JP2003192577A - Masticatory composition - Google Patents

Abstract

<P>PROBLEM TO BE SOLVED: To provide a masticatory composition excellent in sustained release property of a medicinal ingredient and feelings upon use and having high effect of preventing oral diseases. <P>SOLUTION: This masticatory composition comprises a disintegrative granules composed of inorganic powder, an organic polymer and a medicinal ingredient and having 0.06-20 kg/piece disintegrative load. <P>COPYRIGHT: (C)2003,JPO

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to disintegrating granules containing a medicinal ingredient, thereby improving the sustained release of the medicinal ingredient and preventing oral diseases. The present invention relates to a chewing composition having a good feeling in use. [0002] Conventionally, mastication compositions have been used as palatability items, but in recent years, they have attracted attention as oral medicine preventive agents by blending medicinal components. It has been proposed to mix dextranase in chewing gum as an anti-caries chewing composition (JP-A-56-88758). In addition, a technique of blending a medicinal component into a granule has been conventionally known, and it has been proposed to blend a granule blended with a medicinal component into an oral composition (JP-A-03-271215, JP-A-Hei-04). -124123, JP-A-04-
243815). However, when an active ingredient is directly added to chewing gum, most of it is eluted at the beginning of chewing, and its effectiveness cannot be maintained in the mouth for a long time. In addition, when the conventionally known granules are mixed with chewing gum, the inorganic powder is separated and the feeling of use is not good, and the sustained release effect is not good due to easy disintegration. Therefore, there is still room for study on the sustained-release properties and feeling of use of the medicinal component. Further, there is a demand for the development of a chewable composition that improves the sustained release of medicinal components, enhances the effect of preventing oral diseases, and has a good feeling in use. [0003] It is an object of the present invention to provide a chewing composition which is excellent in sustained release of a medicinal component, has a high effect of preventing oral diseases, and has an excellent feeling upon use. The inventors of the present invention have made intensive studies to solve the above-mentioned problems, and as a result, have accomplished the present invention. That is, according to the present invention, it is characterized by containing disintegrable granules comprising an inorganic powder, an organic polymer, and a medicinal component, wherein the disintegration granules have a disintegration load of 0.06 to 20 kg / piece. Is provided. DETAILED DESCRIPTION OF THE INVENTION The disintegration strength of granules used in the present invention is measured by a SUNRHEO METERMode manufactured by Sun Kagaku Co., Ltd.
l Measured using CR-200D, one granule was placed at an interval between two hard surfaces, and this was loaded at a loading speed of 3 mm
Means the load at which the granules begin to disintegrate when compressed at a rate of / min. In the present invention, the collapse load is preferably in the range of 0.06 to 20 kg / piece, particularly 0.5 to 10 kg / piece. Granules having a disintegration load of less than 0.06 kg may have a reduced sustained release property or the granules may be disintegrated during the production of the mastication composition. A foreign-body sensation is felt, and it does not disintegrate at all even by mastication, and may be inferior in use feeling. The mixing ratio (weight ratio) of the inorganic powder and the organic polymer in the granules is preferably in the range of 3: 1 to 1: 3, particularly 2: 1 to 1: 2. When the mixing ratio of the inorganic powder and the organic polymer is more than 3: 1, granules may be separated from the chewing composition and the feeling in use may be reduced, while the mixing ratio of the inorganic powder and the organic polymer is 1: If it is smaller than 3, there is a problem that the sustained release of the medicinal component is reduced. The average particle size of the granules is 100 to 3000 μm, especially 300 to 2 μm.
It is desirable to be in the range of 000 μm. Average particle size is 1
If it is less than 00 μm, problems such as a decrease in particle strength and a decrease in sustained release may occur. If it is more than 3000 μm, there is a problem that a foreign substance sensation is produced when it is blended in the chewing composition. [0007] As the organic polymer compounded in the granules,
Conventionally known various materials used for gum bases, toothpastes, and the like are used. Such organic polymers include any of water-insoluble and water-soluble polymers. For example,
Examples of the water-insoluble polymer include polyvinyl acetate, chicle, and gelton. Examples of the water-soluble polymer include carboxymethyl cellulose alkali metal salts, methyl cellulose, hydroxyethyl cellulose, cellulose derivatives such as sodium carboxymethyl hydroxyethyl cellulose, alkali metal alginate such as sodium alginate, propylene glycol alginate, carrageenan, xanthan gum, tragacanth gum,
