Solid components

Abstract

To provide a solid composition that leaves little unpleasant feeling on the tongue when taken in the mouth, while having an increased content of rosmarinic acid or a salt thereof.SOLUTION: A solid composition contains following components (A) and (B): (A) rosmarinic acid or a salt thereof 1-20 mass% and (B) at least one selected from maltitol and dextrin. The mass ratio between the component (A) and the component (B) [(B) / (A)] is 2.5-14. In the solid composition, the content of the component (B) is 3-60 mass%.SELECTED DRAWING: None

Description

[Technical Field]

[0001] The present invention relates to a solid composition. [Background technology]

[0002] Rosmarinic acid or a salt thereof has been reported to have physiologically active functions such as preventing or improving nocturia and extending the duration of non-REM sleep, and its application to solid compositions such as supplements is being considered, for example (Patent Documents 1 and 2). [Prior art documents] [Patent documents]

[0003] [Patent Document 1] Patent No. 6621558 specification [Patent Document 2] Japanese Patent Publication No. 2020-103172 Summary of the Invention [Problem to be solved by the invention]

[0004] The present inventors conducted research to develop an edible solid composition containing rosmarinic acid. As a result, they found that a solid composition containing rosmarinic acid has a problem in that, when orally ingested, rosmarinic acid irritates the tongue, causing an unpleasant aftertaste. Therefore, they found that adding a sugar alcohol to rosmarinic acid can somewhat reduce the unpleasant aftertaste caused by rosmarinic acid, but also creates a new problem in that, when orally ingested, the sugar alcohol causes an unpleasant aftertaste. An object of the present invention is to provide a solid composition which contains rosmarinic acid or a salt thereof and which is suppressed from leaving an unpleasant aftertaste on the tongue when orally taken. [Means for solving the problem]

[0005] As a result of studies conducted in light of the above-mentioned problems, the present inventors have found that by incorporating a specific sugar alcohol and / or dextrin in a specific quantitative ratio relative to a high concentration of rosmarinic acid or a salt thereof, a solid composition can be obtained that enhances the rosmarinic acid or a salt thereof while suppressing the unpleasant aftertaste left on the tongue when orally ingested.

[0006] That is, the present invention provides a composition comprising the following components (A) and (B): (A) 1 to 20% by mass of rosmarinic acid or a salt thereof, and (B) one or more selected from maltitol and dextrin Including, the mass ratio of component (A) to component (B) [(B) / (A)] is 2.5 to 14; A solid composition is provided. [Effects of the Invention]

[0007] According to the present invention, it is possible to provide a solid composition that is enriched with rosmarinic acid or a salt thereof and that suppresses the unpleasant aftertaste left on the tongue when orally ingested. DETAILED DESCRIPTION OF THE INVENTION

[0008] In the present invention, "(A) rosmarinic acid" is a compound represented by the following formula (1), and is a type of polyphenol.

[0009] [ka]

[0010] Rosmarinic acid exists as optical isomers, and the rosmarinic acid of the present invention may be any one of the optical isomers or a mixture of the optical isomers.

[0011] Rosmarinic acid may be in the form of a salt. The salt is not particularly limited as long as it is physiologically acceptable, and examples thereof include alkali metal salts, alkaline earth metal salts, ammonium salts, and organic amine salts. Examples of alkali metal salts include sodium salts and potassium salts, and examples of alkaline earth metal salts include calcium salts and magnesium salts. Examples of organic amine salts include triethylamine salts, triethanolamine salts, and monoethanolamine salts. Of these, alkali metal salts are preferred.

[0012] Commercially available reagents may be used as component (A), but extracts or purified products thereof from plants rich in component (A) can also be used. Examples of natural products containing component (A) include plants of the Lamiaceae family. Specifically, at least one species selected from the group consisting of red perilla (Perilla frutescens Britton var. acuta Kudo), blue perilla (Perilla frutescens var. crispa f. viridis. Makino), rosemary (Rosmarinus officinalis), lemon balm (Melissa officinalis), sage (Salvia officinalis), and kumisukuchin (Orthosiphon aristatus) are preferred. Conventional extraction methods can be used, including stirring extraction and column extraction. Purification methods are not particularly limited as long as they can increase the purity of rosmarinic acid, but examples include dialysis, ultrafiltration, and chromatography.

