JPH06183939A - Composition for oral cavity - Google Patents

Abstract

PURPOSE:To prepare the composition having a viscosity and a thixotropic property suitable for use, stable with the elapse of time, and used for oral cavities. CONSTITUTION:This composition for oral cavities comprises (1) a nonionic hydrophobic cellulose ether polymer having (a) at least one substituent selected from a group consisting of hydroxyethyl, hydroxypropyl and methyl and (b) a 3-alkoxy-2-hydroxypropoxy in which the alkoxy group is the mixture of a 8-12C alkoxy group and a 14-18C alkoxy group, (2) a cationized polymer selected from the group of cationized hydroxyethyl cellulose, cationized guar gum, and cationized xanthane gum, and (3) a nonionic surfactant.

Description

Detailed Description of the Invention

[0001]

FIELD OF THE INVENTION This invention relates to oral compositions.

[0002]

2. Description of the Related Art JP-A-60-104008 and US Pat. No. 4,584,189 propose to incorporate hydrophobically modified hydroxyethyl cellulose into a dentifrice to impart shape retention. . However, all of them combine hydrophobic groups with different chain lengths.
It does not teach the use (mixed hydrophobic groups). In oral compositions, a viscosity and thixotropy suitable for use are required. In obtaining such preferable physical properties by using a hydrophobic cellulose ether polymer, when a hydrophobic group having a relatively short chain length is used, sufficient viscosity cannot be obtained unless the degree of substitution is high, and the substitution of the hydrophobic group The higher the degree, the worse the solubility in water. For this reason,
Mixing dissolution time at the time of manufacturing the composition for oral cavity becomes longer,
There is a problem that the production efficiency is significantly reduced. On the other hand, when a hydrophobic group having a relatively long chain length is used, the polymer can be hydrophobized only to a relatively low degree of substitution as long as the polymer is water-soluble. In this case, the viscosity can be obtained even at a low degree of substitution, but there is a problem that the thixotropy is inferior because the hydrophobicity is low.

Therefore, in order to solve the above problems, the present inventors have found that the medium-chain (C8-C12) hydrophobic group and the long-chain (C14-C1)
The cellulose ether was modified by using the hydrophobic group of 8) in combination. However, when the composition for oral cavity in which the hydrophobized cellulose ether polymer was used alone as a binder and further mixed with a nonionic surfactant was examined, it was found that the hydrophobized cellulose ether polymer and nonionic interface It has been found that the activator is unstable due to poor compatibility, and the phenomenon of syneresis, that is, separation of liquid from solid, occurs over time. Therefore, in a system in which a hydrophobized cellulose ether polymer having a hydrophobic group having a different chain length and a nonionic surfactant are used in combination, in order to obtain a composition for oral cavity which is stable over time, a new anti-separating agent is added. There is a need.

[0004]

Means for Solving the Problems As a result of intensive studies in view of such circumstances, the present inventors have found that a cellulose ether polymer having two kinds of alkyl hydrophobic groups having different chain lengths and a nonionic surfactant. In the oral composition using a combination of the above, by adding a specific cationized polymer as an anti-synergistic agent, it was found that an oral composition rich in thixotropy and stable over time was obtained, and the present invention was completed. Came to do.

That is, according to the present invention, (1) at least one substituent selected from the group consisting of hydroxyethyl, hydroxypropyl and methyl and (b) an alkoxy group have 8 to 12 carbon atoms and 14 to 14 carbon atoms. 1
A nonionic hydrophobicized cellulose ether polymer having a 3-alkoxy-2-hydroxypropoxy group which is a mixed group of 8; (2) cationized hydroxyethyl cellulose (hereinafter referred to as cationized HEC) and cationized guar gum And a cationized polymer selected from the group consisting of cationized xanthan gum and (3) a nonionic surfactant.

The hydrophobized cellulose ether polymer used in the present invention has a hydroxyl group of a cellulose ether polymer substituted with at least one group selected from the group consisting of hydroxyethyl, hydroxypropyl and methyl.

