Oral composition, bitter taste shielding method for oral composition, and method for producing oral composition

Abstract

The purpose of the present invention is to readily provide an oral composition which contains Atrimol B and in which bitterness is masked. In order to achieve the above-described purpose, the solution of the present invention is to provide an oral composition containing a powder of the following component (a) and at least one powder selected from the following components (B1)-(C): (a) Arimol B, (B1) a cellulose derivative having a viscosity of 2-800 mPa.s at a shear rate in a 2% aqueous solution at 20 DEG C, (B2) 0.5-40% by mass of carrageenan, and (B3) an aqueous solution having a viscosity of 2-800 mPa.s at a shear rate at 20 DEG C, (B4) 0.5-40% by mass of carrageenan, (B5) 0.5-40% by mass of carrageenan, and (B5) 0.5-40% by mass of carrageenan. (B3) is 1%-40% by mass of alpha starch, (B4) is 1%-30% by mass of disaccharide sugar alcohol, (B5) is 1%-40% by mass of straight-chain dextrin or branched-chain dextrin with dextrose equivalent (DE) of 2-20, and (C) is 0.5%-10% by mass of metal salt of higher fatty acid or sucrose fatty acid ester.

Description

Technical Field

[0001] This invention relates to an oral composition, a method for masking the bitterness of an oral composition, and a method for manufacturing an oral composition, particularly an oral composition for use in pharmaceuticals, health foods, and other fields, a method for masking the bitterness of an oral composition, and a method for manufacturing an oral composition with masked bitterness. Background Technology

[0002] Food, medicine, and quasi-drugs ingested orally contain ingredients that have unpleasant tastes. While sour, bitter, salty, and sweet are generally important tastes, overly strong flavors can reduce consumer appeal.

[0003] In recent years, Agrimol B has attracted much attention as an active ingredient in food, pharmaceuticals, and quasi-drugs. It has been found that in addition to activating SIRT1, known as the longevity gene, which can prevent aging and prolong life, it also has a whitening effect by inhibiting melanin production, improving type I allergic reactions, and inhibiting muscle atrophy, among other pharmacological effects.

[0004] Although it is an ingredient with multiple uses and many ongoing studies, when used as an oral formulation of food or medicine, Agrimol B has a strong bitter taste that affects consumer preference, thus reducing its market value and making it difficult to take as a drug.

[0005] As a method for suppressing unpleasant tastes such as strong bitterness in food or medicine, Patent Document 1 discloses an oil-containing food that significantly reduces the bitterness, astringency, and spiciness of flavonoids by using an oil phase containing diacylglycerols and an aqueous phase containing flavonoid glycosides. Patent Document 2 discloses a method for suppressing the astringency of naringin by adding 0.001 to 2 parts by weight of sucralose relative to 1 part by weight of naringin.

[0006] Existing technical documents

[0007] Patent documents

[0008] Patent Document 1: Japanese Patent Application Publication No. 2007-129983

[0009] Patent Document 2: Patent No. 5259149 Summary of the Invention

[0010] The problem to be solved by the present invention

[0011] Generally, when an active ingredient with a very strong bitter taste is formulated into an oral dosage form, additional formulation design is required to mask the bitterness, such as sugar-coated tablets or film-coated tablets as tablets, or film-coated granules as granules. However, such increased manufacturing processes lead to cost issues. On the other hand, a simple and low-cost method has not yet been established to suppress the excessively strong bitterness in foods and oral pharmaceuticals containing Agrimol B. Because dosage forms containing Agrimol B exhibit a strong bitter taste, a simple and low-cost method is needed to suppress this strong bitterness.

[0012] Therefore, the objective of this invention is to readily provide oral compositions that mask the bitterness of Agrimol B.

[0013] Methods for solving problems

[0014] As a result of in-depth research into the above-mentioned issues, the inventors discovered that by coating or granulating powder containing Agrimol B and widely used specific excipients and additives, the strong bitter taste of Agrimol B can be masked in a simple and low-cost manner, thus completing the present invention.

[0015] In other words, the present invention provides the following [1] to [6].

[0016] [1] An oral composition comprising a powder containing component (a) and at least one powder selected from components (B1) to (C), wherein:

[0017] Component (a) is Agrimol B.

[0018] Component (B1) is a cellulose derivative with a viscosity of 2~800 mPa·s at a shear rate in a 2% aqueous solution at 20℃.

[0019] Component (B2) consists of 0.5% to 40% carrageenan by weight.

[0020] Component (B3) consists of 1% to 40% by weight of α-starch.

[0021] Component (B4) is a disaccharide sugar alcohol, comprising 1% to 30% by weight.

[0022] Component (B5) is a linear or branched dextrin with a mass percentage of 1% to 40% and a dextran equivalent (DE) of 2 to 20.

[0023] Component (C) is 0.5% to 10% by mass of metal salts or sucrose fatty acid esters of higher fatty acids.

[0024] Using this oral composition, even when Agrimol B, which has a strong bitter taste, is included, an oral composition that avoids masking the bitterness caused by the bitterness can be obtained by further including a powder containing specific, widely used excipients and additives.

[0025] [2] The oral composition as described in [1], wherein component (a) is component (A) Agrimonia pilosa extract.

[0026] Based on this characteristic, Agrimol B, being a natural product derived from Agrimonia pilosa extract, meets the needs of consumers who prefer natural products. Furthermore, depending on the choice of extraction and purification methods, an oral formulation can be obtained, in which the purity and content of Agrimol B can be easily adjusted as needed, and costs can be reduced.

[0027] [3] An oral composition as described in [1] or [2], wherein the oral composition comprises a powder selected from at least one of components (B1) to (B5) and a powder of component (C).

[0028] Based on this feature, by using a powder containing both component (C) and at least one selected from components (B1) to (B5), an oral composition with an additive effect in which components (B1) to (B5) and component (C) together have a bitterness-inhibiting effect can be obtained.

[0029] [4] An oral composition as described in any of [1] to [3], wherein the ratio of the content of component (B1) to component (C) relative to the content of component (a) is one or more of the following:

[0030] The ratio (B1 / a) of the content of component (B1) to the content of component (a) is 1 to 450;

[0031] The ratio (B2 / a) of the content of component (B2) to the content of component (a) is 2 to 450;

[0032] The ratio (B3 / a) of the content of component (B3) to the content of component (a) is 10 to 450;

[0033] The ratio (B4 / a) of the content of component (B4) to the content of component (a) is 10 to 450;

[0034] The ratio (B5 / a) of the content of component (B5) to the content of component (a) is 5 to 450;

[0035] The ratio (C / a) of the content of component (C) to the content of component (a) is 5 to 100.

[0036] Based on this characteristic, by limiting the proportion of components (B1) to (B5) or component (C) as bitterness masking components to component (a) Agrimol B as a bitterness component, oral compositions that can reliably exert bitterness masking effects can be obtained.

[0037] [5] A method for masking the bitterness of an oral composition, wherein the oral composition is an oral composition containing a powder containing component (a), including at least one powder selected from components (B1) to (C), wherein:

[0038] Component (a) is Agrimol B.

[0039] Component (B1) is a cellulose derivative with a viscosity of 2~800 mPa·s at a shear rate in a 2% aqueous solution at 20℃.

[0040] Component (B2) consists of 0.5% to 40% carrageenan by weight.

[0041] Component (B3) consists of 1% to 40% by weight of α-starch.

[0042] Component (B4) is a disaccharide sugar alcohol, comprising 1% to 30% by weight.

[0043] Component (B5) is a linear or branched dextrin with a mass percentage of 1% to 40% and a dextran equivalent (DE) of 2 to 20.

[0044] Component (C) is 0.5% to 10% by mass of metal salts or sucrose fatty acid esters of higher fatty acids.

