Oral composition

An oral composition with leucine and tryptophan in a specific ratio, combined with other essential amino acids, enhances muscle building and taste, addressing the limitations of existing amino acid supplements.

JP2026056777AActive Publication Date: 2026-04-02TOYO SHINYAKU KK
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Patent Information

Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2024-09-20
Publication Date
2026-04-02

AI Technical Summary

Technical Problem

Existing health foods containing amino acids do not effectively promote muscle strengthening, and compositions with leucine alone often have an unpleasant taste.

Method used

An oral composition containing leucine and tryptophan in a specific ratio, along with other essential amino acids, promotes protein synthesis and muscle building while mitigating the bitter taste of leucine.

Benefits of technology

The composition exhibits excellent muscle-building effects and improved flavor, making it easier to consume, suitable for athletes, healthy individuals, and the elderly.

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Abstract

This invention provides an oral composition containing amino acids that exhibits excellent muscle-building effects. [Solution] An oral composition containing leucine and tryptophan, wherein the oral composition contains 9.0 parts by mass or more of leucine per 1 part by mass of tryptophan.
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Description

Technical Field

[0001] The present invention relates to an oral composition containing leucine and tryptophan.

Background Art

[0002] In recent years, various health foods have been developed against the background of increasing interest in health, etc. For example, health foods containing amino acids have been developed.

[0003] [[ID=I5]] As such health foods containing amino acids, for example, health foods containing amino acids such as alanine, arginine, leucine, etc. and used for enhancing learning and memory ability have been proposed (see, for example, Patent Document 1).

Prior Art Documents

Patent Documents

[0004]

Patent Document 1

Summary of the Invention

Problems to be Solved by the Invention

[0005] An object of the present invention is to provide an oral composition containing amino acids and exhibiting an excellent muscle strengthening effect.

Means for Solving the Problems

[0006] As a result of intensive studies to solve the above problems, the present inventors have found that an oral composition containing leucine and tryptophan in a specific ratio exhibits an excellent muscle strengthening effect, and have completed the present invention.

[0007] That is, the present invention is as follows. [1] An oral composition containing leucine and tryptophan, wherein the leucine is contained in an amount of 9.0 parts by mass or more with respect to 1 part by mass of the tryptophan. [2] The oral composition according to [1] above, further comprising one or more essential amino acids selected from valine, isoleucine, lysine, methionine, histidine, threonine, and phenylalanine. [3] The oral composition according to [1] or [2] above, wherein the leucine content relative to the total content of essential amino acids is 50.0% by mass or more. [4] An oral composition according to any of [1] to [3] above, for muscle building. [Effects of the Invention]

[0008] The oral composition of the present invention exhibits excellent muscle-building effects. [Modes for carrying out the invention]

[0009] The present invention relates to an oral composition containing leucine and tryptophan, characterized in that it contains 9.0 parts by mass or more of leucine per 1 part by mass of tryptophan.

[0010] The oral composition of the present invention contains leucine and tryptophan in specific proportions, thereby promoting protein synthesis in the body and exhibiting excellent muscle-building effects. The oral composition of the present invention can be used for muscle building in athletes and healthy individuals, muscle recovery after illness, and muscle maintenance in the elderly. Furthermore, the oral composition of the present invention has an improved flavor compared to leucine alone, making it easier to consume.

[0011] The following describes each component contained in the oral composition of the present invention. [Leucine] Leucine is a type of amino acid, a branched-chain amino acid, and one of the essential amino acids in humans. It is abbreviated as Leu or L. Leucine exists in isomers such as L-, D-, and DL-, and any of these can be used in the oral composition of the present invention.

[0012] The leucine content in the oral composition of the present invention, relative to the total content of essential amino acids (leucine content when the total content of essential amino acids is taken as 100%), is not particularly limited. However, from the viewpoint of enjoying the effects of the present invention, it is preferably 50.0% by mass or more, more preferably 60.0% by mass or more, and even more preferably 70.0% by mass or more. The upper limit is not particularly limited, but from the viewpoint of taste, it is preferably 90.0% by mass or less, and more preferably 80.0% by mass or less.

[0013] [Tryptophan] Tryptophan is an aromatic amino acid with an indole ring in its side chain. It is one of the essential amino acids in humans, and its systematic name is 2-amino-3-(indolyl)propionic acid, abbreviated as Trp or W. Tryptophan exists in isomers such as L-, D-, and DL-, and any of these can be used in the oral composition of the present invention.

