Tablet composition

Abstract

The present invention addresses the problem of increasing tablet hardness and suppressing abrasion of a tablet containing an acid and a carbonate which are foaming components. The present invention provides a tablet composition which comprises (A) a carbonate, (B) an acid or a salt thereof (excluding carbonates), (C) sorbitol and / or maltose, and (D) a cellulose derivative and / or a gum, and in which: the contained amount of (D) the cellulose derivative and / or the gum is 0.5 mass% or more with respect to the weight of the tablet composition; the contained amount of (C) the sorbitol and / or the maltose is 35 mass% or more with respect to the weight of the tablet composition; and the total contained amount of (A) the carbonate and (B) the acid or a salt thereof (excluding carbonates) is 55 mass% or less with respect to the weight of the tablet composition.

Description

Tablet composition

[0001] The present invention relates to a tablet composition, typically a foaming tablet containing a foaming component.

[0002] Foaming preparations containing a carbonate and an organic acid are known. That is, the foaming preparation contains sodium bicarbonate etc. as a carbonate and contains citric acid, fumaric acid etc. as an organic acid. When the foaming preparation comes into contact with water, the carbonate and the organic acid react to generate carbonic acid and disintegrate. It is known to use the foaming preparation for oral use to cause foaming by contacting with saliva or water in the oral cavity, thereby enhancing its disintegration in the oral cavity, ease of administration, and feeling of taking (Patent Documents 1 to 4). In addition, a topical skin preparation composed of a foaming preparation for the purpose of promoting blood circulation by carbon dioxide gas has also been proposed (Patent Document 5). Furthermore, there are those that expect to use the foaming preparation as a bath agent to cause foaming in bath water and bring about a high hot bath effect by the carbon dioxide gas dissolved in the bath water (Patent Document 6).

[0003] It is also known to make the dosage form of the foaming preparation into a tablet. In that case, in order to enhance the disintegration property while maintaining the tablet hardness, it has been proposed to adjust the particle size of the fumaric acid powder contained therein (see Patent Document 6).

[0004] Japanese Patent Application Laid-Open No. 2018-154573, Japanese Patent Application Laid-Open No. 2021-187772, Japanese Patent Application Laid-Open No. 2007-501273, Japanese Patent Application Laid-Open No. 2022-174508, Japanese Patent Application Laid-Open No. 2022-465, Japanese Patent Application Laid-Open No. 2012-92031

[0005] Although it is also known to make the form of the foaming preparation into a tablet, since the foaming preparation contains a carbonate and an organic acid as foaming components, there are problems that it is difficult to sufficiently increase the tablet hardness and that the tablet is easily worn. In addition, since a tablet composed of a foaming preparation may be taken orally and disintegrated in the oral cavity, the functionality at that time is also important; for example, the feeling of foaming in the oral cavity, the texture (crunchiness) such as ease of cracking in the oral cavity, and the feel in the oral cavity (smoothness) are also required.

[0006] The first objective of the present invention is to sufficiently increase the hardness of a tablet containing a carbonate as an effervescent component and an acid or a salt thereof, while suppressing abrasion. The second objective is to improve the sensory experience (effervescence, crunchiness, mouthfeel) in the oral cavity when the tablet containing a carbonate as an effervescent component and an acid or a salt thereof is taken, while increasing the hardness of the tablet to a certain extent. Preferably, the present invention can solve both the first and second objectives.

[0007] In other words, the present invention relates to the following tablet composition: <1> A tablet composition comprising (A) a carbonate, (B) an acid or a salt thereof (excluding carbonate), (C) sorbitol and / or maltose, and (D) a cellulose derivative and / or gum, wherein the content of (D) the cellulose derivative and / or gum is 0.5% by mass or more relative to the mass of the tablet composition; the content of (C) the sorbitol and / or maltose is 35% by mass or more relative to the mass of the tablet composition; and the total content of (A) the carbonate and (B) the acid or a salt thereof (excluding carbonate) is 55% by mass or less relative to the mass of the tablet composition.

[0008] The present invention preferably relates to the following tablet compositions: <2> The tablet composition according to <1>, wherein the content of (D) cellulose derivatives and / or gums is 8% by mass or less based on the mass of the tablet composition. <3> The tablet composition according to <1> or <2>, wherein the content of (C) sorbitol and / or maltose is 80% by mass or less based on the mass of the tablet composition.

