Method for producing tablet containing fucose and dextrin, mixture, method for improving tableting suitability, and tablet

Abstract

To provide a technique for improving tableting suitability in production of a tablet containing fucose and dextrin.SOLUTION: A method for producing a tablet containing fucose and dextrin, comprising tableting a mixture containing fucose, dextrin, a sugar alcohol (A), and a polysaccharide (B) other than dextrin.SELECTED DRAWING: Absent

Description

[Technical Field]

[0001] The present invention relates to a tablet containing fucose and dextrin and a manufacturing technique thereof. [Background technology]

[0002] Fucose is a monosaccharide that constitutes fucoidan, a sticky component of brown algae such as mozuku and kombu. It is also found in human breast milk and exists as a constituent sugar of small intestinal mucin. In recent years, the useful physiological activities and flavor-improving effects of fucose have attracted attention, and technological developments for functional foods and food additives containing fucose as an active ingredient are actively underway (e.g., Patent Documents 1 to 4).

[0003] Fucose is available on the market in powder form using dextrin as an excipient (for example, Marine Fucose 30 (registered trademark, Yaizu Suisan Kagaku Kogyo Co., Ltd.)). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Publication No. 2023-175314 [Patent Document 2] Japanese Patent Publication No. 2023-175313 [Patent Document 3] Japanese Patent Application Publication No. 2023-133826 [Patent Document 4] Japanese Patent Publication No. 2023-109516 Summary of the Invention [Problem to be solved by the invention]

[0005] The present inventors have found that when tablets are produced using fucose provided in a powder form using dextrin as an excipient as described above, the tableting suitability is low, posing a problem in tableting. In view of such problems, an object of the present invention is to provide a technology for improving the tableting suitability during the production of tablets containing fucose and dextrin. [Means for solving the problem]

[0006] The present invention, which solves the above problems, is as follows. [1] A method for producing a tablet containing fucose and dextrin, comprising tableting a mixture containing fucose, dextrin, a sugar alcohol (A), and a polysaccharide other than dextrin (B).

[0007] [2] A mixture for producing tablets containing fucose and dextrin by tableting, further containing a sugar alcohol (A) and a polysaccharide other than dextrin (B).

[0008] [3] A method for improving tableting suitability when producing tablets containing fucose and dextrin, the method comprising adding a sugar alcohol (A) and a polysaccharide (B) other than dextrin to a mixture before tableting.

[0009] [4] A tablet containing fucose and dextrin, and further containing a sugar alcohol (A) and a polysaccharide other than dextrin (B).

[0010] [5] The sugar alcohol (A) includes a tetraose to dodecose sugar alcohol, The tablet according to [4], wherein the polysaccharide (B) contains a glucose polymer or an ether thereof.

[0011] [6] The sugar alcohol (A) includes erythritol and / or maltitol, The tablet according to [4] or [5], wherein the polysaccharide (B) comprises one or more selected from cellulose or its ether, and corn starch.

[0012] [7] The tablet according to any one of [4] to [6], wherein the sugar alcohol (A) is JIS 80 mesh on.

[0013] [8] The tablet according to any one of [4] to [7], wherein the polysaccharide (B) exhibits a particle size distribution in which particles of 20 μm or less account for 40% or more.

[0014] [9] The tablet according to any one of [4] to [8], wherein the sugar alcohol (A) contains erythritol and maltitol.

[0015]

[10] The tablet described in claim 4, wherein the polysaccharide (B) includes cellulose and corn starch.

[0016]

[11] The sugar alcohol (A) contains erythritol, The tablet according to any one of [4] to

[10] , wherein the polysaccharide (B) contains hydroxypropyl cellulose.

[0017]

[12] The sugar alcohol (A) includes erythritol and maltitol, The tablet according to any one of [4] to

[11] , wherein the polysaccharide (B) comprises cellulose, hydroxypropyl cellulose, and corn starch. [Effects of the Invention]

[0018] As specified in the production method of the present invention, the tableting suitability can be improved by adding a sugar alcohol (A) and a polysaccharide other than dextrin (B) to the mixture before tableting. The mixture of the present invention has excellent suitability for tableting. According to the method for improving tableting suitability of the present invention, it is possible to improve the tableting suitability when producing tablets containing fucose and dextrin. The tablets of the present invention can be produced with high suitability for tableting, and also suppress texture problems caused by dextrin, such as residue in the mouth and adhesion to teeth. DETAILED DESCRIPTION OF THE INVENTION

