KR20090076446A - In-situ melting, gelling and effervescent composition for oral care with multi-layers - Google Patents

Abstract

An oral cleaning composition having multilayer is provided to maintain pH homeostasis of saliva, have excellent dental caries prevention effect and promote the secretion of saliva. A composition for oral cavity clean comprises a layer of porous plastic granule having a porous plastic granule ingredient, bonding agent, water permeable extending agent and gelation agent and a foaming layer. The composition is resolved and forms gel by saliva, water or chewing. The plastic granule having high porosity is produced even in the 500 kg/cm^2 pressure.

Description

Simultaneous Dissolution, Gelling, and Effervescent Oral Hygiene Composition of Multi-Layered Structure {IN-SITU MELTING, GELLING AND EFFERVESCENT COMPOSITION FOR ORAL CARE WITH MULTI-LAYERS}

The present invention relates to the simultaneous dissolution, gelling and foaming oral hygiene composition of a multi-layered structure, and specifically, comprising two or more layers of simultaneous dissolving and gelling of the foaming layer, and dissolving, gelling and foaming by saliva or chewing in the oral cavity. Is achieved at the same time quickly and relates to a tablet oral hygiene composition with improved feeling and effect.

Common types of oral hygiene can be classified into toothpaste, dentifrice, film and spray. The purpose of the use of these oral products includes aesthetics such as whitening of the mouth, prevention of tartar deposition, suppression of bad breath, and treatment and prevention of tooth decay and gum disease.

Meanwhile, the pharmaceutical industry is making fast dissolving tablets so that tablets such as medicines and health supplements can be easily taken. Toshihiro Shimizu et al . Chem . Pharm. Bull. 51 (10) (2003), pointing out that fast dissolving tablets offer great benefits for those who have difficulty swallowing tablet drugs, tablet manufacturing, lyophilization, spray-drying, Disintegrant addition, sublimation, and sugar-induced diluents are used.

For the preparation of fast dissolving tablets, techniques such as lyophilization, molding, and compression processes can be used.

First, lyophilization is a process of drying a solvent, such as a frozen drug solution or a frozen drug suspension containing an excipient. Tablets obtained by lyophilization are generally very light and readily dissolve because they have many voids and plastic structures. However, lyophilization has the disadvantage that the process is relatively expensive, and that the final dosage form is very fragile, easy and of low strength, making blister packaging impossible.

In the molding process, the material dissolved in water or ethanol is compressed into tablets in a wet state below the general tableting pressure and dried to obtain fast-soluble tablets. The main component of the molded tablet is generally water soluble. Molded tablets have many voids, which facilitate water penetration and promote dissolution. On the other hand, as disclosed in U.S. Patent No. 5,082,677 to Van Scoik et al., The molded tablet has a disadvantage in that the strength is so weak that problems occur in the distribution process. In addition, there is a problem that a more complex process than the conventional compression process.

Obtaining fast dissolving tablets using conventional tableting compressors is a very attractive method in terms of manufacturing cost and technology transfer. In the conventional compression process, fast-soluble tablets could not be obtained because the voids in the tablets were not an important factor but the purpose was to increase the tablet strength by compressing at high pressure. The processes performed to obtain many voids include granulation, the use of certain soluble materials, and methods of making a complete tablet and post-treatment, each of which is briefly described below.

First, in the granulation method, wet granules by fluidized bed described in US Pat. No. 6,249,938 to Bonadeo et al., Dry granules described in US Pat. No. 5,939,091 to Eoga et al., Spray drying described in US Pat. No. 6,207,199 to Allen et al. And the scintillation method described in US Pat. No. 6,048,541 to Fuisz et al. Are used to prepare fast dissolving tablets.

In certain diluent methods, it is important to select calcium insoluble salts, specific disintegration combinations, and specific sugar composition diluents. In US Pat. No. 6,596,311 to Dobetti et al., An insoluble inorganic composition is used as a major component of fast dissolving tablets. As a method by adjustment of a sugar or a sugar derivative, Chang, R.-K. Et al., " Pharmaceutical Development & Technology, 24 : 52-58, 2000" reported the use of sugars or sugar derivatives in the formulation of almost all fast-soluble tablets. Next, almost all fast-dissolving tablets in the method of using disintegrants use effervescent conjugate / bases or some combination of non-foamable disintegrants. Such non-foamable disintegrants include carboxymethyl cellulose, cross-polyvinylpyrrolidone, starch, modified starch, carboxymethylated starch, microcrystalline cellulose and the like.

Compression and post-treatment is a method of making weak tablets through various post-treatment processes such as sublimation, sintering, and humidity treatment after the tablets are manufactured at low pressure. In US Pat. No. 6,316,026 to Roser et al., Fast-soluble tablets are prepared using volatiles. Humidity control processes are used to increase the strength of tablets by converting some of the sugars from the amorphous state into the crystalline state to control the humidity during the drying and granulation process to form crystals. Lagoviyer et al., US Pat. No. 6,465,010 discloses a method of increasing the strength of a tablet while raising the temperature to high temperature and then cooling to room temperature.

Little research has been conducted on applying the above-described manufacturing technique of fast dissolving tablets to oral hygiene. In the conventional oral hygiene, there is an example of manufacturing a fast dissolving tablet using a foaming and disintegrating agent using a foamed tablet, but in this case, there was a problem that the conjugated acid used for foaming adversely affects the sensitivity of consumers. In terms of usability, improvements are urgently needed. Specifically, Douglas C.S. US Patent Publications 2004/0101494 A1 and 2004/0101493 A1, et al., Relate to chewable solid unit dosage forms and methods of delivering the active agent into the occlusal surface of a tooth, including tooth and interdental and molar teeth, which may occur during chewing. Remains on the occlusal surface of the drug delivery. However, this formulation can not only provide a good feeling to consumers after using it, but also has the disadvantage that it does not dissolve within a few seconds because the tablet is not fast-soluble, which improves the usability and ease of use. It is required.

