KR100814250B1 - In-situ melting and gelling tablet composition for oral care - Google Patents

Abstract

A tablet-type oral hygienic composition is provided to be directly injected into oral cavity so that it can maintain the health of the oral cavity by being melted and gelled by water or saliva, or mastication, thereby reducing the inconvenience of a conventional liquid phase or an ointment type oral hygienic agent and being easy to carry. A tablet-type oral hygienic composition is characterized in that it is prepared by tabletting porous plastic granules comprising 20-95 wt.% of a porous plastic granule material, 1-90 wt.% of a binder, 0.1-10 wt.% of a gelating agent, 20-80 wt.% of a water permeation expanding agent, 0.01-10 wt.% of a tooth adhesion preventive agent, and 0.01-20 wt.% of a moisturizing agent as necessary ingredients under the pressure of less than 500 kgf/cm^2 and it is in-situ melted and gelled by oral saliva or water, or mastication, wherein the porous plastic granule material has the porosity of more than 0.14 and the density of less than 0.86, the water permeation expanding agent is selected from the group consisting of dextrate, dextrin, dextrose, fructose, lactitol, lactose, maltitol, mannitol, sorbitol, sugar, erythritol, xylitol, microcrystalline cellulose, siliciated microcrystalline cellulose, powder cellulose, cellulose acetate, calcium sulfate, calcium carbonate, silica, dicalcium phosphate, tricalcium phosphate, calcium carboxymethyl cellulose, crosslinked polyvinyl pyrrolidone and a mixture thereof, and the tooth adhesion preventive agent is a surfactant. Further, 0.001-10 wt.% of a foaming agent and 5-70 wt.% of a polishing agent is additionally comprised.

Description

Co-dissolving and gelling tablet oral hygiene composition {IN-SITU MELTING AND GELLING TABLET COMPOSITION FOR ORAL CARE}

1 is a schematic diagram of a general manufacturing method of a co-dissolving gelled tablet of the present invention,

2 is a schematic diagram of a method of adding a gelling agent together with a binder solution in the preparation of the simultaneous dissolving gelled tablet of the present invention,

Figure 3 is a schematic diagram of a method of adding a gelling agent after the production of porous plastic granules in the production of co-dissolving gelled tablet of the present invention,

4 is a schematic diagram of a method for producing a tablet after producing two granules in the preparation of the co-dissolving gelled tablet of the present invention.

The present invention relates to an oral hygiene composition that provides a refreshing feeling in the oral cavity and is easy to deliver an oral hygiene active ingredient, and is in-situ melting and gelling by water or saliva in the mouth or through chewing. It is an oral hygiene composition characterized by being able to brush or gargle.

Common types of oral hygiene can be classified as 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 weak strength and thus has a disadvantage in that a problem occurs in distribution. 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 using disintegration use effervescent diacid / base, 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 because it can give a sense of foreign body after use, but also does not exhibit gel properties like toothpaste within seconds because the tablet is not fast-soluble. There is a demand for improvement of ease of use.

The object of the present invention is not just a quick dissolving tablet, but also has excellent convenience and usability, and simultaneously dissolves and gels oral hygiene of tablets that can be used for various purposes such as chew type, intraoral dissolution crystallization type and toothbrush dissolution gelling type. It is to provide a composition.

Tablet oral hygiene composition of the present invention for achieving the above object,

It is prepared by compressing the porous plastic granules having the essential components of the porous plastic granule material, the binder, the gelling agent, the water penetration extender, the anti-adhesion agent and the moisturizing agent at a pressure of 500 kg / cm 2 or less,

It is characterized in that the in-situ melting and gelling by saliva or water in the mouth, or by chewing (in-situ melting & gelling).

Toothpaste is a representative oral hygiene, buried in a toothbrush and inserted into the oral cavity to implement oral hygiene through brushing. The present invention is in the form of tablets through the chewing in the oral cavity or by simultaneous dissolution and gelation by water or saliva, so that not only brushing, but also rinsing with water to relieve and prevent oral diseases Provides tablet oral hygiene.

Tablet-type oral hygiene according to the present invention has all the functions of the existing oral hygiene cleaning, caries prevention, gum disease prevention, in addition to simultaneous dissolution and gelation by water or saliva is made or dissolved and gelated through chewing Is promoted, is a new concept of oral hygiene products different from the conventional oral hygiene.

The properties of the tablets required for simultaneous dissolution and gelling tablets, with high porosity for ease of penetration of water, should allow water to penetrate into the center of the tablet within a few seconds and have a strength above the proper to facilitate handling. The fast dissolving tablet of the present invention may be composed of high pore plastic granules, water / saliva penetration enhancers, binders, gelling agents, anti-adhesion agents, moisturizers, abrasives, foaming agents, flavors, sweeteners, medicaments, and the like.

