Oral Composition

An oral composition with a specific leucine-to-tryptophan ratio and additional essential amino acids effectively enhances muscle building and improves taste, addressing the limitations of existing amino acid supplements.

JP7818298B1Active Publication Date: 2026-02-20TOYO SHINYAKU KK
View PDF 5 Cites 0 Cited by

Patent Information

Application Number
JP2024163341
Authority / Receiving Office
JP · JP
Patent Type
Patents
Current Assignee / Owner
Filing Date
2024-09-20
Publication Date
2026-02-20
Estimated Expiration
2044-09-20

AI Technical Summary

Technical Problem

Existing health foods containing amino acids do not effectively promote muscle building, 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, to enhance muscle-building effects and improve taste.

Benefits of technology

The composition promotes protein production, exhibits excellent muscle-building effects, and mitigates the bitter taste of leucine, making it easier to ingest.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure 0007818298000001
    Figure 0007818298000001
  • Figure 0007818298000002
    Figure 0007818298000002
  • Figure 0007818298000003
    Figure 0007818298000003
Patent Text Reader

Abstract

Provided is an oral composition that contains amino acids and exhibits excellent muscle-building effects. [Solution] The oral composition contains leucine and tryptophan, and contains 9.0 parts by mass or more of leucine per 1 part by mass of tryptophan.
Need to check novelty before this filing date? Find Prior Art

Description

[Technical Field]

[0001] The present invention relates to oral compositions containing leucine and tryptophan. [Background technology]

[0002] BACKGROUND ART In recent years, with the background of increasing interest in health, various health foods have been developed, for example, health foods containing amino acids.

[0003] Health foods containing such amino acids have been proposed, for example, for enhancing learning and memory abilities, containing amino acids such as alanine, arginine, and leucine (see, for example, Patent Document 1). [Prior art documents] [Patent documents]

[0004] [Patent Document 1] Japanese Patent Application Laid-Open No. 2013-184956 Summary of the Invention [Problem to be solved by the invention]

[0005] An object of the present invention is to provide an oral composition that contains amino acids and exhibits excellent muscle-building effects. [Means for solving the problem]

[0006] As a result of intensive research to solve the above problems, the inventors discovered that an oral composition containing leucine and tryptophan in a specific ratio has an excellent muscle-building effect, and thus completed the present invention.

[0007] That is, the present invention is as follows. [1] An oral composition containing leucine and tryptophan, the 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 [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] The oral composition according to any one of [1] to [3] above, which is for muscle building. [Effects of the Invention]

[0008] The oral composition of the present invention exhibits excellent muscle-building effects. DETAILED DESCRIPTION OF THE INVENTION

[0009] The oral composition of the present invention is an oral composition containing leucine and tryptophan, and is characterized by containing 9.0 parts by mass or more of leucine per part by mass of tryptophan.

[0010] The oral composition of the present invention contains leucine and tryptophan in a specific ratio, which promotes protein production in the body and exhibits an excellent muscle-building effect. The oral composition of the present invention can be used for muscle building in athletes and healthy individuals, muscle recovery after illness, muscle maintenance in the elderly, etc. Furthermore, the oral composition of the present invention has an improved flavor compared to compositions containing leucine alone, making it easier to ingest.

[0011] Each component contained in the oral composition of the present invention will be described below. [Leucine] Leucine is a type of amino acid, a branched-chain amino acid that is essential for humans, and is abbreviated as Leu or L. Leucine exists in the form of isomers, such as L-, D-, and DL-isomers, and any of these can be used in the oral composition of the present invention.

[0012] The leucine content relative to the total content of essential amino acids in the oral composition of the present invention (the leucine content when the total content of essential amino acids is taken as 100%) is not particularly limited, but in order to further enjoy 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 in terms 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 an essential amino acid in humans and has the systematic name 2-amino-3-(indolyl)propionic acid, abbreviated as Trp or W. Tryptophan exists in the form of L-, D-, and DL-isomers, all of which can be used in the oral composition of the present invention.

[0014] The content ratio of leucine and tryptophan in the oral composition of the present invention is, as described above, 9.0 parts by mass or more of leucine per part by mass of tryptophan, but from the viewpoint of better enjoying the effects of the present invention, it is preferably 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 it is, for example, 500.0 parts by mass or less, preferably 100.0 parts by mass or less.

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

[0016] [Ballin] Valine is a branched-chain amino acid. It is one of the essential amino acids for humans and is also known as 2-aminoisovaleric acid, abbreviated as Val or V. Valine exists as an isomer, such as L-, D-, or DL-isomer, and any of these can be used in the oral composition of the present invention.

[0017] [Isoleucine] Isoleucine is a branched-chain amino acid. It is one of the essential amino acids for humans and is also known as 2-amino-3-methylpentanoic acid (2-amino-3-methylvaleric acid), abbreviated as Ile or I. Isoleucine exists in the form of L-, D-, and DL-isomers, all of which can be used in the oral composition of the present invention.