[0019] The present invention will be described in detail below by way of example. In the embodiments of the present invention, A (numerical value) to B (numerical value) means A or more and B or less. Furthermore, the preferred and more preferred embodiments exemplified below can be used in appropriate combinations with each other, regardless of expressions such as "for example," "one," "preferably," and "more preferred." Furthermore, the descriptions of numerical ranges are merely examples, and ranges obtained by appropriately combining the upper and lower limits of each range and the numerical values ​​of the examples can also be preferably used (for example, when A to B or C to D is described, the combinations A to D or C to B can be used). Furthermore, terms such as "contain" or "comprise" may be interpreted as "essentially consisting of" or "consisting only of."

[0020] The present invention is technically characterized in that a tablet containing fucose and dextrin uses a sugar alcohol (A) and a polysaccharide (B) other than dextrin.

[0021] Enantiomers of fucose (also known as 6-deoxygalactose) are known, and in the present invention, any of the L-form, D-form, a mixture thereof, or a racemic form may be used. It is more preferable to use L-fucose, which is abundant in nature.

[0022] There are no limitations on the dextrin used. The present invention is effective in suppressing deterioration in the texture of tablets produced using dextrin with a low DE value. Therefore, the present invention is suitable for use with dextrin having a DE value of preferably 3 to 18, more preferably 3 to 15, even more preferably 3 to 10, even more preferably 3 to 8, and even more preferably 3 to 5.

[0023] In the present invention, fucose powdered using dextrin as an excipient may be used as a raw material. An example of such powdered fucose is Marine Fucose 30 (registered trademark, Yaizu Suisan Kagaku Kogyo Co., Ltd.).

[0024] Although there are no limitations on the sugar alcohol (A) used, it is preferable to use one or more sugar alcohols selected from tetraose, pentose, hexose, heptose, octose, nonaose, decaose, decose, decanoose, or decanoose. Specific examples include erythritol, maltitol, sorbitol, and xylitol. It is particularly preferable to use either or both of erythritol and maltitol as the sugar alcohol (A), and it is particularly preferable to use both of these.

[0025] The sugar alcohol (A) can be used in powder form, and is preferably JIS 80 mesh on, more preferably JIS 60 mesh pass 80 mesh on.

[0026] There is no limitation on the polysaccharide (B) other than dextrin (hereinafter simply referred to as "polysaccharide (B)") to be used, but it is preferable to use a glucose polymer or its ether.

[0027] The glucose polymer may be either an α-glucose polymer or a β-glucose polymer.

[0028] A preferred example of the polymer of α-glucose is starch, and corn starch is particularly preferred.

[0029] A preferred example of the β-glucose polymer is cellulose, and a particularly preferred example is crystalline cellulose.

[0030] Preferred examples of the glucose polymer ether include cellulose ethers, specifically hydroxypropyl cellulose, hydroxypropylmethyl cellulose, and methyl cellulose, with hydroxypropyl cellulose being particularly preferred.

[0031] The polysaccharide (B) used preferably has a particle size distribution in which particles of 20 μm or less account for preferably 40% or more, more preferably 50% or more, and even more preferably 55% or more. The particle size distribution can be measured using a laser diffraction / scattering particle size distribution analyzer. The measurement may be either a dry method or a wet method, and it is preferable to use a polysaccharide (B) that falls within the above-mentioned numerical range in either or both of the measurement methods.

[0032] In one embodiment, cellulose and corn starch are used as polysaccharides (B).

[0033] In one embodiment, erythritol and / or maltitol is used as the sugar alcohol (A), and one or more selected from cellulose or its ether, and corn starch is used as the polysaccharide (B).

[0034] In one embodiment, erythritol is used as the sugar alcohol (A) and hydroxypropyl cellulose is used as the polysaccharide (B).

[0035] In one embodiment, erythritol and maltitol are used as the sugar alcohol (A), and cellulose, hydroxypropyl cellulose and corn starch are used as the polysaccharide (B).