[0013] The solid composition of the present invention contains rosmarinic acid or a salt thereof as component (A), and the content thereof is enhanced to 1 to 20% by mass. From the viewpoint of enhancing physiological effects, the content of component (A) in the solid composition of the present invention is preferably 2% by mass or more, more preferably 2.5% by mass or more, and even more preferably 2.7% by mass or more. From the viewpoint of suppressing an unpleasant aftertaste on the tongue, the content is preferably 18% by mass or less, more preferably 10% by mass or less, and even more preferably 4% by mass or less. The content of component (A) is preferably in the range of 2 to 18% by mass, more preferably 2.5 to 10% by mass, and even more preferably 2.7 to 4% by mass. The content of component (A) is measured according to the "Analysis of rosmarinic acid or a salt thereof" described in the Examples below.

[0014] The solid composition of the present invention contains one or more components selected from maltitol and dextrin as component (B), and from the viewpoint of suppressing an unpleasant aftertaste on the tongue, component (B) is contained in a specific ratio to component (A). Specifically, the mass ratio of component (A) to component (B) [(B) / (A)] is 2.5 to 14, and from the viewpoint of more excellent suppression of an unpleasant aftertaste on the tongue, it is preferably 3 or more, more preferably 3.2 or more, even more preferably 5 or more, even more preferably 8 or more, and preferably 13 or less, more preferably 12 or less, even more preferably 10 or less, and even more preferably 9 or less. The range of such mass ratio [(B) / (A)] is preferably 3 to 13, more preferably 3.2 to 12, even more preferably 5 to 10, and even more preferably 8 to 9.

[0015] Component (B) contains one or more selected from maltitol and dextrin, with maltitol being preferred from the viewpoint of providing a good taste.

[0016] The maltitol used as component (B) can be either crystalline maltitol or crystalline maltitol. Commercially available maltitol may be used. Examples of commercially available maltitol include Amalty MR-100 (manufactured by Mitsubishi Corporation Foodtech Co., Ltd.) and SweetPearl (manufactured by Rocket Co., Ltd.).

[0017] The dextrin of component (B) refers to a material obtained by hydrolyzing raw starch with enzymes or acids. Dextrose equivalent (DE value) is commonly used as an indicator of the degree of hydrolysis of raw starch. The DE value of the dextrin used in the present invention is preferably 2 to 30, more preferably 2 to 13, and even more preferably 2 to 5, from the viewpoint of suppressing an unpleasant aftertaste on the tongue. The DE value can be analyzed by commonly known dextrose measurement methods, such as the Wilstätter-Schudel method. Dextrin has a molecular structure in which sugars are polymerized via glycosidic bonds. The glycosidic bonds may be linear, cyclic, or a mixture of these. Examples of sugar linkages include α-1,4, α-1,6, β-1,2, β-1,3, β-1,4, and β-1,6 bonds. A single linkage or two or more linkages may be used. Commercially available dextrins may be used, such as Sandec #30 (manufactured by Sanwa Starch Co., Ltd.).

[0018] The content of component (B) in the solid composition of the present invention can be appropriately selected so long as the mass ratio [(B) / (A)] falls within the above range. From the viewpoint of suppressing an unpleasant aftertaste on the tongue, the content is preferably 3% by mass or more, more preferably 5% by mass or more, even more preferably 10% by mass or more, even more preferably 15% by mass or more, and is preferably 60% by mass or less, more preferably 45% by mass or less, even more preferably 40% by mass or less, and even more preferably 35% by mass or less. The content of component (B) is preferably in the range of 3 to 60% by mass, more preferably 5 to 45% by mass, even more preferably 10 to 40% by mass, and even more preferably 15 to 35% by mass. The content of component (B) is measured according to the "Analysis of Maltitol" and "Analysis of Dextrin" described in the Examples below.

