KR102084602B1 - Foaming tablet for cleaning oral cavity having improved foamability and stability - Google Patents

Abstract

The present invention relates to a foaming tablet for cleaning an oral cavity having improved foamability and stability. More specifically, the present invention relates to a foaming tablet for cleaning an oral cavity having improved foamability and stability, wherein the foaming tablet is prepared by using, as a base material, a mixed material in which maltodextrin and beta-cyclodextrin are coated on microcrystalline cellulose; adding crospovidone as a disintegrant of the mixed material to improve foamability; and adding sodium lauryl sulfate, an anionic surfactant, to the composition to generate bubbles with saliva and water and thus improve cleaning power in the oral cavity.

Description

Foaming tablet for cleaning oral cavity having improved foamability and stability

The present invention relates to foam tablets for oral cleaning with improved foamability and stability. More specifically, a mixed substrate in which maltodextrin and betacyclodextrin are coated on microcrystalline cellulose as a base material to improve the foamability and stability of the foam for oral cleaning tablets, and crospovidone as a disintegrant of the mixed substrate to improve foamability. The present invention relates to an effervescent tablet having improved foamability and stability, which is prepared by adding sodium lauryl sulfate, an anionic surfactant, into a composition to add bubbles and to generate bubbles together with saliva and water to improve intraoral cleaning ability.

Toothpaste can be used for whitening teeth and removing plaque due to its excellent polishing, but additional tools and time such as water and toothbrush are needed for the oral cleansing effect and the removal of plaque in the mouth. On the other hand, liquid oral cleansers with additional tools removed have a disadvantage in that they are inconvenient to carry, as the containers of such cups need to be accompanied by a large volume of the materials.

In order to improve the drawbacks of toothpaste and liquid mouthwashes, the present inventors have selected from the group consisting of crystalline cellulose, powdered cellulose and dietary fiber in Korean Patent Registration No. 10-294515 'Foaming tablets for oral cleaning and preparation method thereof'. 30 to 70% by weight of the substrate, which is one or more mixtures, 10 to 50% by weight of the blowing agent which is one or two or more mixtures selected from the group consisting of sodium bicarbonate, ammonium bicarbonate, potassium hydrogen carbonate and iron carbonate, and silicon dioxide Abrasive, one or two or more selected from the group consisting of calcium monohydrogen phosphate, calcium carbonate, aluminum hydroxide, precipitated silica, hydrous silicate, hydrous alumina, silica gel, insoluble sodium phosphate, zirconium silicate, sodium bicarbonate, and aluminosilicate 5-20% by weight, citric acid, tartaric acid, malic acid, gluconic acid, ascorbic acid, succinic acid and propionic acid 3-20% by weight of one or two or more mixtures selected from the group consisting of organic acids and 0.05-1.0% by weight of sodium fluoride or fluorine compounds and a suitable amount of flavors, sweeteners and pigments, followed by tableting Oral cleansing foam tablets and a method for preparing the same "have been disclosed.

The foam tablets for oral cleaning disclosed in the patent document showed superior sterilizing activity against periodontal pathogenic microorganisms, removing bad breath in the oral cavity, and taste and flavor than the general toothpaste on the gel or liquid oral cleaning solution. There was a problem in the commercialization because the foamability and stability of the washing foamable tablet is not sufficient.

Therefore, the present inventors are using a mixed substrate coated with maltodextrin and betacyclodextrin on a microcrystalline cellulose core material as a foaming substrate while trying to improve the foamability and stability of a conventional oral cleaning foamable tablet, and a mixed substrate to improve foamability. By adding crospovidone as a disintegrating agent and adding bubbles with saliva and water to improve the oral cleansing ability, an anionic surfactant sodium lauryl sulfate was added to the composition to develop an effervescent and stable foam for oral cleaning. The present invention has been completed.

The problem to be solved by the present invention is to apply a mixed substrate coated with maltodextrin and betacyclodextrin to the microcrystalline cellulose core material as a foamed substrate, adding crospovidone as a disintegrant of the mixed substrate in order to improve the foamability, saliva, water In addition, it is intended to develop an oral cleaning foam having improved foamability and stability by adding an anionic surfactant sodium lauryl sulfate in the composition in order to create bubbles to improve the oral cleaning ability.

