JPS6239129B2 - - Google Patents

Description

[Detailed description of the invention]

The present invention relates to oral compositions containing dextranase. BACKGROUND ART Conventionally, it has been proposed to incorporate dextranase into oral compositions such as toothpastes as an active ingredient for caries prevention in order to prevent the formation of dental plaque (Japanese Patent Publication No. 34897/1983). However, there is a problem in that dextranase is easily deactivated due to the influence of moisture, anion activator, etc. contained in the oral composition. For this reason, various techniques have been proposed to stabilize dextranase.
More preferably, if an anionic activator is not used or the amount of the anionic activator is reduced and a nonionic activator is used as the main activator, it is expected that deactivation of dextranase can be prevented as much as possible. . However, oral compositions using nonionic active agents have not been put into practical use because conventional formulations have inferior usability and stability. Specifically, sucrose fatty acid esters, for example, have been studied as nonionic surfactants, but they have the drawbacks of being extremely bitter, causing discoloration, and poor stability of the formulation; However, the use of these activators as the main activator poses problems in terms of product production. The present inventors have conducted extensive research on oral compositions that have a good feeling of use, excellent formulation stability, and good dextranase stability, and have found that lactitol, maltitol, maltotriel, ,
A fatty acid ester of a sugar alcohol selected from the group consisting of maltotetriitol will be used as the main active agent of a dextranase-containing oral composition.
The inventors have discovered that it is possible to obtain an oral composition that satisfies all aspects of formulation stability and can be suitably used, leading to the present invention. The present invention will be explained in detail below. The present invention incorporates dextranase into oral compositions such as toothpaste, moisturized toothpaste, powdered toothpaste, liquid toothpaste, liquid mouth fresheners such as mouthwash, solid mouth fresheners such as Trota, and chewing gum. In the oral composition containing dextranase, lactitol or the following formula (1) Sugar alcohols (i.e. maltitol,
maltotriitol, maltotetriitol,)
and a fatty acid or a fatty acid derivative. This sugar alcohol fatty acid ester is highly safe, and its foaming properties are equivalent to or better than sucrose fatty acid ester, which is said to be relatively good among nonionic surfactants. It does not have the bitter taste that lauric acid esters have, has a good feeling of use, and has a good reuse effect. Furthermore, both lactitol and the sugar alcohol of formula (1), which are raw materials for the above-mentioned active agent, have properties that are far superior to sucrose in heat resistance, acid resistance, and alkali resistance, and are difficult to ferment.
The fatty acid ester has good stability when blended into toothpaste and has excellent performance as a surfactant in oral compositions, and as mentioned above, the sugar alcohol fatty acid ester is blended with dextranase. By including it as a main active agent in an oral composition, it was possible to obtain an oral composition that has good usability and formulation stability and can stably retain dextranase for a long period of time. . The sugar alcohols used herein can be obtained by reducing lactose, maltose, maltotriose, maltotetraose, by various methods such as electrolytic reduction, high pressure catalytic reduction, or using metal hydrides. I can do it. In this case, when amylose is hydrolyzed to produce maltose, etc., by adjusting the degree of hydrolysis of amylose, for example, products with a large amount of maltose, products with maltotriose as the main component, and products with maltoheptaose etc. It is also possible to produce a mixture with a large amount of maltopentitol, maltohexitol, maltoheptitol, etc. and reduce it as it is to use as a mixed sugar alcohol. No problem. The acyl group of the fatty acid or fatty acid derivative to be reacted with the sugar alcohol may be linear or branched, but preferably has 8 to 20 carbon atoms, particularly 10 to 20 carbon atoms.
More preferred are 18 saturated acyl groups and 16 to 18 unsaturated acyl groups. Such an acyl group is
For example, caprylic, lauroyl, tridecanoyl,
Examples include 2-methyllauroyl, myristoyl, pentadecanoyl, palmitoyl, stearoyl, isostearoyl, and oleoyl, and these may be used alone or as a mixture. Examples of mixtures include coconut oil fatty acid residues, palm oil fatty acid residues, hydrogenated beef tallow fatty acid residues, and the like. The fatty acid ester of the sugar alcohol preferably has an average degree of esterification of 0.5 to 3.0, more preferably 0.8 to 2.0. Also preferred are monoester contents of at least 60% by weight. The amount of the above sugar alcohol fatty acid ester is:
Although not particularly limited, it is preferably 0.1 to 5% (weight%, same hereinafter) of the total. In addition, in the present invention, in addition to the above-mentioned sugar alcohol fatty acid ester, it is also possible to further blend other surfactants. In this case, N-long chain acylamino acids are preferably used as the other active agent, and by using the sugar alcohol fatty acid ester and N-long chain acylamino acids together, the advantages of the sugar alcohol fatty acid ester can be improved. The foamability can be improved without impairing the performance. The N-long chain acylamino acids include one or two amino acids N-substituted with a saturated or unsaturated acyl group having 8 to 20 carbon atoms or a water-soluble salt thereof;