[0009] <4> The tablet composition according to any one of <1> to <3>, wherein the (D) cellulose derivative comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose, ethyl cellulose, methyl cellulose, hydroxyethyl cellulose, and / or carboxymethyl cellulose or a salt thereof. <5> The tablet composition according to any one of <1> to <4>, wherein the (D) gums comprises gum arabic and / or xanthan gum. <6> The tablet composition according to any one of <1> to <5>, wherein the content of the (A) carbonate is 6% by mass or more and 23% by mass or less, based on the mass of the tablet composition. <7> The tablet composition according to any one of <1> to <6>, wherein the (A) carbonate comprises sodium carbonate or magnesium carbonate. <8> The tablet composition according to any one of <1> to <7>, wherein the (B) acid or a salt thereof (excluding carbonate) comprises citric acid, malic acid, fumaric acid, tartaric acid, succinic acid or ascorbic acid, or a salt thereof. <9> The tablet composition according to any one of <1> to <8>, wherein the content of (A) carbonate is 6 to 23% by mass, the content of (C) sorbitol and / or maltose is 35 to 80% by mass, and the content of (D) cellulose derivatives and / or gums is 0.5 to 8% by mass.

[0010] <10> The tablet composition according to any one of <1> to <9>, wherein the tablet composition is an effervescent tablet. <11> The tablet composition according to any one of <1> to <10>, wherein the tablet composition is for oral use or for use in the mouth.

[0011] Furthermore, the present invention relates to the following method for increasing tablet hardness: <12> A method for increasing the tablet hardness of a tablet composition containing (A) a carbonate and (B) an acid or a salt thereof (excluding carbonate), comprising: adding to the tablet composition 35% by mass or more of (C) sorbitol and / or maltose and 0.5% by mass or more of (D) cellulose derivatives and / or gums based on the weight of the tablet composition.

[0012] The tablet composition of the present invention contains a foaming component consisting of a carbonate and an acid or a salt thereof, while having sufficiently high tablet hardness and suppressing abrasion. Therefore, the tablet composition of the present invention can maintain its quality during storage and transportation. Furthermore, while having a certain level of tablet hardness, the tablet composition of the present invention can be disintegrated in the mouth when used as an oral or oral preparation, and the sensory properties (mouthfeel and crunchiness) at that time are improved. Therefore, the tablet composition of the present invention can be applied to various uses as an oral or oral preparation.

[0013] 1. Composition of the tablet composition The tablet composition of the present invention contains (A) a carbonate, (B) an acid or a salt thereof (excluding carbonate), (C) sorbitol and / or maltose, and (D) a cellulose derivative and / or gum, and may further contain (E) any other component.

[0014] (A) Carbonate The (A) carbonate contained in the tablet composition of the present invention generates carbon dioxide gas when the tablet composition comes into contact with water and reacts with (B) acid or its salt (excluding carbonate). (A) Carbonate is preferably a solid substance at room temperature, and examples include calcium carbonate, calcium bicarbonate, sodium carbonate, sodium bicarbonate (sodium hydrogen carbonate), potassium bicarbonate, potassium carbonate, magnesium carbonate, ammonium carbonate, sodium sesquicarbonate, etc. Preferred examples of (A) carbonate include sodium carbonate and magnesium carbonate, which are suitable as components of oral or orally administered tablet compositions. These (A) carbonates may be used alone or in combination of two or more types.

[0015] The content of (A) carbonate in the tablet composition is preferably 6% by mass or more, more preferably 10% by mass or more, and even more preferably 15% by mass or more; on the other hand, it is preferably 28% by mass or less, more preferably 25% by mass or less, and even more preferably 23% by mass or less. By setting the content of (A) carbonate above a certain level, the tablet composition becomes more effervescent, and for example, the effervescence in the mouth can be enhanced when the tablet composition is taken. Furthermore, by setting the content of (A) carbonate below a certain level, the hardness of the tablet composition can be increased.

