Tablets and methods for improving tablet disintegration

Abstract

To provide a tablet containing an active ingredient with low collapsibility when tableted, having desired tablet hardness while ensuring sufficient collapsibility.SOLUTION: A tablet contains (A) an active ingredient having a collapse coefficient (X) of 8 or more, (B) carboxymethyl cellulose or a metal salt thereof, and (C) carrageenan, where the content of the component (B) is 0.5 to 2.0 mass%, and the content of the component (C) is 3.0 to 8.0 mass%. Accordingly, a tablet containing an active ingredient with low collapsibility when tableted, having desired tablet hardness while securing sufficient collapsibility can be provided.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a tablet containing carboxymethylcellulose or a metal salt thereof and carrageenan, more specifically to a tablet containing carboxymethylcellulose or a metal salt thereof, carrageenan, and an active ingredient having a disintegration coefficient of 8 or more. [Background technology]

[0002] Pharmaceuticals and supplements contain various active ingredients to exert their medicinal effects. However, depending on the properties, type, and amount of the active ingredient, the disintegration time can be long. This can cause the active ingredient to be insufficiently absorbed by the body.

[0003] Regarding pharmaceuticals, the Japanese Pharmacopoeia states that in disintegration tests, solid pharmaceuticals must disintegrate within 30 minutes. On the other hand, there is currently no regulation requiring supplements to disintegrate within 30 minutes. However, like pharmaceuticals, there is a demand for supplements to be designed to disintegrate within 30 minutes, and in recent years, the disintegration property of supplements has also been attracting attention.

[0004] Therefore, adding a large amount of disintegrant is considered as a method for improving the disintegration property of tablets. However, adding a large amount of disintegrant reduces the hardness of the tablets, which can cause problems such as breakage during filling or distribution. At the same time, it can also cause problems such as a deterioration in the fluidity of the tableting powder. In order to improve the disintegration of tablets, it is possible to obtain tablets by reducing the tableting pressure, but in this case, the tablets will not have a hardness sufficient to withstand distribution as a product, and therefore the quality of the tablets cannot be guaranteed.

[0005] To address these problems, Patent Document 1 discloses a tablet substrate prepared by absorbing 5 to 100 parts by mass of water into 100 parts by mass of fibrous fibers having an average fiber length of 20 to 1000 μm per particle, followed by drying. Patent Document 2 discloses a composition containing a highly hygroscopic Salacia-containing composition as an active ingredient, as well as carboxymethylcellulose calcium and silicon dioxide. [Prior art documents] [Patent documents]

[0006] [Patent Document 1] Japanese Patent Publication No. 2020-152712 [Patent Document 2] Japanese Patent Application Laid-Open No. 2011-178690 Summary of the Invention [Problem to be solved by the invention]

[0007] However, even in the methods of the above-mentioned patent documents, although improvements in disintegration property and tablet hardness are observed for specific ingredients, when an active ingredient having a property that significantly reduces tablet disintegration property is used, it is not possible to achieve both the tablet disintegration property and the desired hardness that are currently required.

[0008] Therefore, an object of the present invention is to provide a tablet containing an active ingredient that has low disintegrability when made into a tablet, which has sufficient disintegrability and at the same time a desired tablet hardness. [Means for solving the problem]

[0009] As a result of intensive research into the above-mentioned problems, the present inventors have discovered that even when an active ingredient with low disintegrability when made into a tablet is used, the disintegrability of the tablet can be improved by adding a predetermined amount of carboxymethylcellulose or a metal salt thereof and carrageenan, and at the same time, the desired tablet hardness can be maintained, and have completed the present invention.