[0019] The solid composition of the present invention is not particularly limited as long as it is solid at room temperature (20°C ± 15°C), and may take any appropriate form, such as powder, granules, tablets, rods, plates, or blocks. The solid content of the solid composition of the present invention is usually 95% by mass or more, preferably 97% by mass or more. The upper limit of the solid content is not particularly limited and may be 100% by mass. Here, in this specification, the "solid content" refers to the mass of the residue remaining after drying a sample in an electric thermostatic dryer at 105°C for 3 hours and removing volatile substances. Furthermore, the size of the solid composition of the present invention can be appropriately selected depending on the form of the solid composition, as long as it can be ingested by chewing.

[0020] The solid composition of the present invention can be provided as a food, pharmaceutical, or quasi-drug, but is preferably a solid food, more preferably a powdered food, in that the effects of the present invention can be more easily enjoyed. When the solid composition of the present invention is a food, it can be a food with health claims, which includes foods for specified health uses and foods with nutrient functions as defined by the Japanese government, such as foods for suppressing antioxidant activity and preventing or improving blood pressure. Furthermore, when the solid composition of the present invention is a pharmaceutical or quasi-drug, its dosage form may be, for example, granules, powders, tablets, pills, chewable tablets, lozenges, etc. Furthermore, when it is made into a tablet, it may be a divided tablet with a score line.

[0021] The solid composition of the present invention may contain an acceptable carrier as needed to form a solid. For example, excipients (e.g., monosaccharides such as glucose, galactose, fructose, etc.; disaccharides such as sucrose, lactose, maltose, etc.; sugar alcohols such as xylitol, sorbitol, etc. (excluding maltitol); starch hydrolysates such as powdered sugar (excluding starch); oligosaccharides, crystalline cellulose, light anhydrous silicic acid, calcium hydrogen phosphate, etc.), binders (e.g., hydroxypropylmethylcellulose, hydroxypropylcellulose, gelatin, pregelatinized starch, polyvinylpyrrolidone, polyvinyl alcohol, pullulan, methylcellulose, hydrogenated oil, etc.), gelling agents, etc. Examples of carriers include disintegrants (e.g., xanthan gum, locust bean gum, etc.), disintegrants (e.g., carmellose, carmellose calcium, croscarmellose sodium, crospovidone, corn starch, low-substituted hydroxypropyl cellulose, etc.), lubricants (e.g., calcium stearate, magnesium stearate, sucrose fatty acid esters, sodium stearyl fumarate, talc, silicon dioxide, etc.), flavoring agents (e.g., stevia, etc.), fillers, surfactants, dispersants, buffers, antioxidants, preservatives, quality stabilizers, diluents, etc. Furthermore, the solid composition of the present invention may contain one or more additives such as acidulants, amino acids, proteins, vitamins, minerals, flavorings, fruit juices, plant extracts, esters, colorings, milk components, cocoa powder, seasonings, vegetable oils, etc. in order to enhance palatability, etc. The contents of the carrier and additives can be appropriately set within a range that does not impair the object of the present invention.

[0022] The solid composition of the present invention can be produced by conventional methods, and any suitable method can be employed. For example, a powdered solid composition can be produced by mixing specific amounts of component (A) and component (B), and optionally a carrier and / or additives, so that the mass ratio of component (A) to component (B) [(B) / (A)] falls within a predetermined range. The order of mixing component (A) and component (B) is not particularly limited; one may be added to the other, or both may be added simultaneously. Suitable mixing methods, such as stirring and shaking, can be employed, but a mixing device can also be used. The mixing method of the mixing device may be either a rotating container type or a fixed container type. Examples of rotating container types that can be used include horizontal cylindrical, V-type, double-cone, and cubic types. Examples of fixed container types that can be used include ribbon, screw, conical screw, paddle, fluidized bed, and Phillips blenders.

[0023] The mixture can also be compressed to form a desired shape. For example, in the case of tablet form, the mixture can be directly compressed (direct powder compression method), or granulated using dry granulation, wet granulation, or the like and then compressed (granule compression method). When producing tablets by direct compression, a rotary tablet press or a single-punch tablet press can be used as the tablet press. When granulating by granulation and then forming tablets, methods can be used in which granules are produced by extrusion granulation using a cylindrical granulator, spherical granulator, pelleter, or the like; crushing granulation using a speed mill, power mill, or the like; tumbling granulation, stirring granulation, fluidized bed granulation, or the like, followed by drying and sieving, and the resulting granules are compressed in the tablet press to form tablets.