[0016] (B) Acid or salt thereof (excluding carbonate) The (B) acid or salt thereof (excluding carbonate) contained in the tablet composition of the present invention reacts with (A) carbonate when the tablet composition comes into contact with moisture, thereby generating carbon dioxide from (A) carbonate. The acid may be an organic acid or an inorganic acid. As (B) acid or salt thereof, an organic acid or salt thereof is preferred, but not a carbonate. Examples of such acids include formic acid, acetic acid, propionic acid, butanoic acid, valeric acid, lactic acid, ascorbic acid, gluconic acid (monobasic organic acid); oxalic acid, malonic acid, succinic acid, glutaric acid, malic acid, fumaric acid, tartaric acid (dibasic organic acid); citric acid, aconitic acid (tribasic organic acid), or salts thereof. Examples of preferred (B) acid or salt thereof (excluding carbonate) include citric acid, malic acid, fumaric acid, tartaric acid, succinic acid, ascorbic acid, or salts thereof. On the other hand, examples of inorganic acids or their salts include phosphoric acid or its salts. These (B) acids or their salts (excluding carbonates) may be used individually or in combination of two or more.

[0017] The content of (B) acid or its salt (excluding carbonate) in the tablet composition is preferably 6% by mass or more, more preferably 10% by mass or more, and even more preferably 15% by mass or more; on the other hand, it is preferably 28% by mass or less, and more preferably 25% by mass or less. By setting the content of (B) acid or its salt (excluding carbonate) above a certain level, the tablet composition becomes more effervescent, and for example, the effervescence in the mouth can be enhanced when the tablet composition is taken. Furthermore, by setting the content of (B) acid or its salt (excluding carbonate) below a certain level, the hardness of the tablet composition can be increased.

[0018] Furthermore, the total content of (A) carbonate and (B) acid or its salt (excluding carbonate) in the tablet composition is usually 55% by mass or less, preferably 45% by mass or less; on the other hand, it is preferably 12% by mass or more, more preferably 15% by mass or more, even more preferably 25% by mass or more, and even more preferably 35% by mass or more.

[0019] (C) Sorbitol and / or Maltose The (C) sorbitol and / or maltose contained in the tablet composition of the present invention is an ingredient that can act as an excipient. The inventors have found that when sorbitol and / or maltose is included, the hardness of the tablet composition is easily increased, even when the content of the foaming component is high.

[0020] The total content of (C) sorbitol and / or maltose in the tablet composition is usually 35% by mass or more, preferably 40% by mass or more, and more preferably 45% by mass or more; on the other hand, it is preferably 80% by mass or less, more preferably 75% by mass or less, and even more preferably 70% by mass or less. If the total content of (C) sorbitol and / or maltose is above a certain level, it tends to increase the hardness of the tablet composition, and if the total content of (C) sorbitol and / or maltose is excessively high, the amount of other components to be blended becomes relatively low, and for example, it becomes impossible to blend enough foaming components.

[0021] Furthermore, the total content of (C) sorbitol and / or maltose in the tablet composition is preferably 1.5 times or more by mass ratio of the content of (A) carbonate, more preferably 2 times or more; on the other hand, it is preferably 12 times or less.

[0022] (D) Cellulose derivatives and / or gums The (D) cellulose derivatives and / or gums contained in the tablet composition of the present invention are components that can act as binders. The inventors have found that the hardness of tablets can be increased to some extent by including (C) sorbitol and / or maltose in a tablet composition containing a foaming component, but have found that it is effective to further include (D) cellulose derivatives and / or gums in order to further increase the hardness of tablets (to withstand transport) and to reduce the abrasion of tablets.

[0023] Furthermore, the inventors found that while including (C) sorbitol and / or maltose in a tablet composition containing a foaming component increases tablet hardness to some extent, it may not sufficiently reduce the degree of abrasion (see Comparative Example 2 below). Therefore, by including (D) cellulose derivatives and / or gums together with (C) sorbitol and / or maltose, the tablet hardness of the tablet composition was increased and the degree of abrasion was sufficiently reduced.

[0024] (D) Examples of cellulose derivatives include hydroxypropylcellulose (HPC), hydroxypropylmethylcellulose (HPMC), hydroxyethylcellulose, low-substituted hydroxypropylcellulose (LHPC), methylcellulose, ethylcellulose, carboxymethylcellulose (carmellose), or their salts (such as sodium carboxymethylcellulose). (D) When the cellulose derivative is a water-soluble component, the oral functionality (especially the mouthfeel) of the tablet composition improves.