[0010] That is, the present invention provides the following [1] to [5]. [1] A tablet comprising the following components (A) to (C), wherein the content of component (B) is 0.5 to 2.0% by mass, and the content of component (C) is 3.0 to 8.0% by mass. (A) an active ingredient with a disintegration coefficient (X) of 8 or more (B) Carboxymethylcellulose or its metal salt (C) Carrageenan According to the present invention, even when an active ingredient that satisfies certain indexes and has low disintegration properties when made into tablets is used, by adding a predetermined amount of carboxymethylcellulose or a metal salt thereof and carrageenan, it is possible to provide tablets with improved disintegration properties and desired tablet hardness. As will be described in detail later, the disintegration coefficient is an index that indicates the disintegration property of a tablet when a certain active ingredient is used, and the higher the disintegration coefficient, the lower the disintegration property of the tablet when that active ingredient is used. [2] The tablet according to [1], characterized in that the disintegration score (Y) is 15 or more. According to this feature, even for tablets with lower disintegrability due to the type and blending ratio of the active ingredient or the tablet particle mass, it is possible to improve the disintegrability and provide tablets with the desired tablet hardness. [3] The tablet according to [1] or [2], characterized in that the hardness is 11 kgf or more and the disintegration time is 30 minutes or less. According to this feature, even when an active ingredient with low disintegrability when made into a tablet is used, it is possible to provide a tablet that ensures sufficient disintegrability and a desired tablet hardness. [4] The tablet according to any one of [1] to [3], wherein the component (A) is one or more selected from vitamins, minerals, and plant extracts. According to this feature, even when an active ingredient having low disintegrability when made into a tablet is used, by limiting the target active ingredient, it is possible to more reliably improve disintegrability and provide a tablet having the desired tablet hardness. [5] (A) A method for improving the disintegration property of a tablet containing an active ingredient having a disintegration coefficient (X) of 8 or more, comprising the steps of: A method for improving the disintegration property of a tablet, characterized by comprising containing (B) carboxymethylcellulose or a metal salt thereof, and (C) carrageenan. According to the present invention, it is possible to improve the disintegration property of tablets containing an active ingredient that has low disintegration property when made into tablets, and to impart a desired tablet hardness to the tablets. [Effects of the Invention]

[0011] According to the present invention, it is possible to provide tablets containing an active ingredient that has low disintegrability when made into tablets, which have sufficient disintegrability and at the same time a desired tablet hardness. DETAILED DESCRIPTION OF THE INVENTION

[0012] [tablet] The tablet of the present invention is characterized by containing (A) an active ingredient having a disintegration coefficient (X) of 8 or more, (B) carboxymethylcellulose or a metal salt thereof, and (C) carrageenan, wherein the content of component (B) is 0.5 to 2.0% by mass, and the content of component (C) is 3.0 to 8.0% by mass.

[0013] Many active ingredients incorporated into tablets tend to have a long disintegration time when incorporated in a certain amount or more. If this disintegration time is long, the active ingredient may not be sufficiently absorbed in the body, and the expected effect may not be achieved. When an active ingredient that significantly deteriorates disintegrability is incorporated into a tablet, the conventional disintegrant configurations have not been able to impart sufficient disintegrability to the tablet. The present inventors have found that by adding a predetermined amount of carboxymethylcellulose or a metal salt thereof and carrageenan as disintegrants, the tablet can acquire sufficient disintegrability. Furthermore, the tablet configuration of the present invention also has sufficient tablet hardness, which can prevent the occurrence of problems such as breakage during filling, distribution, or opening.

[0014] <Decay Factor (X)> The disintegration coefficient (X) in the present invention is an index indicating the disintegration property inherent to an active ingredient. It is determined as the disintegration time (X) minutes when a tablet containing a specific active ingredient is prepared under certain conditions (the blending ratio of the active ingredient and excipients, tableting pressure, tablet particle size, and mass). More specifically, 100 mg of the mixed powder having the composition shown in Table 1 was placed in a compression property evaluation device (manufacturer: Gamlen Instruments, model: GTP-2) and tableted using a 6 mm diameter flat punch at a compression speed of 60 mm / min and a molding pressure of 500 kgf. The disintegration time (X) minutes of the prepared tablet was then measured, and this (X) was used as the disintegration coefficient. The disintegration time was measured according to the "Disintegration Test Method" described in the Japanese Pharmacopoeia. The raw materials for each component used in the mixed powder were the same as those used in the examples described below. The hardness of the tablets prepared to determine the disintegration coefficient (X) here was set at a tableting pressure of 500 kgf, which is not a value suitable for distribution as a product (hardness of 11 kgf or less). Therefore, the disintegration coefficient (X) is merely an index showing the disintegration property of the active ingredient, and is distinct from the object of the present invention, which is to limit the disintegration time of a tablet to 30 minutes or less.