More than one species is preferably used. The above acyl groups include capryl, lauroyl, tridecanoyl, 2
-Methyl lauroyl, myristoyl, pentadecanoyl, palmitoyl, stearoyl, isostearoyl, oleoyl and the like. Further, it may be a mixture such as a coconut oil fatty acid residue, a palm oil fatty acid residue, a hydrogenated beef tallow fatty acid residue, or a mixed fatty acid residue of coconut oil and hydrogenated beef tallow. Amino acids include glutamic acid, glycine, alanine, and β
-Alanine, phenylalanine, leucine, isoleucine, methionine, proline, tryptophan, valine, serine, etc. are exemplified, and the salts include sodium salt, potassium salt, etc. Furthermore, N-lower alkyl substituted products such as sarcosine and N-methyl-β-alanine can also be used. Particularly preferred N-long chain acylamino acids are alkali metal salts of glutamic acid, sarcosine, and N-methyl-β-alanine N-substituted with a saturated or unsaturated acyl group having 10 to 18 carbon atoms. In addition, when these N-long chain acylamino acids are used in combination with the sugar alcohol fatty acid ester, the N-long chain acylamino acids are used in a ratio of 1 to 2 parts by weight per 1 to 50 parts by weight of the sugar alcohol fatty acid ester. It is preferable to do so. In the present invention, the amount of dextranase blended is not particularly limited, but usually per 1 g of oral composition.
100 to 100,000 units (u/g of oral composition), particularly preferably 1,000 to 50,000 u/g of oral composition. Here, 1 unit refers to the amount of enzyme that produces free reducing sugars equivalent to 1 μg of glucose per minute when the reaction is performed using dextran as a substrate. In this case, in the present invention, in addition to dextranase as an active ingredient, amylase, protease,
Enzymes such as mutanase, lysozyme, and Litetsuque enzyme; alkali metal monofluorophosphates such as sodium monofluorophosphate; fluorides such as sodium fluoride and stannous fluoride;
One or more active ingredients such as tin compounds, chlorhexidine salts, epsilon aminocaproic acid, tranexamic acid, aluminum chlorohydroxylalantoin, dihydrocholesterol, glycyrrhizic acids, sodium chloride, and water-soluble inorganic phosphoric acid compounds may be blended. In particular, when an alkali metal monofluorophosphate such as sodium monofluorophosphate is used in combination with dextranase, it stabilizes dextranase and maintains a high residual rate of dextranase in the dentifrice composition after long-term storage. It is desirable because it can be done. In addition, when dextranase and mutanase are combined, a synergistic effect occurs to dissolve plaque and prevent re-deposition, and the combination of dextranase and Litetsuque enzyme has benefits such as strengthening the efficacy of Liteque enzyme. be. Note that the water-soluble inorganic phosphoric acid compound includes potassium salts or sodium salts of orthophosphoric acid, pyrophosphoric acid, and polyphosphoric acid, and potassium salts are preferred. The oral composition of the present invention can further contain various other ingredients depending on the type thereof, and can be prepared as toothpaste, moist toothpaste, powdered toothpaste,
Liquid toothpaste, mouthwash, etc. can be obtained. For example, toothpaste contains dibasic calcium phosphate.
Dihydrate and anhydride, calcium carbonate, calcium pyrophosphate, inert sodium metaphosphate, anhydrous silicic acid, hydrated silicic acid, aluminosilicate, alumina, aluminum hydroxide, tribasic magnesium phosphate, magnesium carbonate, calcium sulfate, synthetic One or more types of abrasives such as resins may be blended (the blending amount is usually 10 to 90% of the total, especially 20 to 60% in the case of toothpaste). In addition, carrageenan, sodium carboxymethyl cellulose, sodium alginate, gums, polyvinyl alcohol, vegum,
One or more types of hydroxyethyl cellulose and the like may be blended (compounding amount usually 0.3 to 5%). Furthermore, sorbitol, glycerin,
One or more of propylene glycol, 1,3-butylene glycol, polyethylene glycol, xyrite, maltite, lactite, etc. may be blended (the blending amount is usually 10 to 70%). In this case, it is desirable to use propylene glycol as the binder dispersion, but if it is blended in a large amount, the dextranase residual rate during storage will decrease, so sorbit is blended as the main thickener, and propylene glycol and sorbit are used in combination. It is desirable to do so. Furthermore, fragrances such as l-menthol, anethole, carvone, and eugenol, sweeteners such as saccharin sodium, stevioside, neohesperidine dihydrochalcone, thaumatin, glycyrrhizin, and perillartine, preservatives such as parabens, gelatin, peptone, and other ingredients. For example, when manufacturing a toothpaste, it can be manufactured by kneading the above-mentioned desired components with an appropriate amount of water. The toothpaste composition thus obtained is stored in a predetermined container such as an aluminum tube, a laminate tube made by laminating both sides of aluminum foil with plastic, a plastic tube, a bolt-shaped container, an aerosol container, etc. provided for use. Next, an experimental example will be shown. Experimental Example A toothpaste composition having the formulation shown in Table 1 was prepared by a conventional method.