Korean Patent Publication No. 10-2000-0038278 (published Jul. 5, 2000) discloses a foam tablet for oral cleaning and a method of manufacturing the same. Here, a foaming agent which is at least one mixture selected from the group consisting of sodium bicarbonate, ammonium bicarbonate, potassium hydrogen carbonate and iron carbonate on a substrate which is at least one mixture selected from the group consisting of crystalline cellulose and dietary fiber, and citric acid and tartaric acid. Including oral acid, gluconic acid, ascorbic acid, succinic acid and propionic acid, the organic acid containing at least one mixture selected from the group consisting of, abrasive tablets, caries preventives, etc. by mixing and tableting to prepare a foam for oral cleansing tablets. However, such an effervescent tablet has been pointed out as an emotional part, such as causing rejection or avoidance of use due to the taste of organic acids when applied directly to the oral cavity. Therefore, although the improvement of the sensitivity quality is calculated | required, it is considered that it is impossible to improve this in the case of foamed tablets basically.

In addition, in Korean Patent Registration Nos. 10-0731891 and 10-0731892, the porous plastic granules including the porous plastic granule material, the binder, the gelling agent, and the water penetrating extender, etc. are compressed to a pressure of 500 kg / cm 2 or less. Disclosed is a tablet-type oral hygiene composition which is prepared and is co-dissolved and gelled by saliva or water in the mouth, or by chewing. The present formulation is known to have a superior consumer feel compared to effervescent tablets, but has a disadvantage in that its dissolution and gelation rate is slower than effervescent tablets.

An object of the present invention is a tablet-type oral hygiene composition which improves the feeling and effect by dissolving, gelling and foaming by saliva or chewing at the same time by including two or more layers simultaneously dissolving and gelling the foam layer Is to provide.

According to the present invention, a multi-layered tablet oral hygiene composition according to the present invention comprises a porous plastic granule material, a layer comprising porous plastic granules having a binder, a water penetration expander and a gelling agent as essential components, and a foamed acid and At least one foam layer each comprising a carbon dioxide generator as an essential component, and characterized in that it is dissolved and gelled simultaneously with foaming by saliva or water in the oral cavity.

In addition, the solid oral hygiene composition according to the present invention comprises a porous plastic granule material, a binder comprising a porous plastic granules having a binder, a water penetration enhancer and a gelling agent as essential components, and a foamed acid and a carbon dioxide generator as essential components. It comprises at least one foam layer each, characterized in that it is dissolved and gelled simultaneously with foaming by chewing.

Oral hygiene composition of the present invention is a tablet-type oral hygiene consisting of a layer comprising a composition capable of simultaneous dissolving and gelling, and a foaming layer containing a component that can give a feeling of foaming, dissolution, gelation and foaming is simultaneously performed in the oral cavity This aims to differentiate usability and effectiveness.

Tablets having a multilayer structure are often used for enhancing the aesthetics of tablets and the like. Effervescent tablets are tablets having the characteristic of effervescent acid (organic acids such as citric acid and ascorbic acid) and carbon dioxide generating sources (carbonates such as sodium bicarbonate, sodium carbonate, calcium carbonate and magnesium carbonate) mixed and foaming upon contact with moisture. In addition, simultaneous dissolution and gelling oral hygiene are mainly tablet-type oral hygiene in which dissolution and gelation are simultaneously performed by intraoral saliva or chewing.

In the oral care composition according to the present invention, by incorporating a foamable layer and a layer that can be simultaneously dissolved and gelated into one tablet, the effect of promoting gelation is enhanced along with the refreshing feeling caused by foaming. In other words, with the oral hygiene function by the simultaneous dissolving and gelling layer, the carbonate used for foaming can control the pH in the oral cavity to prevent tooth decay caused by the metabolism of organic acids, and salivary secretion due to foaming and taste. Is promoted to increase the intraoral self-cleaning effect, and at the same time there is an effect to increase the dissolution and gelation rate at the same time as the bad breath removal effect.

Hereinafter, the oral care composition of the multilayer structure according to the present invention will be described in detail.

Toothpaste is a representative oral hygiene product, buried in a toothbrush and inserted into the oral cavity to implement oral hygiene through brushing. Oral hygiene composition according to the present invention has all the functions of the existing oral hygiene cleaning, caries prevention, gum disease prevention, through the chewing in the mouth, or quickly dissolved in water or saliva on the toothbrush or mouth, Gelling and foaming make it easy to brush and gargle.

What is necessary for rapid gelling in tablet-type oral hygiene compositions that are co-dissolved and gelled is a high porosity for ease of water penetration, in which water must penetrate into the center of the tablet within seconds and have a strength above the right to facilitate handling. . The oral hygiene composition of the multi-layered structure according to the present invention comprises a solvent composed of a high pore plastic granule material, a water / saliva penetration enhancer, a binder, a gelling agent, an anti-adhesion agent, a moisturizer, an abrasive, a foaming agent, a flavoring agent, a sweetening agent, a medicament agent, and the like. Along with the gelable layer, a foamed layer containing the acid and carbon dioxide generator as essential components is included.

In general, the fast dissolving tablets used in pharmaceuticals are not intended for dissolution and gelation, as in toothpaste, because they are designed to speed up the absorption of the drug in the oral cavity. In the present invention, the composition has a gel texture similar to that of a general toothpaste.