[0045] According to this method of masking bitterness in oral compositions, even in the case of Agrimol B, which has a strong bitter taste, the unpleasant taste caused by bitterness can be eliminated by further containing specific, widely used excipients and additives.

[0046] [6] A method for manufacturing an oral composition as described in [1] to [4], the method comprising a process of stirring and mixing component (a) and at least one powder selected from components (B1) to (C), wherein:

[0047] Component (a) is Agrimol B.

[0048] Component (B1) is a cellulose derivative with a viscosity of 2~800 mPa·s at a shear rate in a 2% aqueous solution at 20℃.

[0049] Component (B2) consists of 0.5% to 40% carrageenan by weight.

[0050] Component (B3) consists of 1% to 40% by weight of α-starch.

[0051] Component (B4) is a disaccharide sugar alcohol, comprising 1% to 30% by weight.

[0052] Component (B5) is a linear or branched dextrin with a mass percentage of 1% to 40% and a dextran equivalent (DE) of 2 to 20.

[0053] Component (C) is 0.5% to 10% by mass of metal salts or sucrose fatty acid esters of higher fatty acids.

[0054] Effects of the present invention

[0055] According to the present invention, oral compositions containing Agrimol B, wherein the bitterness contained therein is masked, can be readily provided. Detailed Implementation

[0056] The following will describe the oral composition of the present invention and the method for masking the bitterness of the oral composition.

[0057] It should be noted that the oral composition and bitterness masking method described in the embodiments are merely exemplary to explain the present invention, and the present invention is not limited thereto.

[0058] [Oral composition]

[0059] The oral composition of the present invention is an oral composition comprising a powder containing component (a) and at least one powder selected from components (B1) to (C), wherein:

[0060] Component (a) is Agrimol B.

[0061] Component (B1) is a cellulose derivative with a viscosity of 2~800 mPa·s at a shear rate in a 2% aqueous solution at 20℃.

[0062] Component (B2) consists of 0.5% to 40% carrageenan by weight.

[0063] Component (B3) consists of 1% to 40% by weight of α-starch.

[0064] Component (B4) is a disaccharide sugar alcohol, comprising 1% to 30% by weight.

[0065] Component (B5) is a linear or branched dextrin with a mass percentage of 1% to 40% and a dextran equivalent (DE) of 2 to 20.

[0066] Component (C) is 0.5% to 10% by mass of metal salts or sucrose fatty acid esters of higher fatty acids.

[0067] First, each component constituting the oral composition of the present invention will be described in detail. Furthermore, unless otherwise specified, the content of each component is indicated as its content in the oral composition.

[0068] <(a) Agrimol B>

[0069] The oral composition of the present invention includes Agrimol B, which is the main component responsible for the bitter taste. Because it contains Agrimol B, which has a strong bitter taste, a strong bitter taste will be perceived when the oral composition is ingested orally.

[0070] In recent years, Agrimol B has attracted much attention as an active ingredient in pharmaceuticals and food products. It has been reported to activate SIRT1, a gene known as the longevity gene, which can prevent aging and extend lifespan. Furthermore, various studies have been conducted on the physiological effects of Agrimol B. For example, it has been found to have various pharmacological effects, including: a whitening effect by inhibiting melanin production (Japanese Patent Application Publication No. 11-335256), an improvement effect on type I hypersensitivity reactions (Japanese Patent Application Publication No. 2022-93893), and an inhibitory effect on muscle atrophy (Japanese Patent Application Publication No. 2022-167403), which has garnered widespread interest in its application in the food and pharmaceutical industries.

[0071] Agrimol B is a compound represented by the following chemical formula 1 (MW: 682.75). The Agrimol B of this invention is not particularly limited in its application as a pharmaceutical, food, veterinary medicine, or feed agent, and can be used through chemical synthesis or extraction, separation, and purification from natural sources such as plants. Alternatively, it can be used as a plant extract containing Agrimol B. Furthermore, commercially available products circulating in the market can also be purchased and used.

[0072] [Chemistry 1]

[0073]

[0074] Agrimol B can be synthesized chemically using phloroglucinol or similar starting materials. For example, it can be synthesized using the method described in Acta Pharmaceutica Sinica 1989, 24(6):431-437, or the method disclosed in Japanese Patent Application Publication No. 11-335256.

[0075] In addition, the synthesized Agrimol B has two forms: (S)-(+)-Agrimol B and its optical isomer (R)-(-)-Agrimol B. The "Agrimol B" used in this article can be a single compound composed of one of them or a mixture of the two.

[0076] The content of component (a) Agrimol B in the oral composition of the present invention is not particularly limited, and can be varied depending on the purity of Agrimol B, its source, and the target and purpose of its application. For example, it accounts for 0.01% to 2% by mass relative to the total oral composition. The lower limit is more preferably 0.01% or more by mass, and even more preferably 0.02% or more by mass. On the other hand, the upper limit is more preferably 1% or less by mass, even more preferably 0.6% or less by mass, and most preferably 0.3% or less by mass. By setting the content of Agrimol B within the above range, the effect of Agrimol B as an active ingredient can be reliably exerted. At the same time, by forming a mixture with components (B1) to (C) described below, the effect of masking the bitterness of Agrimol B can be more reliably exerted.

[0077] <Plant Extracts>

[0078] As described above, the oral composition of the present invention can contain Agrimol B as a plant extract. As for this plant extract, any extract containing Agrimol B is acceptable and not particularly limited, but component (A) of Agrimonia pilosa extract is preferred. Agrimonia pilosa (scientific name: Agrimonia pilosa) is a perennial herb belonging to the genus Agrimonia in the Rosaceae family, growing wild in forest edges, fields, and roadsides in Honshu, Shikoku, and Kyushu. It is also known as Agrimonia pilosa. In the present invention, the whole herb, whether wild or cultivated, can be collected and then naturally or heat-dried before use. Alternatively, commercially available dried Agrimonia pilosa, used as a raw material for traditional Chinese medicine, folk remedies, and health foods (herbal teas), can also be used. Furthermore, the dried whole herb of Agrimonia pilosa can be commercially available under the herbal name Agrimonia pilosa.

[0079] Examples of plant extracts used in this invention include, for instance, extracts obtained with water or various organic solvents, distillates obtained by steam distillation, dried powders, ground materials, and juices pressed from ground materials. From the viewpoint of yield and purity of Agrimonia pilosa extract, extracts obtained with water or various organic solvents are preferred, and extracts obtained with ethanol or aqueous ethanol containing water are more preferred.

[0080] When using water or various organic solvents for extraction, besides water, various organic solvents and mixtures thereof can be used, and well-known extraction methods can be employed. Before extraction, the raw material can be washed alone with hydrophobic or hydrophilic solvents, or mixed organic solvents, either undisturbed or coarsely chopped, to remove impurities such as pigments. Examples of hydrophobic solvents include chloroform, diethyl ether, hexane, cyclohexane, toluene, dichloromethane, petroleum ether, and benzene. Examples of hydrophilic solvents include lower alcohols (e.g., methanol, ethanol, n-propanol, isobutanol, or butanol), ethyl acetate, acetone, isopropanol, and acetonitrile. Water can be added appropriately to the raw material to wet it as needed.

[0081] When using water for extraction, for example, 0.5 to 10 parts by mass of water can be added relative to 1 part by mass of the raw material, and the mixture can be heated at 40°C to 120°C for 5 minutes to 2 hours, preferably 10 minutes to 60 minutes, more preferably 10 minutes to 20 minutes, to carry out the extraction. Stirring can also be used to improve extraction efficiency. Alternatively, extraction can be performed by heating and reflux. After extraction, the mixture is filtered or pressed using a filter cloth, filter screen, or diamond mesh. In this case, pressure can be applied to improve efficiency. Alternatively, centrifugation (1000 to 20000 rpm) can be used to obtain the extract. The extraction and filtration process can be repeated 1 to 5 times to increase the recovery rate.