It is an object of the present invention to provide a composition comprising i) 20 to 35% by weight of a foamed substrate; Ii) 20 to 25% by weight sodium hydrogen carbonate blowing agent; Viii) at least one abrasive selected from 5 to 15% by weight of hard silicic anhydride or anhydrous calcium hydrogen phosphate; Iii) 5 to 10 weight percent citric acid; Iii) 0.05-0.5% by weight sodium lauryl sulfate foaming agent; Viii) 0.1-1.0 wt% crospovidone disintegrant; And iii) 0.05 to 0.5% by weight of a fluorine-based tooth decay preventive agent, comprising: a foamed tablet for oral cleaning with improved foamability and stability, wherein the foam base is a mixed foam in which maltodextrin and betacyclodextrin are coated on a microcrystalline cellulose core material It is a substrate, and in order to improve the foamability and stability of the foamed substrate to provide a foamed tablet for oral cleaning with improved foamability and stability by reducing the content of the foamed substrate in the foamed tablet to 35% by weight or less.

At this time, the foamed substrate is characterized in that it is prepared by coating 8 to 14% by weight of maltodextrin and 3 to 6% by weight of betacyclodextrin on 7 to 12% by weight of the microcrystalline cellulose core material.

In addition, the viscosity of the 1.0 wt% aqueous solution of the maltodextrin and betacyclodextrin-coated microcrystalline cellulose of the foamed substrate is characterized in that 20 to 70 mPa · s as measured at 20 rpm / min rotational speed with a Brookfield rotary viscometer.

Meanwhile, the citric acid and sodium bicarbonate blowing agent foam carbon dioxide gas through an acid base reaction, and sodium lauryl sulfate, an anionic surfactant, creates bubbles together with saliva and water to improve cleaning ability in the oral cavity, and the crospovidone disintegrant is foamed. It is characterized by promoting disintegration of the substrate to improve foamability and stability.

On the other hand, foaming tablets for oral cleaning of the present invention (a) magnesium stearate lubricant; (b) D-mannitol foam enhancer; (c) at least one flavor selected from orange, strawberry, grape, peppermint oil, spearmint oil, menthol, carbon, anerol, eugenol, wintergreen, sage or eucalypto oil; (d) at least one sweetener selected from lactose, maltose, lactitol, sodium saccharin, aspartame, stevioside or licoriceic acid; Or (e) at least one deodorant selected from sage, rosemary, green tea, persimmon extract or shanpinion extract; It further comprises at least one additive selected from.

The effect of the present invention is to apply a mixed substrate coated with maltodextrin and betacyclodextrin to the microcrystalline cellulose core material as a foamed substrate, and to add foam povidone as a disintegrant of the mixed substrate in order to improve the foamability and bubbles with saliva, water Sodium lauryl sulfate, an anionic surfactant, is added to the composition in order to improve the oral cleansing ability, thereby providing effervescent tablets having improved foamability and stability.

The present invention comprises: i) 20 to 35% by weight of the foam substrate; Ii) 20 to 25% by weight sodium hydrogen carbonate blowing agent; Viii) at least one abrasive selected from 5 to 15% by weight of hard silicic anhydride or anhydrous calcium hydrogen phosphate; Iii) 5 to 10 weight percent citric acid; Iii) 0.05-0.5% by weight sodium lauryl sulfate foaming agent; Viii) 0.1-1.0 wt% crospovidone disintegrant; And iii) 0.05 to 0.5% by weight of a fluorine-based tooth decay preventive agent, comprising: a foamed tablet for oral cleaning with improved foamability and stability, wherein the foam base is a mixed foam in which maltodextrin and betacyclodextrin are coated on a microcrystalline cellulose core material It is a substrate, and relates to a foaming tablet for oral cleaning with improved foamability and stability by reducing the content of the foamed substrate in the foamed tablet to 35% by weight or less in order to improve the foamability and stability of the foamed substrate.

On the other hand, foaming tablets for oral cleaning of the present invention (a) magnesium stearate lubricant; (b) D-mannitol foam enhancer; (c) at least one flavor selected from orange, strawberry, grape, peppermint oil, spearmint oil, menthol, carbon, anerol, eugenol, wintergreen, sage or eucalypto oil; (d) at least one sweetener selected from lactose, maltose, lactitol, sodium saccharin, aspartame, stevioside or licoriceic acid; Or (e) at least one deodorant selected from sage, rosemary, green tea, persimmon extract or shanpinion extract; It further comprises at least one additive selected from.