In the present invention, in order to obtain rapid dissolution and gelling properties, high-strength tablets are prepared through the preparation of porous plastic granules in the granulation process, the induction of rapid gelation using high hydrophilic polymers, the use of water penetration extenders, and low pressure tableting in the case of tablets. Attempted to make. In addition, in order to secure the basic function of the toothpaste, such as abrasives, foaming agents, sweeteners and fragrances, such as to give a good feeling to the consumer.

The manufacture of porous plastic granules uses materials that can dissolve quickly or come into contact with water or saliva, or test materials that can be dispersed. At this time, the test materials used should be selected as drugs or foods that can be used harmlessly to the human body. When tableting the plastic granules using a tableting machine, the plastic deformation of the granules is dramatically increased by the contact between the particles.

When the polymer is used as the porous plastic material in the composition of the present invention, the polymer should be free from interference with water due to water film formation due to an increase in viscosity that may occur on the surface of the tablet during dissolution in water. A method of making this type of tablet is to use a proportion of water / saliva penetration enhancer. It is the water penetration extender that serves to prevent the viscous water ingress from the tablet's surface. Generally, the water / saliva penetration extender and the porous plastic granules are different materials, but the plastic granules and the water / saliva penetration extender may be used in common.

Although plastic deformation may be caused by the use of porous plastic granules and water / saliva penetration expander to bond to tablets, it is very important to use a binder to induce strong bonding between raw materials. The binder serves to safely maintain the pores of the porous plastic granules and the function of the water / saliva penetration enhancer. In the absence of a binder, the two materials are separated. Typical binders are in a liquid or ointment semi-solid state, and it is very important that the binders retain the original properties of these two raw materials. The first way to achieve this property is to use high concentration binders that have little reactivity with water, and to give short mixing times at relatively low binder concentrations, which makes porous plastic granule materials and water / saliva penetration extenders inherent in nature. You can also prevent the loss.

The process up to the production and extrusion of the porous plastic granules may change the properties of the components by varying the input position of each component, and may also change the input position according to the desired physical properties.

Hereinafter, each component of the oral care composition of the multilayer structure according to the present invention will be described in detail.

Porous plastic granule material

The high-porous plastic granules added to the composition of the present invention are produced so as not to denature when subjected to a pressure of 500 kg / cm 2 of external pressure.

Porous plastic materials should have a porosity of 0.14 or more and a density of 0.86 or less, and maintain the original shape when plasticizing with a tablet press pressure of 1.27 cm diameter at a pressure of 500 kg / cm2 or less. . In general, in the case of tableting at a pressure of 675 kg / cm 2 or more, rapid dissolution and gelation cannot be maintained due to breakage of voids.

If the porosity of the porous plastic granule material is less than 0.14, water permeability and porosity are very low, so it cannot play a role as the porous plastic granule material.If the density is higher than 0.86, phase separation by gravity occurs after mixing the granular material. As a result, it is not suitable as a porous plastic granule material.

The porous plastic material is preferably soluble in water. The porous plastic material having high water solubility is preferably included in the range of 1 to 98% by weight and more preferably 20 to 95% by weight of the total weight of the composition. If the content of the porous plastic material is less than 1% by weight, the strength of the formulation may tend to be too weak because of insufficient contact. On the other hand, if the content is greater than 98% by weight, it is not preferable because there is no room for water penetration expander, binder, agonist and other additives.

In the composition of the present invention, the porous plastic material can be easily prepared by purchasing a commercial item or using spray drying, a fluidized bed method, or the like. Soluble porous plastic materials include, for example, fructose, lactitol, lactitol, maltitol, maltose, mannitol, sorbitol, sugar, erythritol Maltodextrin, dextrin, ethylcellulose, polymethylmethacrylate, and pregelatinized starch (e.g., LYCATAB by Roquette American Inc.) as well as saccharides such as xylitol. Same organic polymers. Among the above-mentioned substances, the saccharide having the fastest dissolution rate is sorbitol, and erythritol has been found to be ideal for penetration of water / saliva, although its solubility is not high.

Other materials that may have a suitable porous plastic structure include gum arabic, xanthan gum and its derivatives, guar gum and its derivatives, seafood gum, carrageenan, dextran, gelatin, alginate, pectin, starch and starch derivatives (e.g. Hydroxypropyl starch or hydroxyethyl starch), cellulose esters (eg carboxymethyl cellulose or cellulose ether hydroxyethyl-methyl cellulose), homo or copolymers of unsaturated acids (eg acrylic acid or salts thereof), unsaturated Homo or copolymer of amide (e.g. acrylamide), homoimide or copolymer of acrylimine, vinyl polymer (e.g. polyvinyl alcohol), homo or copolymer of vinyl ester (e.g. vinyl pyrrolye) Money, vinyl oxazolidone, vinyl methyl oxazolidone, vinyl amine and vinyl pyridine), alkyl glycols and polyalkylenes Side (e.g. polyethylene oxide), oxyethylene alkyl esters, dexrate, dextrin, dextrose, microcrystalline cellulose, silicidated microcrystalline cellulose, powdered cellulose, cellulose acetate, calcium sulfate, calcium carbonate, calcium diphosphate, triphosphate Calcium, carboxymethyl cellulose calcium salt, silica, etc. are mentioned. Inorganic materials such as calcium carbonate and silica are fast in water absorption but weak in mutual bonding.

Water / saliva penetration extender

Water / saliva penetration extenders in the compositions of the present invention are used for rapid dissolution and gelation. Here, the method of evaluating the water / saliva penetration extender is to put 200 mg of the raw material into a 1.27 cm diameter mold and tablet it with a force of 135 kg and then drop a few drops of water. At this time, when water remains in the form of water droplets, it cannot be used as a water / saliva penetration extender, and if water is spread or absorbed on the surface of the tablet within 60 seconds, it can be used as a water / saliva penetration extender.