[0082] When using an organic solvent for extraction, for example, adding 0.5 to 10 parts by mass of solvent relative to 1 part by mass of the raw material, the extract can be obtained in the same manner as water extraction. The aforementioned hydrophobic and hydrophilic solvents can be used alone or in combination of two or more, and aqueous solvents can also be used. In particular, when the raw material is washed with a hydrophobic solvent before extraction to remove impurities such as pigments, as described above, and when the crude extract after extraction is washed with a hydrophobic solvent as described below, water, lower alcohols, or 50% to 80% (v / v) aqueous lower alcohols are preferably used as the extraction solvent. Examples of such lower alcohols include those previously mentioned. The solvent can be removed by known methods such as filtration, centrifugation, and distillation.

[0083] A preferred extraction method for plant extracts, especially component (A) Agrimonia pilosa extract, is as follows: Wild or cultivated whole herb is collected and dried naturally or by heating. It is then chopped and soaked in approximately 10 times its volume of water or ethanol with a water concentration of 0% to 99.5% (v / v), preferably 1% to 50%, more preferably 5% to 10%, for 3 to 5 days. Extraction is then carried out at room temperature, or at 50°C to 80°C for 5 to 24 hours with a reflux condenser. The extract is then filtered and recovered. Water and ethanol are removed from the extract using a vacuum dryer such as a rotary evaporator or a freeze dryer to obtain the plant extract (solids).

[0084] Next, the process of concentrating the plant extract is carried out. In this process, the plant extract is concentrated by washing with 0% to 40% ethanol to remove 0% to 40% of the ethanol-soluble components.

[0085] Specifically, this plant extract (solids) is washed with 0%–40% ethanol, particularly preferably 10%–30% ethanol, and then the 0%–40% ethanol, particularly preferably 10%–30% ethanol, is removed by filtration or other methods. The filter residue is then dried using a rotary evaporator or a freeze dryer to remove water and ethanol, resulting in a more concentrated plant extract. The concentrated plant extract is then dissolved in 50%–99.5% ethanol, particularly preferably 70%–90% ethanol, and excipients for formulation are added. After freeze-drying, a concentrated plant extract of the desired concentration is obtained. Furthermore, it can be sieved to facilitate mixing with other powders.

[0086] The content of component (A), Agrimonia pilosa extract, in the oral composition of the present invention is not particularly limited and can vary depending on its purity, degree of refining, or the target of application or purpose. For example, it accounts for 0.5% to 70% by mass relative to the total oral composition. As a lower limit, it is more preferably 2% or more by mass, and more preferably 5% or more by mass. On the other hand, as an upper limit, it is more preferably 50% or less by mass, more preferably 40% or less by mass, and most preferably 30% or less by mass. By maintaining the content within the above range, the effect of Agrimonia pilosa extract as an effective component can be reliably exerted. At the same time, by forming a mixture with components (B1) to (C) described below, the bitterness masking effect of Agrimonia pilosa extract can be more reliably exerted.

[0087] The oral composition of the present invention may contain the following components (B1) to (B5) as component (B). By mixing the powder components (B1) to (B5) with the powder containing Agrimol B, an oral composition in which the strong bitterness of Agrimol B is masked can be easily obtained. Each component will be described in detail below.

[0088] <(B1) Cellulose derivatives>

[0089] Cellulose derivatives applicable to the oral composition of the present invention include cellulose derivatives having a viscosity of 2-800 mPa·s at a shear rate of 10 / s for 1 minute in a 2% aqueous solution at 20°C. Cellulose is a high molecular weight compound having a structure in which multiple β-glucose molecules are polymerized in a linear chain via glycosidic bonds. Cellulose derivatives are such cellulose derivatives. There are no particular limitations on the cellulose derivatives applicable to the present invention, as long as they can be used for pharmaceutical, food, veterinary medicine, and feed applications. Examples of cellulose derivatives include the following cellulose derivatives or their salts.

[0090] Specific examples of cellulose derivatives include hydroxypropyl cellulose (HPC), hydroxyethyl cellulose, low-substituted hydroxypropyl cellulose, hydroxypropyl methyl cellulose (HPMC), hydroxyethyl methyl cellulose, hydroxypropyl methyl cellulose acetate succinate, hydroxypropyl methyl cellulose phthalate, etc.; alkyl celluloses include methyl cellulose, ethyl cellulose, etc.; and carboxyl celluloses include carboxymethyl cellulose, potassium carboxymethyl cellulose, calcium carboxymethyl cellulose, sodium carboxymethyl cellulose, carboxymethyl ethyl cellulose, cross-linked sodium carboxymethyl cellulose, and cross-linked carboxymethyl cellulose.

[0091] Furthermore, there is no particular upper limit to the viscosity of the cellulose derivative, but it is preferably below 400 mPa·s.

[0092] From the viewpoint of the bitterness masking effect of the present invention, hydroxyalkyl cellulose is preferred, and hydroxypropyl cellulose (HPC) and hydroxypropyl methylcellulose (HPMC) are more preferred. Furthermore, there is no particular limitation on the upper limit of the viscosity of this hydroxypropyl cellulose, but it is more preferably 400 mPa·s or less, and more preferably 300 mPa·s or less. On the other hand, there is no particular limitation on the lower limit of the viscosity of hydroxypropyl methylcellulose, but it is more preferably 4 mPa·s or more. As an upper limit, it is more preferably 150 mPa·s or less, more preferably 100 mPa·s or less, and particularly preferably 60 mPa·s or less. Moreover, these cellulose derivatives can be used alone or in combination of two or more. Furthermore, there is no particular limitation on the manufacturing method of the cellulose derivatives of the present invention, and known methods can be used. Additionally, commercially available products can also be used as cellulose derivatives.

[0093] The content of component (B1) cellulose derivative is not particularly limited, for example, it is 0.05% to 60% by mass. The lower limit is preferably 0.1% or more by mass, more preferably 0.2% or more by mass, more preferably 1% or more by mass, and most preferably 5% or more by mass. On the other hand, the upper limit is not particularly limited, but it is preferably 50% or less by mass, more preferably 30% or less by mass.

[0094] By setting the content of cellulose derivatives within the above-mentioned range, the bitterness masking effect of the present invention can be fully utilized, the influence of the taste presented by the cellulose derivatives themselves can be minimized, and the freedom of formulation design can be ensured.

[0095] Furthermore, the ratio (B1 / a) of the content of cellulose derivative of component (B1) to the content of Agrimol B of component (a) is not particularly limited, for example, it is 1 to 450. As a lower limit, it is more preferably 1.5 or more, more preferably 7 or more, and most preferably 40 or more. On the other hand, as an upper limit, it is not particularly limited, but it is more preferably 200 or less, more preferably 150 or less.

[0096] By setting the ratio of the content of component (B1) cellulose derivative to the content of component (a) Agrimol B within the above range, the bitterness masking effect of the present invention can be fully utilized, the influence of the flavor presented by the cellulose derivative itself can be minimized, and the freedom of formulation design can be ensured.

[0097] Furthermore, the ratio (B1 / A) of the content of cellulose derivative of component (B1) to that of Agrimonia pilosa extract of component (A) is not particularly limited, for example, it is 0.005 to 2. As a lower limit, it is preferably 0.01 or more, more preferably 0.03 or more, more preferably 0.1 or more, and most preferably 0.2 or more. On the other hand, as an upper limit, it is preferably 1 or less, more preferably 0.7 or less.

[0098] By setting the ratio of the content of component (B1) cellulose derivative to component (A) agrimony extract within the above range, the bitterness masking effect of the present invention can be fully utilized, the influence of the flavor presented by the cellulose derivative itself can be minimized, and the freedom of formulation design can be ensured.