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 tablet composition has a gel texture similar to that of a general toothpaste.

Dissolution and gelation are both competitive processes that require water or saliva. Since some of the water or saliva used must be dissolved and the rest must be gelled, it is technically difficult to simultaneously dissolve and gel.

In the present invention, in order to obtain the simultaneous dissolution and gelling properties, the production of porous plastic granules in the granulation process, gelling and dissolving in the manufacturing process, induction of rapid gelation using a high hydrophilic polymer, the use of water penetration expansion agent and An attempt was made to produce low pressure tablet high strength tablets via a binder solution. 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 stagnant oral hygiene of the present invention utilizes a fast dissolving tablet manufacturing technique and a fast gelling technique. Fast dissolving tablet manufacturing techniques include the preparation of porous plastic granules, the preparation of low pressure high strength tablets with water penetration expanders and binder solutions.

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 can change the physical properties by varying the input position of each component, and can also be changed depending on the desired physical properties.

Hereinafter, each component of the simultaneous dissolving and gelling oral hygiene agent of the fast dissolving tablet type 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.

The porous plastic material should have a porosity of 0.14 or more and a density of 0.86 or less, and maintain the original shape when the tableting pressure is compressed to a pressure of 500 kg / cm2 or less in a mold with a diameter of 1.27 cm. do. In general, tableting at a pressure of 675 kg / cm 2 or more does not maintain the properties of the fast dissolving tablet due to breakage of voids.

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 based on the total weight of the tablet, more preferably 20 to 95% by weight. If the content of the porous plastic material is less than 1% by weight, the strength of the tablet 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. hydroxides). Propyl starch or ethyl hydroxide starch), cellulose esters (eg carboxymethyl cellulose or cellulose ether ethyl hydroxide-methyl cellulose), homo or copolymers of unsaturated acids (eg acrylic acid or salts thereof), homos of unsaturated amides Or homopolymers or copolymers of copolymers (e.g. acrylamides), acrylimines, vinyl polymers (e.g. polyvinyl alcohols), vinyl esters (e.g. vinyl pyrrolidones, vinyls) Oxazolidone, vinyl methyl oxazolidone, vinyl amine and vinyl pyridine), alkyl glycols and polyalkylene oxides (e.g. For example, polyethylene oxide), oxyethylene alkyl esters, dextrates, dextrins, dextrose, microcrystalline cellulose, silicidated microcrystalline cellulose, powdered cellulose, cellulose acetate, calcium sulfate, calcium carbonate, calcium diphosphate, calcium triphosphate, carboxymethyl Cellulose calcium salt, silica, and the like. 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 enhancers in the compositions of the present invention are used to quickly disintegrate tablets. 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, if the water remains in the form of water droplets can not be used as a water / saliva penetration extender, if water is spread or absorbed over the surface of the tablet within 60 seconds 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. Although all kinds of hydrocarbons can be used in the composition of the present invention, 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 polyvinylpyrrolidone, microcrystalline cellulose, cellulose, and erythritol may also be excellent water / saliva penetration extenders.

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

In addition, in the compositions of the present invention, by using a small amount of water-insoluble water penetration extender and increasing the amount of water-soluble water penetration extender compared to tablet oral hygiene which does not necessarily require chewing for simultaneous dissolution and gelling, consumer preference And an increase in usability.

Binder

The binder is widely used in the conventional tablet compression process, and the composition of the present invention prevents separation between components by enhancing the binding force between all raw materials including high porosity plastic granules and water / saliva penetration enhancer, and prevents the separation between the components. It is used for the purpose of obtaining high strength co-dissolution and gel forming tablets. The content of binder is 1 to 90% by weight of the total tablet weight.

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 within 10 seconds, the binder solution is added to the composition of the present invention if the porous material does not completely dissolve and retains pores. Can be used for

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, ethyl cellulose, propyl hydroxide, propyl methyl cellulose, Polymers such as 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. In the composition of the present invention, the gelling agent has a great influence on the gel structure which is most important in the physical properties of the tablet together with the fast solubility of the tablet, and is the most important factor in the usability of the final product. The requirement for the gelling agent is to take water / saliva and have the gel tissue in a few tens of seconds. To check this, the following method can be used: 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 the 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 tablet weight. If the gelling agent content is less than 0.1% by weight, it does not have a viscosity and cannot maintain the form of the tablet after dissolution. When using more than 10.0% by weight, water does not reach the center of the tablet and gelation occurs only on the surface. This is undesirable because of the problem that the binder sticks to the teeth.