Water penetration extenders should be very soluble in water and, if not soluble in water, should be able to absorb water quickly and disperse easily. In general, water / saliva penetration enhancers are hydrocarbons that are very soluble in water used as excipients. In the composition of the present invention, all kinds of hydrocarbons can be used, but organic acids are formed as by-products through the metabolism of Streptococcus mutans, and the components that can eventually cause tooth decay are generally not used in small doses for oral hygiene-related prescriptions. . Such hydrocarbons include, for example, dextrates, dextrins, dextrose, fructose, lactitol, lactose, maltitol, mannitol, sorbitol, sugar, erythritol, and xylitol. Materials that do not dissolve well in water but have good water dispersion and water delivery capabilities include: microcrystalline cellulose, silicidated microcrystalline cellulose, powdered cellulose, cellulose acetate, calcium sulfate, calcium carbonate, silica, calcium diphosphate, Calcium triphosphate, carboxymethyl cellulose calcium salt, and crosslinked polyvinyl pyrrolidone. Combinations of various hydrocarbons and polymers are possible. Preferred raw materials as water / saliva penetration enhancers are pore-rich materials that can be directly tableted. In addition, inorganic materials such as calcium carbonate, silica, calcium phosphate, and the like, which can deliver water, and crosslinked polyvinyl pyrrolidone, microcrystalline cellulose, cellulose, erythritol, and the like, are also excellent water / saliva penetration enhancers.

In the composition of the present invention, since the action of the water penetrating dilator is performed in the oral cavity together with a mechanical tablet crushing operation such as chewing, gelling is performed even if the content of the water penetrating dilator is lower than that of the tablet which is dissolved and gelled only by water or saliva. There may be no difference in time. Water penetration extenders may be used in the range of 1 to 98% by weight of the total weight of the composition, with 20 to 80% by weight being preferred. If the water penetration enhancer is less than 1% by weight, water cannot penetrate into the formulation, and if it is more than 98% by weight, there is no room for adding components other than the water penetration extender, and the amount of saliva generated in the oral cavity for rapid dissolution and gelation. This is undesirable because it requires more saliva or water.

If the composition of the present invention requires mastication for dissolving and gelling, the use of small amounts of water-insoluble water permeation extenders and the increase in the amount of water-soluble water permeation extenders, compared to otherwise, increase consumer preference and usability. Can be derived. The water-insoluble water penetration extenders of the above-mentioned water penetration extenders may preferably be used in the range of 0.01 to 7% by weight.

On the other hand, where the mastication is not essential for dissolution and gelation, it is necessary to use relatively large amounts of water-insoluble water penetration extenders.

Binder

Binders are widely used in conventional granulation and tableting processes, the composition of the present invention prevents separation between each component by enhancing the binding force between all raw materials, including high pore plastic granules and water / saliva penetration enhancer, It is used for the purpose of obtaining a tablet with high strength even in low pressure tableting. The content of the binder can be used in the range of 1 to 90% by weight of the total weight of the composition.

The binder may be liquid or semi-solid, depending on the difference in the granulation process. The most important requirement of the binder is that the pore damage of the porous plastic material obtained above should be minimized. This is possible by using a high concentration of binder saturated above water solubility to lower the activity of water and by uniformly dispersing the low concentration binder solution for a short time. To determine the damage to porosity and solubility, 1 ml of binder solution is added to 0.5 g of porous plastic material, and if the porous material does not completely dissolve and retains pores within 10 seconds, the binder solution is It can be used in the composition.

The binder crystallized after wet granulation drying should preferably dissolve quickly in contact with water. In wet granulation, the type and amount of binder may vary depending on the desired physical properties, such as high plastic properties and good binding properties. Pharmaceutically acceptable organic solvents, such as ethyl alcohol, may also be used as solvents for the binder solution which less damage the pore structure. Binders include the hydrocarbons mentioned in the water penetration enhancer and include acacia, alginic acid, carbopol, carboxymethyl cellulose, cellulose, dextrin, ethyl cellulose, gelatin, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl Polymers such as methyl cellulose, methyl cellulose, polydextrose, polyethylene oxide, polyvinylpyrrolidone and sodium alginate are also included.

Gelling agent

As the gelling agent, water-soluble polymers or natural polymers such as gum that can be easily swollen by water / saliva or the like can be used. The gelling agent in the composition of the present invention has a great influence on the formation of gel tissue and is the most important factor in the usability of the final product. The requirement to be equipped as a gelling agent is to receive water / saliva and have the gel tissue in a few tens of seconds. To check this, you can use the following method: make 200 mg of gelling tablets, drop 1 ml of water and 10 seconds. If a gel-like property is observed within the surface, it can be used as a gelling agent. Another important element of the gelling agent is that when it gels by reacting with water or saliva, it should not form a hydration film on the surface of the tablets and impede penetration of water or saliva.

In order to gel at a high rate, the gelling agent must be hydrophilic and gelation can be achieved by absorbing a small amount of water. In the wet granulation process, the wet granulation should be performed within 5 minutes so that the gelling agent does not block the pores of the porous plastic granules. Gelling agents include acacia gum, agag gum, gellan gum, guar gum, pectin, gelatin, alginic acid, sodium alginate, carboxymethyl cellulose, polyvinylmaleic anhydride maleic acid copolymer, carbopol, polyethylene glycol, polyvinylpyrrolidone, Polyethylene oxide, xanthan gum, carrageenan, super porous hydrogel, and the like may be used, and one or two or more of these polymer mixtures may be used. Among these, xanthan gum (CP Kelco, USA), Carbopol (Noveon, USA), and carboxymethyl cellulose (Hercules, USA) are readily available as commercially available products.