[0015] The disintegration coefficient (X) of the active ingredient of the present invention is not less than 8, and preferably not less than 10. When the disintegration coefficient (X) is not less than 8, the effect of improving the disintegration property of the tablet of the present invention can be more significantly exhibited. Note that the disintegration coefficient (X) of aronia extract, which is generally considered to have poor disintegration property when made into a tablet, is 8.4, that of salacia extract is 14.5, and that of agrimony extract is 15.5.

[0016] [Table 1]

[0017] <Collapse score (Y)> The disintegration score (Y) of the present invention is an index that serves as a guide for the disintegration property of a tablet, and is calculated using the following formula 1, taking into account the disintegration coefficient (X) and the active ingredient content and tablet mass as tablet parameters that are expected to affect the disintegration time.

[0018]

number

[0019] In this way, the disintegration score (Y) can be calculated from the disintegration coefficient (X) and the specific tablet composition, and the higher the disintegration score (Y), the lower the tablet's disintegration ability. Furthermore, by analyzing the relationship between the disintegration score (Y) and the actual disintegration time, it can be used to evaluate or estimate the effect of the disintegrant and other components on the tablet's disintegration ability.

[0020] The disintegration score (Y) of the tablet of the present invention is preferably 15 or more, more preferably 20 or more. If the disintegration score (Y), which is an index of disintegration, is 15 or more, the disintegration of the tablet may cause problems in the absorption of the contained active ingredient. However, even if the tablet has a disintegration score (Y) exceeding this standard, by blending a predetermined amount of carboxymethylcellulose or a metal salt thereof and carrageenan, it is possible to sufficiently shorten the disintegration time and produce a tablet having the desired tablet hardness. There is no particular upper limit for the disintegration score (Y), but it is preferably 80 or less, more preferably 60 or less. A disintegration score of 60 or less ensures the appropriate form and use of the tablet.

[0021] <Tablet Form> (Collapse time) The disintegration time of the tablet of the present invention is preferably within 30 minutes, more preferably within 25 minutes. The standard of within 30 minutes is specified in the Japanese Pharmacopoeia for pharmaceuticals, which stipulates that the disintegration time of uncoated tablets must be within 30 minutes. If the disintegration time exceeds 30 minutes, for example, the active ingredient may not be sufficiently absorbed in the digestive tract, the required blood concentration may not be achieved, or the bioavailability may be reduced, and the expected effect may not be achieved.

[0022] (Tablet hardness) The tablets of the present invention preferably have a hardness of 11.0 kgf or more. This standard was established as a required value when considering the phenomenon of "hardness reduction" that may occur in actual production. A tablet hardness of 11.0 kgf or more can prevent breakage of the tablets during distribution, filling, or when removing them from PTP (Press Through Pack) packaging. The tablet hardness can be set by selecting the raw materials and the tableting pressure during tablet production.

[0023] (Size and Mass) The size of the tablet of the present invention is not particularly limited. It can be changed depending on the purpose of use of the tablet, its form, the desired disintegration property, the subject of administration, etc., but for example, the diameter of the tablet is 6 to 10 mm. The lower limit of the tablet diameter is preferably 6 mm or more. The upper limit of the tablet diameter is preferably 10 mm or less. The mass of the tablet particles is not particularly limited. It can be changed depending on the compounding ratio of the active ingredient, the desired disintegration property, or the density and size of the tablet, but is, for example, 150 to 500 mg. The lower limit of the mass of the particles is preferably 150 mg or more. The upper limit of the mass of the particles is preferably 500 mg or less.