Meanwhile, the foaming tablet for oral cleaning having improved foamability and stability according to the present invention contains 0.05 to 0.5% by weight of an anionic surfactant sodium lauryl sulfate foaming agent in order to generate bubbles together with saliva and water to improve the oral cleaning power, and foamability of the mixed substrate. 0.1 to 1.0% by weight of crospovidone disintegrant to improve.

Hereinafter will be described in more detail with respect to the foam substrate for oral cleaning used in the present invention.

The foam base for oral cleaning used in the present invention uses 20 to 35% by weight relative to the total weight of the foam for oral cleaning. It is preferably prepared by coating 8-14% by weight of maltodextrin and 3-6% by weight of betacyclodextrin on 7-12% by weight of the microcrystalline cellulose core material.

In addition, the average particle size of maltodextrin and betacyclodextrin coated microcrystalline cellulose is 1-50 μm in water dispersion and preferably 3-20 μm.

In addition, the microcrystalline cellulose used at this time has a low affinity with water, but is dispersed and dissolved in colloidal form in water by coating the surface of the microcrystalline cellulose with water-soluble maltodextrin and betacyclodextrin.

In addition, the maltodextrin and betacyclodextrin-coated microcrystalline cellulose is required to have a suitable physical properties of the viscosity, the preferred viscosity of the 1.0 wt% aqueous solution of maltodextrin and betacyclodextrin-coated microcrystalline cellulose at 20 ℃ 20 rpm to Brookfield rotary viscometer It is 20 to 70 mPa · s when measured at a rotational speed per minute.

Maltodextrin, which is used as a coating material for microcrystalline cellulose, is a white fine powder, and the water content is in the range of 4.0 to 8.0%, and the dextrose equivalent weight (DE) is preferably in the range of 12.0 to 20.0. In addition, maltodextrin has low hygroscopicity due to low water content and disperses well when dissolved.

In addition, betacyclodextrin, which is used as a coating material for microcrystalline cellulose, is known to form a clathrate complex with hydrophobic molecules and improves the solubility of each component in the composition of the present invention to improve the foamability and stability of the foam tablet for oral cleaning. Let's do it.

Meanwhile, maltodextrin and betacyclodextrin coated microcrystalline cellulose of the present invention may similarly use a commercially available microcrystalline cellulose having a surface treatment. For example, surface-treated microcrystalline cellulose of Ceolus RC series or SC series of Asahi Kasei Co., Ltd., Japan may be used.

Although the blowing agent according to the present invention can be used to generate carbon dioxide by disintegrating in a weakly acidic aqueous solution, it is preferable to use sodium bicarbonate as the blowing agent. The content of the preferred blowing agent is about 20 to 25% by weight based on the total weight of the foam tablet.

In addition, citric acid, an organic acid according to the present invention, forms an acidic aqueous solution with water or saliva to decompose carbonates such as sodium bicarbonate used as a blowing agent to generate carbon dioxide.

The content of the preferred organic acid is about 5 to 10% by weight based on the total weight of the foamed tablet. Organic acids may also be added in the form of anhydrides to reduce the water content.

Foamed tablet for oral cleaning of the present invention comprises an abrasive selected from 5 to 15% by weight of hard silicic anhydride or calcium hydrogen phosphate.

On the other hand, it is also possible to use calcium silicate as an abrasive. Calcium silicate is a substance having the formula CaSiO ₃ and can be classified into ortho-calcium silicate, meta-calcium silicate, alpha-calcium silicate, triclinic-calcium silicate and the like according to the crystal form, and amorphous calcium silicate may also be used.

The hard silicic anhydride that can be used in the present invention preferably has a surface area of 180 to 200 m ² / g and a density of 1.8 to 2.4 g / cc.

In addition, the abrasive according to the present invention is characterized by removing the plaque or food debris by grinding the enamel of the tooth.