The gelling agent is preferably used in the range of 0.1 to 10.0% by weight of the total weight of the composition. If the gelling agent content is less than 0.1% by weight, it does not have the required viscoelasticity, and when it is used more than 10.0% by weight, water does not reach the center of the preparation and gelation occurs only on the surface. It is not preferable because it occurs.

Tooth attachment inhibitor

When mastication is required for dissolution and gelation in the oral hygiene composition of the present invention, it may be a problem that the product remains between the teeth and degrades the consumer's feeling of use and the quality of the emotion after use. The addition of inhibitors minimizes the phenomenon of adhesion to teeth during chewing.

Components used as anti-adhesion agents include surfactants such as glyceryl monooleate, glyceryl monostearate, and the like, which can be used so as not to adhere to hydrophilic tooth surfaces.

Anti-sticking agents are used in the range of 0.01 to 10% by weight of the total weight of the composition. If less than 0.01% by weight it is difficult to prevent the property attached to the teeth, when used more than 10% by weight will have a negative role in taste and feel.

Moisturizer

In the oral care composition of the present invention, since the porous plastic granules are used, the oral care composition may have a powdery feeling caused by an abrasive after drying. In order to solve this problem, it is possible to use a component that can maintain the moisture content of the granules, that is, a moisturizer. Raw materials which can be used as humectants include glycerin, polyethylene glycol, propylene glycol, sorbitol solution and the like.

Moisturizers may use from 0.01 to 20% by weight of the total weight of the composition. If less than 0.01% by weight it is difficult to prevent the property attached to the teeth, when used more than 20% by weight may cause overwetting of the porous plastic granules.

Lubricant

The role of the lubricant in the manufacture of tablets is to prevent foreign matter from adhering to the punch of the tableting machine during the tableting process, sodium lauryl sulfate, magnesium stearate, stearic acid and the like can be used. Glidants are generally used in the range of 0.1 to 5% by weight of the total weight of the composition.

Foaming Agent / Surfactant

In oral hygiene, foaming agents and surfactants not only cleanse teeth, but also generate bubbles, which is one of the most important attributes in oral hygiene. Generally foaming agents include anionic surfactants, cationic surfactants, nonionic surfactants, amphoteric surfactants, zwitterionic surfactants. Foaming agents can usually be used as a single substance, or a combination of foaming agents can be made by mixing two or more kinds. Foaming agents in the present invention may be used in the range of about 0.001 to 20% by weight of the total weight of the composition, preferably 0.1 to 5% by weight.

As the foaming agent that can be optionally used in a safe and effective amount in the composition of the present invention, sodium lauryl sulfate and sodium coconut monoglyceride sulfonate are most representative of anionic surfactants. Other suitable anionic surfactants include sarcosinates, such as sodium lauroyl sarcosinate, taurate, sodium lauryl sulfoacetate, sodium lauroyl isethionate, sodium laureth carboxylate and sodium dodecyl benzenesulfonate There is. In addition, cochamidopropyl betaine, poloxamer, sorbitan monooleate, PEG-40 sorbitan isostearate, or mixtures thereof may also be used.

abrasive

Abrasives play the most important role in cleaning oral hygiene products, such as plaque removal and food removal. The abrasive must not damage the enamel of the tooth and must be compatible with the other ingredients of the composition. In the composition of the present invention, the abrasive is selected by adjusting the content by selecting a substance which does not cause excessive grinding of dentin and a syringe. Currently abrasives suitable for oral hygiene preparations include silica, calcium pyrophosphate, aluminum hydroxide, tricalcium phosphate, calcium diphosphate dihydrate and anhydrides, including calcium and precipitates, calcium carbonate and the like. In addition, natural fibrous abrasives such as cellulose and derivatives thereof, and natural material ground powders such as egg shells and clam shell ground powders may also be used as abrasives. In the present invention, the abrasive may be used in the range of about 5 to 70% by weight of the total weight of the composition, with 15 to 50% by weight being preferred.

Flavor  And Sweetener

Flavoring agents and sweetening agents can be added to the composition of the present invention to suit consumer preferences. As a flavoring agent, mint, such as peppermint and spearmint, wintergreen, anise, menthol, thymol, methyl salicylate, eucalyptol, eugenol, polypropylene glycol, melon, strawberry, orange, vanillin, and the like may be used. Generally, flavoring agents can be used in the range of 0.001 to 10% by weight of the total weight of the composition.

In addition, a sweetener may be added to the composition of the present invention in order to overcome the basic taste of granules and the like in the tablet manufacturing process. As the sweetener, one or two or more kinds of saccharin, sucralose, sugar, xylitol, sorbitol, lactose, mannitol, maltitol, erythritol, aspartame, taurine, saccharin salt and D-tryptophan may be used. Among the saccharin salts, saccharin sodium is the most widely used. The amount of sweetener is generally used in the range of 0.001 to 20% by weight of the total weight of the composition.

Medicinal agents

As a medicament, depending on the purpose of using the oral hygiene, it is possible to use ingredients that are effective in preventing tooth decay, preventing gum disease, preventing tartar deposition, and whitening.

Drugs used to prevent tooth decay include compounds recognized as safe by the US Food and Drug Administration, including fluoride ions. Examples of the compound that can be used as a source of fluorine ions include sodium fluoride, sodium monofluorophosphate, tin fluoride, and amine fluoride. The amount of fluorine may vary depending on the country, but it is common to use one kind or a mixture of two or more of these sources, preferably to have a fluorine ion concentration in the range of 850 to 1500 ppm.

