KR20180010671A - Oral composition for inhibiting the halitosis - Google Patents

Abstract

The present invention relates to an oral composition for controlling halitosis, capable of effectively removing and inhibiting microorganisms, gum diseases and halitosis causing materials which cause halitosis by improving residual properties in the mouth of zinc ions. The oral composition comprises 35-50 wt% of water and 0.8 to 2 wt% of alginic acid or alginate.

Description

[0001] The present invention relates to an oral composition for inhibiting the halitosis,

The present invention relates to an oral composition for restraining bad breath, which can effectively remove and inhibit microorganisms, gum disease and halitosis causing substances, which cause bad breath, by enhancing oral retention of zinc ions.

Volatile sulfur compounds (VSCs) account for 90% of total volatile substances. Volatile sulfur compounds are generated by metabolic processes of microorganisms that break down components of oral epithelial cells, saliva, serum proteins, food waste, and are caused by compounds in saliva and saliva sediments. Volatile sulfur compounds that cause bad breath include hydrogen sulfide (H ₂ S), methyl mercaptan (CH ₃ SH), and dimethyl sulfide ((CH ₃ ) ₂ S) .

The cause of bad breath is complicated and diverse, but oral causes account for more than 80%. Oral microorganisms causing bad breath include Porphyromonas gingivalis (Prevotella intermedia), Fusobacterium nucre And Fusobacterium nucleatum. In addition, since gum disease can be induced by these bacteria and bacterial metabolites, in order to effectively inhibit bad breath, it is necessary to prevent the gum disease by inhibiting the growth of oral microorganisms as well as volatile sulfur compounds It is important.

It is known that zinc ions change into nonvolatile matter through binding with sulfur of volatile compounds, and it is known to remove the causes of oral malodor due to antimicrobial and anti-pragmatic action.

A method of suppressing halitosis by using the characteristics of zinc ions has been proposed, and accordingly, various attempts have been made to apply it to oral products.

Also disclosed is a method for improving the oral retention of an antimicrobial substance by blending together polymers.

U.S. Patent No. 6,344,184 discloses an oral composition comprising 0.05-0.5% zinc salt and 0.005-0.05% antimicrobial material for the prevention of bad breath. In this patent, the zinc salt is zinc acetate and the antimicrobial material is bis-guanides, Cetyl pyridinium chloride or benzalkonium chloride. Zinc salts and antibacterial substances have been studied extensively and applied to oral products and have been widely used commercially.

Japanese Patent No. 2,806,031 discloses a method of improving the oral retention of triclosan by combining alginic acid having a specific molecular weight with triclosan, a non-ionic antibacterial agent. However, the residual mechanism of triclosan and alginic acid is not explained precisely, and due to the anionic charge of alginic acid, the adhesion to the mucosa and the teeth is not so high, so the actual residual effect of triclosan is not expected.

It is an object of the present invention to provide an oral composition for restraining bad breath, which exhibits an effective oral odor inhibiting effect by enhancing oral cavity persistence of zinc ions.

In order to achieve the object of the present invention, (b) at least one of alginic acid and alginate; (c) at least one of sodium citrate and potassium citrate; And (d) water; wherein 35 to 50% by weight of the water and at least one of the alginic acid and the alginate are contained in an amount of 0.8 to 2% by weight; (a) ) A weight ratio of at least one of sodium citrate and potassium citrate is 1: 1.5 to 1: 2, and a sum of the sodium citrate and potassium citrate is 1 wt% or less.

According to the present invention, the solubility of zinc citrate is improved by sodium citrate or potassium citrate, the zinc ion is crosslinked by alginic acid or alginate to increase the oral retention, and the bad breath suppressing effect can be enhanced.

Hereinafter, the present invention will be described in more detail.

The oral composition for restraining bad breath according to one embodiment of the present invention comprises (a) zinc citrate; (b) at least one of alginic acid and alginate; (c) at least one of sodium citrate and potassium citrate; And (d) water; wherein 35 to 50% by weight of the water and at least one of the alginic acid and the alginate are contained in an amount of 0.8 to 2% by weight; (a) ) The weight ratio of at least one of sodium citrate and potassium citrate is 1: 1.5 to 1: 2, and the sum of the sodium citrate and potassium citrate is 1 wt% or less.