[0024] When the solid composition of the present invention is in the form of granules, it may be granulated by a known granulation method. Examples of the granulation method include spray granulation, fluidized bed granulation, compression granulation, tumbling granulation, stirring granulation, extrusion granulation, and powder coating granulation. The granulation conditions can be appropriately selected depending on the granulation method.

[0025] The solid composition of the present invention can be filled into a package. Examples of the package include bottles, cans, jars, box-shaped containers, stick-shaped packages, and pillow-shaped packages. When filling the package with the solid composition of the present invention, a commercially available filling machine may be used. [Example]

[0026] 1. Analysis of rosmarinic acid or its salts The sample solution was filtered through a 0.45 μm filter and analyzed using a high-performance liquid chromatograph (Model LC-20 Prominence, Shimadzu Corporation) equipped with a Cadenza CDC18 (3 μm, 4.6 mmφ × 150 mm, Imtakt) column at 35°C using a gradient method. The mobile phase A was a 5% acetonitrile solution containing 0.05 mol / L acetic acid, 0.01 mol / L sodium acetate, and 0.1 mmol / L HEDPO, and the mobile phase B was an acetonitrile solution. The flow rate was 1 mL / min, the sample injection volume was 10 μL, and the UV detector wavelength was 325 nm. The gradient conditions were as follows:

[0027] Concentration gradient conditions Time (min) Concentration of solution A (volume %) Concentration of solution B (volume %) 0 100% 0% 10 100% 0% 15 95% 5% 20 95% 5% 22 92% 8% 50 92% 8% 52 10% 90% 60 10% 90% 60.1 100% 0% 70 100% 0%

[0028] 2. Analysis of Maltitol This was carried out by HPLC (high performance liquid chromatography) according to the following method. The analytical equipment configuration is as follows: Detector: Differential refractometer RID-10A (Shimadzu Corporation) Column: Shodex Asahipak NH2P-50 4E, φ4.6 mm x 250 mm (Showa Denko)

[0029] The analysis conditions were as follows: Column temperature: Room temperature Mobile phase: A mixture of acetonitrile and water (81:19 volume ratio) ·Flow rate: 1mL / min Sample injection volume: 20 μL

[0030] The analytical samples were prepared according to the following procedure. 3 g of sample was weighed out, dissolved in 10 mL of water, and neutralized. The solution was subjected to ultrasonic extraction using an ultrasonic cleaner for 30 minutes. Water was added to the solution to make a constant volume of 20 mL. The solution was filtered through a membrane filter to obtain the sample solution. The sample solution was then subjected to high-performance liquid chromatography analysis.

[0031] 3. Analysis of Dextrin To 1.5 mL of the sample and standard solutions of each concentration, add 250 μL of 1N NaOH aqueous solution and 500 μL of 0.5 M PMP (3-methyl-1-phenyl-5-pyrazolone)-methanol solution, and heat at 70°C for 30 minutes. The resulting solution is neutralized with 250 μL of 1N HCl aqueous solution, and 5 mL of chloroform is added and partitioned. The aqueous layer is used as the measurement sample. The measurement sample obtained by the above procedure is measured using high-performance liquid chromatography mass spectrometry under the following conditions.

[0032] Analysis conditions HPLC equipment: ACQUITY UPLC, manufactured by Waters MS equipment: SYNAPT G2-S HDMS model, manufactured by Waters Ionization: ESI ·Mass range: m / z 100-2500 Column: Unison UK-C18 UP (2.0 x 100 mm, 3 μm), manufactured by Intact Mobile phase: Solution C: 0.05% formic acid in water, Solution D: acetonitrile (%D = 15 → 90) ·Flow rate: 0.6mL / min ·Injection volume: 1μL

[0033] 4. Sensory test The feeling of the product remaining on the tongue was evaluated by three panelists based on the following criteria, and then a final score was determined by discussion.