Remineralizing agents can also act as a caries preventer. Remineralization plays a role in regenerating and restoring hydroxyapatite, a major component of teeth. The main component of hydroxyapatite consists of divalent calcium cations and phosphate anions. Therefore, it can be a remineralizing agent if it contains at least one of calcium divalent ions or phosphate anions so as to simultaneously supply calcium ions and phosphate ions or to shift chemical equilibrium in the oral cavity toward the formation of hydroxyapatite. Substances that provide calcium and phosphorus include hydroxyapatite, dicalcium phosphate, calcium chloride, casein phosphate, calcium glycophosphate, sodium monophosphate, dibasic sodium phosphate, sodium triphosphate, potassium monophosphate, This includes potassium diphosphate, potassium triphosphate, and the like. In general, the remineralizing agent is preferably used in the range of 0.001 to 20% by weight of the total composition. If it is less than 0.001% by weight, the effect of remineralization is inferior, and if it is more than 20% by weight, the property of the formulation is lost.

One purpose of using oral hygiene products is to prevent gum disease as well as to alleviate gum disease that is progressing through antiseptic or anti-inflammatory action against harmful microorganisms that survive in the oral cavity. For this purpose, thymol, cyclohexidine, cetylpyridinium chloride, triclosan, xantholizol, etc., which are known as antimicrobial agents, may be used, and vitamins and enzymes may also be used for anti-inflammatory action.

In addition to gum disease, hydrogen peroxide, carbamide peroxide, calcium peroxide, and the like, which have a whitening effect, may be used, and sodium pyrophosphate, acidic pyrophosphate, potassium pyrophosphate, sodium metaphosphate, etc. may also be used to obtain tartar deposition inhibitory effect. Generally, these agents are generally used in the range of 0.001 to 10% by weight of the entire composition.

In addition, in order to form the foam layer in the tablet-type oral hygiene composition of the multi-layer structure according to the present invention, an organic acid as a foaming acid and a carbonate-containing component as a carbon dioxide generating source are required.

Effervescent

In the composition of the present invention, an organic acid may be used as the foaming acid, and in particular, a raw material usable to the human body is used. As the organic acid, one or two or more of ascorbic acid, citric acid, citric acid, tartaric acid, malic acid, gluconic acid, succinic acid and propionic acid may be used in combination. The content of the organic acid in the composition of the present invention is preferably 0.01 to 10.0% by weight of the total weight of the tablet. When the content of the organic acid is less than 0.01% by weight of the tablet weight, the acid value is weak, the foaming amount is significantly reduced, and when it is higher than 10.0% by weight, the taste is too strong and difficult to use.

CO2 source

For the foaming of the composition of the present invention may be used a carbonate that reacts with the organic acid to generate carbon dioxide, which is a raw material that is widely used to inflate the substrate in foods with increased volume, such as bread, cake. As the source of carbon dioxide, one containing a carbonic acid (CO ₃ ) group in the molecular formula, such as sodium bicarbonate, ammonium bicarbonate, potassium bicarbonate, calcium carbonate, magnesium carbonate, iron carbonate, etc., the content is 0.1 to 80 of the total weight of the tablet Weight percent is preferred. When the carbon dioxide source is less than 0.1% by weight, the amount of foaming is very small and difficult to recognize, and when it is higher than 80% by weight, it is a factor that inhibits tableting.

The manufacturing process of the multi-layered tablet oral hygiene composition according to the present invention is as follows:

First, the solid materials used in the preparation of the porous plastic granules are precisely weighed and then placed in a pharmaceutical high speed mixer or fluidized bed granulator and mixed with a binder solution, and mixed without impairing the porosity of the particles. Mix until the powder ingredients can be combined. The mixed raw material is sieved using a 10 to 50 mesh sieve, and then dried at room temperature or in a conveyor belt until the water content is less than 10%. When the dried granules are sieved through 10 to 50 mesh again, the porous plastic granules are completed. After adding the flavoring agent, the active ingredient and the lubricating agent to the finished plastic granules, the mixture is mixed again. have. Maintaining the tableting pressure at 500 kg / cm 2 or less is because the maximum pressure for obtaining granules without problems in distribution while maintaining the porosity of the porous plastic granules.

Disperse one or two or more of the porous plastic granules, water penetration enhancer, gelling agent or other solid ingredients in a dry state using a high-speed mixing granulator, mix the organic acid first, and then add the carbon dioxide source last. After sieving using a sieve of 10 to 50 mesh and tableting to prepare a foam layer composition.

The prepared foam layer composition is prepared through multi- or triple tableting to prepare multi-layer co-dissolving, gelling and foaming oral hygiene.

The tablet-type oral hygiene composition of the multi-layer structure according to the present invention prepared according to this method is dissolved, gelled and foamed within 15 minutes by water / saliva in the oral cavity, and within 30 seconds upon chewing. In addition, the tablet-type oral hygiene composition of the present invention can be attached to a toothbrush, etc. while maintaining the original form of the tablet while dissolving and gelling can be brushed or gargle for oral hygiene.

Oral hygiene tablets of the multi-layered structure according to the present invention is completely dissolved and gelated within 30 seconds at the time of mastication, within 15 minutes when dissolved, it is excellent in the prevention of tooth decay by maintaining the homeostasis of saliva pH in the oral cavity, salivary secretion In addition to the excellent effect of suppressing bad breath by the self-cleaning action, there is an advantage that the use of tablets is excellent.

Hereinafter, the present invention will be described in more detail with reference to preferred embodiments of the present invention. However, these examples are only illustrative to aid the understanding of the present invention, and the scope of the present invention is not limited thereto.

A multi-layered tablet oral hygiene composition according to the present invention was prepared according to the following process.