Tooth attachment inhibitor

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 tablet. 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

Since porous plastic granules are used in the tablet-type oral hygiene, it may have a powdery feeling caused by an abrasive or the like 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 that can be used as humectants include glycerin, polyethylene glycol, propylene glycol, sorbitol solution and the like.

Moisturizing agents may use 0.01 to 20% by weight of the total weight of the tablet. 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 tablet.

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 compositions of the present invention can be used in the range of about 0.001 to 20% by weight of the total weight of the stagnation, 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, including plaque removal and food removal in oral care products. 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 tablet.

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 remineralization effect is lowered. If it is more than 20% by weight, the tablet loses its original properties.

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, etc., which have a weak effect, may be used, and sodium pyrophosphate, acid pyrophosphate, potassium pyrophosphate, sodium metaphosphate, etc. may also be used to obtain calculus deposition inhibiting effect. Generally, these agents are generally used in the range of 0.001 to 10% by weight of the entire composition.

The fast dissolving tablet co-dissolving and gelling oral hygiene according to the present invention is prepared using the above ingredients. Figures 1 to 4 schematically show the manufacturing process of these tablets, Figure 1 is a general manufacturing method of the co-dissolving gelling tablet of the present invention, Figure 2 is a method of adding a gelling agent with a binder solution, Figure 3 The method of adding the gelling agent after the preparation of the porous plastic granules, and FIG. 4 shows a schematic diagram of the method of preparing the tablet after preparing the two granules.

The oral hygiene agent of the present invention will be described with reference to the method of FIG.

First, precisely weigh the solid raw materials used in the preparation of porous plastic granules, and then put them in a pharmaceutical high speed mixer and add a binder solution to mix them. All powder raw materials are mixed without impairing the porosity of the particles. Mix until 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 mixing the flavoring agent, the active ingredient and the lubricating agent into the finished plastic granules, the mixture is mixed again, and then compressed at a pressure of 500 kg / cm 2 or less at a relatively low pressure to obtain a simultaneous dissolving gelled oral hygiene tablet containing the porous plastic granules. 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.

2 and 3 is a change in the step of adding the gelling agent in the method of Figure 1, in the method of Figure 4 to prepare two kinds of granules and tableted it at low pressure to obtain simultaneous dissolution and gelling tablets.

Tablet-type oral hygiene according to the present invention prepared according to such a method is dissolved and gelated within 30 seconds by saliva in the oral cavity, it is possible to chew to increase the gelation rate, attached to a toothbrush, etc. After dissolving and gelling while maintaining the form of the brush, it may be brushed or gargled for oral hygiene.

The characteristics of the tablet oral hygiene according to the invention are summarized as follows:

First, the tablet oral hygiene is present in the form of tablets before contact with water, and is simultaneously dissolved and gelled through chewing in the oral cavity or by water or saliva.

Secondly, tablets with simultaneous dissolution and gelation are made by the preparation of high pore plastic granules, the addition of a water penetration expander, a binder to enhance tablet strength, and the addition of a gelling agent to give a gel-like texture.

Third, sweeteners, flavoring agents, and the like are used to improve the usability in the oral cavity, and pharmacological agents such as fluorine compounds are used to prevent tooth decay, gum disease, tartar deposition, and the like through oral drug delivery.

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.

EXAMPLE

Co-dissolving and gelling tablet oral hygiene according to the present invention was prepared according to the manufacturing process shown in FIG.

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

In Comparative Example 1, a gelling agent and an anti-adhesion agent were not used, and in Comparative Example 2, an anti-adhesion agent and a moisturizer were not used.

Example Comparative example One 2 to 4 5 One 2 Sorbitol 72.13 - 26.11 52.53 - Xylitol - 67.13 26.02 - 76.03 Sodium Lauryl Sulfate 2.00 2.00 2.00 2.00 2.00 Cabopol 1.50 1.50 1.50 - 1.50 Precipitated silica 15.00 20.00 - - 20.00 Calcium carbonate - - 35.00 35.00 - Sodium bicarbonate 1.00 1.00 1.00 - - Trisodium Phosphate 0.40 0.40 0.40 - - Xanthan Gum 1.00 - 1.00 - - Carboxymethyl Cellulose Sodium - 1.00 - - - Crosslinked polyvinylpyrrolidone 1.00 - - - - Cross-linked cellulose - 1.00 - - - Microcrystalline cellulose - - 1.00 10.00 - glycerin 5.00 5.00 5.00 - - Sodium fluoride 0.22 0.22 0.22 0.22 0.22 Saccharin Sodium 0.25 0.25 0.25 0.25 0.25 Glyceryl Monostearate 0.5 0.5 0.5 - - gun 100.00 100.00 100.00 100.00 100.00

Four binder solutions were prepared as shown in Table 2 below.