[0099] <(B2) Carbohydrate>

[0100] Carrageenan is a polysaccharide with a main chain structure consisting of straight chains of D-galactose linked by α-1,3 and β-1,4 bonds. There are no particular limitations on the carrageenan that can be used in this invention, as long as it is suitable for pharmaceutical, food, veterinary medicine, and feed applications. Examples include Kappa carrageenan, Iota carrageenan, and Lambda carrageenan, all of which are applicable to this invention. Furthermore, there are no particular limitations on the source of the carrageenan; carrageenan from seaweeds such as *Eucheuma cottonii* and *Eucheuma spinosum* can be used. Moreover, these carrageenan can be used alone or in combination of two or more. Additionally, commercially available products can also be used as carrageenan.

[0101] The content of component (B2) carrageenan is 0.5% to 40% by mass relative to the total oral composition. As a lower limit, it is more preferably 1% or more by mass, and more preferably 5% or more by mass. On the other hand, there is no particular limitation on the upper limit, but it is more preferably 30% or less by mass, and more preferably 20% or less by mass.

[0102] By setting the content of carrageenan within the above range, the bitterness masking effect of the present invention can be fully utilized, the influence of the flavor presented by carrageenan itself can be minimized, and other effects (e.g., thickening effect) can be expected for oral compositions containing carrageenan.

[0103] Furthermore, the ratio (B2 / a) of carrageenan content to agrimol B content (a) is not particularly limited, and for example, is 2 to 450. As a lower limit, 7 or more is preferred, and 30 or more is more preferred. On the other hand, as an upper limit, 200 or less is preferred, and 150 or less is more preferred.

[0104] By setting the ratio of carrageenan (B2) to agrimol B (a) within the above range, the bitterness masking effect of the present invention can be fully utilized, the influence of the flavor presented by carrageenan itself can be minimized, and other effects (e.g., thickening effect) can be expected for oral compositions containing carrageenan.

[0105] Furthermore, the ratio of carrageenan content of component (B2) to agrimony extract of component (A) ((B2) / (A)) is not particularly limited, for example, it is 0.01 to 2. As a lower limit, it is more preferably 0.03 or more, more preferably 0.05 or more, and most preferably 0.1 or more. On the other hand, as an upper limit, it is more preferably 1 or less, and more preferably 0.7 or less.

[0106] By setting the proportion of carrageenan relative to component (A) Agrimonia pilosa extract within the aforementioned range, the bitterness-masking effect of the present invention can be fully utilized, while minimizing the influence of the flavor inherent in carrageenan itself. Furthermore, other effects (e.g., thickening effect) can be expected for oral compositions containing carrageenan.

[0107] <(B3)α-starch>

[0108] Alpha-modified starch is obtained through a gelatinization and drying method, such as gelatinizing and drying a starch aqueous suspension by heating methods like spray drying, rotary drying, or extrusion granulation. There are no particular limitations on the gelatinization and drying method described above; any method that allows partial or complete solubility in cold water is acceptable. There are no particular limitations on the alpha-modified starch that can be used in this invention, as long as it can be used in pharmaceuticals, food, veterinary medicines, and feed, and any degree of alpha modification is acceptable. Furthermore, there are no particular limitations on the types of starch used as raw materials for alpha-modified starch; examples include corn starch, wheat starch, rice starch, potato starch, cassava starch, high amylose starch, hydroxypropyl starch, starch hydrolysate, acetate starch, phosphate starch, octenyl succinate starch, carboxymethyl starch, phosphate cross-linked starch, oxidized starch, dialdehyde starch, acid-treated starch, sweet potato starch, sago starch, and pea starch. In addition to alpha modification, processed starches obtained through chemical treatments such as esterification, etherification, oxidation, and cross-linking can also be used.

[0109] From the viewpoint of the bitterness masking effect of the present invention, α-modified corn starch, α-modified tapioca starch, and partially α-modified corn starch are preferred. Furthermore, this α-modified starch can be used alone or in combination of two or more types. Moreover, the manufacturing method of the α-modified starch of the present invention is not particularly limited and can be manufactured using known methods. Alternatively, commercially available products can also be used as the α-modified starch.

[0110] The content of component (B3) α-starch is 1% to 40% by mass relative to the total oral composition. As a lower limit, it is more preferably 1% or more by mass. On the other hand, as an upper limit, it is more preferably 30% or less by mass, and more preferably 20% or less by mass.

[0111] By setting the content of α-starch within the above range, the bitterness masking effect of the present invention can be fully utilized, and the influence of the flavor presented by α-starch itself can be minimized. In addition, other effects can be expected for oral compositions containing α-starch (e.g., as a binder).

[0112] Furthermore, the ratio (B3 / a) of the content of α-starch (B3) to that of Agrimol B (a) is not particularly limited, and is, for example, 10 to 450. As a lower limit, it is more preferably 20 or more, and more preferably 40 or more. On the other hand, as an upper limit, it is more preferably 200 or less, and more preferably 150 or less.

[0113] By setting the ratio of component (B3) α-starch to component (a) Agrimol B within the above-mentioned range, the bitterness masking and improvement effect of the present invention can be fully utilized, and the influence of the flavor presented by α-starch itself can be minimized. In addition, other effects can be expected for oral compositions containing α-starch (e.g., as a binder).

[0114] Furthermore, the ratio (B3 / A) of the content of α-starch (B3) to the content of Agrimonia pilosa extract (A) is not particularly limited, for example, it is 0.05 to 2. As a lower limit, it is more preferably 0.1 or more, and more preferably 0.2 or more. On the other hand, as an upper limit, it is more preferably 1 or less, and more preferably 0.7 or less.

[0115] By setting the ratio of the content of α-starch (B3) to the extract of Agrimonia pilosa (A) within the above range, the bitterness masking effect of the present invention can be fully utilized, and the influence of the flavor presented by α-starch itself can be minimized. In addition, other effects (e.g., binder) can be expected for oral compositions containing α-starch.

[0116] <(B4) Disaccharide sugar alcohols>

[0117] Sugar alcohols can be sugars with an alcohol group (-OH) obtained by adding hydrogen to the molecule of a sugar. They are used as low-calorie sweeteners that are difficult to digest. Furthermore, they are widely used as food quality improvers to extend shelf life, retain moisture, inhibit coloring, and in the fields of patient food, cosmetics, and pharmaceuticals. There are no particular limitations on the sugar alcohols that can be used as disaccharides in this invention, as long as they can be used in pharmaceuticals, food, veterinary medicines, and feed. Examples include maltitol (reduced maltose), lactitol (reduced lactose), and reduced baraglinose (reduced isomaltulose). From the viewpoint of the bitterness masking effect of this invention, maltitol and reduced baraglinose are preferred. Furthermore, these disaccharide sugar alcohols can be used alone or in combination of two or more. There are no particular limitations on the manufacturing method of the disaccharide sugar alcohols of this invention; they can be manufactured using known methods. Additionally, commercially available products can be used as disaccharide sugar alcohols.

[0118] (B4) The content of disaccharide sugar alcohol is 1% to 30% by mass. As a lower limit, it is more preferably 5% or more by mass. On the other hand, as an upper limit, it is more preferably 20% or less by mass.

[0119] By setting the content of disaccharide sugar alcohols within the above-mentioned range, the bitterness masking effect of the present invention can be fully utilized, and the influence of the flavor presented by the sugar alcohols themselves can be minimized. In addition, it is expected that the oral composition containing sugar alcohols can have other effects as a food quality improver, such as retaining moisture and inhibiting coloring.

[0120] Furthermore, the ratio (B4 / a) of the sugar alcohol content of component (B4) disaccharide to component (a) Agrimol B is not particularly limited, for example, it is 1 to 450. As a lower limit, it is more preferably 20 or more, more preferably 40 or more. On the other hand, as an upper limit, it is more preferably 200 or less, more preferably 150 or less, and most preferably 100 or less.