【table】

[Table] The lactitol lauric acid monoester used has an esterification degree (DS) of 1.1.
Maltitol lauric acid monoesters include esters obtained from mixed sugar alcohols containing about 85% of n=1, about 10% of n=2, and about 5% of n=3 in formula (1). The polymer used had a degree of polymerization of 1.1 and a degree of polymerization () of 1.2. Next, the feeling of use (flavor and foaming) of each of the above toothpastes was evaluated in a sensory test by an expert panel. In addition, after each toothpaste was stored at -5°C and 40°C for one month, liquid separation, rough skin, and discoloration were examined to evaluate the stability of the toothpaste. Furthermore, immediately after preparing each toothpaste and
The amount of dextranase after storage at 40°C for one month was measured to evaluate the residual activity of dextranase. The results are shown in Table 2. The evaluation criteria are as follows. Usage Flavor 〇: Good flavor △: Slightly bad flavor ×: Bad flavor Foaming ◎: Foams very well 〇: Foams well △: Slightly foams ×: Almost no foaming Toothpaste stability Liquid separation 〇: No liquid separation △: Slightly Liquid separation occurs ×: Skin roughness with significant liquid separation 〇: Good smooth appearance △: 〃 Slightly bad ×: 〃 Bad discoloration〇: No discoloration △: Slight discoloration ×: Dextranase residual activity with significant discoloration〇 : Dextranase residual rate 80% or more △: 〃 30-80% ×: 〃 30% or less