[0024] (Properties) The tablet form is not particularly limited as long as it exhibits the effects of the present invention, and various forms are possible. Examples include ordinary tablets, orally disintegrating tablets, vaginal tablets, adhesive tablets, sublingual tablets, etc., but ordinary tablets and orally disintegrating tablets are preferred, and ordinary tablets are more preferred in terms of ensuring storage stability and ease of designing tablet hardness.

[0025] <(A) Active ingredient with a disintegration coefficient (X) of 8 or more> As described above, the tablet of the present invention contains an active ingredient having a disintegration coefficient (X) of 8 or more. The active ingredient refers to a substance that exhibits a desired physiological activity when the tablet is taken into the body. The substance that serves as the active ingredient is not particularly limited, and may be, for example, a general physiologically active substance used in pharmaceuticals, quasi-drugs, over-the-counter drugs, herbal medicines, natural medicines, cosmetics, health foods, nutrient-functional foods, foods for specified health uses, foods for special dietary uses, supplements, veterinary drugs, etc.

[0026] The tablet of the present invention can be more preferably used for food or supplement applications. Compared to pharmaceuticals, food and supplements generally contain multiple active ingredients. According to the configuration of the present invention, not only is it effective for a single active ingredient, but even when multiple active ingredients are contained, it can have a significant effect on the disintegration and tablet hardness of the active ingredients or the entire tablet.

[0027] The active ingredient of the present invention is preferably an ingredient that reduces the disintegration property of tablets when incorporated into the tablet. Even when such an active ingredient is incorporated into the tablet, by incorporating a predetermined amount of carboxymethylcellulose or a metal salt thereof and carrageenan, it is possible to produce a tablet having a desired tablet hardness while sufficiently improving the disintegration property.

[0028] The content of the active ingredient (A) having a disintegration coefficient (X) of 8 or more in the tablet of the present invention is not particularly limited and can be changed depending on the type of active ingredient, the potency related to physiological activity, the form of the tablet, the desired disintegrability and hardness, etc., but is, for example, 5 to 80% by mass. The lower limit of the content of this ingredient (A) is preferably 10% by mass or more. The upper limit of the content of ingredient (A) is preferably 70% by mass or less. If the content of ingredient (A) is 5% by mass or more, appropriate medicinal efficacy can be obtained, and if it is 80% by mass or less, it is easy to adjust the desired hardness, disintegrability, dissolution, etc. Furthermore, when two or more active ingredients are blended, even if the disintegration coefficient of the active ingredient alone is 8 or less, the composite material can be used as the active ingredient of the present invention as long as the composite material has a disintegration coefficient of 8 or more. Note that the disintegration coefficient of the composite material is not derived by calculation from the disintegration coefficients of the individual ingredients, but is the actual value measured by applying the composite material to the formulation in Table 1 and measuring it, and this value is taken as the disintegration coefficient (X).

[0029] More specific examples of active ingredients include vitamins such as carotene, vitamin B, vitamin C, and folic acid; minerals; amino acids such as glycine, glutamine, and ornithine; amino sugars such as glucosamine and N-acetylglucosamine; proteins such as collagen and elastin; mucopolysaccharides such as chondroitin; various nucleic acids such as DNA; various flavonoids such as catechin and polyphenols; carotenoids such as astaxanthin, lycopene, and lycopene; phospholipids such as phosphatidylserine and phosphatidylcholine; fatty acids such as EPA and DHA; ubiquinones such as coenzyme Q10; enzymes; dietary fiber; herbs, fruits, and plants and their extracts; fish oil; probiotic bacteria such as lactic acid bacteria; and yeast extracts such as cysteine ​​peptide-containing yeast extract.