[0025] Preferred (D) cellulose derivatives include hydroxypropyl cellulose (HPC), hydroxypropyl methylcellulose (HPMC), ethyl cellulose, methylcellulose, hydroxyethyl cellulose, carboxymethylcellulose, or salts thereof, and more preferably hydroxypropyl cellulose (HPC) and hydroxypropyl methylcellulose (HPMC).

[0026] For hydroxypropyl cellulose (HPC), it is preferable to use one with a particle size D50 of 10 to 190 μm. More specifically, particle sizes D50 of 10 to 50 μm, 60 to 130 μm, or 140 to 190 μm can be used. Furthermore, for hydroxypropyl cellulose (HPC), it is preferable to use one with a degree of substitution by hydroxypropoxy groups of 80.5% or less. On the other hand, for hydroxypropyl methylcellulose (HPMC), it is preferable to use one with an average particle size (laser method) of 5 to 20 μm, and more specifically, one with an average particle size of 8 to 15 μm can be used.

[0027] Furthermore, it is preferable to use hydroxypropyl methylcellulose (HPMC) with a degree of substitution by methoxy groups of 19 to 30%. More specifically, HPMC with a degree of substitution by methoxy groups of 19 to 24% or 27 to 30% can be used. In addition, HPMC with a degree of substitution by hydroxypropoxy groups of 4 to 12% can be used. These cellulose derivatives may be used individually or in combination of two or more.

[0028] Examples of (D) gums include components referred to as thickening polysaccharides, such as gum arabic, xanthan gum, and guar gum. Preferred (D) gums are gum arabic or xanthan gum, and more preferably gum arabic. These gums may be used individually or in combination of two or more.

[0029] Since the tablet composition of the present invention may disintegrate in the oral cavity, if the tablet composition contains water-insoluble components, it may cause a gritty sensation in the mouth (on the tongue) of the user, worsening the texture. For this reason, it is preferable that the (D) cellulose derivatives and / or gums used as binders are not water-insoluble components.

[0030] The total content of (D) cellulose derivatives and / or gums in the tablet composition is usually 0.5% by mass or more, preferably 2% by mass or more, and more preferably 4% by mass or more, relative to the tablet composition; on the other hand, it is preferably 10% by mass or less, and more preferably 8% by mass or less. When the total content of (D) cellulose derivatives and / or gums is above a certain level, it is easier to increase the hardness of the tablet composition and reduce the degree of abrasion. Also, when the total content of (D) cellulose derivatives and / or gums is below a certain level, it is easier to improve the texture when taking the tablet composition, for example, the crunchiness (the feeling of being able to break it crisply without feeling an unpleasant stickiness).

[0031] (E) Any other components The tablet composition of the present invention may contain (E) any other components, such as additives such as lubricants, fluidizers, disintegrants, excipients, sweeteners, and colorants. The tablet composition of the present invention may also contain physiologically active ingredients, vitamins, minerals, polyphenols, carotenoids, flavonoids, amino acids, plant-derived ingredients, animal-derived ingredients, fungi, dietary fiber, etc.

[0032] Examples of lubricants include calcium stearate, magnesium stearate, stearic acid, and sodium stearyl fumarate. Examples of fluidizers include silicon dioxide, light anhydrous silicic acid, talc, and magnesium aluminometasilicate. When the tablet composition is for oral or bodily use, it may be preferable to add a sweetener, and examples of sweeteners include aspartame, acesulfame potassium, sucralose, stevia, and thaumatin.

[0033] 2. Properties and Uses of the Tablet Composition The tablet composition of the present invention is characterized by having a tablet hardness of a certain level or higher. The tablet hardness of the tablet composition may be 42 N or higher, preferably 45 N or higher, more preferably 50 N or higher, even more preferably 55 N or higher, and even more preferably 60 N or higher. The tablet hardness can be measured by the method described in the examples of this specification.

[0034] The tablet composition of the present invention may be a so-called uncoated tablet, or it may be a film-coated tablet obtained by film-coating an uncoated tablet.

[0035] The tablet composition of the present invention contains an effervescent component, and can disintegrate by generating carbon dioxide gas upon contact with water. In other words, the tablet composition of the present invention can be used as an effervescent tablet. Effervescent tablets can be used as oral tablets (foods, health foods, pharmaceuticals), as well as as bath additives, insecticides, etc. Despite containing an effervescent component, the tablet composition of the present invention has high tablet hardness and suppressed abrasion, making it less susceptible to abrasion and breakage during storage and transportation, thus making it easy to maintain high quality.