[0036] In the present invention, any component may be used alone or in combination of two or more in an appropriate amount within a range that does not impair the effects of the present invention. Examples of the optional component include oily components, lubricants, excipients, disintegrants, binders, functional components other than the above components, colorants, and flavors. Specific examples of the optional component include the following components:

[0037] Examples of oily components include various fatty acid esters, hydrocarbons, higher fatty acids, and higher alcohols. Examples of lubricants include gum arabic, cocoa butter, carnauba wax, hydrated silicon dioxide, dried aluminum hydroxide gel, glycerin, magnesium silicate, liquid paraffin, sucrose fatty acid esters, stearyl alcohol, stearic acid, gelatin, lactose, sucrose, carboxymethyl calcium, carboxymethyl ammonium, fumaric acid, and beeswax. Examples of excipients include gum arabic, kaolin, cocoa butter, fructose, silicon dioxide, citric acid or a salt thereof, stearic acid or a salt thereof, carboxymethyl calcium, carboxymethyl ammonium, polyvinylpyrrolidone, macrogol, calcium hydrogen phosphate, sodium hydrogen phosphate, sucrose, and glucose. Examples of disintegrants include polyvinylpyrrolidone. Examples of binders include carboxymethyl calcium, carboxymethyl ammonium, gelatin, and vinylpyrrolidone.

[0038] The fucose content in the tablet is not particularly limited, but is preferably 0.4 to 80% by mass, 1 to 60% by mass, more preferably 5 to 40% by mass, and even more preferably 10 to 30% by mass.

[0039] The content of dextrin in the tablet is not particularly limited, but is preferably 1 to 80% by mass, more preferably 5 to 60% by mass, even more preferably 10 to 50% by mass, and still more preferably 20 to 40% by mass.

[0040] The content of the sugar alcohol (A) in the tablet is preferably 1 to 60% by mass, more preferably 5 to 50% by mass, even more preferably 10 to 40% by mass, and still more preferably 15 to 30% by mass.

[0041] The content of the polysaccharide (B) in the tablet is preferably 1 to 60% by mass, more preferably 5 to 50% by mass, even more preferably 10 to 40% by mass, and still more preferably 15 to 30% by mass.

[0042] When a cellulose ether is used, the content of the cellulose ether in the tablet is preferably 0.01 to 50% by mass, more preferably 0.05 to 30% by mass, even more preferably 0.1 to 20% by mass, and still more preferably 0.2 to 10% by mass.

[0043] The mass ratio of the polysaccharide (B) to the sugar alcohol (A) contained in the tablet is preferably 0.001-20, more preferably 0.01-10, even more preferably 0.02-5, and even more preferably 0.03-2.

[0044] In one embodiment, the mass ratio of the polysaccharide (B) to the sugar alcohol (A) contained in the tablet is preferably 0.1 to 10, more preferably 0.5 to 2, and even more preferably 0.7 to 1.5.

[0045] In one embodiment, the tablet contains erythritol and maltitol as the sugar alcohol (A), and the mass ratio of maltitol to erythritol is preferably 0.1 to 10, more preferably 0.5 to 2, and even more preferably 0.7 to 1.5.

[0046] In one embodiment, the tablet contains cellulose and cornstarch as the polysaccharide (B), and the mass ratio of the cornstarch to the cellulose is preferably 0.1 to 10, more preferably 0.5 to 2, and even more preferably 0.7 to 1.5.

[0047] The present invention relates to a mixture of the above-mentioned fucose, dextrin, sugar alcohol (A), polysaccharide (B), and selected optional ingredients, and compresses the mixture to produce tablets.

[0048] Tablet manufacturing methods include direct compression, wet compression, dry compression, etc. In the present invention, any method may be employed as long as it includes a step of tableting a mixture containing fucose, dextrin, sugar alcohol (A), and polysaccharide other than dextrin (B).

[0049] The manufacturing method of the present invention includes the steps of preparing a mixture of the above-mentioned components and compressing it into tablets. The compression conditions, such as compression pressure, vary depending on the tablet press, the type and amount of components, the tablet diameter, etc., but can be adjusted appropriately taking into account disintegration properties, tablet strength, oral disintegration rate, etc. The compression pressure can be set preferably to 1000 kg or more, more preferably 1200 kg or more, and preferably 2400 kg or less, more preferably 2000 kg or less.

[0050] The hardness of the tablet is not particularly limited, but is preferably 5 to 20 kgf, more preferably 5 to 15 kgf, even more preferably 6 to 13 kgf, and even more preferably 7 to 12 kgf. The tablet hardness is measured by placing a tablet vertically on an anvil and applying static pressure to the tablet with a moving plunger, and the force required to break the tablet. For example, the hardness can be measured using a Pharma test WHT-2ME (manufactured by Japan Machinery Co., Ltd.).

