Tablet and method for improving tablet disintegration

Abstract

To provide a tablet with sufficient disintegration and desired tablet hardness, in tablets containing an active ingredient with low disintegration when formed into a tablet.SOLUTION: Provided is a tablet containing: (A) an active ingredient having a disintegration coefficient (X) of 8 or more; (B) sodium carboxymethylcellulose; and (C) agar, the content of the component (B) being 0.5 to 2.0 mass%, and the content of the component (C) being 1.0 to 7.0 mass%. As a result, it is possible to provide a tablet having a desired tablet hardness while ensuring sufficient disintegration, in tablets containing an active ingredient with low disintegration when formed into a tablet.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to a tablet containing sodium carboxymethylcellulose and agar, more particularly to a tablet containing sodium carboxymethylcellulose, agar, and an active ingredient having a disintegration coefficient of 8 or more. [Background technology]

[0002] Various active ingredients are blended into medicines and supplements to exert their medicinal effects. However, depending on the nature, type, and amount of the active ingredient, the disintegration time may be long. This causes the problem that the active ingredient is not sufficiently absorbed by the body.

[0003] Regarding pharmaceuticals, the Japanese Pharmacopoeia states that pharmaceuticals in their pure form must disintegrate within 30 minutes in disintegration tests. On the other hand, there is currently no regulation for supplements that requires disintegration time to be 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, as a method for improving the disintegration of tablets, it is considered to add a large amount of disintegrant. However, adding a large amount of disintegrant reduces the hardness of the tablet, which causes problems such as breakage during filling or distribution. At the same time, it may also cause problems such as deterioration of the fluidity of the tablet powder. In order to improve the disintegration of tablets, it is possible to obtain tablets by lowering the tableting pressure, but in this case, the tablets do 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 base material obtained 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, and then drying the fibrous fibers. Patent Document 2 discloses a composition containing carboxymethylcellulose calcium and silicon dioxide, with a highly hygroscopic Salacia-containing composition as an active ingredient. [Prior art documents] [Patent documents]

[0006] [Patent Document 1] JP 2020-152712 A [Patent Document 2] JP 2011-178690 A 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 can be observed for specific ingredients, when an active ingredient having a property of significantly decreasing tablet disintegration property is used, it is not possible to simultaneously achieve 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 having low disintegrability when made into a tablet is used, the disintegrability of the tablet can be improved and at the same time a desired tablet hardness can be maintained by adding a predetermined amount of sodium carboxymethylcellulose and agar, 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 1.0 to 7.0% by mass. (A) an active ingredient having a disintegration coefficient (X) of 8 or more (B) Sodium carboxymethylcellulose (C)Agar According to the present invention, even when an active ingredient that satisfies a certain index and has low disintegrability when made into a tablet is used, by incorporating a predetermined amount of sodium carboxymethylcellulose and agar, it is possible to provide a tablet having a desired tablet hardness with improved disintegrability. Although details will be described later, the disintegration coefficient is an index that represents the disintegrability of a tablet when a certain active ingredient is used, and a higher disintegration coefficient indicates a lower disintegrability of a tablet using that active ingredient. [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 having low disintegrability when made into a tablet is used, it is possible to provide a tablet having 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, plant extracts, and phytosterols. 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 a 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, comprising comprising comprising: (B) sodium carboxymethylcellulose; and (C) agar. According to the present invention, in a tablet using an active ingredient that has low disintegrability when made into a tablet, it is possible to improve the disintegrability and impart a desired tablet hardness. Effect of the Invention

[0011] According to the present invention, it is possible 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. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0012] [tablet] The tablet of the present invention is characterized in that it contains (A) an active ingredient having a disintegration coefficient (X) of 8 or more, (B) sodium carboxymethylcellulose, and (C) agar, and the content of the ingredient (B) is 0.5 to 2.0 mass%, and the content of the ingredient (C) is 1.0 to 7.0 mass%.