[0034] Evaluation criteria for residual sensation on the tongue 4: No lingering feeling. 3: Almost no lingering feeling. 2: There is a slight lingering feeling. 1: I feel a lingering aftertaste.

[0035] Examples 1 to 3 and Comparative Examples 1 to 3 The components were mixed in the proportions shown in Table 1 to obtain 10 g of powdered food. 50 mg of the obtained powdered food was directly orally ingested, and a sensory evaluation was performed. The results are shown in Table 1. As the evaluation standard for the sensory evaluation, the panelists agreed that Comparative Example 1, which does not contain component (B) maltitol, would be scored as "1.0 (lingering feeling)," and then other powdered foods containing component (B) were evaluated to determine the extent to which the lingering feeling was suppressed.

[0036] [Table 1]

[0037] Examples 4 to 5 and Comparative Examples 4 to 6 The components were mixed in the proportions shown in Table 2 to obtain 10 g of powdered food. 50 mg of the obtained powdered food was directly orally ingested, and a sensory evaluation was performed. The results are shown in Table 2. As the evaluation standard for the sensory evaluation, the panelists agreed that Comparative Example 4, which does not contain component (B) maltitol, would be scored as "2.5 (somewhat lingering aftertaste)." After that, they evaluated other powdered foods containing component (B) to evaluate the extent to which the lingering aftertaste was suppressed.

[0038] [Table 2]

[0039] Examples 6 to 8 and Comparative Example 7 The components were mixed in the proportions shown in Table 3 to obtain 10 g of powdered food. 50 mg of the obtained powdered food was directly orally ingested, and a sensory evaluation was performed. The results are shown in Table 3. As the evaluation standard for the sensory evaluation, the panelists agreed that Comparative Example 7, which does not contain component (B) maltitol, would be scored as "1.0 (lingering feeling)." After that, they evaluated other powdered foods containing component (B) to evaluate the extent to which the lingering feeling was suppressed.

[0040] [Table 3]

[0041] Examples 9-10 and Comparative Examples 8-9 The components were mixed in the proportions shown in Table 4 to obtain 10 g of powdered food. 50 mg of the obtained powdered food was directly orally ingested, and a sensory evaluation was performed. The results are shown in Table 4. As the evaluation standard for the sensory evaluation, the panelists agreed that Comparative Example 8, which does not contain component (B) maltitol, would be scored as "1.0 (lingering feeling)." After that, they evaluated other powdered foods containing component (B) to evaluate the extent to which the lingering feeling was suppressed.

[0042] [Table 4]

[0043] Example 3, Example 11, Comparative Example 1, and Comparative Examples 10 to 11 The components were mixed in the proportions shown in Table 5 to obtain 10 g of powdered food. 50 mg of the obtained powdered food was directly orally ingested, and a sensory evaluation was performed. The results are shown in Table 5. As the evaluation standard for the sensory evaluation, the panelists agreed that Comparative Example 1, which does not contain component (B) maltitol, would be scored as "1.0 (lingering aftertaste)." After that, other powdered foods containing component (B) and other powdered foods containing sugar alcohols other than component (B) were evaluated to determine the extent to which the lingering aftertaste was suppressed.

[0044] [Table 5]

[0045] Tables 1 to 5 show that by incorporating component (B) in a specific ratio relative to component (A), a solid composition can be obtained that enhances rosmarinic acid while suppressing the unpleasant aftertaste left on the tongue when orally ingested.

[0046] The solid composition of the present invention can be prepared by a conventional method according to the formulation shown below.