[0036] Furthermore, the effervescent tablets of the present invention have an improved texture when taken, and can therefore preferably be used as oral or mouth-disintegrating tablets. The effervescent tablets may also be orally disintegrating tablets designed to be licked and disintegrated in the mouth, or chewable tablets designed to be chewed in the mouth. For example, the effervescent tablets of the present invention have a certain level of tablet hardness, a high effervescence in the mouth, a good crunchiness in the mouth, and high smoothness under the tongue.

[0037] 3. Manufacturing of Tablet Compositions The tablet composition of the present invention can be manufactured by any method as long as the predetermined components are included, for example, by direct compression or indirect compression (wet granulation compression or dry granulation compression). Direct compression is a method of forming tablets by compressing a mixture of the raw material components of the tablet (mixed powder); it is a method in which the components to be compressed are not granulated (granules are not produced). Indirect compression is a method in which the entire amount of the raw material components of the tablet are granulated and the resulting granules are compressed into tablets, or a part of the raw material components of the tablet are granulated and the resulting granules are mixed with the remaining raw material components and compressed into tablets.

[0038] In direct compression manufacturing, all the raw materials constituting the tablet composition may be mixed together at once; or some of the raw materials may be mixed first, and then some of the other raw materials may be added and mixed. For example, (A) a carbonate, (B) an acid or a salt thereof (excluding carbonate), (C) sorbitol and / or maltose, and (D) a cellulose derivative and / or gum may be mixed, and then (E) any other component may be added and mixed to the resulting mixture.

[0039] In direct compression manufacturing, the particle sizes of each raw material mixed are not particularly limited, as long as they are adjusted to ensure uniform mixing. The particle size (D50) of each raw material is set in the range of 50 to 300 μm as a guideline.

[0040] Granulated granules in the indirect tableting method can be obtained by granulating all or part of the raw material components by fluidized bed granulation, rolling granulation, agitation granulation, or extrusion granulation. For example, raw material components containing (A) carbonate, (B) acid or its salt (excluding carbonate), and (C) sorbitol and / or maltose can be granulated; (D) cellulose derivatives and / or gums or (E) other optional components (such as lubricants) can be added and mixed to the obtained granules; and the resulting mixture can be compressed into tablets. Granulation can be performed, for example, by introducing raw material components containing (A) carbonate, (B) acid or its salt (excluding carbonate), and (C) sorbitol and / or maltose into a granulator, and spraying a predetermined binding solution (water or aqueous solution) onto the granulated material that has been fluidized in the granulator. However, the method of producing tablets by the indirect tableting method is not limited to this.

[0041] When tableting the mixture for tableting, the tableting pressure may be set according to the tablet hardness of the obtained tablet composition, and is generally set in the range of 3 to 20 kN. The tableting method is not particularly limited, and tableting can be performed using a single-punch tableting machine, a continuous tableting machine, a rotary tableting machine, a layered tableting machine, or the like.

[0042] 4. Method for increasing the hardness of a tablet composition The present invention relates to a method for increasing the tablet hardness of a tablet composition (preferably a foaming tablet) containing (A) a carbonate and (B) an acid or a salt thereof (excluding carbonates). Since the foaming tablet contains (A) a carbonate, there has generally been a problem that it is difficult to increase the tablet hardness. If the tablet hardness of the tablet composition is low, abrasion and defects are likely to occur during storage or transportation of the tablet composition, deteriorating its quality. Therefore, according to the method for increasing the hardness of the tablet composition of the present invention, the quality of the tablet composition containing a foaming component can be significantly improved.

[0043] Regarding the content of each suitable component and the suitable production method of the tablet composition in the method for increasing the hardness of the tablet composition, it is as described for the tablet composition of the present invention. As one embodiment of the method of the present invention, in the process of developing the tablet composition to be a product, by adjusting the contents of (C) sorbitol and / or maltose, and (D) cellulose derivatives and / or gums to a predetermined range, there is an aspect in which the hardness is higher than before adjustment. Further, as another embodiment, in the production process of a product (tablet composition) in which the contents of (C) sorbitol and / or maltose, and (D) cellulose derivatives and / or gums are within a predetermined range, there is an aspect of inspecting that the hardness of the obtained tablet composition satisfies the set specifications.