[0018] [lysine] Lysine is a basic amino acid. It is one of the essential amino acids for humans and is also called lysine, abbreviated as Lys or K. Lysine exists in the form of isomers, such as L-, D-, and DL-isomers, all of which can be used in the oral composition of the present invention.

[0019] [Methionine] Methionine is a hydrophobic amino acid containing sulfur in the side chain. It is one of the essential amino acids for humans and is abbreviated as Met or M. Methionine exists as an isomer, such as L-, D-, or DL-isomer, and any of these can be used in the oral composition of the present invention.

[0020] [Histidine] Histidine is an aromatic amino acid with a heteroaromatic ring in the side chain. It is an essential amino acid in humans and is abbreviated as His or H. Histidine exists in the form of L-, D-, and DL-isomers, all of which can be used in the oral composition of the present invention.

[0021] [Threonine] Threonine, a type of amino acid with a hydroxyethyl group in the side chain, is also called threonine. It is one of the essential amino acids in humans and is abbreviated as Thr or T. Threonine has two optically active centers, and therefore exists as four isomers: L-threonine, D-threonine, L-allothreonine, and D-allothreonine. All of these isomers can be used in the oral composition of the present invention.

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

[0023] In the present 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 independently from proteins) have different properties as compounds from amino acids that exist as components of proteins, and the two are clearly distinguished.

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

[0025] In the oral composition of the present invention, one or more of the other essential amino acids may be used. In order to obtain the effects of the present invention more effectively, it is preferable that the composition satisfies one or more conditions selected from the following (A1) to (G1):

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

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

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

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

[0030] In addition to the above-mentioned leucine, tryptophan, and other essential amino acids, the oral composition of the present invention may contain other commonly used substances, such as various excipients, binders, glossing agents, lubricants, stabilizers, diluents, bulking agents, thickeners, emulsifiers, antioxidants, pH adjusters, colorants, flavors, and additives.

[0031] The intake amount of the oral composition of the present invention is not particularly limited, but from the viewpoint of further enjoying 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. The upper limit of the intake amount is not particularly limited, but from the viewpoint of further enjoying 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 that can be taken orally, and may be any of pharmaceuticals (including quasi-drugs), so-called health foods, foods for specified health uses, and foods with functional claims.

[0033] Examples of the form of the oral composition of the present invention include tablets, capsules, powders, granules, liquids, rods, plates, blocks, solids, rounds, pastes, creams, caplets, gels, chewable tablets, and sticks, 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 can be distinguished from other products in that it is used for muscle building. For example, the scope of the present invention includes products that display the muscle building function on the product itself, packaging, instructions, or promotional materials. Functional food claims also include those that certify muscle building as a scientific basis for their functionality.

[0035] Specifically, examples include products that claim to have functions such as inhibiting, maintaining, or increasing muscle mass (muscle weight, muscle cross-sectional area, muscle density), inhibiting, maintaining, or improving muscle quality, inhibiting, maintaining, or increasing muscle strength, etc. More specifically, examples include products that claim to "increase muscle strength," "support muscle-building ability," "suppress muscle breakdown," "support muscle training," "support body building," "macho," "slim-macho," "maintain muscle mass and strength," etc.

[0036] The oral composition for muscle building of the present invention is not limited to those labeled on the product packaging, etc., with the combined components of the present invention (leucine and tryptophan) as the active ingredient for muscle building. For example, it may be a product in which the active ingredient is not specified. Furthermore, even general foods that are manufactured and sold with suggested functions and uses are included in the scope of the oral composition for muscle building of the present invention. For example, there are products sold with personal testimonials from people who have taken the product posted on their websites, etc., mentioning its functions and uses.

[0037] The subjects who can take the oral composition of the present invention are not particularly limited as long as they are people who need to strengthen their muscles, but preferred examples include people who want to get in shape, athletes, and elderly people with weak legs and hips. [Example]

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

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

[0040] [Test substance] The following substances were used as test substances. Leucine: Reagent for L-leucine Lysine: L-Lysine monohydrochloride reagent Valine: Reagent for L-valine Isoleucine: Reagent for L-isoleucine Tryptophan: L-tryptophan reagent Phenylalanine: Reagent for L-phenylalanine 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 through a 0.2 μm filter and diluted with the same medium to a concentration of 10 μM to obtain a test substance preparation solution. Each test substance preparation solution was mixed to obtain the mass composition ratios listed in Tables 1 to 7 to prepare test substance-containing media.

[0042] The specific experimental procedures are as follows. In a 37°C, 5% CO2 incubator, 75 cm 2 C2C12 cells were cultured in a flask with 10% FBS-DMEM. Then, the cells were suspended by trypsinization and placed in each well of a collagen-coated 96-well plate at 8 × 10 3 The cells were seeded at a density of 100 cells / well and pre-cultured for 24 hours in a 5% by volume CO 2 incubator at 37°C.