Meanwhile, the foaming tablet for oral cleaning having improved foamability and stability according to the present invention contains 0.05 to 0.5% by weight of an anionic surfactant sodium lauryl sulfate foaming agent in order to generate bubbles together with saliva and water to improve the oral cleaning power, and foamability of the mixed substrate. 0.1 to 1.0% by weight of crospovidone disintegrant to improve.

In addition, foam tablets for oral cleaning improved in the foamability and stability of the present invention contains a fluorine-based caries preventive agent of 0.05 to 0.5% by weight. Fluorine-based tooth decay preventive uses a compound containing fluorine ions for the purpose of preventing tooth decay. As the fluorine-based caries preventive agent, at least one selected from sodium fluoride, sodium monofluorophosphate, tin fluoride, and amine fluoride may be used.

The preferred content of fluorine ions in the fluorine-based caries preventer is in the range from 800 to 1600 ppm.

In addition, foaming tablets for oral cleaning of the present invention (a) magnesium stearate lubricant; (b) D-mannitol foam enhancer; (c) at least one flavor selected from orange, strawberry, grape, peppermint oil, spearmint oil, menthol, carbon, anerol, eugenol, wintergreen, sage or eucalypto oil; (d) at least one sweetener selected from lactose, maltose, lactitol, sodium saccharin, aspartame, stevioside or licoriceic acid; Or (e) at least one deodorant selected from sage, rosemary, green tea, persimmon extract or shanpinion extract; It may further comprise one or more additives selected from.

The magnesium stearate glidant used in the present invention serves to prevent foreign matter from being inserted into the punch of the tableting machine during the tableting process during tablet manufacture. The amount of the lubricant is preferably in the range of 0.5 to 1.5% by weight based on the total weight of the blowing agent.

The present invention may add at least one flavor selected from orange flavor, strawberry flavor, grape flavor, peppermint oil, spearmint oil, menthol, carbon, anerol, eugenol, wintergreen, sage or eucalypto oil. The content of the paint is preferably in the range of 1.5 to 3.0% by weight based on the total weight of the blowing agent.

The present invention may add one or more sweeteners selected from lactose, maltose, lactitol, sodium saccharin, aspartame, stevioside or licoriceic acid. The sweetener content is preferably in the range of 0.8 to 1.5% by weight based on the total weight of the blowing agent.

The present invention may add at least one bad breath remover selected from sage, rosemary, green tea, persimmon extract or shanpinion extract. The content of the bad breath remover is preferably in the range of 0.1 to 0.5% by weight based on the total weight of the blowing agent.

Hereinafter, the present invention will be described in more detail with reference to Preparation Examples, Preparation Examples and Examples.

Preparation Example Preparation of Foamed Tablet for Oral Washing of the Present Invention

(Step 1) Preparation of Mixed Substrate

A mixed substrate was prepared by dispersing maltodextrin and betacyclodextrin in a coating machine by suction mixing method using 80 mg of microcrystalline cellulose as a core material and 110 mg of maltodextrin and 45 mg of betacyclodextrin as a coating material. 235 mg is prepared.

(Step 2) Preparation of the Foaming Agent Composition

On the 235 mg mixed substrate prepared in step 1, 230 mg of sodium bicarbonate blowing agent, 60 mg of hard silicic anhydride and 30 mg of anhydrous calcium hydrogen phosphate abrasive, 70 mg of citric acid, 1 mg of sodium lauryl sulfate, 8 mg An appropriate amount of sweetener, flavoring agent, and lubricant is added to the crospovidone disintegrant in to prepare a foaming agent composition having a total weight of 1000 mg.

(Step 3) Preparation of the foam tablet for oral cleaning

The blowing agent composition prepared in step 2 is mixed, stipulated, and compressed to prepare a foam for oral cleaning.

Preparation Example 1 Preparation of Foam for Oral Washing (Microcrystalline Cellulose Monocomponent Foam Base)

(Step 1) Preparation of Substrate

235 mg of microcrystalline cellulose is prepared as foam substrate.

(Step 2) Preparation of the Foaming Agent Composition

On the 235 mg microcrystalline cellulose substrate prepared in step 1, 230 mg of sodium bicarbonate blowing agent, 60 mg of hard silicic anhydride and 30 mg of anhydrous calcium hydrogen phosphate, 70 mg of citric acid, 1 mg of sodium lauryl sulfate, An appropriate amount of sweetener, fragrance, glidant is added to 8 mg crospovidone disintegrant to prepare a total weight of 1000 mg blowing agent composition.