[0044] Hereinafter, the present invention will be described in more detail with reference to examples, but the technical scope of the present invention should not be construed as being limited by the description of the examples.

[0045] A. Production of tablet composition A-1. Raw materials used for the production of the tablet composition The raw materials used for the production of the tablet compositions of each example and comparative example are shown below.

[0046] A-1-1: Carbonate, Sodium Bicarbonate, Magnesium Carbonate

[0047] A-1-2: Organic Acids, Citric Acid, Malic Acid, Fumaric Acid, Tartaric Acid, Succinic Acid, Ascorbic Acid

[0048] A-1-3: Sugar Alcohols or Sugars, Sorbitol (Sorbitol FP 100M, Produce Food Science), Maltose (Sun Malt Midori, Nagase Vita (Maltose content 89% by mass)), Maltitol, Erythritol, Xylitol, Lactose, Sugar, Glucose

[0049] A-1-4: Binders, etc., Hydroxypropyl Cellulose (Cellney SSL-SFP (D50: 20μm), Nippon Soda), Hydroxypropyl Methyl Cellulose (Metrose NE-04VF, Shin-Etsu Chemical Co., Ltd.), Gum Arabic (Arabic Cole SS (Food Additive Gum Arabic), San-Ei Pharmaceutical Trading), Ethyl Cellulose (Etcell, Standard 7 FP Premium (Average particle size: 5 - 15μm), IFF Pharma), Methyl Cellulose (Metrose MCE-4, Shin-Etsu Chemical Co., Ltd.), Xanthan Gum (San Ace, San-Ei Gen F.F.I.), Hydroxyethyl Cellulose (HEC Daicel SP900, Daicel), Sodium Carboxymethyl Cellulose (CMC1150, Daicel), Crystalline Cellulose, Partially Gelatinized Starch

[0050] A-1-5: Other Components, Dextrin, Microcrystalline Silicon Dioxide, Calcium Stearate [[ID=​​​​​

[0053] B-1. Measurement of Tablet Hardness The hardness (unit: Newtons N) of the tablet compositions obtained in each example and comparative example was measured in accordance with the Japanese Pharmacopoeia "Method for Measuring Tablet Hardness". Specifically, a digital hardness tester (Fujiwara Seisakusho Co., Ltd.) was used as the measuring device, and the hardness of each tablet was measured by applying a load to its side. The hardness of three tablets for each example and comparative example was measured, and the average values ​​are shown in Tables 1 to 4.

[0054] B-2. Evaluation of Abrasion Degree The abrasion degree (unit: %) of the tablet compositions obtained in each example and comparative example was measured in accordance with the Japanese Pharmacopoeia "Test Method for Tablet Abrasion Degree". A FRIABILATOR EF-2 (ELECTROLABINDIA PVT. LTD.) was used as the measuring device. Specifically, the weight g(X) of 10 tablets was measured and placed in a test drum. After rotating the drum 100 times at 25 rpm, the tablets were removed and their weight g(Y) was measured. The abrasion degree was calculated based on the following formula: Abrasion degree [%] = 100 × (X - Y) / X

[0055] B-3. ​​Sensory Evaluation of Effervescence Three panelists evaluated the effervescence of one tablet obtained in each example and comparative example when placed in the mouth, according to the following criteria. The average value of the evaluation results of the three individuals was obtained. An average value of less than 2 points is indicated by △, and an average value of 2 points or more is indicated by ○, as shown in Tables 1 to 4. 5 points: A pleasant effervescence is felt quite strongly. 4 points: A pleasant effervescence is felt strongly. 3 points: A pleasant effervescence is felt. 2 points: A pleasant effervescence is felt slightly. 1 point: A pleasant effervescence is not felt very strongly.

[0056] B-4. Sensory Evaluation of Texture (Crunch) Three panelists evaluated the texture (crispness) of one tablet obtained from each example and comparative example when chewed, according to the following criteria. The average value of the evaluation results of the three panelists was obtained. An average value of less than 2 points is indicated by △, and an average value of 2 points or more is indicated by ○, as shown in Tables 1 to 4. 4 points: Very high crunchiness 3 points: High crunchiness 2 points: Slightly high crunchiness 1 point: Low crunchiness

[0057] B-5. Sensory evaluation of texture (mouthfeel, smoothness) Three panelists evaluated the texture (mouthfeel, smoothness) of one tablet obtained from each example and comparative example by placing it in their mouths and chewing it, using △ for roughness and ○ for smoothness (if all panelists gave a ○ rating, ○ is shown in Tables 1-4).