[0030] (vitamin) Vitamins in the tablet of the present invention are not particularly limited, but examples thereof include vitamins belonging to the vitamin A group, such as retinal, retinol, retinoic acid, carotene, dehydroretinal, lycopene, and pharmacologically acceptable salts thereof, thiamine, thiamine disulfide, dicethiamine, octotiamine, shikotiamine, bis-ibutiamine, bis-bentiamine, prosultiamine, benfotiamine, fursultiamine, riboflavin, flavin adenine dinucleotide, pyridoxine, pyridoxal, hydroxocobalamin, cyanocobalamin, methylcobalamin, deoxyadenocobalamin, folic acid, tetrahydrofolic acid, dihydrofolic acid, nicotinic acid, nicotinamide, nicotinic alcohol, pantothenic acid, panthenol, biotin, choline, inositol, and panthenol. Vitamins belonging to the vitamin B group, such as gallic acid and pharmacologically acceptable salts thereof; vitamins belonging to the vitamin C group, such as ascorbic acid and derivatives thereof, erythorbic acid and derivatives thereof, and pharmacologically acceptable salts thereof; vitamins belonging to the vitamin D group, such as ergocalciferol, cholecalciferol, hydroxycholecalciferol, dihydroxycholecalciferol, dihydrotachysterol, and pharmacologically acceptable salts thereof; vitamins belonging to the vitamin E group, such as tocopherol and derivatives thereof, ubiquinone derivatives, and pharmacologically acceptable salts thereof; and other vitamins, such as carnitine, ferulic acid, γ-oryzanol, orotic acid, rutin (vitamin P), eriocitrin, hesperidin, and pharmacologically acceptable salts thereof. These vitamins may be formulated alone or in combination of two or more.

[0031] (mineral) The minerals in the tablet of the present invention are not particularly limited, but examples thereof include calcium, phosphorus, magnesium, potassium, iron, manganese, selenium, copper, chloride, molybdenum, chromium, zinc, and iodine salts thereof. These minerals may be blended alone or in combination of two or more.

[0032] (Plant extract powder) The plant extract powder that can be used in the tablet of the present invention is not particularly limited. Powdered extracts can be obtained, for example, by extracting fruits, seeds, leaves, etc., or their pulverized products with water or polar solvents such as various organic solvents, or by steam distillation, and then adding additives such as excipients as necessary and drying the resulting extract. Commercially available products can also be used regardless of the production method.

[0033] More specifically, the plant extract powder is one or more selected from bacopa extract, artichoke extract, ginkgo leaf extract, bilberry extract, milk thistle extract, agrimony extract, and African mango extract. These plant extracts may be blended alone or in combination of two or more.

[0034] <(B) Carboxymethylcellulose or its metal salt> The tablet of the present invention contains carboxymethylcellulose or a metal salt thereof. Carboxymethylcellulose is a compound obtained by esterifying the hydroxyl groups in cellulose, and crosslinked polymers thereof or salts thereof are commonly used as disintegrants. The carboxymethylcellulose or metal salt thereof that can be used in the present invention is not particularly limited, but examples include carboxymethylcellulose, potassium carboxymethylcellulose, calcium carboxymethylcellulose, sodium carboxymethylcellulose, and croscarmellose sodium. Carboxymethylcellulose sodium and calcium carboxymethylcellulose, which do not have intramolecular crosslinks, are more preferably used because they have appropriate disintegrability. Of these, sodium carboxymethylcellulose, which does not have a chelate structure, is even more preferably used. These can be produced by known methods, or commercially available products can be used.

[0035] The content of (B) carboxymethylcellulose or a metal salt thereof in the tablet of the present invention is 0.5 to 2.0% by mass. The lower limit of the content of this component (B) is preferably 1.0% by mass or more. The upper limit of the content of component (B) is preferably 2.0% by mass or less. If the content of component (B) is less than 0.5% by mass, sufficient tablet disintegration may not be achieved, and the active ingredient may not exhibit the expected effect. If the content of component (B) exceeds 2.0% by mass, the tablet hardness may not be maintained at the desired level, and the tablet may break during distribution, filling, or when removing the tablet from the PTP.