[0047] [Prescription example 1] tablet Rosmarinic acid 4.6% by mass Maltitol 43.0% by mass Calcium stearate 0.5% by mass Lactose 51.9% by mass Total 100.0% by mass

[0048] [Prescription example 2] tablet Rosmarinic acid 4.6% by mass Dextrin (DE2-5) 43.0% by mass Calcium stearate 0.5% by mass Lactose 51.9% by mass Total 100.0% by mass

[0049] [Prescription example 3] tablet Rosmarinic acid 4.6% by mass Maltitol 43.0% by mass Calcium stearate 0.5% by mass Pregelatinized starch 25.0% by mass Xanthan gum 2.5% by mass Locust bean gum 2.5% by mass Lactose 21.9% by mass Total 100.0% by mass

[0050] [Prescription Example 4] tablet Rosmarinic acid 4.6% by mass Maltitol 43.0% by mass Calcium stearate 0.5% by mass Pregelatinized starch 16.0% by mass Xanthan gum 12.0% by mass Locust bean gum 12.0% by mass Lactose 11.9% by mass Total 100.0% by mass

[0051] [Prescription Example 5] tablet Rosmarinic acid 4.6% by mass Dextrin (DE2-5) 43.0% by mass Calcium stearate 0.5% by mass Pregelatinized starch 25.0% by mass Xanthan gum 2.5% by mass Locust bean gum 2.5% by mass Lactose 21.9% by mass Total 100.0% by mass

[0052] [Prescription Example 6] tablet Rosmarinic acid 4.6% by mass Dextrin (DE2-5) 43.0% by mass Calcium stearate 0.5% by mass Pregelatinized starch 16.0% by mass Xanthan gum 12.0% by mass Locust bean gum 12.0% by mass Lactose 11.9% by mass Total 100.0% by mass

[0053] [Prescription Example 7] Tablets with coating layer Oral tablets having 25 parts by weight of a coating layer on the surface of the solid dosage form per 100 parts by weight of the solid dosage form described below.

[0054] <Solid dosage section> Rosmarinic acid 4.6% by mass Maltitol 43.0% by mass Calcium stearate 0.5% by mass Lactose 51.9% by mass Total 100.0% by mass <Coating layer> Pregelatinized starch 50.0% by mass Xanthan gum 25.0% by mass Locust bean gum 25.0% by mass Total 100.0% by mass

[0055] [Prescription Example 8] Tablets with coating layer Oral tablets having 5 parts by mass of coating layer on the surface of the solid dosage form per 100 parts by mass of the solid dosage form described below.

[0056] <Solid dosage section> Rosmarinic acid 4.6% by mass Maltitol 43.0% by mass Calcium stearate 0.5% by mass Lactose 51.9% by mass Total 100.0% by mass <Coating layer> Pregelatinized starch 33.3% by mass Xanthan gum 16.7% by mass Locust bean gum 16.7% by mass Erythritol 33.3% by mass Total 100.0% by mass

[0057] [Prescription Example 9] Tablets with coating layer Oral tablets having 25 parts by weight of a coating layer on the surface of the solid dosage form per 100 parts by weight of the solid dosage form described below.

[0058] <Solid dosage section> Rosmarinic acid 4.6% by mass Dextrin (DE2-5) 43.0% by mass Calcium stearate 0.5% by mass Lactose 51.9% by mass Total 100.0% by mass <Coating layer> Pregelatinized starch 50.0% by mass Xanthan gum 25.0% by mass Locust bean gum 25.0% by mass Total 100.0% by mass

[0059] [Prescription Example 10] Tablets with coating layer Oral tablets having 5 parts by mass of coating layer on the surface of the solid dosage form per 100 parts by mass of the solid dosage form described below.

[0060] <Solid dosage section> Rosmarinic acid 4.6% by mass Dextrin (DE2-5) 43.0% by mass Calcium stearate 0.5% by mass Lactose 51.9% by mass Total 100.0% by mass <Coating layer> Pregelatinized starch 33.3% by mass Xanthan gum 16.7% by mass Locust bean gum 16.7% by mass Erythritol 33.3% by mass Total 100.0% by mass

Claims

1. The following components (A) and (B): (A) 2.3 to 6.8% by mass of rosmarinic acid or a salt thereof, and (B) Maltitol Including, the mass ratio of component (A) to component (B) [(B) / (A)] is 3.2 to 14; Solid composition.

2. The solid composition according to claim 1, wherein the content of component (B) is 3 to 60 mass %.

3. A solid composition according to claim 1 or 2, wherein the mass ratio of component (A) to component (B) [(B) / (A)] is 3.2 to 12.

7.

4. The solid composition according to any one of claims 1 to 3, which is a powdered food.

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