[0058]

[0059]

[0060]

[0061]

[0062] First, as shown in Comparative Example 1 of Table 3, the composition consisting of a foaming component ((A) carbonate and (B) acid or its salt (excluding carbonate)), dextrin, fine silicon dioxide, and calcium stearate could not be formed into tablets.

[0063] Next, as shown in Comparative Example 2 of Table 3, a composition consisting of a foaming component ((A) carbonate and (B) acid or its salt (excluding carbonate)), dextrin, (C) sorbitol, fine silicon dioxide, and calcium stearate could be molded into tablets; however, it was found that the tablet hardness was not sufficiently high and that the tablets were prone to abrasion. In other words, because the tablets of Comparative Example 2 did not contain (D) cellulose derivatives and / or gums, sufficient tablet hardness could not be obtained, and brittleness occurred, making them prone to abrasion. The same was true for the tablets of Comparative Example 5 (which had a low content of (D) cellulose derivatives and / or gums), and although the tablet hardness of these tablets was increased to some extent, there was a tendency for abrasion to be not sufficiently suppressed.

[0064] Although the tablets of Comparative Examples 3 and 4 in Table 3 ((D) cellulose derivatives and / or gums not contained) showed some improvement in tablet hardness, their mouthfeel was slightly worsened. This is thought to be because the tablets of Comparative Examples 3 and 4 contain water-insoluble crystalline cellulose or partially pregelatinized starch, which affects the mouthfeel in the oral cavity and reduces smoothness.

[0065] Comparative Examples 6 to 11 in Table 4 are tablets made from a composition consisting of a foaming component ((A) carbonate and (B) acid or its salt (excluding carbonate)), various sugars or sugar alcohols, (D) hydroxypropyl cellulose, fine silicon dioxide, and calcium stearate. However, none of these tablets achieved sufficient hardness. In other words, it was found that these tablets did not achieve sufficient hardness because they did not contain (C) sorbitol and / or maltose.

[0066] Comparative Examples 12 and 13 in Table 4 are tablets made of a composition comprising a foaming component ((A) carbonate and (B) acid or its salt (excluding carbonate)), dextrin, (C) sorbitol and / or maltose, (D) hydroxypropyl cellulose, fine silicon dioxide, and calcium stearate; however, the content of (C) sorbitol and / or maltose is low. Therefore, it was found that the tablet hardness of these tablets did not increase.

[0067] Furthermore, Comparative Example 14 in Table 4 was a tablet with an excessive amount of foaming components ((A) carbonate and (B) acid or its salt (excluding carbonate)), and the tablet hardness was not sufficiently increased.

[0068] In contrast, the examples shown in Tables 1 to 3 are tablets containing foaming components ((A) carbonates and (B) acids or their salts (excluding carbonates)), (C) sorbitol and / or maltose, and (D) cellulose derivatives and / or gums, with optimized content of these components. These tablets possess a certain level of hardness and sufficiently suppress abrasion. Moreover, many of these tablets yielded satisfactory results in various sensory evaluations.

[0069] As can be seen from the comparison between Examples 1-3 and Examples 24-27, sufficient results were obtained in various evaluations for each of the following as (D) cellulose derivatives and / or gums: hydroxypropyl cellulose, hydroxypropyl methylcellulose, gum arabic, methylcellulose, xanthan gum, hydroxyethylcellulose, and sodium carboxymethylcellulose. In particular, tablet hardness was increased to a certain extent, abrasion was suppressed, and the mouthfeel was also well evaluated. Hydroxypropyl cellulose, hydroxypropyl methylcellulose, and gum arabic were able to sufficiently increase tablet hardness; methylcellulose, xanthan gum, hydroxyethylcellulose, and sodium carboxymethylcellulose were also able to maintain tablet hardness while improving the effervescence and texture.

[0070] As shown in Example 23, when ethylcellulose was included as (D) cellulose derivative and / or gum, the tablet hardness could be sufficiently increased (66N). On the other hand, ethylcellulose is a water-insoluble component, and the texture evaluation sometimes decreased slightly.