[0013] Many of the active ingredients incorporated in tablets tend to have a long disintegration time when incorporated in a certain amount or more. If the disintegration time is long, the active ingredient may not be sufficiently absorbed in the body, and the expected effect may not be obtained. When an active ingredient that significantly deteriorates disintegration property is incorporated in a tablet, the composition of the disintegrant used in the past could not impart sufficient disintegration property to the tablet. The present inventors have found that the tablet can acquire sufficient disintegration property by adding a predetermined amount of sodium carboxymethylcellulose and agar as disintegrants. In addition, according to the composition of the tablet of the present invention, the tablet has sufficient tablet hardness, and the occurrence of the problem of breakage during filling, distribution, or opening can be suppressed.

[0014] <Decay Factor(X)> The disintegration coefficient (X) in the present invention is an index showing the disintegration property inherent to an active ingredient. It is obtained as the disintegration time (X) minutes when a tablet containing a specific active ingredient is prepared under certain conditions (mixing ratio of active ingredient and excipient, tableting pressure, tablet grain size, mass). More specifically, 100 mg of the mixed powder having the composition shown in Table 1 is put into a compression property evaluation device (manufacturer name: Gamlen Instruments, model: GTP-2), and tableted using a Φ6 mm flat punch at a compression speed of 60 mm / min and a molding pressure of 500 kgf. Then, the disintegration time (X) minutes of the prepared tablet is measured, and this (X) is taken as the disintegration coefficient. The disintegration time is measured according to the "Disintegration Test Method" described in the Japanese Pharmacopoeia. The raw materials of each component used in the mixed powder are the same as those in the examples described below. The hardness of the above tablets prepared to determine the disintegration coefficient (X) here is set at a tableting pressure of 500 kgf, and is therefore not 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 an active ingredient, and is distinct from the object of the present invention, which is to limit the disintegration time of a tablet to within 30 minutes.

[0015] The disintegration coefficient (X) of the active ingredient of the present invention is 8 or more, and preferably 10 or more. If the disintegration coefficient (X) is 8 or more, the effect of improving the disintegration property of the tablet of the present invention can be more significantly exhibited. 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 guideline for the disintegration property of a tablet. In addition to the disintegration coefficient (X), the disintegration score (Y) is calculated according to the following formula 1 using the active ingredient blending ratio and tablet mass as tablet parameters that are expected to vary 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. Furthermore, by analyzing the relationship between the disintegration score (Y) and the actual disintegration time, it can be used to evaluate and estimate the effect of the disintegrant and other components on the tablet's disintegration.

[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 active ingredient contained therein. However, even if the tablet has a composition in which the disintegration score (Y) exceeds this standard, it is possible to sufficiently shorten the disintegration time and prepare a tablet having a desired tablet hardness by blending a predetermined amount of sodium carboxymethylcellulose and agar. The upper limit of the disintegration score (Y) is not particularly limited, but is preferably 80 or less, more preferably 60 or less. By being 60 or less, the appropriate form and use of the tablet is ensured.

[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. Regarding the standard of within 30 minutes, the Japanese Pharmacopoeia on pharmaceuticals specifies that the disintegration time of uncoated tablets is within 30 minutes. If the disintegration time exceeds 30 minutes, for example, the active ingredient is not sufficiently absorbed in the digestive tract, the required blood concentration is not obtained, or the bioavailability is reduced, and the expected effect may not be obtained.

