9.0, more preferably 7.0 to 8.6, and still more preferably 8.1 to 8.6. You may adjust by adding a pH adjuster. Examples of the pH adjuster include organic acids such as citric acid, lactic acid and malic acid or salts thereof, and inorganic compounds such as hydrochloric acid, sodium hydroxide and potassium hydroxide.

Further, the water content of the gel oral composition is usually 20 to 60%, particularly 30 to 50%.

Hereinafter, although an Example, a comparative example, and a formulation example are shown and this invention is demonstrated concretely, this invention is not restrict | limited to the following Example. In the following examples, “%” means “% by mass” unless otherwise specified.

[Examples and Comparative Examples]
A gel dentifrice composition having the composition shown in Table 1 and the components shown in Tables 2 to 7 was prepared by a conventional method, and the evaluations shown in (1) to (4) below were performed. Furthermore, about the gel-like dentifrice composition of Table 5, evaluation shown to following (5) was also performed. The results are shown in the table.

(1) Evaluation of inhibitory effect on discoloration of preparations Each of three gel dentifrice compositions filled in an 8 mm diameter laminated tube was stored at 50 ° C for 1 month or at -5 ° C for 1 month, and then at room temperature. (20 ° C), the gel dentifrice composition was extruded 10 cm onto the straw paper, and the change in color tone of the 50 ° C stored product compared to the -5 ° C stored product was observed by sensory evaluation of 5 expert panelists. The degree of discoloration was sensory-evaluated according to the four-grade rating criteria. The average value of the score results of five people for three was determined, and the discoloration inhibiting effect of the preparation was determined according to the following four-stage evaluation criteria.
(Score standard)
4 points: No discoloration.
3 points: Almost no discoloration is observed.
2 points: Discoloration is observed.
1 point: Significant discoloration is observed.
(Evaluation criteria)
◎: 3.5 points or more and 4.0 points or less ○: 3.0 points or more and less than 3.5 points △: 2.0 points or more and less than 3.0 points ×: Less than 2.0 points

(2) Evaluation of spinnability After about 1 g of each of the three gel-like dentifrice compositions filled in a laminate tube having a diameter of 8 mm was placed on a commercially available toothbrush, the tube and the brush were pulled upward. The spinnability of the gel dentifrice composition was tested. The spinnability refers to the property that the dentifrice composition stretches like a yarn when taken out from the tube. The length of the dentifrice composition was measured and evaluated according to the following four grades. The average value of the three was evaluated according to the following four-level evaluation criteria, and the spinnability (no spinnability) was determined.
(Score standard)
4 points: Yarn length is less than 0.5 cm and kneading is good.
3 points: The yarn length is 0.5 cm or more and less than 1 cm, but there is no problem in use.
2 points: The length of the yarn is 1 cm or more and less than 1.5 cm, which is problematic in use.
1 point: The length of the yarn is 1.5 cm or more, which is problematic in use.
(Evaluation criteria)
◎: 3.5 points or more and 4.0 points or less ○: 3.0 points or more and less than 3.5 points △: 2.0 points or more and less than 3.0 points ×: Less than 2.0 points

(3) Evaluation of liquid separation stability After storing 3 gel-like dentifrice compositions filled in an 8 mm diameter laminated tube at 50 ° C. for 1 month, the gel-like dentifrice composition was placed on a straw half paper. The area of the liquid extruding 10 cm and exuding on the straw half paper was measured, and the degree of liquid separation was evaluated according to the following four grades. The average value of the three score results was obtained, and the liquid separation stability was determined according to the following four evaluation criteria.
(Score standard)
4 points: No liquid separation is observed.
3 points: When extruded, liquid separation is hardly observed, and there is no problem in use.
2 points: When extruded, 1 to 3 cm ² of liquid separation is observed at the mouth.
1 point: When extruding, liquid separation is recognized in the mouth part exceeding 3 cm ² .
(Evaluation criteria)
◎: 3.5 points or more and 4.0 points or less ○: 3.0 points or more and less than 3.5 points △: 2.0 points or more and less than 3.0 points ×: Less than 2.0 points

(4) Evaluation of shape retention over time Three of each of the gel dentifrice compositions were extruded 10 mm each onto a toothbrush having a brush head width of 10 mm and a length of 20 mm, and the shape after 3 minutes was visually confirmed. The average value of the three samples was evaluated according to the following four-stage evaluation criteria, and the temporal retention was determined.
(Evaluation criteria)
A: There is no change in shape, and it does not hang from the toothbrush.
○: Almost no change in shape, and does not hang from the toothbrush.
Δ: Slightly changed in shape and slightly hung from the toothbrush.
X: There is a change in shape and it hangs down from the toothbrush.