[0014] As described above, the content ratio of leucine and tryptophan in the oral composition of the present invention is 9.0 parts by mass or more of leucine per 1 part by mass of tryptophan. However, to better enjoy the effects of the present invention, it is preferable to have 10.0 parts by mass or more, more preferably 50.0 parts by mass or more, and even more preferably 75.0 parts by mass or more. There is no particular upper limit, but for example, it is preferably 500.0 parts by mass or less, and preferably 100.0 parts by mass or less.

[0015] <Other amino acids> The oral composition of the present invention preferably contains other essential amino acids besides leucine and tryptophan. This allows for a balanced intake of essential amino acids, thereby more effectively promoting muscle growth. Specific examples of other essential amino acids include valine, isoleucine, lysine, methionine, histidine, threonine, and phenylalanine.

[0016] [Balin] Valine is a type of amino acid and is a branched-chain amino acid. It is one of the essential amino acids in humans, also known as 2-aminoisovaleric acid, and is represented by the abbreviations Val or V. Valine exists in isomers such as L-form, D-form, and DL-form, and any of them can be used in the oral compositions of the present invention.

[0017] [Isoleucine] Isoleucine is a type of amino acid and is a branched-chain amino acid. It is one of the essential amino acids in humans, also known as 2-amino-3-methylpentanoic acid (2-amino-3-methylvaleric acid), and is represented by the abbreviations Ile or I. Isoleucine exists in isomers such as L-form, D-form, and DL-form, and any of them can be used in the oral compositions of the present invention.

[0018] [Lysine] Lysine is a type of amino acid and is a basic amino acid. It is one of the essential amino acids in humans, also known as lysine, and is represented by the abbreviations Lys or K. Lysine exists in isomers such as L-form, D-form, and DL-form, and any of them can be used in the oral compositions of the present invention.

[0019] [Methionine] Methionine is a type of amino acid and is a hydrophobic amino acid containing sulfur in its side chain. It is one of the essential amino acids in humans, and is represented by the abbreviations Met or M. Methionine exists in isomers such as L-form, D-form, and DL-form, and any of them can be used in the oral compositions of the present invention.

[0020] [Histidine] Histidine is a type of amino acid and is an aromatic amino acid having a heteroaromatic ring in its side chain. It is one of the essential amino acids in humans, and is represented by the abbreviations His or H. Histidine exists in isomers such as L-form, D-form, and DL-form, and any of them can be used in the oral compositions of the present invention.

[0021] [Threonine] Threonine is an amino acid that has a hydroxyethyl group in its side chain, and is also called threonine. It is one of the essential amino acids in humans and is abbreviated as Thr or T. Because threonine has two optically active sites, there are four isomers: L-threonine, D-threonine, L-alrosreonine, and D-alrosreonine. Any of these can be used in the oral composition of the present invention.

[0022] [Phenylalanine] Phenylalanine is an aromatic amino acid with a benzyl group in its side chain. It is one of the essential amino acids in humans and is abbreviated as Phe or F. Phenylalanine exists in isomers such as L-, D-, and DL-, and any of these can be used in the oral composition of the present invention.

[0023] In this invention, essential amino acids refer to amino acids that exist as free amino acids, and do not include amino acids that exist as components of proteins. Free amino acids (amino acids that exist individually and independently from proteins) have different properties as compounds from amino acids that exist as components of proteins, and the two are clearly distinguishable.

[0024] Furthermore, the essential amino acids in this invention can be used not only as free forms but also in the form of salts. Examples of salt forms include acid addition salts and salts with bases, and it is preferable to select a salt that is pharmacologically acceptable. Specific examples of salts include inorganic bases, organic bases, inorganic acids, and salts with organic acids. In this invention, free forms or inorganic salts are preferred, free forms or hydrochloride salts are more preferred, and free forms are particularly preferred, in order to better enjoy the effects of this invention. The amino acids in this invention can be commercially available products that are normally available as food ingredients.

[0025] In the oral composition of the present invention, one or more other essential amino acids may be used. To better enjoy the effects of the present invention, it is preferable to satisfy one or more conditions selected from (A1) to (G1) below.