[0007]

[Chemical 1] [In the formula, R ₁ means an alkyl group having 8 to 12 carbon atoms]
Groups represented by and

[0008]

[Chemical 2] [Wherein R ₂ represents an alkyl group having 14 to 18 carbon atoms] is a compound further substituted with a group to form an ether bond.

Of these, the substitution degree by at least one group selected from the group consisting of hydroxyethyl, hydroxypropyl and methyl is not particularly limited as long as the cellulose ether polymer is water-soluble, and is generally commercially available. Any thing can be used. In addition, although not particularly limited, the M.S. of the hydrophobic group of the medium chain (C7 to C12) is 0.0005 to 0.03, and the long chain (C14 to
The M.S. of the hydrophobic group of C18) is preferably 0.0005 to 0.005. Here, "MS" means the average number of moles of substituents attached per glucose unit. In applying the hydrophobized cellulose ether polymer to an oral composition, the amount thereof is usually 0.1 to 5% by weight, preferably 0.1 to 3% by weight based on the total amount of the composition.
% By weight.

The cationized HEC used in the present invention is obtained by adding a compound obtained by adding ammonium chloride to hydroxyethyl cellulose, preferably glycidyltrimethylammonium chloride or 3-chloro-2-hydroxypropyltrimethylammonium chloride. Is a cationic polymer (hydroxyethyl cellulose hydroxypropyl trimethyl ammonium chloride ether). Further, although not particularly limited, the average molecular weight of hydroxyethyl cellulose is 1,000,000 or more, preferably 1,500,000 or more, more preferably 1,500,000 to 3,000,000, and the cationic substituent group added per glucose unit is The degree of cationization, which represents the average number of moles, is 0.05 to 0.5 mol / glucose.

Cationized guar gum and cationized xanthan gum are compounds obtained by adding ammonium chloride to guar gum and xanthan gum, respectively.
Preferred is a cationic polymer (hydroxypropyltrimethylammonium chloride guar gum and hydroxypropyltrimethylammonium chloride xanthan gum) obtained by adding glycidyltrimethylammonium chloride or 3-chloro-2-hydroxypropyltrimethylammonium chloride. Also, although not particularly limited, the nitrogen content is 0.
5 to 5% by weight, preferably 0.5 to 3% by weight.

These cationized polymers may be used alone or in combination of two or more as an anti-synergistic agent.
It is mixed in a ratio of 1 to 5% by weight.

The surfactant used in the present invention is a nonionic surfactant. Polyoxyethylene / polyoxypropylene block copolymers are preferable, and those commercially available under the trade name of "Pluronic" from BASF Corporation in the United States can be used. The nonionic surfactant is 1 to 20% by weight based on the total amount of the composition.
Blend in the ratio of.

The oral composition of the present invention can be made into a dosage form such as toothpaste, ointment, pasta, cream and the like by a method known per se. For example, desired compositions such as toothpaste and gingival massage preparation can be obtained. Abrasives, flavors, humectants, sweeteners, medicinal components and the like can be added according to the application within a range that does not impair the effects of the present invention. No other binder is necessary.

For example, in the case of dentifrice, a non-silica abrasive such as dicalcium phosphate, dihydrate and anhydrate, monobasic calcium phosphate, tribasic calcium phosphate, calcium carbonate, calcium pyrophosphate, water. Aluminum oxide, alumina, insoluble sodium metaphosphate, magnesium triphosphate, magnesium carbonate, calcium sulfate, polymethylmethacrylate, synthetic resin and the like can be blended alone or in combination of two or more. The blending amount thereof is usually 5.0 to 90% by weight based on the total amount of the composition, and particularly 5 to 60% by weight in the case of toothpaste.

As a wetting agent, sorbit, glycerin, ethylene glycol, propylene glycol,
1,3-butylene glycol, polyethylene glycol, polypropylene glycol, xylit, maltite, lactit and the like can be blended alone or in combination of two or more kinds. The compounding amount thereof is usually 5 to 70% by weight based on the total amount of the composition.

