Orally-taken composition

Abstract

To provide an orally-taken composition which includes 3-hydroxyisovaleric acid and / or salt thereof and a taste of which is improved.SOLUTION: An orally-taken composition can mitigate an unpleasant taste typical of 3-hydroxyisovaleric acid and / or salt thereof and be readily ingested by adding vitamin D and / or vitamin B6 into the 3-hydroxyisovaleric acid and / or the salt thereof.SELECTED DRAWING: None

Description

[Technical field]

[0001] The present invention relates to oral compositions comprising 3-hydroxyisovaleric acid and / or a salt thereof, which have an improved taste. [Background technology]

[0002] 3-Hydroxyisovaleric acid and its salts are metabolic products of essential amino acids and have functions such as improving muscle mass, reducing muscle tissue damage during exercise, reducing body fat, and toning the body. They are known to be effective in preventing or improving conditions such as muscle atrophy associated with aging (sarcopenia) and conditions in which mobility is reduced due to disorders of the musculoskeletal system (locomotor syndrome).

[0003] Since the amount of 3-hydroxyisovaleric acid contained in food is small, and the amount of metabolic production from leucine is also small, oral compositions that can supply 3-hydroxyisovaleric acid and / or its salts as supplements have been developed. For example, Patent Document 1 discloses that a tablet containing calcium 3-hydroxyisovalerate and crystalline cellulose with an average particle size of 65 to 100 μm can suppress tableting failure and suppress the formation of unevenness on the surface. In addition, Patent Document 2 discloses that an oral composition containing calcium 3-hydroxyisovalerate and terpene exhibits excellent muscle-building and anti-obesity effects. [Prior art documents] [Patent documents]

[0004] [Patent Document 1] JP 2015-218158 A [Patent Document 2] JP 2019-85392 A Summary of the Invention [Problem to be solved by the invention]

[0005] 3-Hydroxyisovaleric acid and its salts have the disadvantages of being difficult to ingest due to their unpleasant taste, which causes tongue numbness, strong bitterness, etc. Therefore, there is a demand for improving the unpleasant taste of oral compositions containing 3-hydroxyisovaleric acid and / or its salts and improving their palatability.

[0006] Therefore, an object of the present invention is to provide an oral composition which contains 3-hydroxyisovaleric acid and / or a salt thereof and has an improved taste. [Means for solving the problem]

[0007] The present inventors have conducted extensive research to solve the above problems and have found that by incorporating vitamin D and / or vitamin B6 together with 3-hydroxyisovaleric acid and / or a salt thereof in an oral composition, the unpleasant taste peculiar to 3-hydroxyisovaleric acid and / or a salt thereof can be improved, making the composition easier to ingest. The present invention was completed through further research based on this finding.

[0008] That is, the present invention provides the following aspects. Item 1. An oral composition comprising (A) 3-hydroxyisovaleric acid and / or a salt thereof, and (B) vitamin D and / or vitamin B6. Item 2. The oral composition according to Item 1, comprising both a vitamin D group and a vitamin B6 group as the component (B). Item 3. The oral composition according to Item 1 or 2, comprising a total amount of the component (B) of 0.0001 to 100 parts by weight per 100 parts by weight of the component (A). Item 4. The oral composition according to any one of Items 1 to 3, comprising 0.0001 to 50 parts by weight of a vitamin D type and 0.25 to 50 parts by weight of a vitamin B6 type per 100 parts by weight of the component (A). Item 5. The oral composition according to any one of Items 1 to 4, which is a food or drink. Item 6. A method for masking the unpleasant taste of 3-hydroxyisovaleric acid and / or a salt thereof, comprising allowing (A) 3-hydroxyisovaleric acid and / or a salt thereof and (B) vitamin D and / or vitamin B6 to coexist in an oral composition. Effect of the Invention

[0009] According to the present invention, the unpleasant taste peculiar to 3-hydroxyisovaleric acid and / or its salts (tongue numbness, strong bitterness) can be improved and the taste preference can be increased, making it possible to provide foods, beverages, oral medicines, etc. that allow easy intake of 3-hydroxyisovaleric acid and / or its salts. DETAILED DESCRIPTION OF THE PREFERRED EMBODIMENTS

[0010] 1. Oral Compositions The oral composition of the present invention is characterized by containing 3-hydroxyisovaleric acid and / or a salt thereof (sometimes referred to as component (A)), and vitamin D and / or vitamin B6 (sometimes referred to as component (B)). The oral composition of the present invention will be described in detail below.