[0026] (A1) Contains valine, with a mass ratio of valine to 1 part by mass of tryptophan of 3.0 parts by mass or more. (B1) Contains isoleucine, with a mass ratio of isoleucine to 1 part by mass of tryptophan of 3.0 parts by mass or more. (C1) Contains lysine, with a mass ratio of lysine to 1 part by mass of tryptophan of 5.0 parts by mass or more. (D1) Contains methionine, with a mass ratio of methionine to 1 part by mass of tryptophan of 1.5 parts by mass or more. (E1) Contains histidine, with a mass ratio of histidine to 1 part by mass of tryptophan of 1.1 parts by mass or more. (F1) Contains threonine, with a mass ratio of threonine to 1 part by mass of tryptophan of 3.7 parts by mass or more. (G1) Contains phenylalanine, with a mass ratio of phenylalanine to 1 part by mass of tryptophan of 2.0 parts by mass or more.

[0027] Furthermore, in order to better enjoy the effects of the present invention, it is preferable to satisfy one or more conditions selected from (A2) to (D2) below. (A2) Contains lysine and methionine, with a mass ratio of methionine to 1 part by mass of lysine of 0.3 parts by mass or more. (B2) Contains lysine and histidine, with a mass ratio of histidine to 1 part by mass of lysine of 0.25 parts by mass or more. (C2) Contains lysine and threonine, with a mass ratio of threonine to 1 part by mass of lysine of 0.65 parts by mass or less. (D2) Contains lysine and phenylalanine, with a mass ratio of phenylalanine to 1 part by mass of lysine of 0.4 parts by mass or more.

[0028] Furthermore, in order to better enjoy the effects of the present invention, it is preferable to satisfy one or more conditions selected from (A3) to (C3) below. (A3) Contains methionine and histidine, with a mass ratio of histidine to 1 part by mass of methionine of 0.75 parts by mass or less. (B3) Contains methionine and threonine, with a mass ratio of threonine to 1 part by mass of methionine of 2.5 parts by mass or less. (C3) Contains methionine and phenylalanine, with a mass ratio of phenylalanine to 1 part by mass of methionine of 1.5 parts by mass or more.

[0029] Furthermore, in order to better enjoy the effects of the present invention, it is preferable to satisfy one or more conditions selected from (A4) to (B4) below. (A4) Contains histidine and threonine, with a mass ratio of threonine to 1 part by mass of histidine of 2.8 parts by mass or less. (B4) Contains histidine and phenylalanine, with a mass ratio of phenylalanine to 1 part by mass of histidine of 1.8 parts by mass or more.

[0030] The oral composition of the present invention may contain other commonly used substances in addition to the above-mentioned leucine, tryptophan, and other essential amino acids. Examples of other substances include various excipients, binders, glazing agents, lubricants, stabilizers, diluents, fillers, thickeners, emulsifiers, antioxidants, pH adjusters, colorants, flavorings, and additives.

[0031] There are no particular restrictions on the amount of oral composition of the present invention to be taken, but in order to better enjoy the effects of the present invention, the daily intake of leucine may be 200 mg / day or more, preferably 1000 mg / day or more, and more preferably 1500 mg / day or more. There are no particular restrictions on the upper limit of intake, but in order to better enjoy the effects of the present invention, the daily intake of leucine may be 15000 mg / day or less, preferably 5000 mg / day or less, and more preferably 2500 mg / day or less.

[0032] The oral composition of the present invention is not particularly limited as long as it is in a form for oral intake, and may be any of the following: pharmaceuticals (including quasi-drugs), so-called health foods, foods for specified health uses, or foods with functional claims.

[0033] Examples of the oral composition of the present invention include tablets, capsules, powders, granules, liquids, rods, plates, blocks, solids, rounds, pastes, creams, caplets, gels, chewables, sticks, and the like, with tablets, capsules, powders, granules, and liquids being preferred.

[0034] The oral composition of the present invention can be used as an oral composition for muscle building. Such an oral composition for muscle building is not particularly limited as long as it contains leucine and tryptophan and is distinguishable from other products in that it is used for muscle building. For example, any product that displays a statement indicating muscle building function on the product itself, packaging, instructions, or promotional materials is included within the scope of the present invention. Furthermore, in the case of foods with functional claims, products that base their functionality on muscle building are included.