[0043] After removing the medium from each well, the wells were washed once with PBS, and 100 μL / well of medium containing the test substance was added, followed by culturing for 3 hours in a 37° C., 5% by volume CO 2 incubator. The medium used was 10% FBS-amino acid-free DMEM, and the total molar concentration of the test substance in the medium was 10 μM. As a control, 10% FBS-amino acid-free DMEM medium containing no test substance was added. This was designated Comparative Example 1.

[0044] After 3 hours of incubation, the medium was removed, and 150 μL of Cell Counting Kit-8 (Dojindo Laboratories) diluted 20-fold with amino acid-free DMEM was added to each well. The plates were placed in a 37°C, 5% CO2 incubator to allow for adequate color development, and the absorbance at 450 nm of the formazan product, which is proportional to the number of viable cells in each well, was measured.

[0045] The WST-8 color reagent in the Cell Counting Kit-8 is reduced to formazan by the action of dehydrogenase via electron transfer substances. The more viable cells there are, the higher the dehydrogenase activity and the greater the amount of formazan produced. Since formazan has a maximum absorption around 450 nm, the amount of formazan produced was measured based on this absorbance to confirm C2C12 proliferation. Higher formazan absorbance indicates greater C2C12 proliferation, so this absorbance serves as an indicator of myoblast-stimulating activity. As a blank, the absorbance of Cell Counting Kit-8 alone 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-stimulating activity of each test substance well, and evaluated relative to the cell-stimulating activity of the control well of Comparative Example 1, as shown in the formula below. Specifically, the cell-stimulating activity (%) of each test substance well, calculated using the formula below, minus 100 (the cell-stimulating activity (%) of the control well of Comparative Example 1), was subtracted to obtain the percentage change (%). The results are shown in Tables 1 to 7.

[0047] Cell stimulating activity (%) = (absorbance of each test substance well - absorbance of blank) x 100 / (absorbance of control well - absorbance of blank)

[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 to 3, the compositions of Examples 1 to 26 of the present invention, in which tryptophan was blended at a specific ratio relative to leucine, exhibited cell-activating activity, as evident from a comparison with the control (Comparative Example 1) in which no essential amino acids were blended. In particular, higher cell-activating activity was observed when leucine was contained in an amount of 50.0 mass% or more or when other essential amino acids were blended in desired ratios. Furthermore, the compositions of Examples 1 to 26 of the present invention exhibited significantly improved cell-activating activity compared to compositions containing only essential amino acids (Comparative Examples 2 to 10) and a composition in which leucine and tryptophan were not blended in a specific ratio (Comparative Example 11).

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

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

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

[0059] [Preparation of test substance (drink)] Each essential amino acid was mixed with water to obtain the blending ratio shown in Table 8, and beverages containing 1% by mass of leucine were prepared for the Examples and Comparative Examples.

[0060] [Evaluation method] Six subjects with knowledge of sensory testing were asked to consume the prepared beverages and evaluate the bitterness and sweetness of the beverages according to the following evaluation criteria.

[0061] <Sensory evaluation criteria> Bitterness 2. Compared to the comparative example, the bitterness is perceived as weaker. 1. Compared to the comparative example, the bitterness is slightly weaker. 0 Bitterness remains the same compared to the comparative example -1 Compared to the comparative example, the bitterness is slightly stronger -2 Compared to the comparative example, the bitterness is stronger

[0062] ●Sweetness 2. Compared to the comparative example, the sweetness is stronger. 1. Compared to the comparative example, the sweetness is slightly stronger. 0 Sweetness remains the same compared to the comparative example -1 The sweetness is slightly weaker than the comparative example -2 The sweetness is weaker than the comparative example

[0063] [Test Results] The average scores for each item are shown in Table 8.

[0064] [Table 8]

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

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

Claims

[Claim 1] 1. An oral composition comprising leucine and tryptophan, The composition contains 9.0 parts by mass or more of the leucine per 1 part by mass of the tryptophan, The content of the leucine relative to the total content of essential amino acids is 70.0% by mass or more, In addition, the following conditions (I) to (III) (I) Contains lysine and methionine, and the mass ratio of methionine to 1 mass part of lysine is 0.3 mass parts or more. (II) Contains lysine and histidine, and the mass ratio of histidine to 1 part by mass of lysine is 0.25 parts by mass or more. (III) Contains lysine and phenylalanine, and the mass ratio of phenylalanine to 1 part by mass of lysine is 0.4 parts by mass or more. An oral composition that satisfies one or more conditions selected from the following (excluding (A) to (B) described below). (A) A sleep-improving composition containing theanine, tryptophan, and leucine (B) An oral composition containing leucine, a medium-chain fatty acid, and vitamin D.

Citation Information

Patent Citations

  • Amino acid-containing composition for preventing or improving skeletal muscle mass loss in the elderly

    JP2008534599A

  • Food for augmenting learning and memorizing capacity

    JP2013184956A

  • Amino acid-containing composition for blood-pressure reduction

    JP2014141443A

  • Motor function improving agent, respiratory function improving agent, or cognitive ability improving agent

    JP2016210720A

  • Sleep improving composition

    JP2022014307A