Gums such as karaya gum and gum arabic; and synthetic binders such as polyvinyl alcohol, sodium polyacrylate and polyvinyl vilolidone. The compounding amount is preferably 1 to 50% in the granule, and more preferably 5 to 50%.
It is good to be 40%, more preferably 10 to 30%. [0008] As the inorganic powder to be incorporated into the granules, various conventionally known inorganic powders used for dentifrices and the like are used. Examples of such substances include precipitated silica, silica gel, aluminosilicate, silica-based abrasives such as zirconosilicate, dibasic calcium phosphate dihydrate and anhydride, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, Alumina, magnesium carbonate, tertiary magnesium phosphate, zirconium silicate and the like can be mentioned. These inorganic powders are usually 0.1 to 10
Those having an average particle diameter of 0 μm are used, and those having an average particle diameter of 0.5 to 50 μm are preferably used. The compounding amount is preferably 1 to 50% in the granule, preferably 10 to 40%.
% Is better. As the medicinal component to be incorporated into the granules, various conventionally known components can be used. As such, for example, enzymes such as dextranase, mutanase, amylase, protease, lysozyme, lytic enzyme,
Fluorides such as sodium fluoride, potassium fluoride, stannous fluoride, strontium fluoride and sodium monofluorophosphate; water-soluble phosphate compounds such as potassium and sodium orthophosphoric acid; allantoinchlorohydroxyaluminum , Hinokitiol, ascorbic acid, lysozyme chloride, glycyrrhizic acid and its salts, sodium chloride, tranexamic acid, epsilon aminocaproic acid,
Dl-tocopherol acetate, α-bisabolol, isopropylmethylphenol, chlorhexidine salts, cetylpyridinium chloride, azulene, glycyrrhetinic acid, copper chlorophyllin sodium, copper compounds such as copper gluconate, aluminum lactate, strontium chloride, potassium nitrate, berberine, hydroxamic acid and In addition to its derivatives, sodium tripolyphosphate, methoxyethylene, maleic anhydride copolymer, polyvinylpyrrolidone, epidihydrocholesterine, benzethonium chloride, dihydrocholesterol, trichlorocarbanide, zinc citrate, soft touki extract, oak extract, clove, Examples include plant extracts such as rosemary, ogre, safflower, vitamins, and the like. The compounding amount of the medicinal component may be any effective amount and is not particularly limited.
The amount is 001 to 5%, preferably 0.01 to 3%. In the granules, in addition to the above ingredients, flavors, acidulants,
A coloring agent, a pH adjuster, a preservative and the like can be appropriately compounded. The shape of the granules is more preferably spherical, but may be pulverized mass. Also, granules are
Polynuclear granules in which the inorganic powder is dispersed in the organic polymer may be used, or granules having a structure in which the inorganic powder is simply bonded to the organic polymer may be used. [0011] The mastication composition of the present invention is characterized by containing the above granules, and the form of the composition may be any form suitable for mastication, for example, a sheet, granule, sphere, block ( Cuboid). The composition of the present invention can be produced by blending the granules in a chewing base, further blending auxiliary components, and molding into a desired shape. The chewing base in this case can be a conventional gum base. In the composition of the present invention, the ratio of granules is preferably 0.1 to 50%, and more preferably 1 to 50%.
It is good to be ~ 20%. The composition of the present invention preferably contains, in addition to the granules, a sweetener, a cleaning agent, an abrasive, and a fragrance commonly used in oral compositions. As a sweetener, glucose, xylose, monosaccharides such as fructose, reducing disaccharides such as maltose, sucrose, non-reducing disaccharides such as trehalose, xylitol, erythritol, sorbitol, lactitol, sugar alcohols such as maltitol, Reduced balatinose, palatinose, lactose, reduced lactose, reduced maltose syrup, reduced syrup, oligosaccharides,
One or several types of glucose, reduced starch saccharified matter, fructose, aspartame, stevia, and saccharin can be arbitrarily blended. As the cleaning agent, various conventionally known cleaning agents used for toothpaste and the like are used. Examples of the inorganic polishing agent include precipitated silica, silica gel, aluminosilicate, silica polishing agents such as zirconosilicate, dibasic calcium phosphate, dihydrate and anhydride, calcium pyrophosphate, calcium carbonate, aluminum hydroxide, Alumina, magnesium carbonate, tertiary magnesium phosphate,
Zirconium silicate and the like can be mentioned. Examples of the synthetic resin-based abrasive include polyethylene beads and polypropylene beads. These abrasives are usually 0.1 to
Those having an average particle diameter of 100 μm are used, and preferably those having an average particle diameter of 0.5 to 50 μm are used. [0013] As the fragrance, natural flavors such as pevermint oil, spearmint oil, anise oil, eucalyptus oil, winter green oil, cassia oil, clove oil, thyme oil,