[0036] <(C) Carrageenan> The tablet of the present invention contains carrageenan. Carrageenan is a polysaccharide naturally extracted mainly from red algae. Carrageenan is a galactan having a linear structure consisting of alternating α(1→3) and β(1→4) bonds, and some or all of the β(1→4)-linked galactose units exist as 3,6-anhydro-D-galactose and its sulfate ester. Carrageenan is classified into three types, kappa, iota, and lambda, depending on the amount of sulfate groups and anhydro groups contained in the molecule. Any of these types, or a mixture of these, can be used. Among these, from the viewpoints of disintegration property and tablet hardness, a mixture containing kappa carrageenan or kappa carrageenan is preferred, and kappa carrageenan is more preferred.

[0037] The content of (C) carrageenan in the tablet of the present invention is 3.0 to 8.0% by mass. The lower limit of the content of (C) carrageenan is preferably 5.0% by mass or more. The upper limit of the content of (C) carrageenan is preferably 6.0% by mass or less. If the content of (C) carrageenan is less than 3.0% by mass, sufficient tablet disintegration properties may not be obtained, and the active ingredient may not exhibit the expected effect. If the content of (C) carrageenan exceeds 8.0% by mass, the tablet hardness may not be maintained at the desired level, and the tablet may break during distribution, filling, or when removing the tablet from the PTP.

[0038] <Other ingredients> The tablet of the present invention may contain additives such as excipients, binders, lubricants, stabilizers, preservatives, fluidizing agents, thickeners, colorants, etc. Furthermore, disintegrants other than carboxymethylcellulose or its metal salts and carrageenan may be contained within the range in which the effects of the present invention are achieved.

[0039] The excipient is not particularly limited, and examples thereof include microcrystalline cellulose, lactose, sucrose, mannitol, glucose, starch, calcium phosphate, calcium sulfate, etc. These excipients may be used alone or in combination of two or more. The addition of an excipient can adjust the volume of the useful substance.

[0040] The binder is not particularly limited, and examples thereof include hydroxyethyl cellulose, hydroxypropyl methylcellulose, hydroxypropyl cellulose, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic acid, polymethacrylic acid, glucose, sucrose, lactose, maltose, dextrin, sorbitol, mannitol, macrogol, paraffin, gum arabic, gelatin, agar, starch, starch hydrolysates, and pullulan. These binders may be used alone or in combination of two or more. The addition of a binder provides binding strength to the powder ingredients contained in component (A) while simultaneously increasing fluidity, allowing for the production of stable tablets.

[0041] The lubricant is not particularly limited, and examples thereof include talc, colloidal silica, magnesium stearate, calcium stearate, magnesium carbonate, sodium benzoate, palmitic acid, sodium stearyl fumarate, waxes, hydrogenated vegetable oils, fats, polyethylene glycol, etc. These lubricants may be blended alone or in combination of two or more. Addition of a lubricant can prevent tableting problems such as sticking during tablet production.

[0042] The other disintegrants are not particularly limited as long as they exhibit the effects of the present invention, and examples thereof include corn starch, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, sodium carboxymethyl starch, cross-polyvinylpyrrolidone, alginate, etc. These disintegrants may be blended alone or in combination of two or more.

[0043] [Tablet manufacturing method] There are no particular limitations on the method for manufacturing the tablets of the present invention, and the present invention used as a food or pharmaceutical can be manufactured using known additives that are acceptable for food or pharmaceutical use, and conventional formulation methods used in the food or pharmaceutical fields can be applied.

[0044] For example, there are methods in which various raw materials such as active ingredients, excipients, binders, lubricants, etc. are mixed and compressed into tablets, and methods in which various raw materials are granulated by agitation mixing granulation method or fluidized bed granulation method, and then a lubricant is added and mixed, followed by compression. However, the timing of adding tablet ingredients is not limited to these.

[0045] The apparatus used for tableting may be, for example, a general tableting apparatus such as a rotary tableting machine used for producing tablets. In the case of tablets with a diameter of 6 to 10 mm, the tableting pressure during tableting is preferably 500 to 2000 kgf.