[0022] (Tablet hardness) The tablet of the present invention preferably has a hardness of 11.0 kgf or more. This standard was set as a required value when assuming the phenomenon of "hardness reduction" that may occur in actual production. If the tablet hardness is 11.0 kgf or more, it is possible to prevent the tablet from being damaged during distribution, filling, or when removing the tablet from a PTP (Press Through Pack) package. The tablet hardness can be set by the selection of 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 required 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 blending 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 properties of the tablet are not particularly limited as long as the effects of the present invention are achieved, and various properties can be used. For example, ordinary tablets, orally disintegrating tablets, vaginal tablets, adhesive tablets, sublingual tablets, etc. are mentioned, but ordinary tablets and orally disintegrating tablets are preferred, and ordinary tablets are more preferred from the viewpoint 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 can be the active ingredient is not particularly limited, and may be, for example, a general physiologically active substance used in medicines, quasi-drugs, OTC medicines, Chinese herbal medicines, herbal medicines, cosmetics, health foods, nutritional functional foods, foods for specified health uses, foods for special dietary uses, supplements, veterinary medicines, etc.

[0026] The tablet of the present invention can be more preferably used for food or supplement use.Compared to medicines, 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 if it contains multiple active ingredients, it can have a significant effect on the disintegration and tablet hardness due to the configuration of the entire active ingredient or the entire tablet.

[0027] The active ingredient of the present invention is preferably an ingredient that reduces the disintegration property of a tablet when it is blended in the tablet. Even when such an active ingredient is blended in the tablet, by blending a predetermined amount of sodium carboxymethylcellulose and agar, it is possible to produce a tablet having a desired tablet hardness while exhibiting a sufficient improvement effect on 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 disintegration property and hardness, etc., and 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, an appropriate medicinal effect can be obtained, and if it is 80% by mass or less, it is easy to adjust the desired hardness, disintegration property, dissolution property, 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 applied 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 single ingredients, but is the actual measured value obtained by applying the composite material to the formulation in Table 1 and measuring it, and this is taken as the disintegration coefficient (X).

[0029] More specific examples of active ingredients include vitamins such as carotene, vitamin B, vitamin C, folic acid, etc., minerals, amino acids such as glycine, glutamine, ornithine, amino sugars such as glucosamine, 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, lycopene, etc., 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 extracts thereof, fish oil, probiotic bacteria such as lactic acid bacteria, yeast extracts such as cysteine ​​peptide-containing yeast extract, etc.

[0030] (vitamin) Vitamins in the tablet of the present invention are not particularly limited, but examples thereof include vitamins belonging to vitamin A group, such as retinal, retinol, retinoic acid, carotene, dehydroretinal, lycopene, and pharmacologically acceptable salts thereof, thiamine, thiamine disulfide, dicethiamine, octotiamine, shikotiamine, bis-ibuthiamine, 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, bread Vitamins belonging to vitamin B group such as gamic acid and pharmacologically acceptable salts thereof, vitamins belonging to vitamin C group such as ascorbic acid and its derivatives, erythorbic acid and its derivatives, and pharmacologically acceptable salts thereof, vitamins belonging to vitamin D group such as ergocalciferol, cholecalciferol, hydroxycholecalciferol, dihydroxycholecalciferol, dihydrotachysterol, and pharmacologically acceptable salts thereof, vitamins belonging to vitamin E group such as tocopherol and its derivatives, ubiquinone derivatives, and pharmacologically acceptable salts thereof, as well as carnitine, ferulic acid, γ-oryzanol, orotic acid, rutin (vitamin P), eriocitrin, hesperidin, and pharmacologically acceptable salts thereof, etc. These vitamins may be blended 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 kinds.

[0032] (Plant extract powder) The plant extract powder that can be used in the tablet of the present invention is not particularly limited. The powder extract can be obtained, for example, by crushing fruits, seeds, leaves, etc., or extracting fruits, seeds, leaves, etc. with polar solvents such as water or various organic solvents, or by distilling the distillate obtained by steam distillation, and then mixing it with additives such as excipients as necessary and drying it. It is to be noted that commercially available products can also be used regardless of the manufacturing 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] (Phytosterols) Phytosterols (plant sterols) are fat-soluble substances derived from plants that have a sterol skeleton in their structure. Phytosterols that can be used in the present invention are not particularly limited, but examples include β-sitosterol, campesterol, stigmasterol, brassicasterol, etc. These phytosterols may be blended alone or in combination of two or more.