(Step 3) Preparation of the foam tablet for oral cleaning

The blowing agent composition prepared in step 2 is mixed, stipulated, and compressed to prepare a foam for oral cleaning.

Preparation Example 2 Preparation of Foam for Oral Washing (No Sodium Lauryl Sulfate and Crospovidone Added)

(Step 1) Preparation of Mixed Substrate

A mixed substrate was prepared by dispersing maltodextrin and betacyclodextrin in a coating machine by suction mixing method using 80 mg of microcrystalline cellulose as a core material and 110 mg of maltodextrin and 45 mg of betacyclodextrin as a coating material. 235 mg is prepared.

(Step 2) Preparation of the Foaming Agent Composition

235 mg of the mixed substrate prepared in step 1 was prepared with 230 mg of sodium bicarbonate blowing agent, 60 mg of hard silicic anhydride and 30 mg of anhydrous calcium hydrogen phosphate, 79 mg of citric acid, and an appropriate amount of sweetener, flavoring, glidant. Add to prepare a blowing agent composition with a total weight of 1000 mg.

(Step 3) Preparation of the foam tablet for oral cleaning

The blowing agent composition prepared in step 2 is mixed, stipulated, and compressed to prepare a foam for oral cleaning.

Example 1 Foamability Test

Three kinds of the oral cleansing foam composition prepared in step 2 in the preparation example 1 and the oral cleansing foam composition prepared in Comparative Example 1 1g, 1 g of the oral cleansing foam composition prepared in Comparative Example 2 Samples were used. 1 g of each sample is placed in 10 ml of artificial saliva (50 mM KCl, 1 mM KH ₂ PO 4, 1 mM CaCl ₂ , 0.1 mM MgCl ₂ ), and the mixture of the sample and the artificial saliva is foamed while stirring at 200 rpm. The elution of the foamed sample in artificial saliva was measured for a minute. The results are shown in Table 1.

time Dissolution rate (%) Preparation Example Comparative Example 1 Comparative Example 2 15 seconds 6 5 7 30 seconds 20 21 17 1 minute 32 33 28 3 minutes 52 42 39 5 minutes 85 68 71 10 minutes 99 88 91

As shown in Table 1, the foaming agent composition for oral cleansing prepared in the preparation example of the present invention exhibited a higher foaming dissolution rate than the foaming agent compositions prepared in Comparative Examples 1 and 2 when foamed and eluted in saliva for at least 3 minutes. This means that the maltodextrin and betacyclodextrin-coated microcrystalline cellulose mixed substrate of the present invention is foamed and eluted higher than the foaming agent composition prepared in Comparative Examples 1 and 2 after a predetermined period of 3 minutes or more in saliva.

However, when the foam dissolution was within 3 minutes, there was no significant difference in the foam dissolution rate between the foaming agent composition for oral cleaning of the present invention and the foaming agent compositions prepared in Comparative Examples 1 and 2.

Example 2 Texture and Foaming Stability Test

Foaming of the foamed tablet according to texture and oral foaming degree using a total of 300 foamed tablets, including 100 tablets for oral cleansing tablets prepared in Examples and 100 tablets for oral cleansing prepared in Comparative Examples 1 and 2, respectively. Stability was tested. Tissues and foaming stability of the foam tablets for oral lavage were measured in a cross test of 20 panelists. The results are shown in Table 2.

(Judgement criteria of texture and foam stability)

Rating 1: Very poor rejection due to poor texture and foam stability

Rating 2: Rejection due to poor texture and foam stability

Rating 3: Normal texture and foam stability with no rejection

Rating 4: Good texture and foam stability, no rejection

Rating 5: Very good texture and foam stability, no rejection

Preparation Example Comparative Example 1 Comparative Example 2 Texture and Foam Stability Rating 4.2 ± 0.4 3.8 ± 0.5 3.6 ± 0.6

As shown in Table 2, the foam tablet for oral cleaning of the present invention was confirmed that the texture and foam stability was excellent. In particular, in the case of effervescent tablets for oral cleaning of the present invention, by using maltodextrin and beta cyclodextrin coated microcrystalline cellulose mixed substrate Comparative Preparation Example 1 without using a mixed substrate or Comparative Preparation without using sodium lauryl sulfate and crospovidone The texture and foaming stability of the foamed tablets of Example 2 are believed to be improved.