[0011] [(A) 3-Hydroxyisovaleric acid and / or its salt] 3-Hydroxyisovaleric acid, also known as 3-hydroxy-3-methylbutyric acid or HMB, is a known compound that is known to have functions such as improving muscle mass, reducing muscle tissue damage during exercise, reducing body fat, and toning the body.

[0012] The salt of 3-hydroxyisovaleric acid is not particularly limited, as long as it is edible, and examples thereof include alkaline earth metal salts such as calcium salt and magnesium salt; alkali metal salts such as sodium salt and potassium salt; inorganic acid salts such as hydrochloride, hydrobromide, sulfate, hydroiodide, nitrate and phosphate; and organic acid salts such as citrate, oxalate, acetate, formate, propionate, benzoate, trifluoroacetate, maleate, tartrate, methanesulfonate, benzenesulfonate and paratoluenesulfonate.

[0013] In the oral composition of the present invention, as the component (A), one kind selected from 3-hydroxyisovaleric acid and salts thereof may be used alone, or two or more kinds thereof may be used in combination.

[0014] Of the components (A), preferred are salts of 3-hydroxyisovaleric acid, more preferred are alkaline earth metal salts of 3-hydroxyisovaleric acid, and even more preferred are calcium 3-hydroxyisovalerate.

[0015] The content of the component (A) in the oral composition of the present invention may be appropriately set depending on the content of other components blended in the oral composition, the form of the oral composition, the amount taken per time, etc., and may be, for example, 2 to 99.5% by weight. More specifically, when the oral composition of the present invention is solid, the content of the component (A) may be 20 to 99.5% by weight, preferably 25 to 90% by weight, more preferably 50 to 80% by weight. When the oral composition of the present invention is semi-solid or liquid, the content of the component (A) may be 2 to 60% by weight, preferably 3 to 50% by weight, more preferably 4 to 40% by weight.

[0016] In addition, 3-hydroxyisovaleric acid and / or its salts have a specific unpleasant taste, and the higher the content in an oral composition, the stronger the unpleasant taste when ingested. However, by containing vitamin D and / or vitamin B6, the oral composition of the present invention improves the unpleasant taste even when the content of 3-hydroxyisovaleric acid and / or its salts is as high as about 25% by weight or more (particularly, about 40% by weight or more or 50% by weight or more), making it easier to ingest.

[0017] [(B) Vitamin D and / or Vitamin B6] In the oral composition of the present invention, the unpleasant taste of 3-hydroxyisovaleric acid and / or a salt thereof is improved by containing vitamin D and / or vitamin B6.

[0018] Specific examples of vitamin D include vitamin D2 (ergocalciferol) and vitamin D3 (cholecalciferol). As vitamin D, either vitamin D2 or vitamin D3 may be used alone, or both may be used in combination. Among vitamin D, vitamin D3 is preferred.

[0019] Specific examples of vitamin B6 include pyridoxine, pyridoxal, pyridoxamine, and their salts.Specific examples of vitamin B6 in the form of a salt include inorganic acid salts such as hydrochloride and phosphate; organic acid salts such as acetate.Specific examples of vitamin B6 in the form of a salt include pyridoxine hydrochloride, pyridoxal phosphate, pyridoxamine phosphate, etc.Among vitamin B6, pyridoxine and its salts are preferred, and pyridoxine hydrochloride is more preferred.

[0020] In the oral composition of the present invention, as component (B), one kind selected from vitamin D and vitamin B6 may be used alone, or two or more kinds thereof may be used in combination.

[0021] From the viewpoint of more effectively improving the unpleasant taste of 3-hydroxyisovaleric acid and / or its salt, it is preferable to use a combination of vitamin D and vitamin B6 as component (B). When vitamin D and vitamin B6 are used in combination as component (B), the ratio between them is not particularly limited, but for example, 0.5 to 10000 parts by weight, preferably 0.7 to 5000 parts by weight, more preferably 1 to 2500 parts by weight of vitamin B6 per 1 part by weight of vitamin D is mentioned.