[0121] By setting the ratio of the sugar alcohol content of component (B4) disaccharide to component (a) Agrimol B within the above range, the bitterness masking and improvement effect of the present invention can be fully utilized, and the influence of the sugar alcohol itself can be minimized. In addition, it is expected that it can exert other effects as a food quality improver, such as retaining moisture and inhibiting coloring, on oral compositions containing sugar alcohol.

[0122] Furthermore, the ratio (B4 / A) of the disaccharide sugar alcohol content in component (B4) to the agrimony extract in component (A) is not particularly limited, for example, it is 0.05 to 2. As a lower limit, it is more preferably 0.1 or more, and more preferably 0.2 or more. On the other hand, as an upper limit, it is more preferably 0.7 or less, and more preferably 0.5 or less.

[0123] By setting the ratio of sugar alcohol content to component (A) Agrimonia pilosa extract within the above-mentioned range, the bitterness masking effect of the present invention can be fully utilized, and the influence of the sugar alcohol itself can be minimized. In addition, it is expected that the oral composition containing sugar alcohol can have other effects as a food quality improver, such as retaining moisture and inhibiting coloring.

[0124] <(B5) Linear-chain dextrin or branched-chain dextrin>

[0125] Dextrin is produced by breaking down starch, the raw material, using enzymes and acids. The dextrins usable in the oral composition of this invention are linear or branched dextrins with a DE (dextrose equivalent) of 2 to 20. Linear dextrins refer to dextrins in which glucose is linked in a straight chain, while branched dextrins (also called branched dextrins) refer to dextrins in which glucose is linked in a chain and also has branches. The dextrin of this invention can be a mixture of these linear and branched dextrins.

[0126] There are no particular limitations on the linear or branched dextrins with a DE of 2 to 20 that can be used in this invention, as long as they can be used in pharmaceuticals, food, veterinary drugs, and feed. For example, the glycosidic bonds of such sugars can be any combination of α-1,4, α-1,6, β-1,2, β-1,3, β-1,4, β-1,6, or α-1,6.

[0127] The lower limit of DE is preferably 4, and the upper limit of DE is preferably 18. Furthermore, this DE value can be analyzed using known methods for the determination of dextrin, for example, the Willstätterschüdel method.

[0128] Furthermore, these dextrins can be used alone or in combination of two or more. Additionally, the method for manufacturing the dextrins of this invention is not particularly limited and can be manufactured using known methods. Alternatively, commercially available products can also be used as dextrins.

[0129] The DE of component (B5) is 2 to 20, and the content of linear dextrin or branched dextrin accounts for 1% to 40% by mass percentage relative to the total oral composition. As a lower limit, it is more preferably 2% or more by mass percentage, more preferably 5% or more by mass percentage, and most preferably 10% or more by mass percentage. On the other hand, there is no particular limitation as an upper limit, but it is more preferably 30% or less by mass percentage.

[0130] By setting the content of linear dextrin or branched dextrin within the above range, the bitterness masking effect of the present invention can be fully utilized, the influence of the taste presented by dextrin itself can be minimized, and the freedom of formulation design can be ensured.

[0131] Furthermore, without impairing the effects of the present invention, dextrins having a cyclic structure, such as cyclodextrins, may also be included. The content of dextrins having a cyclic structure is not particularly limited and may vary depending on the content of Agrimol B and (B5) linear or branched dextrins; for example, it may be 2% or less by mass relative to the oral composition. More preferably, it is 0.5% or less by mass; more preferably, 0.1% or less by mass; particularly preferably, 0.01% or less by mass; and most preferably, it substantially excludes dextrins having a cyclic structure. The term "substantially" here means excluding unavoidable inclusions.

[0132] Furthermore, the content of linear or branched dextrin (B5) of component (B5) with a DE of 2 to 20 is not particularly limited in the ratio (B5 / a) to component (a) Agrimol B, for example, it is 5 to 450. As a lower limit, it is more preferably 30 or more, and more preferably 70 or more. On the other hand, as an upper limit, it is more preferably 200 or less, and more preferably 150 or less.

[0133] By setting the ratio of dextrin content to component (a) Agrimol B within the above range, the bitterness masking and improvement effect of the present invention can be fully utilized, the influence of the taste presented by dextrin itself can be minimized, and the freedom of formulation design can be ensured.

[0134] Furthermore, the content of linear or branched dextrin (B5), a component with a DE of 2 to 20, relative to the ratio (B5 / A) of Agrimonia pilosa extract (A), is not particularly limited, for example, it is 0.03 to 2. As a lower limit, it is more preferably 0.15 or more, and more preferably 0.3 or more. On the other hand, as an upper limit, it is more preferably 1 or less, and more preferably 0.7 or less.

[0135] By setting the content of (B5) linear or branched dextrin with a DE of 2 to 20 relative to the component (A) Agrimonia pilosa extract within the above range, the bitterness masking effect of the present invention can be fully utilized, the influence of the taste presented by the dextrin itself can be minimized, and the freedom of formulation design can be ensured.

[0136] Furthermore, the oral composition of the present invention may include the following component (C). By mixing the powder of component (C) with a powder containing Agrimol B, an oral composition in which the strong bitterness of Agrimol B is masked can be easily obtained. Component (C) will be described in detail below.

[0137] <(C) Metal salts of higher fatty acids or sucrose fatty acid esters>

[0138] There are no particular limitations on the metal salts or sucrose fatty acid esters of the higher fatty acids that can be used in this invention. Preferably, metal salts of higher aliphatic carboxylic acids with 10 to 22 carbon atoms are used as the metal salts of the higher fatty acids, for example, decanoic acid, lauric acid, myristic acid, palmitic acid, stearic acid, benzyl acid, oleic acid, and erucic acid. Furthermore, there are no particular limitations on such metal salts, and for example, sodium salts, lithium salts, calcium salts, magnesium salts, zinc salts, and aluminum salts are included. From the viewpoint of the bitterness masking effect of this invention, metal salts of stearic acid are preferred among these metal salts of higher fatty acids, with calcium stearate and magnesium stearate being more preferred. In addition, these metal salts of higher fatty acids can be used alone or in combination of two or more.

[0139] There are no particular limitations on the sucrose fatty acid esters used; any sucrose bonded to fatty acid esters can be used, regardless of HLB, the number of carbon atoms in the fatty acid, or the degree of esterification. There are also no particular limitations on the fatty acids that form ester bonds with sucrose; examples include lauric acid, myristic acid, palmitic acid, stearic acid, benzolic acid, and erucic acid. Furthermore, metal salts of these higher fatty acids or sucrose fatty acid esters can be combined alone or in combination of two or more.

[0140] The content of component (C) – metal salts of higher fatty acids or sucrose fatty acid esters – accounts for 0.5% to 10% by mass relative to the total oral composition. As a lower limit for the content of metal salts of higher fatty acids or sucrose fatty acid esters, it is preferably 1% or more by mass, more preferably 2% or more by mass. On the other hand, as an upper limit, it is preferably 7% or less by mass, more preferably 5% or less by mass. Setting the content of component (C) – metal salts of higher fatty acids or sucrose fatty acid esters – within the above range allows for full utilization of the bitterness masking effect of the present invention and minimizes the influence of the flavor inherent in the metal salts of higher fatty acids or sucrose fatty acid esters themselves. Furthermore, it is expected to impart other effects (e.g., as a lubricant) to the oral composition containing metal salts of higher fatty acids or sucrose fatty acid esters.

[0141] Furthermore, the ratio (C / a) of the content of metal salts or sucrose fatty acid esters of higher fatty acids in component (C) to component (a) Agrimol B is not particularly limited, for example, it is 5 to 100. As a lower limit, it is more preferably 10 or more. On the other hand, as an upper limit, it is more preferably 60 or less.