(5) Evaluation of intraoral irritation A sensory test was conducted using 10 expert panelists as evaluators. About 0.5 g of the gel dentifrice composition was placed on a commercially available toothbrush and brushed for 3 minutes. The intraoral irritation felt during use was subjected to sensory evaluation according to the following four grades. The average value of the score result of 10 persons was calculated | required, and the absence of intraoral irritation | stimulation was determined with the following four-stage evaluation criteria. ○ The above were judged to be acceptable because of low oral irritation.
(Score standard)
4 points: No irritation.
3 points: There is almost no irritation.
2 points: There is some irritation.
1 point: There is considerable stimulation.
(Evaluation criteria)
◎: 3.5 points or more and 4.0 points or less ○: 3.0 points or more and less than 3.5 points △: 2.0 points or more and less than 3.0 points ×: Less than 2.0 points

Details of the raw materials used are shown below.
(A) L-ascorbyl magnesium phosphate:
Wako Pure Chemical Industries, Ltd. (B) Sodium dihydrogen phosphate for biochemistry:
Wako Pure Chemical Industries, Ltd. (C) xanthan gum for biochemistry:
DSP Gokyo Food & Chemicals Co., Ltd., Monato Gum DA
Viscosity (25 ° C): 1,300 mPa · s
Thixotropic index; 4.7
(D) Sodium polyacrylate:
Made by Toagosei Co., Ltd., Leogic 260H
Viscosity (25 ° C): 8,800 mPa · s
Thixotropic index; 5.1
(E) Thickening silica E1:
DSL. CARPLEX # 67, manufactured by Japan
Specific surface area 350 m ² / g
(E) Thickening silica E2:
DSL. CARPLEX # 67, manufactured by Japan
Specific surface area 400m ² / g
(F) Polyoxyethylene (20) hydrogenated castor oil:
NIKKOL HCO 20 manufactured by Nikko Chemicals Co., Ltd.
(F) Polyoxyethylene (5) stearyl ether:
EMALEX 605, manufactured by Nippon Emulsion Co., Ltd.
(G) Sodium alginate:
Kimika Argin manufactured by Kimika Co., Ltd. Viscosity (25 ° C): 2,600 mPa · s
The viscosity of xanthan gum is the viscosity of a 1% aqueous solution of xanthan gum containing 1% potassium chloride, and was measured with a Brookfield rotary viscometer (rotor No. 3, rotation speed 60 rpm, measurement time 30 seconds). The viscosity of sodium polyacrylate is the viscosity of a 0.5% aqueous solution, and was measured with a Brookfield type rotational viscometer (rotor No. 5, rotation speed 20 rpm, measurement time 2 minutes). Each thixotropic index (apparent viscosity (η1) at 5 rpm / apparent viscosity (η2) at 50 rpm) is a B-type viscometer (manufactured by Toki Sangyo Co., Ltd., VISCOMETER TVB-10, H2 rotor, measurement time 3 Min).
The specific surface area of the thickening silica was measured at 25 ° C. using a specific surface area measuring device (manufactured by Nikkiso Co., Ltd., automatic specific surface area meter, BET multipoint method, measurement gas; nitrogen).
The viscosity of sodium alginate is the viscosity of a 2% aqueous solution, and was measured with a Brookfield type rotational viscometer (rotor No. 3, rotation speed 12 rpm, measurement time 3 minutes).
The pH (25 ° C.) of each gel dentifrice composition was about 8.3.

Note: (G) The gel dentifrice composition (Example 19) containing sodium alginate had a very smooth and improved skin surface compared to that of Example 1.

Note: (G) The gel dentifrice composition (Examples 24 to 31) containing sodium alginate had a very smooth and improved skin surface compared to that of Example 1.

A prescription example is shown below. The raw materials used are the same as in the examples.

[Prescription example] Gel dentifrice (pH 8.3)
(A) L-ascorbyl magnesium phosphate 0.3%
(B) Sodium dihydrogen phosphate 0.5
(C) Xanthan gum 1
(D) Sodium polyacrylate 0.4
(E) Thickening silica E1 (specific surface area: 350 m ² / g) 4.5
(F) Polyoxyethylene (20) hydrogenated castor oil 1
(F) Polyoxyethylene (5) Stearyl ether 1
(G) Sodium alginate 0.8
Sorbit liquid (70%) 60
Saccharin sodium 0.1
Propylene glycol 4
Polyethylene glycol 4000 0.4
Sodium lauryl sulfate 1.5
Sodium sulfate 1
Citric acid 0.1
Sodium hydroxide 0.3
Fragrance 1
Purified water balance
Total 100%
(C) / (D) = 2.5

Claims

A gel-like composition for oral cavity containing no abrasive,
(A) Ascorbic acid ester or salt thereof 0.1 to 3% by mass,
(B) orthophosphoric acid or a salt thereof 0.1 to 3% by mass,
(C) xanthan gum 0.7-2% by mass,
(D) Polyacrylic acid or a salt thereof 0.1 to 1% by mass
And (E) thickening silica 0.1 to 10% by mass
A gel-like composition for oral cavity, wherein (C) / (D) is 1.0 to 10 in terms of mass ratio.
The gel oral composition according to claim 1, wherein (B) orthophosphoric acid or a salt thereof is one or more selected from orthophosphoric acid, a normal salt thereof and a hydrogen salt.
3. The gel oral composition according to claim 2, wherein (B) orthophosphoric acid or a salt thereof is hydrogen phosphate.
Further, (F) polyoxyethylene hydrogenated castor oil having an average addition mole number of ethylene oxide of 10 to 60 moles and an alkyl group having 14 to 18 carbon atoms and an average addition mole number of ethylene oxide of 5 to 10 moles The gel oral composition according to any one of claims 1 to 3, comprising 0.1 to 4% by mass of one or more nonionic surfactants selected from polyoxyethylene alkyl ethers.
The gel oral composition according to any one of claims 1 to 4, further comprising (G) 0.1-2% by mass of alginic acid or a salt thereof.
The gel oral composition according to any one of claims 1 to 5, which is a gel dentifrice.