[0022] In the oral composition of the present invention, the ratio of component (A) to component (B) is, for example, 0.0001 to 150 parts by weight, preferably 0.001 to 125 parts by weight, and more preferably 0.001 to 100 parts by weight of component (B) in total per 100 parts by weight of component (A). Specific examples of the ratio of component (A) to component (B) for each type of component (B) are as follows. By satisfying such a ratio, the unpleasant taste of 3-hydroxyisovaleric acid and / or a salt thereof can be improved more effectively. (B) When vitamin D is contained alone as an ingredient (A) 0.0001 to 150 parts by weight, preferably 0.001 to 125 parts by weight, and more preferably 0.001 to 100 parts by weight of vitamin D group per 100 parts by weight of the component (A). (B) Vitamin B 6 When a class is included alone : 0.25 to 150 parts by weight, preferably 0.3 to 125 parts by weight, and more preferably 0.3 to 100 parts by weight of vitamin B6 per 100 parts by weight of the component (A). (B) Vitamin D and vitamin B 6 When both types are included The total amount of vitamin D group and vitamin B6 group is 0.25 to 150 parts by weight, preferably 0.25 to 125 parts by weight, and more preferably 0.25 to 100 parts by weight, per 100 parts by weight of the component (A).

[0023] The content of component (B) in the oral composition of the present invention may be appropriately set depending on the content of component (A), the content of other components blended in the oral composition, the form of the oral composition, the amount taken per time, etc., and may be, for example, 0.000004 to 50% by weight in total of component (B).

[0024] When the oral composition of the present invention is a solid, the content of the component (B) is more specifically 0.000004 to 60% by weight, preferably 0.00006 to 55% by weight, more preferably 0.0002 to 50% by weight. When the oral composition of the present invention is a solid, specific examples of the content of each type of component (B) are as follows. (B) When vitamin D is contained alone as an ingredient The vitamin D group is 0.00004 to 60% by weight, preferably 0.00006 to 55% by weight, and more preferably 0.0002 to 50% by weight. (B) Vitamin B 6 When a class is included alone : Vitamin B6 is 0.1 to 60% by weight, preferably 0.2 to 55% by weight, and more preferably 0.2 to 50% by weight. (B) Vitamin D and vitamin B 6 When both types are included : Vitamin D's are 0.00004 to 30% by weight, preferably 0.00006 to 27% by weight, and more preferably 0.0002 to 25% by weight; Vitamin B6's are 0.1 to 30% by weight, preferably 0.2 to 27% by weight, and more preferably 0.2 to 25% by weight.

[0025] When the oral composition of the present invention is semi-solid or liquid, the content of component (B) is more specifically 0.000004 to 5% by weight, preferably 0.0004 to 2.5% by weight, more preferably 0.0001 to 1.3% by weight, based on the total amount of component (B). When the oral composition of the present invention is semi-solid or liquid, specific examples of the content of each type of component (B) are as follows: (B) When vitamin D is contained alone as an ingredient The content of vitamin D is 0.000004 to 5% by weight, preferably 0.0004 to 0.3% by weight, and more preferably 0.0001 to 0.04% by weight. (B) Vitamin B 6 When a class is included alone Vitamin B6: 0.01 to 5% by weight, preferably 0.02 to 2.5% by weight, more preferably 0.02 to 1% by weight. (B) Vitamin D and vitamin B 6 When both types are included : Vitamin D's are 0.000004 to 2.5 wt %, preferably 0.0004 to 0.3 wt %, and more preferably 0.0001 to 0.04 wt %; Vitamin B6's are 0.01 to 2.5 wt %, preferably 0.02 to 1.25 wt %, and more preferably 0.02 to 1.0 wt %.

[0026] [Other ingredients] The oral composition of the present invention may contain other nutritional components and pharmacological components in addition to the components (A) and (B). Such nutritional components and pharmacological components are not particularly limited as long as they can be used in foods and internal medicines, and examples thereof include vitamins (other than the component (B)), amino acids, minerals, carbohydrates, fatty acids, flavorings, seasonings, plant extracts, antioxidants, hypoglycemic agents, anticholesterol agents, and immunoactivators. These components may be used alone or in combination of two or more. The content of these components is appropriately set depending on the type of additives used and the purpose of the oral composition.