Binder solution usage One 2% Hydroxypropyl Cellulose Solution 25 g 2 70% Sorbitol solution 25 g 3 2% Hydroxypropylmethyl Cellulose Solution 25 g 4 2% carboxymethyl cellulose solution 25 g

The binder solution of Table 2 was mixed with the porous plastic granule material of Table 1 as shown in Table 3 below to prepare porous plastic granules of Examples 1 to 5, and Comparative Examples 1 and 2.

The obtained porous plastic granules were dried at room temperature for at least 2 hours and then compressed using a tableting machine. At the time of tableting, lubricant is added at a rate of 1 to 2% for smooth tableting. The type and amount of lubricant are shown in Table 3 below.

Examples and Comparative Examples Binder Solution Used Used lubricant Example 1 2 Magnesium Stearate 1% Example 2 One Magnesium Stearate 2% Example 3 2 Magnesium Stearate 1% Example 4 4 Magnesium Stearate 2% Example 5 3 Magnesium Stearate 1% Comparative Example 1 One Magnesium Stearate 1% Comparative Example 2 2 Magnesium Stearate 2%

For the tablets of the Examples and Comparative Examples obtained through tableting, the dissolution / gelling time was determined by the following method: 5 seconds, 10 seconds, 15 seconds, 20 seconds, 30 in a 20 ml water filled 100 ml beaker The tablets were taken out at the interval of seconds and 1 minute, and the tablets were pressed with a spatula to visually measure the degree of penetration of water into the center of the tablets. In addition, after 2, 4, 6, 10, and 15 times mastication, the feeling of the gel felt in the oral cavity and the sensitivity at the time of mastication are shown on a 1 to 5 point scale. The sensitivity scale was 5 good, 4 good, 3 good, 2 bad, and 1 bad.

Dust friability of the tablets was measured using a US Pharmacopoeia standard instrument (Electrolab, Friabilator (USP)).

Table 4 below shows the dissolution / gelation time, sensitivity upon chewing and dust blowing up of the tablets.

Examples and Comparative Examples Dissolution / gelation time Emotion when authoring Dust blowing Example 1 25 sec 4 0.5% Example 2 30 seconds 4 0.5% Example 3 30 seconds 4 1.0% Example 4 25 sec 4 1.0% Example 5 15 seconds 5 0.5% Comparative Example 1 Inmeasurement One 0.5% Comparative Example 2 Inmeasurement 2 0.5%

As shown in Table 4, Examples 1 to 5 all showed a good dissolution / gelation time and dust blowing ability was also similar to the comparative example. That is, in the case of the tablet prepared in Comparative Example, the dissolution rate was not measured at 30 seconds or more, whereas the tablet of the present invention was confirmed that dissolution and gelation occurred simultaneously within 30 seconds.

In addition, the formulations of the examples both at the time of chewing and at the time of chewing showed a good score or higher, whereas the comparative examples 1 and 2 without the addition of the anti-adhesive agent were found to have a bad or very bad feeling. In particular, in the case of Comparative Example 2, it was found that not only the object of purification after use fits on the teeth but also the dissolution time is very late.

Next, the time-lapse stability of the tablets prepared in Examples and Comparative Examples confirmed the state of the tablets through visual observation after temperature aging and evaluated according to the following criteria and the results are shown in Table 5 below:

◎: stable (no discoloration, no shape change, etc.)

○: relatively stable (appears slightly discolored in appearance but is not a problem in quality)

Δ: relatively unstable (discoloration in appearance, change in shape)

×: very unstable

Room temperature 40 ℃ 50 ℃ 60 ℃ Example 5 2 weeks ◎ ◎ ◎ ◎ 4 Weeks ◎ ◎ ◎ ○ 6 Weeks ◎ ◎ ◎ ○ 8 Weeks ◎ ◎ ○ ○ Comparative Example 1 2 weeks ◎ ◎ ◎ ◎ 4 Weeks ◎ ◎ ◎ ○ 6 Weeks ◎ ◎ ◎ ○ 8 Weeks ◎ ◎ ○ ○

As shown in Table 5, the time-lapse stability of the composition prepared in Example was found to be on the same level as the comparative example.