[0035] <(B) Sodium carboxymethylcellulose> The tablet of the present invention contains sodium carboxymethylcellulose. Carboxymethylcellulose is a compound obtained by esterifying the hydroxyl group in cellulose, and crosslinked polymers thereof and their salts are generally used as disintegrants. Sodium salts in which hydrogen of this carboxymethylcellulose is replaced by sodium, a monovalent metal, are called sodium carboxymethylcellulose, and are widely used as disintegrants and in other applications in foods, medicines, and other fields. Because sodium carboxymethylcellulose has water solubility and appropriate disintegrability, it can more appropriately exert the effects of the present invention compared with croscarmellose having intramolecular crosslinks and calcium carboxymethylcellulose having a chelate structure, which is a divalent metal salt. The sodium carboxymethylcellulose that can be used in the present invention is not particularly limited, and can be produced by a known method or commercially available products can be used.

[0036] The content of (B) sodium carboxymethylcellulose 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 cannot be obtained, and the active ingredient may not exhibit the expected effect. If the content of component (B) is more than 2.0% by mass, the tablet hardness cannot be maintained at the desired hardness, and the tablet may be damaged during distribution, filling, or when the tablet is taken out of the PTP.

[0037] <(C) Agar> The tablet of the present invention contains agar. Agar is a polymeric polysaccharide extracted from red algae, which has a linear structure with a basic skeleton of repeated D-galactose and anhydro-L-galactose, and is composed of agarose (neutral polysaccharide) and agaropectin (acidic polysaccharide). There is no particular limit to the agar that can be used in the present invention. For example, refined agar for disintegration and Ina agar can be mentioned. These can be produced by known methods, or commercially available products can be used.

[0038] The content of (C) agar in the tablet of the present invention is 1.0 to 7.0% by mass. The lower limit of the content of (C) agar is preferably 3.0% by mass or more. The upper limit of the content of (C) agar is preferably 6.0% by mass or less. If the content of (C) agar is less than 1.0% by mass, sufficient tablet disintegration is not obtained, and the active ingredient may not exhibit the expected effect. If the content of (C) agar is more than 7.0% by mass, the tablet hardness cannot be maintained at the desired hardness, and the tablet may be damaged during distribution, filling, or when the tablet is removed from the PTP.

[0039] <Other ingredients> The tablet of the present invention may contain additives such as excipients, binders, lubricants, stabilizers, preservatives, flow agents, thickeners, colorants, etc. Furthermore, disintegrants other than sodium carboxymethylcellulose and agar may be contained within the range in which the effects of the present invention are achieved.

[0040] 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 bulk of the useful substance can be adjusted by adding the excipient.

[0041] The binder is not particularly limited, and examples thereof include carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylmethylcellulose, hydroxypropylcellulose, polyvinylpyrrolidone, polyvinyl alcohol, polyacrylic acid, polymethacrylic acid, glucose, sucrose, lactose, maltose, dextrin, sorbitol, mannitol, macrogol, paraffin, gum arabic, gelatin, agar, starch, starch hydrolysate, pullulan, etc. These binders may be blended alone or in combination of two or more. By adding a binder, it is possible to impart a binding force to the powder component of the raw material contained in component (A) and at the same time increase the fluidity, thereby producing a stable tablet.

[0042] 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, hardened vegetable oils, fats, and polyethylene glycol. These lubricants may be used alone or in combination of two or more. Addition of a lubricant can suppress the occurrence of tableting problems such as sticking during tablet production.

[0043] The other disintegrants are not particularly limited as long as they can achieve the effects of the present invention, and examples thereof include corn starch, low-substituted hydroxypropyl cellulose, microcrystalline cellulose, croscarmellose sodium, sodium carboxymethyl starch, croscarmellose polyvinylpyrrolidone, alginate, etc. These disintegrants may be blended alone or in combination of two or more kinds.