[0046] [Other embodiments] The present invention also provides a method for imparting disintegrability and tablet hardness to a composition using an active ingredient that has low disintegrability when made into a tablet, or to a pulverized product obtained by pulverizing a tablet. For example, tablets having sufficient disintegrability and a desired tablet hardness can be produced by adding a predetermined amount of carboxymethylcellulose or a metal salt thereof and carrageenan to the composition or pulverized product, followed by granulation and tableting. The timing of adding carboxymethylcellulose or a metal salt thereof and carrageenan is not limited, and when the composition contains carboxymethylcellulose or a metal salt thereof or carrageenan, the addition may be performed so that the composition after addition reaches the predetermined amount according to the present invention. [Example]

[0047] Hereinafter, examples of the present invention will be described, but the present invention is not limited to these examples, and various modifications are possible within the technical concept of the present invention.

[0048] (1) Test Example 1: Effect of combining carboxymethylcellulose or its metal salt with carrageenan in tablets containing multivitamins Tests were conducted to examine the effect of blending carboxymethylcellulose or its metal salt with carrageenan in tablets containing multivitamins (vitamins and minerals) as the active ingredient. More specifically, tablets in Examples 1 to 9 and Comparative Examples 1 to 8 were produced with the blends shown in Tables 3 to 5, and the tablet hardness and disintegration properties were measured and evaluated. The raw materials used in the examples are shown in Table 2 below.

[0049] [Table 2]

[0050] <Tablet manufacturing> Tablets of the examples and comparative examples were produced according to the following procedure. The raw materials were mixed at the raw material blending ratio (mass%) shown in Table 3, triturated, and sieved to prepare powder for tableting. The prepared powder for tableting was compressed using a single punch tableting machine N-30E (manufactured by Okada Seiko Co., Ltd.) with a punch shape of φ8 mm and R6 and a tableting pressure of 1000 kgf to obtain tablets with a diameter of approximately 8 mm and a particle mass of 250 mg.

[0051] <Tablet hardness measurement> The hardness of the tablets produced in the above tablet production was measured using a New Speed ​​Checker TS-75N (manufactured by Okada Seiko Co., Ltd.). The average value of five sample tablets was measured, and the average value was taken as the tablet hardness. The tablet hardness was evaluated according to the following evaluation criteria.

[0052] (Evaluation criteria for tablet hardness) 〇: Tablet hardness 11.0 kgf or more ×: Tablet hardness less than 11.0 kgf

[0053] <Tablet disintegration test> The disintegration time of the produced tablets was measured according to "6.09 Disintegration Test Method" described in the general testing methods of the "17th Edition of the Japanese Pharmacopoeia." Ion-exchanged water was used as the test liquid. The disintegration tester used was a disintegration tester manufactured by Toyama Sangyo Co., Ltd. (NT-610 (trade name), manufactured by Toyama Sangyo Co., Ltd.).

[0054] The test was performed using a test liquid (purified water) volume of 900 mL, and the disintegration time in water at 37°C was measured for 6 sample tablets, and the average value was taken as the disintegration time. Disintegrability was evaluated based on the disintegration time according to the following evaluation criteria.

[0055] (Evaluation criteria for disintegration) 〇: Disintegration time is 30 minutes or less ×: Disintegration time exceeds 30 minutes

[0056] <Overall rating> As an overall evaluation of the tablets, those that met the criteria for both the hardness test and the disintegration test were given a ◯, and others were given an ×. Overall evaluation: Tablet hardness test: 〇, disintegration test: 〇 Overall rating: ×: Tablet hardness test: 〇, disintegration test: × Overall rating: ×: Tablet hardness test ×, disintegration test 〇

[0057] [Table 3]

[0058] The vitamin and mineral composition and disintegration coefficient (X) of the active ingredients in one 250 mg tablet of the multivitamin and mineral used in this test example are shown in Tables 4 and 5. The disintegration coefficient (X) of the total active ingredients in this example was 12.6, and the disintegration score (Y) was 20.1.