[0142] By setting the ratio of the content of the metal salt of higher fatty acids or sucrose fatty acid ester of component (C) to component (a) Agrimol B within the above range, the bitterness masking and improvement effect of the present invention can be fully utilized, and the influence of the taste presented by the metal salt of higher fatty acids or sucrose fatty acid ester itself can be minimized. In addition, it is expected to impart other effects (e.g., as a lubricant) to oral compositions containing metal salt of higher fatty acids or sucrose fatty acid ester.

[0143] Furthermore, the ratio (C / A) of the content of metal salts or sucrose fatty acid esters of higher fatty acids in component (C) to the content of Agrimonia pilosa extract in component (A) is not particularly limited, for example, it is 0.02 to 0.5. As a lower limit, it is preferably 0.05 or more. On the other hand, as an upper limit, it is preferably 0.3 or less, and more preferably 0.25 or less.

[0144] By setting the content of the metal salt or sucrose fatty acid ester of the higher fatty acid in component (C) relative to the extract of Agrimonia pilosa in component (A) within the above range, the bitterness masking effect of the present invention can be fully utilized, and the influence of the flavor presented by the metal salt or sucrose fatty acid ester of the higher fatty acid itself can be minimized. In addition, it is expected to impart other effects (e.g., as a lubricant) to oral compositions containing metal salt or sucrose fatty acid ester of higher fatty acids.

[0145] <Ingredient (C) / Ingredient (B)>

[0146] Furthermore, the ratio (C / B) of the content of the metal salt or sucrose fatty acid ester of the higher fatty acids in component (C) to the content of components (B1) to (B5) in component (B) is not particularly limited, and is, for example, 0.025 to 1. As a lower limit, it is more preferably 0.05 or more, and more preferably 0.1 or more. On the other hand, as an upper limit, it is more preferably 0.5 or less, and more preferably 0.25 or less.

[0147] By setting the ratio of the content of metal salts of higher fatty acids or sucrose fatty acid esters of component (C) to the content of components (B1) to (B5) of component (B) within the above range, the influence on the presented flavor can be minimized, and additional effects can be expected to be imparted to the oral composition containing components (B1) to (B5) and metal salts of higher fatty acids or sucrose fatty acid esters of component (C).

[0148] The oral composition of the present invention can be in any combination, including any combination of two or more of the above-mentioned components (B1) to (B5), or component (C), as long as it achieves the effects of the present invention. Furthermore, more preferably, any one or more of the above-mentioned components (B1) to (B5), or component (C) satisfies the above-mentioned content and / or content ratio. More preferably, any one or more of the above-mentioned components (B1) to (B5), or component (C) satisfies the above-mentioned content and content ratio.

[0149] (Other ingredients)

[0150] In addition to Agrimol B and plant extracts containing Agrimol B, the oral composition of this invention may also include active ingredients and additives as needed. Specific examples of additives include excipients, binders, disintegrants, lubricants, stabilizers, preservatives, colorants, flavorings, sweeteners, etc. Furthermore, it may also include Agrimol-like components (Agrimol A to Agrimol G or Agrimophor) other than Agrimol B found in Agrimonia pilosa extract.

[0151] As an active ingredient, it is not subject to special restrictions as long as it exerts its efficacy and effect and can be used in pharmaceuticals, food, veterinary drugs, feed, etc. For example, pharmaceutical ingredients and functional ingredients used in pharmaceuticals, quasi-drugs, over-the-counter drugs, traditional Chinese medicine, medicinal materials, cosmetics, cosmetics, health foods, supplements, veterinary drugs, feed, etc.

[0152] Specific examples of pharmaceutical ingredients and functional components include, for instance, vitamins A, D, E, B1, B2, B6, B12, folic acid, biotin, nicotinic acid, nicotinamide, pantothenic acid, iron, copper, zinc, manganese, selenium, chromium, molybdenum, polyglutamic acid, vine tea polyphenols, lipid regulators, antidiabetic agents, antihypertensive drugs, vasodilators, β-adrenergic receptor blockers, cardiac ion channel agents, antiarrhythmic agents, anticoagulants, central nervous system modifiers, sympathetic stimulants, parasympathetic stimulants, muscarinic receptor agonists, dopamine agonists, sedatives, antidepressants, anti-anxiety drugs, hypnotics, animal-derived substances, plant-derived substances, lapidin, and nobil. Dietary fiber including etin, sulforaphane, ampelopsin, curcumin, resveratrol, geraniol, ossajin, isoliquiritigenin, hydroxytyrosol, 25-hydroxycholecalciferol, S-adenosylmethionine, anthocyanin, proteoglycan, N-acetylglucosamine, collagen, blueberry extract, carrot powder, malt extract, lotus seed extract powder, Acanthopanax senticosus, licorice, yam, cinnamon, fennel, amomum villosum, bifidobacteria, lactic acid bacteria, yeast, and polydextrose. Preferably, these are active ingredients expected to have an synergistic effect with the essential components of this invention, enhancing their anti-aging properties. Furthermore, these pharmaceutical and functional ingredients can be used alone or in combination of two or more.

[0153] <Types of oral components>

[0154] The oral formulations of this invention are not particularly limited in form, as long as they can be used as pharmaceuticals, food, veterinary medicines, feed, etc. For example, besides directly using powder as a powder or granule, other forms include tablets such as naked tablets, sugar-coated tablets, buccal tablets, film-coated tablets, and chewable tablets; solid preparations such as pills, soft capsules, hard capsules, and granules; suspensions; emulsions; syrups; elixirs; and throat lozenges. From the viewpoint of achieving low cost, powder form is preferred, and powder mixtures obtained by mixing the powders of each component are more preferred. These formulations can be prepared using known formulation methods. Furthermore, these formulations can be used, depending on the purpose, in processed foods, health foods (nutritional supplements, functional foods, foods for patients, foods for specific health purposes, functionally labeled foods, etc.), supplements, foods for patients (hospital foods, patient foods, nursing foods, etc.), snacks, oils, dairy products, sterilized foods, microwave foods, frozen foods, seasonings, health products, beverages, and nutritional drinks. Preferably, it is used for oral administration as an anti-aging treatment.

[0155] [Manufacturing method of oral components]

[0156] The method for manufacturing the oral composition of the present invention is not particularly limited and can be manufactured by known methods. For example, in addition to the process of stirring and mixing each component (a) or (A) with one or more of components (B1) to (C), processes such as heating, drying, pulverizing, and sieving can be added as needed, and the order and conditions of these processes are not particularly limited.

[0157] By virtue of the above features, the oral composition of the present invention can mask the bitterness produced by the inclusion of component (a)Agrimol B in the oral composition through the action of the specific components (B1) to (C) mentioned above.

[0158] [Methods for masking bitterness in oral components]

[0159] The method for reducing the flavor of the oral composition of the present invention is to include at least one powder selected from components (B1) to (C) in an oral composition containing component (a) Agrimonia pilosa extract or component (A) containing component (a) Agrimonia pilosa extract.

[0160] Furthermore, the bitterness-masking methods constituting the oral composition, including Agrimol B, Agrimonia pilosa extract, cellulose derivatives, carrageenan, α-starch, disaccharide sugar alcohols, linear or branched dextrins, and metal salts or sucrose fatty acid esters of higher fatty acids, can be the same as those used in the oral composition of the present invention.

[0161] Similarly, there are no particular restrictions on the amount of these cellulose derivatives, carrageenan, α-starch, disaccharide sugar alcohols, linear dextrins or branched dextrins, and metal salts of higher fatty acids or sucrose fatty acid esters added. For example, as long as it meets the requirements of the above description of cellulose derivatives, carrageenan, α-starch, disaccharide sugar alcohols, linear dextrins or branched dextrins, and metal salts of higher fatty acids or sucrose fatty acid esters in oral composition, it is acceptable.

[0162] By virtue of the above features, the bitterness masking method of the oral composition of the present invention can mask the bitterness produced by the presence of Agrimol B in the oral composition through the action of components (B1) to (C).