[0051] Application of the present invention can improve tableting suitability. In this specification, a tablet having a certain hardness is evaluated as having "high tableting suitability" when it can be produced with a smaller tableting force. Tableting suitability can be quantitatively expressed as a value obtained by dividing hardness (kgf) by tableting force (kg). In the examples described below, a value calculated by the following formula is used as the tableting suitability index. Hardness (kg) x 100 / striking force (kg) By applying the present invention, it is possible to achieve a hitting pressure suitability index of 0.45 or more, preferably 0.5 or more.

[0052] The mass per tablet is not particularly limited, but is preferably 100 to 3000 mg, more preferably 140 to 2500 mg, even more preferably 200 to 2000 mg, even more preferably 300 to 1850 mg, even more preferably 400 to 1800 mg, and even more preferably 500 to 1700 mg.

[0053] The tablets of the present invention thus produced exhibit properties of suppressing adhesion to teeth, discomfort, and retention in the mouth when orally ingested. [Example]

[0054] [Test Example 1] Pre-tabletting mixtures were prepared using the formulations investigated in Comparative Examples 1 to 5 and Examples 1 to 6 shown in Table 1, and tablet production was investigated by tableting these. The tablet press had a mechanical capacity of being able to apply a hammering force of up to 3000 kg, but was set to stop when a load of 2500 kg or more was applied. In practice, the maximum hammering force for this tablet press was 2400 kg. For each formulation investigated, the hammering force (kg) that could be achieved to form a tablet and the tablet hardness (kgf) at that time were recorded. In addition, the tablet suitability index was calculated using the following formula. Hardness (kgf) x 100 / impact pressure (kg) Then, as an overall evaluation, if the calculated tablet suitability index was less than 0.45, it was marked with "x", and if it was 0.45 or more, it was marked with "o". The results are also shown in Table 1.

[0055] [Table 1]

[0056] As shown in Table 1, when producing tablets containing fucose and dextrin, when the pre-tabletting mixture contained only either the sugar alcohol (A) or the polysaccharide (B), the tableting suitability was low (Comparative Examples 1 to 5). In Comparative Examples 3 and 4, the mixture had poor fluidity and could not even be tableted.

[0057] In contrast, when sugar alcohol (A) and polysaccharide (B) were added to the pre-tabletting mixture in producing tablets containing fucose and dextrin, the tabletting suitability index was significantly improved (Examples 1 to 6).

[0058] From the above results, it was found that when producing tablets containing fucose and dextrin, the tableting suitability can be improved by adding sugar alcohol (A) and polysaccharide (B) to the pre-tabletting mixture.

[0059] [Test Example 2] Tablet production was investigated by preparing pre-tabletting mixtures using the formulations investigated in Comparative Examples 6 to 10 and Examples 7 to 13 shown in Table 2 and compressing these mixtures. Table 3 also shows the contents (mass%) of sugar alcohol (A) and polysaccharide (B), which are key components of the present invention, in the tablets. [Table 2]

[0060] [Table 3]

[0061] The tablets of Comparative Examples 6 to 10 and Examples 7 to 13 were eaten by skilled evaluators, and the load at the first chewing and retention in the molars were evaluated according to the following indices. The results are shown in Table 3. <Load during initial chewing> 1. Lightweight and does not put strain on the back teeth 2. It is slightly light and does not put much strain on the back teeth. 3 There is a slight load on the back teeth 4. It is heavy and puts pressure on the back teeth. 5. It is very heavy and puts a lot of strain on the back teeth. <Stagnation in the back teeth> 1. No adhesion to teeth 2. There is a little adhesion to the teeth. 3. Adhesion to teeth 4. High adhesion to teeth 5. High adhesion to teeth

[0062] The evaluation scores from the two sensory evaluations described above were added together to calculate a total score. The overall evaluation was then marked with an "x" if the total score was 7 or more, and marked with an "o" if the total score was less than 7 (Table 3).

[0063] As shown in Table 3, when only one of the sugar alcohol (A) and the polysaccharide (B) was contained in addition to fucose and dextrin, the chewing load was high, there was a lot of adhesion to the teeth, and the texture when eaten was poor (Comparative Examples 6, 7, and 10). Comparative Examples 8 and 9 could not be produced because they could not be compressed into tablets.