First, Table 1 below shows the composition of the raw materials used to prepare the layer comprising the porous plastic granules.

Ingredient Porous Plastic Granules Composition Sorbitol 51.88 Erythritol 5.00 Xylitol 10.00 Sodium Lauryl Sulfate 3.00 Cabopol 2.50 Precipitated silica 20.00 Sodium bicarbonate 1.00 Xanthan Gum 1.00 Crystalline cellulose 5.00 Sodium fluoride 0.22 Saccharin Sodium 0.40 Citric acid 0.00 gun 100.00

Porous plastic granules were prepared by using 5% hydroxypropyl cellulose in the porous plastic granules mixed in the composition of Table 1, dried, and 1.0% of a lubricant was added to prepare a tableting material (precursor 1).

Table 2 is a foam layer composition (precursor 2), a composition prepared so that it can be compressed directly.

Ingredient Foam layer composition Sorbitol 30.00 Precipitated silica 2.00 Sodium bicarbonate 35.00 Crystalline cellulose 28.00 Citric acid 4.50 Lubricant 0.50 gun 100.00

Using layer precursor 1 comprising porous plastic granules prepared in the composition of Table 1 and foamed layer precursor 2 prepared in the composition of Table 2, combinations, double, triple or 4 in the weight percent ratios of Table 3 below. The tablets of the Examples and Comparative Examples were prepared by compression.

Number of floors Composition of layers Example Comparative example One 2 3 4 One 2 One Precursor1 50 60 20 25 100 2 Precursor2 50 20 60 25 100 3 Precursor1 20 25 4 Precursor2 20 25 Sum 100 100 100 100

In Table 3 above, the number of layers is divided into layers according to the order of tableting, and it is also possible to tablet at once using a device or to divide tablets at several times. The comparative example is suitable for comparing the respective physical properties.

In the examples of Table 3, it is preferred to place foam layer precursor 2 outmost, but the reverse is also possible.

The hardness of the tablets of the prepared examples and comparative examples was measured, and the efficacy evaluations such as dissolution and gelation rate, caries prevention effect by pH homeostasis and bad breath control effect.

effect Test Example

(1) tablet strength measurement

The intensity of 10 tablets was measured using a texture analyzer (TA XT Plus, TA Instrument) and the average value was determined as the strength of the tablet. The measured value is the read value which is not converted. Table 4 shows the strength of the tablets prepared in Examples and Comparative Examples.

Example 1 Example 2 Example 3 Example 4 Comparative Example 1 Comparative Example 2 Strength (kg) 7.8 ± 0.5 7.6 ± 0.6 7.1 ± 0.3 8.1 ± 0.4 7.8 ± 0.3 8.4 ± 0.6

As shown in Table 4, the strength of the tablet measured using the Texture Analyzer could not find a difference between the Example and the comparative example. That is, it was confirmed that the strength of the tablets prepared according to the present invention is similar to the general tablets, which is sufficient strength to solve the distribution problem.

(2) measuring dissolution time of tablets

One tablet was placed in 200 ml of distilled water, followed by visual observation while stirring at a stirring speed of 200 rpm, and the time until no longer present in the form of tablets was measured. In addition, when chewing, the time for dissolution and gelation was evaluated emotionally. Table 5 shows the dissolution time of the tablets prepared in Examples and Comparative Examples and the time of dissolution / gelation during chewing.

Example 1 Example 2 Example 3 Example 4 Comparative Example 1 Comparative Example 2 Dissolution time (distilled water) 8 minutes 10 minutes 6 minutes 8 minutes 15 minutes 1 minute Dissolution / Gelation Time (authored) 10 sec 15 seconds 9 sec 11 seconds 30 seconds 9 sec

In the above Table 5, in the case of distilled water dissolution time, it was confirmed that the dissolution time is reduced by more than 60% compared to the tablet of Comparative Example 1 prepared only by the porous plastic granule layer, which is important for user sensitivity In tablet-type oral hygiene which is a factor, it can be said to be a remarkable improvement in physical properties. The tablet of Comparative Example 2 containing only the foam layer had a very fast dissolution rate but provided a very inappropriate feeling in terms of emotion when used by consumers.

(3) Evaluation of the usability of tablets

For the tablets prepared in Examples 1, 2 and Comparative Example 2, the feeling of usability was evaluated by cross-testing for 30 consumers. The results are shown in Table 6 below.

* Feeling criteria

Rating 5: Very good feeling and no rejection.

Rating 4: Feeling good and no rejection.

Rating 3: Feeling good and no rejection.

Rating 2: Poor feeling and slight rejection.

Rating 1: Very poor feeling and very bad rejection.

Example 1 Example 2 Comparative Example 2 Feeling rating 3.9 ± 0.4 4.2 ± 0.5 1.2 ± 0.2

As shown in Table 6 above, the tablets of the Example was confirmed that there is a significant improvement in the emotional use compared to the tablet of Comparative Example 2 including only the foam layer. Particularly, the tablet of Example 2 was obtained by triple tableting of precursor 1 and foamed layer precursor 2 including porous plastic granules in the order of precursor 1: precursor 2: precursor 2 = 60: 20: 20. Can be.

(4) prevention of tooth decay

In order to test the preventive effect of the cavities, the tablets of Example 1 and Comparative Example 1 were cross-tested in 10 subjects, and the pH of the oral saliva was measured over time. The results are shown in Table 7.

Example 1 Comparative Example 1 Immediately after use 1 hours 2 hours Immediately after use 1 hours 2 hours pH 6.8 6.7 6.5 6.8 5.9 5.0

As shown in Table 7, the pH of the tablet of Example 1 was kept constant, while in the tablet of Comparative Example 1 it was confirmed that the pH of the saliva decreases over time and may cause tooth decay.