[0059] [Table 4]

[0060] [Table 5] The vitamin B oil-coated raw material is a food additive preparation in which B vitamins are granulated and coated with oil (hardened rapeseed oil, 25%).The mineral oil-coated raw material is a food additive preparation in which yeast containing zinc gluconate, ferric pyrophosphate, copper gluconate, and minerals is granulated and coated with oil (hardened rapeseed oil, 25%).

[0061] As a result of the test, tablets containing multivitamins and minerals were able to achieve both the desired tablet hardness (11.0 kgf or more) and sufficient disintegrability (disintegration time within 30 minutes) when a specified amount of carboxymethylcellulose sodium or carboxymethylcellulose calcium and carrageenan was blended (Examples 1 to 9). On the other hand, when either carboxymethylcellulose sodium or carboxymethylcellulose calcium and carrageenan were not blended (Comparative Examples 1, 2, 4, and 5), or when the blending amounts of carboxymethylcellulose sodium or carboxymethylcellulose calcium and carrageenan deviated from the blending amounts of the present invention (Comparative Examples 3, 6, and 7), they failed to meet the standards for either tablet hardness or disintegrability.

[0062] Furthermore, when starch (Comparative Example 8), a widely used disintegrant, was added in the prescribed amount according to the present invention instead of sodium carboxymethylcellulose or calcium carboxymethylcellulose, the disintegrability criteria could not be met.

[0063] (2) Test Example 2: Effect of combining carboxymethylcellulose or its metal salt with carrageenan in tablets containing plant extract powder To examine the effect of blending carboxymethylcellulose or its metal salt with carrageenan in tablets containing plant extracts as active ingredients, tablets were produced in the same manner as in Test Example 1 for the Examples and Comparative Examples shown in Table 6, and tests were conducted on tablet hardness and disintegration. In Test Example 2, bacopa extract powder and matured hop extract were used as the plant extract powder. The disintegration coefficients (X) of the active ingredients were 14.0 for bacopa extract powder and 8.2 for matured hop extract. The disintegration coefficient (X) of the composite material was 10.65. The disintegration score (Y) in this test example was 15.4.

[0064] [Table 6]

[0065] As a result of the test, when the tablets containing plant extract powder were blended with predetermined amounts of sodium carboxymethylcellulose and carrageenan (Examples 10 and 11), the desired tablet hardness (11.0 kgf or more) and sufficient disintegrability (within 30 minutes) were achieved. On the other hand, when neither sodium carboxymethylcellulose nor carrageenan was included (Comparative Examples 9 and 10), the disintegrability criteria could not be met. [Industrial Applicability]

[0066] The present invention can provide tablets containing an active ingredient that has low disintegrability when formed into tablets, which can ensure sufficient disintegrability while at the same time having a desired tablet hardness. The present invention can be utilized in designing the composition of tablets in various fields, such as pharmaceuticals, quasi-drugs, veterinary products, foods, and supplements, depending on the intended use.

Claims

1. The composition contains the following components (A) to (C), wherein the content of the component (B) is 0.5 to 2.0 mass % and the content of the component (C) is 3.0 to 8.0 mass %, A tablet characterized in that the component (A) contains one or more selected from vitamins, minerals, and plant extract powders. (A) an active ingredient having a disintegration coefficient (X) of 8 or more (B) Carboxymethylcellulose or its metal salt (C) Carrageenan

2. The tablet according to claim 1, characterized in that the disintegration score (Y) is 15 or more.

3. 3. The tablet according to claim 1 or 2, characterized in that the tablet has a hardness of 11 kgf or more and a disintegration time of 30 minutes or less.

4. (A) A method for improving the disintegration property of a tablet containing an active ingredient having a disintegration coefficient (X) of 8 or more, comprising the steps of: The component (A) contains one or more selected from vitamins, minerals, and plant extract powders, A method for improving the disintegration property of a tablet, comprising incorporating (B) carboxymethylcellulose or a metal salt thereof, and (C) carrageenan.

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