[0163] Example

[0164] The embodiments of the present invention will be described below, but the present invention is not limited to these embodiments, and various modifications can be made within the scope of the technical concept of the present invention.

[0165] [Test Example 1: Bitterness Masking Effect of Oral Compositions Containing Agrimol B]

[0166] The bitterness masking effect of oral compositions containing Agrimol B was tested. Specifically, the bitterness masking effect was evaluated on powder mixtures of Agrimol B-containing Agrimol extract with cellulose derivatives, carrageenan, α-starch, disaccharide sugar alcohols, linear or branched dextrins, and metal salts or sucrose fatty acid esters of higher fatty acids. Furthermore, the Agrimol extract used in the examples contained 0.452% by weight of Agrimol B.

[0167] <Preparation of Test Samples>

[0168] After weighing each ingredient in the formulations listed in Tables 1-14, each sample was mixed using a mixer (transparent mixer S-3, Tsutsui Rikikaku Equipment Co., Ltd.). Samples passing through a 30-mesh sieve were used as specimens for the oral compositions of Reference Example 1, Comparative Examples 1-29, and Examples 1-82, respectively. Unless otherwise specified, the values ​​in each table represent the mass percentage of each component relative to the total mass of the oral composition. Details of the ingredients used in this test example are shown in Table 1 below.

[0169] [Table 1]

[0170]

[0171] <Sensory Evaluation>

[0172] The oral components obtained from the above-mentioned specimens were placed in the mouth and their bitterness was assessed according to the following evaluation criteria. Furthermore, the assessment was decided by a panel of three experts.

[0173] (Evaluation Criteria)

[0174] The evaluation criteria were determined by the aforementioned expert panel members based on the following criteria for bitterness, when comparing the raw material with that of Agrimonia pilosa. Furthermore, ○ and ◎ were deemed acceptable due to their superior bitterness masking effect (Example), and the individual results are shown in the respective tables.

[0175] ◎••• I didn't taste any bitterness

[0176] ○•••I tasted a slight bitterness (but it wasn't unpleasant).

[0177] △•••I felt an unpleasant bitter taste

[0178] •••The bitterness is comparable to that of the raw material of Agrimonia pilosa.

[0179] <(B1) Cellulose derivatives>

[0180] In the formulations shown in Table 2 below, the masking effect of cellulose derivatives with different viscosities on the bitterness of Agrimonia pilosa extract was evaluated. The results of the sensory evaluation are also shown in Table 2. In addition, Reference Example 1 and Comparative Examples 1-4 show the results of containing only Agrimonia pilosa extract and excipients (cellulose).

[0181] [Table 2]

[0182]

[0183] (result)

[0184] Based on the results of Reference Example 1 and Comparative Examples 1-4, an unpleasant bitter taste was noticeable when the content of Agrimonia pilosa extract was 2.5% or more by mass.

[0185] Furthermore, the results of Comparative Examples 5 and 6 show that cellulose derivatives with viscosity outside the scope of the present invention failed to achieve the standard bitterness masking effect. On the other hand, the results of Examples 1 to 13 clearly demonstrate that cellulose derivatives with viscosity within the scope of the present invention can achieve a sufficient bitterness masking effect.

[0186] <(B2) Carbohydrate>

[0187] In the formulations shown in Table 3 below, the masking effect of carrageenan and other thickening polysaccharides on the bitterness of Agrimonia pilosa extract was evaluated. The results of the sensory evaluation are also shown in Table 3.

[0188] [Table 3]

[0189]

[0190] (result)

[0191] The results of Examples 14-24 show that Kappa carrageenan, Iota carrageenan, and Lambda carrageenan all effectively masked bitterness, clearly meeting the standard. On the other hand, as shown in Comparative Examples 7-14, thickening polysaccharides other than carrageenan did not have a bitterness-masking effect and failed to meet the standard. Furthermore, as shown in Comparative Example 14 and the results of Examples 14-24 above, it is clear that a certain amount of carrageenan is required to achieve a sufficient bitterness-masking effect.

[0192] <(B3)α-starch>

[0193] ((B3) A review of the types of α-starch)

[0194] In the formulations shown in Table 4 below, the effects of α-starch and other starches on masking the bitterness of Agrimonia pilosa extract were evaluated. The results of the sensory evaluation are also shown in Table 4.

[0195] [Table 4]

[0196]

[0197] ((B3) Review of the amount of α-starch)

[0198] Next, the effect of α-starch content on masking the bitterness of Agrimonia pilosa extract was evaluated in the formulations shown in Table 5 below. The results of the sensory evaluation are also shown in Table 5.

[0199] [Table 5]

[0200]

[0201] (result)

[0202] As shown in the results of Comparative Examples 15-17 in Table 4, β-starch did not mask the bitterness of Agrimonia pilosa extract. In contrast, as shown in the results of Examples 25-27, unpleasant bitterness disappeared in at least a portion of the α-substituted starch, and a sufficient bitterness masking effect meeting the standard was achieved.

[0203] In addition, as shown in Table 5, it is clear that in order to obtain the masking effect of α-starch, the content of α-starch needs to be above a certain level.

[0204] <(B4) Disaccharide sugar alcohols>

[0205] In the formulations shown in Table 6 below, the masking effect of various sugar alcohols on the bitterness of Agrimonia pilosa extract was evaluated. The results of the sensory evaluation are also shown in Table 6.

[0206] [Table 6]

[0207]

[0208] (result)

[0209] The results of Comparative Examples 23 and Examples 37-44 clearly demonstrate that the bitterness masking effect of Agrimonia pilosa extract can be obtained in oral compositions containing only disaccharide sugar alcohols as component (B). To achieve sufficient masking, the content of the disaccharide sugar alcohol must be above a certain level. On the other hand, as shown in Comparative Examples 19-22, other sugars were unable to adequately mask the unpleasant bitterness, failing to meet the standard.

[0210] <(B5) Linear-chain dextrin or branched-chain dextrin>

[0211] In the formulations shown in Table 7 below, the masking effect of various dextrins on the bitterness of Agrimonia pilosa extract was evaluated. The results of the sensory evaluation are also shown in Table 7.

[0212] [Table 7]

[0213]

[0214] (result)

[0215] The results of Comparative Examples 27 and Examples 46-53 clearly demonstrate that when a powdered oral composition containing only linear or branched dextrins with DE within a specific range is used as component (B), a bitterness masking effect of Agrimonia pilosa extract can be obtained. To achieve sufficient masking, the content of component (B5) needs to be above a certain level. On the other hand, when only γ-cyclodextrin containing an intramolecular cyclic structure is included, or when only linear or branched dextrins with DE outside the scope of this invention are included, as shown in Comparative Examples 24-26, the unpleasant bitterness cannot be adequately masked, and the standard cannot be met.

[0216] <(C) Metal salts or sucrose fatty acid esters of higher fatty acids>

[0217] In the formulations shown in Table 8 below, the masking effect of metal salts or sucrose fatty acid esters of higher fatty acids on the bitterness of Agrimonia pilosa extract was evaluated. The results of the sensory evaluation are also shown in Table 8.

[0218] [Table 8]

[0219]

[0220] (result)

[0221] The results from Examples 54-61 show that in oral compositions containing only metal salts or sucrose fatty acid esters of higher fatty acids as component (C), sufficient masking effect on the bitterness of Agrimonia pilosa extract can be obtained. In contrast, other fatty acid esters in Comparative Example 28 failed to adequately mask the unpleasant bitterness and did not meet the standard.

[0222] Furthermore, the results of Comparative Example 29 show that when the ratio of calcium stearate to Agrimol (C / a) is 1.11, it is insufficient to mask the unpleasant bitterness.

[0223] [Example 2: Additive effect of components (B) and (C)]

[0224] The bitterness masking effect of the oral composition was evaluated in the case of a mixture of component (A) Agrimonia pilosa and an oral composition containing powders of components (B1) to (B5) respectively, with component (C) being mixed in.