[0044] [Tablet manufacturing method] The method for producing the tablets of the present invention is not particularly limited, and the present invention used as a food or medicine can be produced using known additives that are acceptable for use as a food or medicine, and conventional formulation techniques used in the food or medicine fields can be applied.

[0045] For example, there are a method of tableting a mixed powder obtained by mixing various raw materials such as an active ingredient, an excipient, a binder, and a lubricant, a method of granulating various raw materials by a stirring mixing granulation method or a fluidized bed granulation method, adding and mixing a lubricant, and tableting, etc. The timing of adding tablet ingredients is not limited to this.

[0046] The apparatus used for tableting may be, for example, a general tableting molding apparatus such as a rotary tableting machine used for tablet production. In the case of tablets with a diameter of 6 to 10 mm, the tableting pressure during tableting is preferably 500 to 2000 kgf.

[0047] [Other embodiments] The present invention also provides a method for imparting disintegrability and tablet hardness to a composition using an active ingredient with low disintegrability when made into a tablet, or to a crushed product obtained by crushing a tablet. For example, a tablet having sufficient disintegrability and a desired tablet hardness can be produced by adding a predetermined amount of sodium carboxymethylcellulose and agar to the composition or crushed product, and granulating and tableting the composition. The timing of adding sodium carboxymethylcellulose and agar is not limited, and when the composition contains sodium carboxymethylcellulose or agar, they may be added so that the composition after addition has the predetermined amount according to the present invention. EXAMPLES

[0048] Hereinafter, examples of the present invention will be described, however, the present invention is not limited to these examples, and various modifications are possible within the technical concept of the present invention.

[0049] (1) Test Example 1: Effect of combining sodium carboxymethylcellulose and agar in a tablet containing multivitamins A test was conducted on the effect of blending sodium carboxymethylcellulose and agar in a tablet containing multivitamins (vitamins and minerals) as an active ingredient. More specifically, the tablets of Examples 1 to 6 and Comparative Examples 1 to 9 were manufactured 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.

[0050] [Table 2]

[0051] <Tablet manufacturing> Tablets of the examples and comparative examples were produced according to the following procedure. The raw materials were mixed in the raw material blending ratio (mass%) of the composition in Table 3, triturated and sieved to obtain powder for tableting. The prepared powder for tableting was tableted with 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 about 8 mm and a grain mass of 250 mg.

[0052] <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 regarded as the tablet hardness. The tablet hardness was evaluated according to the following evaluation criteria.

[0053] (Evaluation criteria for tablet hardness) 〇: Tablet hardness 11.0kgf or more ×: Tablet hardness less than 11.0 kgf

[0054] <Tablet disintegration test> The disintegration time of the produced tablets was measured according to "6.09 Disintegration Test Method" described in the general test method of "Japanese Pharmacopoeia, 17th Edition". Ion-exchanged water was used as the test liquid. The disintegration tester used was a disintegration tester (NT-610 (trade name), manufactured by Toyama Sangyo Co., Ltd.).

[0055] The test was performed with a liquid volume of 900 mL (purified water), and the disintegration time in water at 37° C. was measured for 6 sample tablets, and the average value was recorded as the disintegration time. The disintegration time was evaluated according to the following evaluation criteria.

[0056] (Evaluation criteria for disintegration) ○: Disintegration time is 30 minutes or less ×: Disintegration time exceeds 30 minutes

[0057] <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 "good" rating, and others were given a "bad" rating. 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

[0058] [Table 3]

[0059] The composition of vitamins and minerals in one tablet with a tablet weight of 250 mg and the disintegration coefficient (X) of the active ingredients in the multivitamin / 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 13.1, and the disintegration score (Y) was 20.9.

[0060] [Table 4]

[0061] [Table 5] The vitamin B oil-coated raw material is a food additive preparation in which vitamin B complex is 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%).