As discussed above, the simultaneous dissolving / gelling oral hygiene according to the present invention is not present in the ointment or liquid state as in the conventional products, but is characterized in that it is in a tablet formulation. The tablet-type oral hygiene of the present invention acts to maintain oral health through water or saliva or by chewing to be dissolved and gelled by direct injection into the oral cavity. As such, the formulation of the present invention has the advantage of reducing the inconvenience of the conventional liquid or ointment oral hygiene as well as easy to carry.

Claims (19)

It is prepared by tableting porous plastic granules with the essential components of porous plastic granule material, binder, gelling agent, water penetration enhancer, tooth adhesion inhibitor and moisturizer at a pressure of 500 kg / cm 2 or less, In-situ melting & gelling by, or chewing, Porous plastic granular material has a porosity of at least 0.14 and a density of at most 0.86, Water penetrant extenders include dextrates, dextrins, dextrose, fructose, lactitol, lactose, maltitol, mannitol, sorbitol, sugar, erythritol, xylitol, microcrystalline cellulose, silicified 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, A tablet anti-oral hygiene composition, characterized in that the surfactant. 2. The oral care composition of claim 1, wherein gelation occurs within 30 seconds in the oral cavity. The oral care composition of claim 1, wherein the content of the porous plastic granule material is 20 to 95 wt% based on the total weight of the tablet. The oral hygiene composition according to claim 1, wherein the content of the binder is 1 to 90% by weight based on the total weight of the tablet. The oral hygiene composition according to claim 1, wherein the content of the gelling agent is 0.1 to 10% by weight based on the total weight of the tablet. The oral hygiene composition according to claim 1, wherein the content of the water penetration extender is 20 to 80% by weight based on the total weight of the tablet. The oral hygiene composition according to claim 1, wherein the content of the anti-sticking agent is 0.01 to 10% by weight based on the total weight of the tablet. The oral hygiene composition according to claim 1, wherein the content of the moisturizing agent is 0.01 to 20% by weight based on the total weight of the tablet. The method of claim 1, wherein the porous plastic granule material is fructose, lactitol, lactitol, maltitol, maltose, mannitol, mannitol, sorbitol, sugar, erythritol erythritol, xylitol, maltodextrin, dextrin, ethylcellulose, polymethylmethacrylate, pregelatinized starch, gum arabic, xanthan gum and derivatives thereof, guar gum and derivatives thereof, seafood gum , Carrageenan, dextran, gelatin, alginate, pectin, starch and starch derivatives, cellulose esters, homo or copolymers of unsaturated acids, homo or copolymers of unsaturated amides, homo or copolymers of acrylimines, vinyl polymers, vinyl esters Homo or copolymers of alkyl glycols and polyalkylene oxides, oxyethylene alkyl esters, dexates, dextrins, dextrose, microcrystalline cellulose, yarns Ethoxylated microcrystalline cellulose, powdered cellulose, cellulose acetate, sulfuric acid, calcium carbonate, calcium phosphate, tricalcium phosphate, carboxymethyl cellulose calcium salt, silica, or the oral care composition, characterized in that a mixture thereof. delete The method of claim 1, 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, ethyl cellulose, propyl hydroxide, propylmethyl cellulose, methyl cellulose, polydextrose, polyethylene oxide, polyvinylpyrrolidone, sodium alginate, or mixtures thereof Oral hygiene composition. The gelling agent of claim 1, wherein the gelling agent is acacia gum, agar gum, gellan gum, guar gum, pectin, gelatin, alginic acid, sodium alginate, carboxymethyl cellulose, polyvinylmaleic maleic anhydride copolymer, carbopol, polyethylene glycol, Oral hygiene composition, characterized in that the polyvinylpyrrolidone, polyethylene oxide, xanthan gum, carrageenan, super porous hydrogel, or mixtures thereof. The oral care composition of claim 1, wherein the anti-sticking agent is glyceryl monooleate, glyceryl monostearate, or a mixture thereof. The oral care composition of claim 1, wherein the moisturizing agent is glycerin, polyethylene glycol, propylene glycol, sorbitol solution, or mixtures thereof. The oral care composition of claim 1, further comprising at least one selected from caries preventive, tartar preventive, gum disease preventive, antibacterial, anti-inflammatory and whitening agents in an amount of 0.001 to 10% by weight. The oral care composition of claim 1, wherein the foaming agent is further included in an amount of 0.001 to 10% by weight. 2. The oral care composition of claim 1, wherein the abrasive further comprises an amount of from 5 to 70 percent by weight. The oral care composition of claim 1, further comprising at least one of 0.001 to 10% by weight of flavoring agent and 0.001 to 20% by weight of sweetener of the total weight of the tablet. 2. The oral care composition of claim 1, wherein the glidant is further included in an amount of 0.1 to 5% by weight.

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