Further, as a flavoring agent, menthol, carboxylic acid, anethole, eugenol, methyl salicylate, limonene, ocimene, n-decyl alcohol, citronell, α-terbineol, methyl acetate, citronenyl acetate, methyl eugenol, cineol. , Linalool, ethyl linalool, varnish, thymol, spearmint oil, peppermint oil, lemon oil, orange oil, sage oil, rosemary oil, cinnamon oil, perilla oil,
Wintergreen oil, clove oil, eucalyptus oil, etc., alone or in combination of two or more kinds, blended in a proportion of about 0.1 to 10% by weight, preferably about 0.5 to 5% by weight, based on the total amount of the composition. can do.

As sweeteners, saccharin sodium, acesulfame potassium, stevioside, neohesperidyl dihydrochalcone, glycyrrhizin, perillartine, thaumatin, asparatyl phenylalanyl methyl ester, p-methoxycinnamic aldehyde, etc. It can be blended in a proportion of 0.01 to 1% by weight, preferably 0.05 to 0.5% by weight.

Further, in the oral composition of the present invention, cationic fungicides (eg, quaternary ammonium compounds such as benzalkonium chloride, dodecyltrimethylammonium chloride, benzethonium chloride, etc.), cetylpyridinium chloride, etc. are used as medicinal components. Compounds, pyrimidine derivatives such as hexetidine, amidine derivatives such as hexamidine isethionate, bispyridine derivatives such as octenidine, mono-biguanides such as p-chlorobenzyl-biguanide, bis-biguanides such as chlorhexidine and alexidine, poly Hexamethylene biguanide hydrochloride and other polybiguanides), nonionic bactericides such as triclosan, amphoteric bactericides such as dodecyldiaminoethylglycine, dextranase, amylase, protease, mutanase, lysochy. , Lytic enzyme (Ritekku enzyme)
Enzymes such as, sodium monofluorophosphate, alkali metal monofluorophosphates such as potassium monofluorophosphate, sodium fluoride, fluorides such as stannous fluoride, tranexamic acid and epsilon aminocaproic acid, aluminum chlorhydroxyl allantoin, Dihydrocholesterol, glycyrrhizin salts, glycyrrhetinic acid, glycerophosphate, chlorophyll, sodium chloride, caropeptide, water-soluble inorganic phosphate compounds and the like can be blended alone or in combination of two or more.

[0020]

EXAMPLES Next, the present invention will be described more specifically with reference to Examples and Comparative Examples, but the present invention is not limited to these Examples. In addition, unless otherwise specified
"%" Represents% by weight.

A toothpaste was prepared according to a conventional method according to the formulation shown in Table 1. The blending amount in Table 1 is% by weight. (Measurement of viscosity) Fill a toothpaste into a glass bottle,
After standing for a time, the viscosity is measured. The apparatus uses a Brookfield viscometer and measures for 2 minutes at a rotor No. 7 and 20 rpm. Under these conditions, a toothpaste with a viscosity of 500
The viscosity is preferably adjusted to fall within this viscosity range, since the viscosity is preferably 1300 poise.

(Stability of Properties) A toothpaste having the above viscosity range is filled in a laminate tube and left at 55 ° C. for 1 month. Then, the tube is squeezed out, and the presence or absence of solid-liquid separation is visually determined. The evaluation was performed according to the following criteria. ○: No solid-liquid separation ×: Solid-liquid separation

(Result)

[Table 1]

From the results shown in Table 1, in the combined use system of the hydrophobized HEC and the pluronic surfactant, the syneresis is carried out at 55 ° C. for 1 month without any additive (Comparative Example 6). Also,
Toothpaste containing xanthan gum, hydroxyethyl cellulose, hydroxypropylmethyl cellulose and polyvinylpyrrolidone which are non-ionic binders and sodium polyacrylate which is an anionic binder as additives are all at 55 ° C for 1 month. It was found that the liquid was released under the conditions, but only the toothpaste containing the cationized HEC was not released and was stable (Comparative Examples 1 to 5 and Examples 1 and 2).