Sage oil, lemon oil, orange oil, peppermint oil, cardamom oil, coriander oil, mandarin oil, lime oil, lavender oil, rosemary oil / laurel oil, camomil oil,
Caraway oil, marjoram oil, bay oil, lemongrass oil, origanum oil, pine needle oil and the like.
Further, as a single item flavor, menthol, carvone, anethole, cineol, methyl salicylate, cinamic aldehyde, eugenol, thymol, linalool, linalool acetate, limonene, mentone, menthyl acetate, pinene, octyl aldehyde, citral, pregon, carbyl acetate, Anisaldehyde, ethyl acetate, ethyl butyrate, allyl cyclohexane propionate, methyl anthranilate, ethyl methyl anthranilate, vanillin, undecalactone,
Examples include hexanal, ethyl alcohol, propyl alcohol, butanol, and isoamyl alcohol. Examples of the compounded flavors that also include a single flavor and / or a natural flavor include strawberry flavor, apple flavor, banana flavor, pineapple flavor, grape flavor, mango flavor, tropical fruit flavor, butter flavor, milk flavor, fruit mix flavor, and the like. In addition to the above components, gum base, acidulant, softener, colorant, brightener, thickener, emulsifier, pH adjuster,
Preservatives and the like can be appropriately compounded. In addition, vitamins, plant extracts and the like can be appropriately blended. Each of the above-mentioned additive components can be used in a usual amount conventionally used. The chewing composition of the present invention has improved sustained release of medicinal components, and has a high oral disease prevention effect. Next, the present invention will be described in more detail by way of examples. Reference Example 1 Granules A and B having the component compositions (%) shown in Table 1 were prepared as follows. (Preparation method of granules) The ground vinyl acetate resin powder and dicalcium phosphate are mixed. Separately, sodium alginate is dissolved in a small amount of water to form a paste. After mixing the powder and the pasty solution, the mixture was granulated by an extrusion-type granulator and dried. The dried granules were pulverized and classified to obtain granules A.
Similarly, granules B were obtained. In the granules A and B, the particle size was about 1000 μm, and the collapse load was about 3 kg / piece. [Table 1] *: 10,000 units / g of dextranase Examples 1-2, Comparative Example 1 A chewing composition (chewing gum) having the component composition (parts) shown in Table 2 was prepared by a conventional method. [Table 2] Experimental Example 1 (Release effect of medicinal components) 2 g of each sample was chewed for 10 minutes to collect saliva every 1 minute, and the dextranase activity in the saliva was measured by the Somogi method. Table 3 shows the results. One unit of dextranase is an enzymatic activity that produces a reducing sugar equivalent to 1 μmol of glucose per minute at 40 ° C. [Table 3] The compositions of Examples 1 and 2 showed higher dextranase activity after 5 minutes of mastication than the composition of Comparative Example 1, indicating that the sustained release was high. Experimental Example 2 (Effect of plaque adhesion inhibition)
(Patient Hygiene Performance) method was used to evaluate plaque adhesion. As the specific teeth, a total of six teeth were used on the buccal side of the upper left and right # 6, the lingual side of the lower right and left # 6, and the lip side of the upper right # 1 and the lower left # 1. After the test subject was bitten by erythrosin Wafer and stained, each tooth was divided into five parts. If there was plaque in each part, one point was added, and if not, zero point was given. The average score per tooth was calculated for each person (up to 5 points). The scores were compared using each sample for 2 weeks. Table 4 shows the results. It was found that Examples 1 and 2 exhibited a higher plaque suppressing effect than that of Comparative Example 1. [Table 4] Reference Example 2 Granules C, D and E were prepared in the same manner as in Reference Example 1, except that a mixture having the component composition (%) shown in Table 5 was used. Each of these granules has a particle size of about 15
The collapse load was about 2 kg / piece. [Table 5] Examples 3 to 8 Using the granules obtained in Reference Example 2, the component compositions (parts) shown in Table 6 were used.
Was prepared. All of these compositions were excellent in the sustained release properties of the medicinal components and the effect of inhibiting plaque adhesion. [Table 6]

──────────────────────────────────────────────────続 き Continued on the front page (51) Int.Cl. ⁷ Identification symbol FI Theme coat ゛ (Reference) A61K 47/32 A61K 47/32 47/36 47/36 A61P 1/02 A61P 1/02 // A61K 38 / 46 A61K 37/54 F term (reference) 4B014 GB13 GK10 GK12 GL01 GL03 4C076 AA69 AA95 BB01 BB22 BB23 CC21 CC31 DD26 DD38 EE07 EE30 FF02 FF05 FF31 FF68 4C084 AA03 BA44 DC22 MA01 MA34 MA52 MA57 NA12 NA12

Claims (1)

Claims 1. Disintegrable granules comprising an inorganic powder, an organic polymer, and a medicinal component, wherein the disintegration load is 0.06 to 2
A chewing composition comprising disintegrating granules of 0 kg / piece.