[0225] <(B1) Cellulose Derivatives and Components (C)>

[0226] In the formulations shown in Table 9 below, the additive effect of masking bitterness from Agrimonia pilosa extract was evaluated in the case of powder mixtures containing either component (B1), a cellulose derivative with proven effects, or component (C). The results of the sensory evaluation are also shown in Table 9.

[0227] [Table 9]

[0228]

[0229] <(B2) Carrageenan and Component (C)>

[0230] In the formulations shown in Table 10 below, the additive effect of masking bitterness from Agrimonia pilosa extract was evaluated in the case of powder mixtures containing either component (B2) carrageenan (both of which have been shown to have proven effects) or component (C). The results of the sensory evaluation are also shown in Table 10.

[0231] [Table 10]

[0232]

[0233] <(B3)α-Alpha starch and components (C)>

[0234] In the formulations shown in Table 11 below, the additive effect of masking bitterness from Agrimonia pilosa extract was evaluated in the case of powder mixtures containing either component (B3) α-starch, which has been shown to have proven effectiveness, or component (C). The results of the sensory evaluation are also shown in Table 11.

[0235] [Table 11]

[0236]

[0237] <(B4) Sugar alcohols and components of disaccharides (C)>

[0238] In the formulations shown in Table 12 below, the additive effect of *Agrimonia pilosa* extract on bitterness masking was evaluated in the case of powder mixtures containing either a sugar alcohol of the (B4) disaccharide class, both of which have been shown to have proven effects, or component (C). The results of the sensory evaluation are also shown in Table 12.

[0239] [Table 12]

[0240]

[0241] <(B5) Linear-chain dextrins or branched-chain dextrins and component (C)>

[0242] In the formulations shown in Table 13 below, the additive effect of bitterness masking effect of Agrimonia pilosa extract was evaluated in the case of a powder mixture containing (B5) linear or branched dextrin with a DE of 2-20, both of which have been confirmed to have bitterness masking effect, and any of component (C). The results of the sensory evaluation are also shown in Table 13.

[0243] [Table 13]

[0244]

[0245] (result)

[0246] As shown in Tables 9-13, the oral compositions formed by creating powders containing either component (B) or component (C) achieved the highest rating "◎" in sensory evaluation because they both exhibited a masking effect to the degree to which bitterness was imperceptible. Therefore, it was confirmed that components (B) and (C) have an additive effect on the bitterness masking effect of Agrimonia pilosa extract.

[0247] [Example 3: Manufacturability of the Tablets and Confirmation of Bitterness Masking Effect]

[0248] <Preparation of Tablets>

[0249] The raw materials were mixed according to the formulation shown in Table 14, sieved through a 30-mesh screen, and then mixed using a mixer. The resulting mixture was then formed into tablets using a single-punch tablet forming machine (manufactured by Okada Seiko Co., Ltd., N-30E) to obtain the tablets of Examples 81 and 82. The tablet forming conditions were: tablet ø 9 mm, R12, tablet weight 300 mg / tablet, and forming pressure 1,000 kgf.

[0250] <Sensory evaluation and review of scalding properties>

[0251] The tablets were held in the mouth after being beaten, and the bitterness was assessed using the same sensory evaluation as described above. Furthermore, beating properties were also evaluated. When no beating obstacles such as cracking or sticking occurred, the beating property was assessed as "no problem." These evaluation results are shown in Table 14.

[0252] [Table 14]

[0253]

[0254] (result)

[0255] As shown in Table 14, the tablets prepared by pounding the powder containing Agrimonia pilosa extract, component (B3) α-starch, and component (C) also received the highest rating in the sensory evaluation. Therefore, it is evident that when prepared as tablets, the same bitterness masking effect on components (B) and (C) of Agrimonia pilosa extract can be achieved as with the aforementioned powder mixture. Furthermore, it is also evident that the tablet preparation exhibits excellent pounding properties.

[0256] As stated above, it has been confirmed that the bitterness of oral compositions containing Agrimol B can be masked by including components (B1) to (C), and these compositions can be formulated into tablets.

[0257] Industrial utilization potential

[0258] This invention allows for the easy formulation of oral compositions containing Agrimol B and masking its bitterness, thereby providing Agrimol B as an active ingredient with beneficial effects, applicable to pharmaceuticals, quasi-drugs, oral cosmetics, oral health foods (nutritional supplements, functional nutritional products, foods for patients, foods for specific health purposes, functionally labeled foods, etc.), supplements, and feeds.

Claims

1. An oral composition, characterized in that, The powder includes a powder containing component (a) below, and a powder selected from components (B1) to (C) below, wherein: Component (a) is Agrimol B. Component (B1) is a cellulose derivative with a viscosity of 2~800 mPa·s at a shear rate in a 2% aqueous solution at 20℃. Component (B2) consists of 0.5% to 40% carrageenan by weight. Component (B3) consists of 1% to 40% by weight of α-starch. Component (B4) is a disaccharide sugar alcohol, comprising 1% to 30% by weight. Component (B5) is a linear or branched dextrin with a mass percentage of 1% to 40% and a dextran equivalent (DE) of 2 to 20. Component (C) is 0.5% to 10% by mass of metal salts or sucrose fatty acid esters of higher fatty acids.

2. The oral composition as described in claim 1, characterized in that, The component (a) is component (A) Agrimonia pilosa extract.

3. The oral composition as described in claim 1 or 2, characterized in that, The oral composition includes a powder selected from at least one of components (B1) to (B5) and a powder of component (C).

4. The oral composition as described in claim 1 or 2, characterized in that, The ratio of the content of component (B1) to component (C) relative to the content of component (a) is one or more of the following: The ratio (B1 / a) of the content of component (B1) to the content of component (a) is 1 to 450; The ratio (B2 / a) of the content of component (B2) to the content of component (a) is 2 to 450; The ratio (B3 / a) of the content of component (B3) to the content of component (a) is 10 to 450; The ratio (B4 / a) of the content of component (B4) to the content of component (a) is 10 to 450; The ratio (B5 / a) of the content of component (B5) to the content of component (a) is 5 to 450; The ratio (C / a) of the content of component (C) to the content of component (a) is 5 to 100.

5. A method for masking bitterness in an oral composition, wherein the oral composition is an oral composition containing a powder of component (a), including at least one powder selected from components (B1) to (C), characterized in that: Component (a) is Agrimol B. Component (B1) is a cellulose derivative with a viscosity of 2~800 mPa·s at a shear rate in a 2% aqueous solution at 20°C. Component (B2) consists of 0.5% to 40% carrageenan by weight. Component (B3) consists of 1% to 40% by weight of α-starch. Component (B4) is a disaccharide sugar alcohol, comprising 1% to 30% by weight. Component (B5) is a linear or branched dextrin with a mass percentage of 1% to 40% and a dextran equivalent (DE) of 2 to 20. Component (C) is 0.5% to 10% by mass of metal salts or sucrose fatty acid esters of higher fatty acids.

6. A method for manufacturing an oral composition, said oral composition comprising component (a) and at least one powder selected from components (B1) to (C), characterized in that, The method includes a step of stirring and mixing component (a) and at least one powder selected from components (B1) to (C), wherein: Component (a) is Agrimol B. Component (B1) is a cellulose derivative with a viscosity of 2~800 mPa·s at a shear rate in a 2% aqueous solution at 20℃. Component (B2) consists of 0.5% to 40% carrageenan by weight. Component (B3) consists of 1% to 40% by weight of α-starch. Component (B4) is a disaccharide sugar alcohol, comprising 1% to 30% by weight. Component (B5) is a linear or branched dextrin with a mass percentage of 1% to 40% and a dextran equivalent (DE) of 2 to 20. Component (C) is 0.5% to 10% by mass of metal salts or sucrose fatty acid esters of higher fatty acids.

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