In the case of [Table], it was 〓×〓.
From the results shown in Table 2, the toothpaste of the present invention was evaluated to be excellent in all aspects of usability, toothpaste stability, and residual dextranase activity. In addition, in the above toothpaste formulation, when lactitol or maltitol coconut oil fatty acid ester, hydrogenated tallow fatty acid ester, or oleic acid ester is used instead of lactitol lauric acid monoester and maltitol lauric acid monoester,
As above, it has excellent dextranase residual activity,
It was also found that the usability and toothbrushing stability were good. Examples are shown below. Example 1 Toothpaste dicalcium phosphate 50.0% Silicic anhydride 2.0 Sorbit 20.0 Lactitol laurate (DS1.2) 2.0 Carrageenan 1.0 Gelatin 0.3 Satucharin sodium 0.1 Flavor 1.0 Dextranase 3000u/g Toothpaste water Remaining 100.0% Example 2 Toothpaste Aluminum hydroxide 50.0% Propylene glycol 2.0 Sorbit 18.0 Maltitol coconut oil fatty acid ester (in formula (1), about 85% of n=1, about 10% of n=2, and about 5 of n=3) DS1.4, 1.2) 2.0 Sodium alginate 1.0 Satucalin sodium 0.1 Flavor 1.0 Dextranase 7500u/g Toothpaste water Balance 100.0% Example 3 Toothpaste calcium carbonate 50.0% Glycerin 20.0 Lactitol myristate ester (DS1.6)
1.0 Lauroyl sarcosinate 0.5 Carrageenan 0.5 Carboxymethyl cellulose 0.5 Sodium monofluorophosphate 0.76 Satucalin sodium 0.1 Fragrance 1.0 Dextranase 2000u/g toothpaste water remaining 100.0% Example 4 Toothpaste dibasic calcium phosphate 50.0% Sorbit 25.0 Lactate tall palmitine Acid ester (DS1.2)
3.0 Carrageenan 0.3 Sodium alginate 0.7 Hydroxyethyl cellulose 1.0 Chlorhexidine hydrochloride 0.01 Satucalin sodium 0.1 Fragrance 1.0 Dextranase 12000u/g Toothpaste water Remaining 100.0% Example 5 Toothpaste Silicic anhydride 20.0% Sorbit 30.0 Glycerin 20.0 Lac Titol laurate ( DS1.5) 2.5 Carrageenan 0.7 Sodium alginate 0.3 Sodium saccharin 0.1 Fragrance 1.0 Dextranase 5000u/g Toothpaste Water Remaining 100.0% Example 6 Junsei toothpaste calcium carbonate 75% Glycerin 12 Sodium Satucalin 0.1 Lactitol coconut oil fatty acid ester ( DS1.1)
1.0 Maltitol coconut oil fatty acid ester (obtained from mixed sugar alcohol containing about 80% of n=1 and about 20% of n=2 in formula (1),
DS1.1, 1.2) 1.0 Fragrance 1.0 Dextranase 1000u/g toothpaste water remaining 100.0% Example 7 Liquid toothpaste glycerin 35% Sodium polyacrylate 5.0 Lactitol laurate (DS1.2) 2.0 Satucalin sodium 0.1 Ethanol 3.0 Fragrance 1.0 Dextranase 3000u/ml toothpaste water remaining 100.0% Example 8 Mouthwash ethanol (90%) 20% Satucalin sodium 0.2 Maltitol palmitate (approximately 65% of n=1 in formula (1)) , about 25% of n=2, n
obtained from a mixed sugar alcohol consisting of about 5% of n=3 and about 5% of n=4, DS1.3,
1.5） 1.0 Fragrance 1.0 Dextranase 10000u/ml Mouthwash Water Remaining 100.0% Example 9 Toothpaste Aluminum Hydroxide 50.0% Propylene Glycol 3.0 Sorbit 20.0 Maltitol Laurate *(DS=2.0,
= 2.6) 3.0 Carrageenan 1.0 Saccharin sodium 0.1 Fragrance 1.0 Dextranase 10000u/g toothpaste Remaining amount 100.0% * In formula (1), n = 1 (maltitol) approximately 20%, n = 2 (maltotriitol) approximately 40%, n = 3 (maltotetriitol) approximately 20%, n = 4 (maltopentitol) approximately 10%, n = 5 (maltohexitol) from a mixed sugar alcohol containing about 5% and n=6 (maltoheptitol). All of the oral compositions of Examples 1 to 9 had good dextranase stability, formulation stability, and feeling of use.

Claims (1)

[Scope of Claims] 1. A dextranase-containing oral composition containing a fatty acid ester of a sugar alcohol selected from the group consisting of lactitol, maltitol, maltotriitol, and maltotetriitol. 2 Fatty acid ester of sugar alcohol has 8 carbon atoms
The oral composition according to claim 1, which has 20 saturated or unsaturated acyl groups and an average degree of esterification of 0.5 to 3.0. 3. The oral composition according to claim 1 or 2, wherein the fatty acid ester of sugar alcohol has a monoester content of 60% by weight or more.