A toothpaste was prepared according to a conventional method according to the following formulation. Example 3 Ingredients Amount Dibasic calcium phosphate dihydrate 40% Glycerin 20 Pluronic F88 5 (average degree of polymerization polyoxyethylene: 194 polyoxypropylene: 39) Hydrophobized hydroxypropylmethylcellulose 1.5 (alkoxy substitution of hydrophobic groups) Degree MS is C ₁₀ 0.01, C ₁₈ 0.0005) Cationized HEC 1.0 (HEC average molecular weight 2,000,000, cationization degree 0.25) Fragrance 1.0 Saccharin sodium 1.0 Chlorhexidine hydrochloride 1 0.0 Water balance 100.0% The obtained toothpaste was stable over time, did not release water, and had an excellent feeling of use.

A toothpaste was prepared according to a conventional method according to the following formulation. Example 4 Ingredients Amount of aluminum hydroxide 50% Sorbitol 20 Pluronic F88 5 (average degree of polymerization polyoxyethylene: 194 polyoxypropylene: 39) Hydrophobized hydroxyethyl cellulose 1.0 (alkoxy substitution degree of hydrophobic group M.S. , C ₁₀ 0.005, C ₁₈ 0.0005) Cationized HEC 1.0 (HEC average molecular weight 2 million, cationization degree 0.45) Fragrance 1.0 Saccharin sodium 1.0 Sodium fluoride 0.2 Cetylpyridinium chloride 0.2 Water balance 100.0% The obtained toothpaste was stable over time, did not release water, and had an excellent feeling of use.

A gingival massage cream was prepared according to the following formulation. Example 5 Ingredients Amount Glycerin 20% Pluronic F127 2 (average degree of polymerization polyoxyethylene: 200 polyoxypropylene: 70) Hydrophobized hydroxyethyl cellulose 1.5 (alkoxy substitution degree MS of hydrophobic group is C ₁₀₀₎ 0.005, C ₁₈ 0.0005) Cationized HEC 1.0 (HEC average molecular weight 2,000,000, cationization degree 0.45) Perfume 1.0 Tocopherol nicotinate 1.0 Dipotassium glycyrrhizinate 0.5 Water balance 100. 0% The obtained massage cream was stable with time and did not release water, and an excellent feeling of use was obtained.

A toothpaste was prepared according to a conventional method according to the formulation shown in Table 2. In Table 2, the blending amount is% by weight. The viscosity measurement and the property stability determination were performed in the same manner as in Table 1.

[0029]

[Table 2]

From the results shown in Table 2, in the combined use system of the hydrophobized HEC and the pluronic surfactant, the liquid was separated under the condition of 55 ° C. for 1 month without the additive (Comparative Example 12). Also,
Toothpaste containing xanthan gum, hydroxyethyl cellulose, hydroxypropylmethyl cellulose and polyvinylpyrrolidone which are non-ionic binders and sodium polyacrylate which is an anionic binder as additives are all at 55 ° C for 1 month. It was found that liquid was released under the conditions, but only toothpaste containing cationized guar gum or cationized xanthan gum was stable and did not release liquid (Comparative Examples 7 to 11 and Examples 6 and 7).

A toothpaste was prepared according to a conventional method according to the following formulation. Example 8 Ingredients Amount Calcium phosphate dihydrate 40% Glycerin 20 Pluronic F88 5 (Average degree of polymerization polyoxyethylene: 194 Polyoxypropylene: 39) Hydrophobized hydroxypropylmethylcellulose 1.5 (Alkoxy substitution of hydrophobic group) Degree MS is C ₁₀ 0.01, C ₁₈ 0.0005) Cationized guar gum 1.0 (Nitrogen content: 1.5%) Fragrance 1.0 Saccharin sodium 1.0 Chlorhexidine hydrochloride 1.0 Water balance A total of 100.0% of the obtained toothpaste was stable with time and did not separate water, and an excellent feeling of use was obtained.