[0035] Specifically, examples include products that claim to have functions such as suppressing, maintaining, or increasing the decline of muscle mass (muscle weight, muscle cross-sectional area, muscle density), suppressing, maintaining, or improving the decline of muscle quality, and suppressing, maintaining, or increasing the decline of muscle strength. More specifically, examples include products that claim to "enhance muscle strength," "support the ability to build muscle," "suppress muscle breakdown," "support muscle training," "support body building," "muscular," "lean and muscular," and "maintain muscle mass and strength."

[0036] Furthermore, the oral muscle-enhancing composition of the present invention is not limited to products in which the combination of components (leucine and tryptophan) of the present invention is indicated as the active ingredient for muscle enhancement on the product packaging, etc. For example, it may be a product in which the active ingredient is not specified. Also, even general food products that are manufactured and sold with a suggested function or use are included in the scope of the oral muscle-enhancing composition of the present invention. For example, this includes products that are sold with testimonials from people who have consumed them, mentioning the function or use as personal impressions, posted on websites, etc.

[0037] The oral composition of the present invention is not particularly limited to individuals who require muscle strengthening, but is preferably used by people who aim to lose weight, athletes, and elderly people with weakened legs and hips. [Examples]

[0038] The present invention will be described in more detail below based on examples, but the present invention is not limited thereto.

[0039] <Test 1: Evaluation of cell-activating activity> The cell-activating activity of the mouse myoblast cell line (C2C12) was confirmed using the oral composition of the present invention. C2C12 is widely used as a model for evaluating effects such as muscle mass increase, and by confirming its cell-activating activity, the muscle-enhancing effect can be confirmed.

[0040] [Test substance] The following substances were used as test materials. • Leucine: Reagents of L-leucine • Lysine: Reagent for L-lysine monohydrochloride • Valine: L-valine reagent • Isoleucine: Reagent of L-isoleucine • Tryptophan: L-tryptophan reagent • Phenylalanine: L-phenylalanine reagent • Methionine: L-methionine reagent • Histidine: L-histidine reagent • Tryptophan: L-tryptophan reagent

[0041] (Preparation of test substance) Each test substance was suspended in 10% FBS-amino acid-free DMEM medium to a concentration of 20 mM. The suspension was sterilized by passing it through a 0.2 μm filter, and the resulting solutions were diluted to a concentration of 10 μM in the same medium to obtain the test substance preparation solutions. The test substance-containing media were prepared by mixing each test substance preparation solution to achieve the mass composition ratios shown in Tables 1 to 7.

[0042] The specific experimental procedure is as follows: 75cm in a 37℃, 5V %CO2 incubator 2 C2C12 cells were cultured in a flask using 10% FBS-DMEM. Then, cells suspended by trypsin were placed in each well of a collagen-coated 96-well plate in groups of 8 × 10⁶. 3 Cells were seeded at a cell density of cells / well and pre-cultured for 24 hours in a 37°C, 5V %CO2 incubator.

[0043] After removing the culture medium from each well, wash once with PBS, add 100 μL / well of culture medium containing the test substance, and incubate for 3 hours in a 37°C, 5V %CO2 incubator. 10% FBS-amino acid-free DMEM was used as the culture medium, and the total molar concentration of the test substance in the medium was set to 10 μM. In addition, a 10% FBS-amino acid-free DMEM medium, which did not contain the test substance, was added as a control. This was designated as Comparative Example 1.

[0044] After 3 hours of incubation, the culture medium was removed, and 150 μL of CellCounting Kit-8 (Dojin Chemical Co., Ltd.), diluted 20-fold with amino acid-free DMEM, was added to each well. After standing in a 37°C, 5V %CO2 incubator to allow for appropriate color development, the absorbance of the formazan product at 450 nm, which is proportional to the number of viable cells in each well, was measured.

[0045] The chromogenic reagent WST-8 in CellCounting Kit-8 is reduced to formazan by the action of dehydrogenase via electron transport molecules. The more living cells there are, the higher the dehydrogenase activity and the greater the formazan production. Since formazan has a maximum absorption around 450 nm, its production was measured based on this absorbance to confirm C2C12 proliferation. A higher absorbance based on formazan indicates that C2C12 has proliferated, and therefore this absorbance serves as an indicator of myoblast activation activity. Additionally, as a blank, the absorbance of CellCounting Kit-8 diluted 20-fold with amino acid-free DMEM was measured.