[0027] Furthermore, in order to prepare the oral composition of the present invention into a desired formulation, it may contain bases and additives, etc., in addition to the above-mentioned (A) and (B) components, as necessary. Such bases and additives are not particularly limited as long as they can be used in foods and internal medicines, and examples thereof include excipients, disintegrants, lubricants, binders, thickeners, lower alcohols, solid oils, higher alcohols, water-soluble polymers, surfactants, polyhydric alcohols, pH adjusters, buffers, antioxidants, preservatives, chelating agents, water, etc. These may be used alone or in combination of two or more. The content of these bases and additives is appropriately set depending on the type of components used and the purpose of the oral composition.

[0028] [Dosage form / formulation] The dosage form of the oral composition of the present invention is not particularly limited as long as it can be orally ingested or administered, and may be any of solid, semi-solid, or liquid, which may be appropriately selected depending on the type and application of the oral composition.

[0029] The formulation of the oral composition of the present invention is not particularly limited as long as it can be orally ingested or administered, and specific examples thereof include foods, beverages, and medicines for internal administration.

[0030] When the oral composition of the present invention is formulated into a food or drink, the (A) component and the (B) component may be prepared as they are or in combination with other food materials or additives into a desired form. Examples of such food or drink include general food or drink, as well as specific health foods, nutritional supplements, functional foods, and foods for sick people. The form of these food or drink is not particularly limited, but specifically includes supplements such as capsules (soft capsules and hard capsules), tablets (including coated tablets), granules, powders, and jellies; beverages such as nutritional drinks, fruit juice drinks, carbonated drinks, and lactic acid drinks; and luxury items such as dumplings, ice cream, sherbet, gummy candies, and candies. Among these food or drink, supplements are preferred, and tablets, capsules, granules, and powders are more preferred.

[0031] When the oral composition of the present invention is formulated into an oral pharmaceutical preparation, the (A) component and the (B) component may be prepared into a desired form as is or in combination with other additives.Specific examples of such oral pharmaceutical preparations include capsules (soft capsules, hard capsules), tablets (including coated tablets), granules, powders, jellies, syrups, liquids, etc.Among these oral pharmaceutical preparations, tablets, capsules, granules, and powders are preferred.

[0032] [Application] The oral composition of the present invention can be used for various applications utilizing the functionality of the component (A). Specifically, the oral composition of the present invention can be used for applications such as improving muscle mass (increasing muscle mass, suppressing the decrease in muscle mass), reducing muscle tissue damage during exercise, reducing body fat, and toning. In particular, the oral composition of the present invention has the effect of increasing muscle mass in young people and maintaining muscle mass in middle-aged and elderly people, so it is suitable for increasing muscle mass in people in their 30s or younger and for suppressing the decrease in muscle mass in people in their 40s or older.

[0033] In addition, the oral composition of the present invention can also be used for preventing or improving sarcopenia or locomotive syndrome.

[0034] [Intake or dosage] The intake or dosage of the oral composition of the present invention is not particularly limited and is appropriately set depending on the formulation form, application, the contents of the components (A) and (B), etc. For example, in the case of an adult, the intake or dosage of the component (A) per day may be set to about 1000 to 2000 mg, preferably about 1000 to 1500 mg.

[0035] 2. Method for masking the unpleasant taste of 3-hydroxyisovaleric acid and / or its salts As described above, the unpleasant taste of 3-hydroxyisovaleric acid and / or a salt thereof can be improved by causing 3-hydroxyisovaleric acid and / or a salt thereof to coexist with vitamin D and / or vitamin B6 in an oral composition. Therefore, the present invention further provides a method for masking the unpleasant taste of 3-hydroxyisovaleric acid and / or a salt thereof, which comprises causing (A) 3-hydroxyisovaleric acid and / or a salt thereof and (B) vitamin D and / or vitamin B6 to coexist in an oral composition.