[0071] As can be seen from the comparison between Examples 1 and 4-7, sufficient results were obtained in various evaluations even when the content of (D) cellulose derivatives and / or gums was adjusted. However, it was confirmed that the higher the content of (D) cellulose derivatives and / or gums, the higher the tablet hardness and the more the tablet abrasion was suppressed; and that the texture (crunchiness) was improved when the content of (D) cellulose derivatives and / or gums was below a certain level.

[0072] As can be seen from the comparison between Examples 1 and 8-11, it was found that sufficient results could be obtained in various evaluations for either (C) sorbitol or maltose.

[0073] As can be seen from the comparison between Examples 1 and 12-16, even when the content of the effervescent component ((A) carbonate and (B) acid or its salt (excluding carbonate)) was adjusted, sufficient results were obtained in various evaluations. However, it was confirmed that when the amount of the effervescent component was above a certain level, the effervescence tended to improve, and when the amount of the effervescent component was below a certain level, the tablet hardness tended to increase.

[0074] As can be seen from the comparison between Examples 1 and 17-21, it was found that even when various types of acids were used in the foaming components, sufficient results could be obtained in various evaluations. Furthermore, as can be seen from the comparison between Examples 1 and 22, it was found that even when the carbonates used in the foaming components were changed, sufficient results could be obtained in various evaluations.

[0075] The tablet composition of the present invention contains an effervescent component while maintaining sufficiently high tablet hardness and suppressing abrasion. Therefore, it can be applied to various uses as an effervescent formulation. Furthermore, the tablet composition of the present invention has a certain level of tablet hardness while improving the sensory experience in the oral cavity when taken (such as mouthfeel and crunchiness), so it can be applied to various uses as an oral or oral tablet composition, such as in food and pharmaceuticals.

Claims

1. A tablet composition comprising (A) a carbonate, (B) an acid or a salt thereof (excluding carbonate), (C) sorbitol and / or maltose, and (D) a cellulose derivative and / or gum, wherein: the content of (D) the cellulose derivative and / or gum is 0.5% by mass or more relative to the mass of the tablet composition; the content of (C) the sorbitol and / or maltose is 35% by mass or more relative to the mass of the tablet composition; and the total content of (A) the carbonate and (B) the acid or a salt thereof (excluding carbonate) is 55% by mass or less relative to the mass of the tablet composition.

2. The tablet composition according to claim 1, wherein the content of (D) cellulose derivatives and / or gums is 8% by mass or less relative to the mass of the tablet composition.

3. The tablet composition according to claim 1 or 2, wherein the content of (C) sorbitol and / or maltose is 80% by mass or less relative to the mass of the tablet composition.

4. The tablet composition according to claim 1 or 2, wherein the (D) cellulose derivative comprises hydroxypropyl methylcellulose, hydroxypropyl cellulose, ethyl cellulose, methylcellulose, hydroxyethyl cellulose, and / or carboxymethylcellulose or a salt thereof.

5. The tablet composition according to claim 1 or 2, wherein the (D) gums include gum arabic and / or xanthan gum.

6. The tablet composition according to claim 1 or 2, wherein the content of (A) carbonate is 6% by mass or more and 23% by mass or less, based on the mass of the tablet composition.

7. The tablet composition according to claim 1 or 2, wherein the (A) carbonate comprises sodium carbonate or magnesium carbonate.

8. The tablet composition according to claim 1 or 2, wherein the (B) acid or salt thereof (excluding carbonates) comprises citric acid, malic acid, fumaric acid, tartaric acid, succinic acid, or ascorbic acid, or a salt thereof.

9. The tablet composition according to claim 1 or 2, wherein the content of (A) carbonate is 6 to 23% by mass, the content of (C) sorbitol and / or maltose is 35 to 80% by mass, and the content of (D) cellulose derivatives and / or gums is 0.5 to 8% by mass.

10. The tablet composition according to claim 1 or 2, wherein the tablet composition is an effervescent tablet.

11. The tablet composition according to claim 1 or 2, wherein the tablet composition is for oral use or for use in the mouth.

12. A method for increasing the hardness of a tablet composition containing (A) a carbonate and (B) an acid or a salt thereof (excluding carbonate), comprising: a method of adding to the tablet composition 35% by mass or more of (C) sorbitol and / or maltose and 0.5% by mass or more of (D) cellulose derivatives and / or gums based on the weight of the tablet composition.

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