Zinc citrate, which has zinc sulfate, zinc lactate, zinc chloride, zinc acetate, zinc citrate and the like but has the least metal taste unique to zinc ion, is applied to the present invention. The zinc citrate used in the composition of the present invention is used in an amount of 0.1 to 2% by weight of the composition. Below these concentration ranges, the effect of suppressing bad breath is weak. In addition, The metal taste of the composition tends to increase and the feeling of use of the composition deteriorates.

The total content of the alginic acid or alginate salt capable of ionic crosslinking with the zinc ion used in the present invention is used in an amount of 0.8 to 2% by weight in the composition. When the concentration is below this range, the effect of zinc ion on the oral cavity residue is insignificant Beyond that, the cost is higher than that of the effect raising factor and deviates from the typical properties of the general dentifrice composition.

Also, the dentifrice composition of the present invention comprises 35 wt% to 50 wt% water based on the total weight of the composition. Below this, the alginic acid or alginate will not fully hydrate in the toothpaste formulation and will not aggregate and crosslink with the zinc ion, and will not have the homogeneity of the formulations to have as a finished product. If it is contained in an amount of more than 50% by weight, the formation of the beads becomes insufficient and the dispersibility and phase stability of the whole composition including zinc citrate, which is a bad breath inhibitory substance, becomes poor.

According to one embodiment of the present invention, the weight ratio of zinc citrate to at least one of sodium citrate and potassium citrate for improving the solubility of zinc citrate is preferably 1: 1.5 to 1: 2.

When the weight ratio is less than 1: 1.5, the effect of improving the solubility of zinc citrate is insignificant. When the weight ratio is more than 1: 2, the solubility improvement effect is not greatly different.

According to an embodiment of the present invention, the sum of the weight of at least one of sodium citrate and potassium citrate is preferably 1% by weight or less. When the content is more than 1% by weight, the acidity is increased by sodium citrate or potassium citrate, which is used as an acidifier, and an unpleasant acid taste can be felt when used.

The oral composition according to the present invention is prepared by using the appropriate ingredients according to the kind of the product. For example, in the case of a dentifrice composition, it is usually prepared by blending it with ingredients contained in toothpaste. Such ingredients include abrasives such as alumina, precipitated silica, calcium carbonate, calcium hydrogen phosphate, sodium bicarbonate and the like; Wetting agents such as sorbitol, glycerin, polyethylene glycol and the like, foaming agents such as sodium lauryl sulfate, sodium laurylsacosinate, cocamidopropyl betaine, alkylpolyglucoside and the like; Preservatives such as sweetening agents such as sodium saccharin, aspartame, acesulfame potassium, stevioside, etc .; preservatives such as methyl parahydroxybenzoate, propyl p-oxybenzoate and the like; Medicinal agents such as sodium fluoride, vitamins, cetylpyridinium chloride and the like; Spices; Pigment; pH adjusters and the like.

Hereinafter, the present invention will be described in more detail by way of non-limiting examples. Unless specifically defined in the following examples,% represents weight%.

Experimental Example  One: Sodium citrate  And Of potassium citrate  Depending on the content Zinc citrate  Solubility and sensory evaluation

Zinc citrate or sodium citrate or potassium citrate compositions as shown in Table 1 below were prepared and stirred for 30 minutes to evaluate the solubility of zinc citrate in the composition.

Also, 12 sensory evaluation subjects were divided into two groups according to the degree of bitter taste or unpleasant taste of each evaluation composition according to the degree of 5 points scale (5: very unpleasant, 4: unpleasant, 3: normal, 2: uncomfortable, 1: Respectively.