A toothpaste was prepared according to a conventional method according to the following formulation. Example 9 Ingredients Amount of aluminum hydroxide 50% Sorbitol 20 Pluronic F88 5 (average degree of polymerization polyoxyethylene: 194 polyoxypropylene: 39) Hydrophobized hydroxyethyl cellulose 1.0 (alkoxy substitution degree MS of hydrophobic group: , C ₁₀ 0.005, C ₁₈ 0.0005) Cationized xanthan gum 1.0 (Nitrogen content: 2%) Fragrance 1.0 Sodium saccharin 1.0 Sodium fluoride 0.2 Cetylpyridinium chloride 0.2 Water balance 100.0% The obtained toothpaste was stable over time and did not release water, and thus an excellent feeling of use was obtained.

A gingival massage cream was prepared according to the following formulation. Example 10 Ingredients Amount Glycerin 20% Pluronic F127 2 (average degree of polymerization polyoxyethylene: 200 polyoxypropylene: 70) Hydrophobized hydroxyethyl cellulose 1.5 (alkoxy substitution degree MS of the hydrophobic group is C ₁₀₀₎ 0.005, C ₁₈ 0.0005) Cationized guar gum 1.0 (Nitrogen content: 1%) Fragrance 1.0 Tocopherol nicotinate 1.0 Dipotassium glycyrrhizinate 0.5 Water balance 100.0% Total massage obtained The cream was stable over time and did not release water, and an excellent feeling of use was obtained.

[0034]

INDUSTRIAL APPLICABILITY According to the present invention, a hydrophobicized cellulose ether polymer having a hydrophobic group in which two kinds of alkyl substituents having different chain lengths are combined, a nonionic surfactant and a specific cationized polymer are blended. As a result, an oral composition having appropriate water solubility as an oral composition, viscosity and thixotropy suitable for use, and stable over time can be obtained.

Claims (10)

[Claims] 1. (1) At least one substituent selected from the group consisting of (a) hydroxyethyl, hydroxypropyl and methyl and (b) an alkoxy group have 8 to 1 carbon atoms.
Nonionic hydrophobicized cellulose ether polymer having 3-alkoxy-2-hydroxypropoxy group, which is a mixed group of 2 and 14-18, and (2) cationized hydroxyethyl cellulose, cationized guar gum and cationized xanthan gum. An oral composition comprising a cationized polymer selected from the group consisting of (3) and (3) a nonionic surfactant. 2. A hydrophobized cellulose ether polymer,
The oral composition according to claim 1, wherein 0.1 to 5% by weight based on the total weight of the composition and 0.1 to 5% by weight of the cationized polymer are included in the total weight of the composition. 3. The degree of substitution (MS) of 3-C _8-12 alkoxy-2-hydroxypropoxy group in the hydrophobized cellulose ether polymer is 0.0005 to 0.03, and 3
The oral composition according to claim 1, wherein the degree of substitution (MS) of the -C _14-18 alkoxy-2-hydroxypropoxy group is 0.0005 to 0.005. 4. The cationized polymer is cationized hydroxyethyl cellulose, and the hydroxyethyl cellulose has an average molecular weight of 1,000,000 or more and a degree of cationization of not more than 0.1.
The oral composition according to claim 1, wherein the composition is 05 to 0.5 mol / glucose. 5. The oral composition according to claim 1, wherein the cationized polymer is hydroxyethyl cellulose hydroxypropyltrimethylammonium chloride ether. 6. The cationized polymer has a nitrogen content of 0.1.
The oral composition according to claim 1, which is 5 to 5% by weight of cationized guar gum or cationized xanthan gum. 7. The oral composition according to claim 1, wherein the cationized polymer is hydroxypropyltrimethylammonium chloride guar gum. 8. The oral composition according to claim 1, wherein the cationized polymer is hydroxypropyltrimethylammonium chloride xanthan gum. 9. The oral composition according to claim 1, wherein the nonionic surfactant is a polyoxyethylene / polyoxypropylene block copolymer. 10. The oral composition according to claim 9, wherein the polyoxyethylene / polyoxypropylene block copolymer is blended in an amount of 1 to 20 parts by weight.