[0046] The difference between the absorbance of each test substance well and the absorbance of the blank was calculated as the cell-activating activity in each test substance well, and was evaluated relatively against the cell-activating activity of the control well, Comparative Example 1, as shown in the formula below. Specifically, the value obtained by subtracting 100 (the cell-activating activity of the control well, Comparative Example 1) from the cell-activating activity (%) of each test substance well calculated from the formula below was shown as the percentage change (%). The results are shown in Tables 1 to 7.

[0047] Cellular activation activity (%) = (Absorbance of each test substance well - Absorbance of the blank well) × 100 / (Absorbance of the control well - Absorbance of the blank well)

[0048] [Table 1]

[0049] [Table 2]

[0050] [Table 3]

[0051] [Table 4]

[0052] [Table 5]

[0053] [Table 6]

[0054] [Table 7]

[0055] As shown in Tables 1-3, the compositions of Examples 1-26 of the present invention, in which tryptophan was blended with leucine in a specific ratio, exhibited cell-activating activity, as is evident from the comparison with the control (Comparative Example 1) which did not contain any essential amino acids. In particular, higher cell-activating activity was observed by including 50.0% by mass or more of leucine, or by blending other essential amino acids in desired ratios. Furthermore, the compositions of Examples 1-26 of the present invention showed significantly improved cell-activating activity compared to compositions containing essential amino acids alone (Comparative Examples 2-10) and compositions in which leucine and tryptophan were not blended in specific ratios (Comparative Example 11).

[0056] As described above, the composition of the present invention, by setting the component ratio of tryptophan to leucine to a specific ratio, allows for the balanced administration of essential amino acids effective for protein synthesis in the body, thereby improving the cell-activating activity of C2C12. Therefore, the oral composition of the present invention can promote muscle strengthening.

[0057] Furthermore, as shown in Tables 4-7, when specific essential amino acids are combined in specific proportions, the cell-activating activity is significantly improved. Therefore, by applying this to the composition of the present invention, the cell-activating activity can be further enhanced.

[0058] <Test 2: Sensory Test> Among the essential amino acids, leucine is known to have a bitter taste. The oral composition of the present invention was evaluated to determine whether it has the effect of mitigating the bitter taste of leucine by the following method.

[0059] [Preparation of the test substance (beverage)] The beverages of the Examples and Comparative Examples were prepared by mixing each essential amino acid with water in the proportions shown in Table 8, and containing 1% by mass of leucine.

[0060] [Evaluation Method] Six subjects with knowledge of sensory evaluation were given the prepared beverages to consume, and their bitterness and sweetness were evaluated according to the following criteria.

[0061] <Criteria for sensory evaluation> ●Bitterness 2. Compared to the comparative example, the bitterness is perceived as weaker. 1. Compared to the comparative example, the bitterness is perceived as slightly weaker. Compared to the comparative example, the bitterness remains unchanged. -1 Compared to the comparative example, the bitterness is slightly stronger. -2 Compared to the comparative example, the bitterness is more pronounced.

[0062] ●Sweetness 2. Compared to the comparative example, it tastes sweeter. 1. Compared to the comparison example, it tastes slightly sweeter. Compared to the comparative example, the sweetness remains unchanged. -1 Compared to the comparison example, the sweetness is perceived as slightly weaker. -2 Compared to the comparison example, the sweetness is perceived as weaker.

[0063] [Test Results] Table 8 shows the average score for each item.

[0064] [Table 8]

[0065] The results in Table 8 show that the oral composition of the present invention has the effect of mitigating the bitterness of leucine and making it easier to ingest the leucine-containing composition. [Industrial applicability]

[0066] The oral composition of the present invention is industrially useful because it can be used as a health food or the like.

Claims

1. An oral composition containing leucine and tryptophan, An oral composition containing 9.0 parts by mass or more of leucine per 1 part by mass of tryptophan.

2. The oral composition according to claim 1, further comprising one or more essential amino acids selected from valine, isoleucine, lysine, methionine, histidine, threonine, and phenylalanine.

3. The oral composition according to claim 2, wherein the leucine content relative to the total content of essential amino acids is 50.0% by mass or more.

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