(Unit: wt%) Ingredients Evaluation example One 2 3 4 5 6 7 8 9 Zinc citrate 0.1 0.5 0.5 0.5 2 0.1 0.5 0.5 2 Sodium citrate 0.2 0.75 0.4 0.25 1.5 0.1 - 0.25 One Potassium citrate - - 0.4 0.75 1.5 - - 0.25 0.5 Purified water to 100 to 100 to 100 to 100 to 100 to 100 to 100 to 100 to 100 Solubility evaluation × × Sensory evaluation
(Bitter / unpleasant taste) 2.2 2.6 2.8 3.1 4.1 2.2 2.3 2.2 3.9

As a result of evaluation, the solubility of zinc citrate in the compositions of Evaluation Examples 1 to 5 was higher than those of Evaluation Examples 6 to 9, and the evaluation of the bitter taste and unpleasant taste was good when the sum of the contents of sodium citrate and potassium citrate was less than 1% by weight.

Experimental Example  2 : Polymer  Zinc ion transport and residual effect according to composition

As shown in Table 2, compositions containing zinc salts and polymers were applied to Vitro-Skin® (IMS Technologies) to compare the delivery and residual effects of zinc ions.

1) Experimental process

(1) Cut Vitro-skin® to a certain size of square.

(2) Remove the silicon film on the surface by repeating the process of immersing the square Vitro-skin® in hexane and drying.

(3) Immerse square Vitro-skin® in artificial saliva.

(4) Remove artificial saliva, and immerse Vitro-skin® in 25% diluted composition of Table 2 and stir.

(5) Repeat the washing procedure by immersing Vitro-skin® in purified water and stirring.

(6) Immerse Vitro-skin® in artificial saliva.

(7) Analyze zinc concentration in artificial saliva.

(Unit: wt%) Ingredients Evaluation example 10 11 12 13 14 15 16 17 18 19 20 Zinc citrate 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 0.5 Sodium citrate 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 0.8 glycerin 4 4 4 4 4 4 4 4 4 4 4 Sodium alginate 0.5 0.8 1.5 2.0 - - 3.0 - - - - Calcium alginate - - - - 2.0 - - - - - - Potassium alginate - - - - - 2.0 - - - - - SCMC - - - - - - - 0.8 - - - Carrageenan - - - - - - - - 0.8 - - Poloxamer 407 - - - - - - - - - 0.8 - Xanthan gum - - - - - - - - - - 0.8 Purified water to 100 to 100 to 100 to 100 to 100 to 100 to 100 to 100 to 100 to 100 to 100

* SCMC = Sodium carboxymethylcellulose

The artificial saliva used in the experiment is shown in Table 3 below and the concentration of zinc in the artificial saliva was quantified by using a zinc concentration analyzing kit (model: WAK-Zn (D), KUORITSU (Japan)) and ultraviolet-visible light absorbance .

Ingredients content Potassium chloride 624.6 mg Sodium chloride 866.6 mg Potassium monophosphate 33.8 mg Magnesium chloride 59.6 mg Calcium chloride hexahydrate 166.6 mg Purified water to 1,000 ml

2) Experimental results

The experimental results of Experimental Example 2 are shown in Table 4.

division Zinc concentration  ( ppm )



Evaluation example





10 0.19 11 0.52 12 0.68 13 0.76 14 0.72 15 0.71 16 0.74 17 0.04 18 0.17 19 0.18 20 0.18

The experimental results showed that the concentrations of zinc ions contained in artificial saliva of the evaluation examples 10 to 16 containing alginic acid or alginate were higher than those of the evaluation examples 17 to 20 in which alginic acid or alginate was not contained. In the evaluation examples 11 to 16 in which the content of sodium alginate was 0.8 to 2% by weight in the evaluation examples 10 to 16, the zinc ion concentration was drastically higher than that of the evaluation example 10 in which the content of the alginate was less than 0.8% by weight, , The concentration of zinc ions remained as compared with the sodium alginate content did not significantly increase,

Experimental Example  3: In the dentifrice composition Purified water  Depending on the content Of sodium alginate  Sign Language

To evaluate the degree of hydration of sodium alginate according to the purified water content in the dentifrice composition, the composition was prepared with the composition shown in Table 5. The homogeneity of each composition was compared with the naked eye immediately after preparation, and the degree of hydration of sodium alginate in the dentifrice composition was estimated based on the results. The evaluation results are shown in the following table.