Example 3 Oral Washing Effect Test

The oral lavage effect was tested using a total of 150 effervescent tablets, including 50 tablets for oral cleansing prepared in the preparation examples and 50 tablets for oral cleansing prepared in Comparative Examples 1 and 2, respectively. The oral cleansing effect of the foam tablet for oral lavage was measured through a crossover test on 10 panelists. The results are shown in Table 3.

(Oral cleaning effect judgment standard)

Rating 1: Bad oral cleaning effect, very bad breath

Rating 2: Poor breath due to poor oral cleaning effect

Rating 3: Oral cleansing effect is moderate, bad breath is weak

Rating 4: No bad breath due to good oral cleaning effect

Rating 5: Very good oral cleansing effect with a mild fragrance

Preparation Example Comparative Example 1 Comparative Example 2 Mouthwash Effect Rating 4.3 ± 0.5 3.7 ± 0.6 3.4 ± 0.4

As shown in Table 3, in the case of the foam tablet for oral cleaning of the present invention was confirmed that the oral cleaning effect is excellent. In particular, in the case of effervescent tablets for oral cleaning of the present invention, by using a microcrystalline cellulose mixed substrate coated with maltodextrin and betacyclodextrin, not only facilitates dispersion of abrasives and organic acids in saliva, but also facilitates dispersion of flavors and sweeteners. It is believed that the oral cleaning effect is improved compared to the foaming tablets of Preparation Comparative Example 1 without using a base material or Preparation Comparative Example 2 without using sodium lauryl sulfate and crospovidone.

Claims (5)

Iii) 20 to 35% by weight of foamed substrate;
Ii) 20 to 25% by weight sodium hydrogen carbonate blowing agent;
Iii) at least one abrasive selected from 5 to 15% by weight of hard silicic anhydride or anhydrous calcium hydrogen phosphate;
Iii) 5 to 10 weight percent citric acid;
Iii) 0.05-0.5% by weight sodium lauryl sulfate foaming agent;
Viii) 0.1-1.0 wt% crospovidone disintegrant; And
Iii) 0.05 to 0.5% by weight of fluorine-based tooth decay preventive agents;
In the foam and oral cleaning foam improved stability including,
The foamed base material is a mixed foamed base material coated with maltodextrin and betacyclodextrin on a microcrystalline cellulose core material. Foam for oral cleaning with improved foamability and stability.
According to claim 1, wherein the foam base is foamed and characterized in that it is prepared by coating 8 to 14% by weight of maltodextrin and 3 to 6% by weight of betacyclodextrin to 7 to 12% by weight of the microcrystalline cellulose core material Foam for oral cleaning with improved stability.
The viscosity of the 1.0 wt% aqueous solution of maltodextrin and betacyclodextrin-coated microcrystalline cellulose, which are the foamed substrates, is 20 to 70 mPa · s when measured at a 20 rpm / min rotational speed with a Brookfield rotary viscometer. Effervescent tablet for oral cleaning.
The method of claim 1, wherein the citric acid and sodium bicarbonate blowing agent foams carbon dioxide gas through an acid base reaction, and sodium lauryl sulfate, an anionic surfactant, creates bubbles together with saliva and water to improve the oral cleaning power, and the cross Povidone disintegrant is a foam for oral cleaning, characterized in that to promote the disintegration of the foam base material to improve the foamability and stability.
The method according to any one of claims 1 to 4,
(a) magnesium stearate lubricant;
(b) D-mannitol foam enhancer;
(c) at least one flavor selected from orange, strawberry, grape, peppermint oil, spearmint oil, menthol, carbon, anerol, eugenol, wintergreen, sage or eucalypto oil;
(d) at least one sweetener selected from lactose, maltose, lactitol, sodium saccharin, aspartame, stevioside or licoriceic acid; or
(e) at least one deodorant selected from sage, rosemary, green tea, persimmon extract or shanpinion extract;
Foam tablet for oral cleaning, characterized in that it further comprises one or more additives selected from.