[0062] As a result of the test, the tablets containing multivitamins and minerals were able to achieve both the desired tablet hardness (11.0 kgf or more) and sufficient disintegrability (within 30 minutes) when the prescribed amounts of sodium carboxymethylcellulose and agar were blended (Examples 1 to 6). On the other hand, when either sodium carboxymethylcellulose or agar was not included (Comparative Examples 1 to 3, 5), or when the blending amounts of sodium carboxymethylcellulose and agar were outside the blending amounts of the present invention (Comparative Examples 4, 6), the standards for either tablet hardness or disintegrability could not be met.

[0063] Furthermore, even when starch (Comparative Example 7) or calcium carboxymethylcellulose (Comparative Examples 8 and 9), which are widely used disintegrants, were added in the prescribed amounts according to the present invention instead of sodium carboxymethylcellulose, the standards for either tablet hardness or disintegrability could not be met.

[0064] (2) Test Example 2: Effect of combining sodium carboxymethylcellulose and agar in tablets containing plant extract powder Regarding the effect of blending sodium carboxymethylcellulose and agar in tablets containing plant extract as an active ingredient, for the examples and comparative examples shown in Table 6, tablets were manufactured in the same manner as in Test Example 1, and tests were conducted on tablet hardness and disintegration. In Test Example 2, bacopa extract powder and aged hop extract were used as the plant extract powder. The disintegration coefficient (X) of the active ingredient was 14.0 for bacopa extract powder and 8.2 for aged hop extract. The disintegration coefficient (X) of the composite material was 10.65. The disintegration score (Y) in this test example was 15.4.

[0065] [Table 6]

[0066] As a result of the test, when the tablet containing the plant extract powder was mixed with a specified amount of sodium carboxymethylcellulose and agar (Examples 7 and 8), 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 agar was included (Comparative Examples 10 and 11), the standard for disintegrability could not be met.

[0067] (3) Test Example 3: Effect of combining sodium carboxymethylcellulose and agar in tablets containing phytosterol Regarding the effect of blending sodium carboxymethylcellulose and agar in tablets containing phytosterol as a fat-soluble substance derived from plants, tablets of the examples and comparative examples shown in Table 7 were manufactured and tested for tablet hardness and disintegration in the same manner as in Test Example 1, except that they were made in 300 mg amounts. In Test Example 3, Riken Phytosterol 85 was used as the phytosterol. The disintegration coefficient (X) of Riken Phytosterol 85 was 120, and the disintegration score (Y) of the tablet in this test example was 54.

[0068] [Table 7]

[0069] As a result of the test, the tablet containing phytosterols was able to achieve both the desired tablet hardness (11.0 kgf or more) and sufficient disintegrability (within 30 minutes) when a prescribed amount of sodium carboxymethylcellulose and agar was blended (Example 9). On the other hand, when starch, which can be used as a general disintegrant, was used instead of agar (Comparative Example 12), the standard for disintegrability could not be met. [Industrial Applicability]

[0070] According to the present invention, it is possible to provide a tablet containing an active ingredient that has low disintegrability when made into a tablet, which has a desired tablet hardness while ensuring sufficient disintegrability. The present invention can be utilized in various fields such as pharmaceuticals, quasi-drugs, veterinary products, foods, and supplements in designing the tablet configuration according to the purpose of use.

Claims

1. Contains the following components (A) to (C) and cellulose, The component (A) contains one or more selected from vitamins, minerals, plant extract powders, and phytosterols, A tablet, characterized in that the content of the component (B) is 0.5 to 2.0 mass%, and the content of the component (C) is 3.0 to 7.0 mass%. (A) an active ingredient having a disintegration coefficient (X) of 8 or more (B) Sodium carboxymethylcellulose (C) Purified agar for disintegration

2. The tablet according to claim 1, characterized in that the sum of the contents of the (B) component and the (C) component is 5.0 mass% 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, plant extract powders, and phytosterols, A method for improving the disintegration properties of a tablet, comprising comprising: (B) sodium carboxymethylcellulose; (C) purified agar for disintegration; and cellulose.

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