(Unit: wt%) division Ingredients Example  One Example  2 Comparative Example  One Comparative Example  2 Viscosity modifier Silicon dioxide 20 20 20 20 Wetting agent Sorbitol 40 35 50 45 Foaming agent Alkylpolyglucoside 1.7 1.7 1.7 1.7 Binder Sodium alginate 0.8 0.8 0.8 0.8 Sweetener Sodium saccharin 0.2 0.2 0.2 0.2 Active ingredient Zinc citrate 0.5 0.5 0.5 0.5 pH adjusting agent Sodium citrate 0.8 0.8 0.8 0.8 Spices Combination fragrance One One One One solvent Purified water 35 40 25 30 Degree of hydration of sodium alginate × ×

* Complete hydration: not fully hydrated: ×

As shown in Table 5, when Examples 1 and 2 and Comparative Examples 1 and 2 were compared, when the content of purified water in the composition was 35% by weight or more, sodium alginate was completely hydrated and became a homogeneous composition.

Experimental Example 4 : Clinical Comparative Experiment on Bad Breath Suppression Effect of the Present Invention

1) Preparation of dentifrice composition

The composition of Table 6 was mixed to prepare a dentifrice composition.

(Unit: wt%) division Ingredients Example  3 Comparative Example  3 Viscosity modifier Silicon dioxide 20 20 Wetting agent Sorbitol 30 30 Foaming agent Alkylpolyglucoside 2 2 Binder Carboxymethylcellulose sodium - 1.2 Binder Sodium alginate One - Sweetener Sodium saccharin 0.2 0.2 Spices Combination fragrance 0.8 0.8 Active ingredient Zinc citrate 0.5 0.5 Active ingredient Cetylpyridinium chloride 0.05 0.05 pH adjusting agent Sodium citrate 0.8 0.8 antiseptic Paraoxybenzoic acid ester 0.1 0.1 solvent Purified water to 100 to 100

In the present invention, three men and three women who feel bad breath feeling were selected as experimental subjects. Example 3 Toothpaste was evaluated first and toothpaste used for one week was used and then evaluated with Comparative Example 3 toothpaste. The evaluation method was as follows. Before toothbrushing, toothbrushing was done with toothpaste. Immediately after waking up the next morning, oral hygrometer was measured with Oral Chroma (Model: CHM-2, FIS Co., Japan). How to use Oral Chroma is as follows. Before the measurement, the breathing syringe is placed on the lips and breathing is performed for 30 seconds to 60 seconds. Then, oral cavity breath is taken and injected into the instrument. The results are shown in Table 7 below.

2) Comparison of the effect of inhibiting bad breath

(Unit: ppb) Subject Example 3 Comparative Example 3 H ₂ S CH ₃ SH (CH _{3) 2} S H ₂ S CH ₃ SH (CH _{3) 2} S One 52 6 9 182 10 10 2 123 49 11 535 53 65 3 53 5 8 179 60 19

In the case of using the toothpaste of Example 3 and the toothpaste of Comparative Example 3, the oral odor of Oral Chroma was measured. Therefore, toothpastes which used alginic acid and alginate together with zinc salts and zinc ions, which are capable of ionic crosslinking, are more effective in inhibiting halitosis than other toothpastes.

Claims (3)

(a) zinc citrate;
(b) at least one of alginic acid and alginate;
(c) at least one of sodium citrate and potassium citrate; And
(d) water;
35% to 50% by weight of the water,
Wherein at least one of the alginic acid and alginate is contained in an amount of 0.8 to 2% by weight,
Wherein the weight ratio of (a) zinc citrate to (c) at least one of the sodium citrate and potassium citrate is from 1: 1.5 to 1: 2,
Wherein the total sum of sodium citrate and potassium citrate is 1 wt% or less. The dentifrice composition according to claim 1, wherein the alginate is at least one salt selected from the group consisting of sodium alginate, potassium alginate, calcium alginate, propylene glycol alginate and triethanolamine alginate. The dentifrice composition according to claim 1, wherein the zinc citrate is contained in an amount of 0.1 to 2% by weight.