[0064] In contrast, tablets containing sugar alcohol (A) and polysaccharide (B) in addition to fucose and dextrin were found to be extremely easy to eat because they placed less strain on the body when chewed and did not stick to the teeth as much.

[0065] [Test Example 3] Tablet production was investigated by preparing pre-tabletting mixtures using the formulations investigated in Comparative Examples 11 and 12 and Examples 14 to 18 shown in Table 4 and compressing these mixtures. Table 5 also shows the contents (mass%) of sugar alcohol (A) and polysaccharide (B), which are key components of the present invention, in the tablets. [Table 4]

[0066] [Table 5]

[0067] The tablets of Comparative Examples 11 and 12 and Examples 14 to 18 were subjected to a disintegration test. Specifically, the tablets were placed in stirred water, and the time it took for visual confirmation that all six tablets used in the test had disappeared was measured. The results are shown in Table 5. Furthermore, the tablets of Examples 14 to 18 were eaten by skilled evaluators, and the texture was evaluated according to the following criteria. The results are shown in Table 5. <roughness> 1. No roughness 2. A little rough 3. Feels rough 4. Slightly rough texture 5 also has a very strong azalea feel.

[0068] As shown in Table 5, it was found that the tablets of the Examples containing both sugar alcohol (A) and polysaccharide (B) were superior in disintegration property compared to the tablets of the Comparative Examples containing only one of these. In particular, the tablets of Examples 17 and 18 showed superior disintegration property compared to the other Examples. Similarly, it was found that the tablets of Examples 17 and 18 had a reduced crumbly feeling compared to the tablets of the other Examples.

[0069] The results shown in Table 5 indicate that the inclusion of hydroxypropyl cellulose is preferable for improving disintegration properties and texture.

[0070] Furthermore, the results shown in Table 5 indicate that the inclusion of erythritol and maltitol as sugar alcohols is preferable for improving disintegration properties and texture.

[0071] Furthermore, the results shown in Table 5 indicate that the inclusion of cellulose and cornstarch as polysaccharides is preferable for improving disintegrability and texture.

[0072] [Manufacturing example] A pre-tabletting mixture was prepared according to the formulation shown in Table 6, and the tablets of Examples 19 to 22 were produced by tableting this mixture. [Table 6]

[0073] The pre-tabletting mixtures prepared with the formulations of Examples 19 to 22 are excellent in suitability for tabletting. Furthermore, the tablets of Examples 19 to 22 are extremely easy to eat because they impose a light load on chewing and do not stick to the teeth as much. [Industrial Applicability]

[0074] The present invention can be applied to tablet manufacturing technology.

Claims

1. A method for producing a tablet containing fucose and dextrin, the method comprising tableting a mixture containing fucose, dextrin, a sugar alcohol (A) and a polysaccharide other than dextrin (B).

2. A mixture for producing a tablet containing fucose and dextrin by tableting, the mixture further containing a sugar alcohol (A) and a polysaccharide other than dextrin (B).

3. A method for improving tableting suitability when producing tablets containing fucose and dextrin, the method comprising adding a sugar alcohol (A) and a polysaccharide (B) other than dextrin to a mixture before tableting.

4. A tablet containing fucose and dextrin, and further containing a sugar alcohol (A) and a polysaccharide other than dextrin (B).

5. The sugar alcohol (A) includes a tetraose to dodecose sugar alcohol, The tablet according to claim 4, wherein the polysaccharide (B) comprises a glucose polymer or an ether thereof.

6. The sugar alcohol (A) includes erythritol and / or maltitol, The tablet according to claim 4, wherein the polysaccharide (B) comprises one or more selected from the group consisting of cellulose or its ether, and corn starch.

7. The tablet according to claim 4, wherein the sugar alcohol (A) has a JIS 80 mesh size.

8. 5. The tablet according to claim 4, wherein the polysaccharide (B) has a particle size distribution in which particles of 20 μm or less account for 40% or more.

9. The tablet according to claim 4, wherein the sugar alcohol (A) comprises erythritol and maltitol.

10. The tablet according to claim 4, wherein the polysaccharide (B) comprises cellulose and corn starch.

11. The sugar alcohol (A) contains erythritol, The tablet according to claim 4, wherein the polysaccharide (B) comprises hydroxypropyl cellulose.

12. The sugar alcohol (A) includes erythritol and maltitol, The tablet according to any one of claims 4 to 11, wherein the polysaccharide (B) comprises cellulose, hydroxypropyl cellulose, and corn starch.

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