(5) bad breath control effect

The bad breath inhibitory effect of the tablet of Example 1 and the comparative example 1 was measured by the sensory evaluation method using the following scoring system with time. The results are shown in Table 8 below. In addition, the saliva secretion was closely associated with bad breath control and is shown in Table 8.

* Bad breath sensory score scale (J. Clin . Dent. 10: 131-34, 1999)

0 points | pieces: There is no smell. Toothpaste reverberation is felt.

1 point | piece: A smell is very weak.

2 points | pieces: A smell is weak.

3 points | pieces: The smell can be recognized clearly.

4 points | pieces: It smells but is not unpleasant.

5 points | pieces: It smells like it seems unpleasant.

6 points | pieces: A smell is unpleasant.

7: Smell is unpleasant.

8 points | pieces: A bad smell is unpleasant.

9 points | pieces: The smell is unpleasantly unpleasant.

Example 1 Comparative Example 1 Immediately after 1 hours 2 hours 3 hours Immediately after 1 hours 2 hours 3 hours Bad breath index 0 2.5 3.2 3.9 0 3.9 5.4 6.7 Saliva secretion 2 mL / min 2 mL / min 2 mL / min 2 mL / min 2 mL / min 0.5 mL / min 0.5 mL / min 0.3 mL / min

As shown in Table 8, the bad breath inhibitory effect of the tablet according to Example 1 was confirmed to be superior to the tablet of Comparative Example 1. This effect is judged to be because saliva secretion is maintained at a constant level by using the tablet of Example 1.

From the above test results, the oral hygiene tablet of the multi-layered structure according to the present invention prepared in the Example was completely dissolved and gelled within 30 seconds at the time of mastication and within 15 minutes at the time of dissolution, so that the dissolution and gelation were faster than those of the tablet prepared in the Comparative Example. It can be seen that gelation takes place.

In addition, the tablet according to the present invention prepared in Example maintains the homeostasis of saliva pH in the oral cavity, compared with the tablet prepared in the comparative example is superior in caries prevention effect, promotes saliva secretion and bad breath by the self-cleaning action The inhibitory effect was also superior to the tablet of the comparative example. Moreover, in terms of the tablet's usability, the tablets of the Examples were superior to the tablets of the Comparative Examples, showing the level of consumer preference.

On the other hand, the hardness of the tablet having a multilayer structure according to the present invention was measured by the Texture Analyzer as a result of 0.5 to 15 kg, it was also confirmed that the level is similar to 1 to 50 kg of the general tablet.

Claims (8)

Intraoral cavity comprising at least one layer each comprising a porous plastic granule material, a binder, a water permeation expansion agent, and a gelling agent comprising a porous plastic granule as an essential component, and a foamed layer as an essential component of an acid and a carbon dioxide source. A tablet-type oral hygiene composition having a multi-layer structure, characterized in that it is dissolved and gelled simultaneously with foaming by saliva or water. At least one layer each comprising a porous plastic granule material, a binder, a water penetration expander, and a gelling agent comprising a porous plastic granule as an essential component, and a foamed layer as an essential component of an acid and a carbon dioxide generator. A tablet-type oral hygiene composition having a multi-layer structure, characterized in that it is dissolved and gelled simultaneously with foaming. The multi-layered tablet oral hygiene composition according to claim 1, which is dissolved and gelled within 15 minutes. The multi-layered tablet oral hygiene composition according to claim 2, which is dissolved and gelled within 30 seconds. The method of claim 1 or 2, wherein the porous plastic granule material is fructose, lactitol, lactitol, maltitol, maltose, mannitol, sorbitol, sugar, Erythritol, xylitol, maltodextrin, dextrin, ethyl cellulose, polymethylmethacrylate, pregelatinized starch, microcrystalline cellulose, silicified microcrystalline cellulose, powdered cellulose, A fast-soluble oral and throat hygiene composition, characterized in that it is cellulose acetate, calcium sulfate, calcium carbonate, calcium diphosphate, calcium triphosphate, carboxymethyl cellulose calcium salt, silica, or mixtures thereof. The binder according to claim 1 or 2, wherein the binder is dexrate, dextrin, dextrose, fructose, lactitol, lactose, maltitol, mannitol, sorbitol, sugar, erythritol, xylitol, acacia, alginic acid, carbopol ), Carboxymethyl cellulose, cellulose, dextrin, ethyl cellulose, gelatin, hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropylmethyl cellulose, methyl cellulose, polydextrose, polyethylene oxide, polyvinylpyrrolidone, sodium alginate, or these Fast dissolving mouth and throat hygiene composition, characterized in that a mixture of. The water penetration dilator according to claim 1 or 2, wherein the water penetration extender is dexrate, dextrin, dextrose, fructose, lactitol, lactose, maltitol, mannitol, sorbitol, sugar, erythritol, xylitol, microcrystalline cellulose, silylation Genus characterized in that it is microcrystalline cellulose, powdered cellulose, cellulose acetate, calcium sulfate, calcium carbonate, silica, calcium diphosphate, calcium triphosphate, carboxymethyl cellulose calcium salt, crosslinked polyvinyl pyrrolidone, or mixtures thereof Soluble oral and throat hygiene compositions. The gelling agent according to claim 1 or 2, wherein the gelling agent is acacia gum, agar gum, gellan gum, guar gum, pectin, gelatin, alginic acid, sodium alginate, carboxymethyl cellulose, polyvinylmaleic anhydride maleic acid copolymer, carbopol , Oral polyethylene glycol, polyvinylpyrrolidone, polyethylene oxide, xanthan gum, carrageenan, super porous hydrogel, or a mixture thereof.