[0036] In the masking method of the present invention, the types, contents, and ratios of the (A) and (B) components used, other components that can be blended in the oral composition, and the dosage form, shape, and uses of the oral composition are as described in the section "1. Oral Composition" above. EXAMPLES

[0037] The present invention will now be described in more detail with reference to examples, but the present invention is not limited to these examples in any way.

[0038] Test Example 1 Powders were prepared with the compositions shown in Table 1. One trained panelist ingested 1 g of the resulting powder together with water, and the taste was evaluated according to the following criteria. <Taste evaluation criteria> ××: Tongue numbness and extremely bitter taste make it difficult to ingest. ×: Numbness in the tongue and a strong bitter taste, very unpleasant. △: There is a slight numbness in the tongue and a bitter taste, but the discomfort is tolerable. ○: The numbness of the tongue and bitterness are reduced, and there is not much discomfort. ◎: The numbness of the tongue and bitterness are significantly reduced, and there is no discomfort.

[0039] The results are shown in Table 1. When calcium 3-hydroxyisovalerate was contained alone, the tongue felt numb and the bitter taste was extremely strong (Comparative Example 1). In contrast, when calcium 3-hydroxyisovalerate was contained together with vitamin D3 or pyridoxine hydrochloride, the unpleasant taste of calcium 3-hydroxyisovalerate was improved (Examples 1 and 2). Furthermore, when both vitamin D3 and pyridoxine hydrochloride were contained, the unpleasant taste of calcium 3-hydroxyisovalerate was improved even when the contents of these were low (Example 5), and the more the contents of these were increased, the less unpleasant taste of calcium 3-hydroxyisovalerate was felt (Examples 3 and 4).

[0040] [Table 1]

[0041] Test Example 2 Tablets having the composition shown in Table 2 were prepared in a conventional manner.

[0042] [Table 2]

[0043] Thirteen subjects in their 20s to 60s (2 in their 20s, 4 in their 30s, 4 in their 40s, 3 in their 50s and 60s) were given the tablets once a day for four weeks in the above-mentioned doses. The subjects' muscle mass was measured using a body composition analyzer (product name "WELL SCAN", Canon Life Care Solutions Inc.) before and after taking the tablets for four weeks, and the change in muscle mass was calculated according to the following formula, and the change in muscle mass by generation (average value) and the change in muscle mass for all subjects (average value, standard deviation, significant difference by t-test) were calculated. Change in muscle mass = muscle mass after 4 weeks of taking the tablets - muscle mass before taking the tablets

[0044] The results are shown in Table 3. As a result, it was observed that by taking tablets containing calcium 3-hydroxyisovalerate, vitamin D3, and pyridoxine hydrochloride, muscle mass increased in subjects in their 30s or younger, and muscle mass tended to be maintained in subjects in their 40s or older, confirming that the tablets improve muscle mass (increase and maintenance of muscle mass).

[0045] [Table 3]

[0046] Formulation examples Powders, tablets and granules were manufactured with the compositions shown in Tables 4 and 5. The obtained tablets and granules had a significantly reduced tongue numbness and bitterness, and did not cause any discomfort when ingested. In addition, when the obtained tablets and granules were taken once a day for four weeks, improvement in muscle mass (increase and maintenance of muscle mass) was observed.

[0047] [Table 4]

[0048] [Table 5]

Claims

1. (A) 3-hydroxyisovaleric acid and / or a salt thereof, and (B) vitamin D and / or vitamin B 6 An oral composition comprising:

2. The component (B) includes vitamin D and vitamin B 6 The oral composition of claim 1 , comprising both

3. The oral composition according to claim 1 or 2, comprising a total amount of 0.0001 to 100 parts by weight of the component (B) per 100 parts by weight of the component (A).

4. 0.0001 to 50 parts by weight of vitamin D and vitamin B per 100 parts by weight of the component (A) 6 The oral composition according to any one of claims 1 to 3, comprising 0.25 to 50 parts by weight of a compound.

5. The oral composition according to any one of claims 1 to 4, which is a food or drink.

6. In the oral composition, (A) 3-hydroxyisovaleric acid and / or its salt and (B) vitamin D and / or vitamin B 6 A method for masking the unpleasant taste of 3-hydroxyisovaleric acid and / or a salt thereof, comprising the step of:

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