Minoxidil-containing composition

A minoxidil composition with tocopherol derivatives, mucopolysaccharides, and eucalyptus oil effectively inhibits discoloration, addressing the issue of composition stability in minoxidil formulations.

JP2025161483APending Publication Date: 2025-10-24ROHTO PHARM CO LTD
View PDF 1 Cites 0 Cited by

Patent Information

Application Number
JP2024064697
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Filing Date
2024-04-12
Publication Date
2025-10-24

AI Technical Summary

Technical Problem

Minoxidil compositions are prone to discoloration due to the presence of tocopherol and its derivatives, which were previously identified as accelerators of this discoloration, and existing solutions have not effectively addressed this issue.

Method used

A composition comprising minoxidil, tocopherol and its derivatives, mucopolysaccharides, and eucalyptus oil, with specific content ranges of each component, effectively inhibits discoloration by combining these components in a way that counteracts their individual discoloration-promoting effects.

Benefits of technology

The composition efficiently suppresses discoloration even when containing high amounts of minoxidil and tocopherol derivatives, maintaining stability and effectiveness.

✦ Generated by Eureka AI based on patent content.

Smart Images

  • Figure 2025161483000001
    Figure 2025161483000001
  • Figure 2025161483000002
    Figure 2025161483000002
  • Figure 2025161483000003
    Figure 2025161483000003
Patent Text Reader

Abstract

To provide a composition containing minoxidil.SOLUTION: A composition containing (A) minoxidil, (B) at least one selected from tocopherol and derivatives thereof, and (C) at least one selected from mucopolysaccharides and (D) eucalyptus oil.SELECTED DRAWING: None
Need to check novelty before this filing date? Find Prior Art

Description

[Technical Field]

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

[0002] Minoxidil (2,4-diamino-6-piperidinopyrimidine 3-oxide) is used for hair growth (hair restoration) and to treat alopecia.

[0003] In such applications, minoxidil is often combined with other ingredients (for example, solvents such as water and alcohol) to form a composition (for example, a liquid). In such compositions, discoloration may be observed, and attempts have been made to improve or suppress such discoloration.

[0004] For example, Patent Document 1 discloses a topical composition containing 2 wt% or more minoxidil, tocopherol and / or its derivatives, propylene glycol, 30 wt% or more lower alcohol, and an acid, and describes that this composition can inhibit the progression of discoloration over time by incorporating tocopherol and / or its derivatives into a minoxidil-containing topical composition. [Prior art documents] [Patent documents]

[0005] [Patent Document 1] Japanese Patent Application Publication No. 2018-48124 Summary of the Invention [Problem to be solved by the invention]

[0006] An object of the present invention is to provide a composition containing minoxidil (minoxidil-containing composition) and the like. [Means for solving the problem]

[0007] As mentioned above, minoxidil appears to be prone to discoloration (discoloration over time) due to (or in the presence of) tocopherol and its derivatives (such as tocopherol acetate).

[0008] In this context, the present inventor discovered that the discoloration of minoxidil can be accelerated (promoted) by specific components other than tocopherol and its derivatives, and that, quite unexpectedly, such discoloration can actually be inhibited by tocopherol and its derivatives, which were identified as components that accelerate discoloration in Patent Document 1. After further research, the present inventors have completed the present invention.

[0009] That is, the present invention relates to the following inventions. [1] A composition comprising (A) minoxidil, (B) at least one selected from tocopherol and its derivatives, and (C) a mucopolysaccharide. [2] A composition comprising (A) minoxidil, (B) at least one selected from tocopherol and its derivatives, and (D) eucalyptus oil. [3] A composition comprising (A) minoxidil, (B) at least one selected from tocopherol and its derivatives, (C) mucopolysaccharide, and (D) eucalyptus oil. [4] The composition according to any one of [1] to [3], wherein component (B) contains tocopherol acetate. [5] The composition according to [1], [3] or [4], wherein component (C) comprises at least one selected from hyaluronic acid, chondroitin sulfate, heparin, heparinoids, and salts thereof. [6] The composition according to any one of [1] to [5], wherein the content of component (A) is 1 w / v% or more, and the content of component (B) is 0.1 to 100 parts by mass per 100 parts by mass of component (A). [7] The composition according to any one of [1], [3] to [6], wherein the content of component (C) is 0.00001 to 0.2 w / v %. [8] The composition according to any one of [2] to [7], wherein the content of component (D) is 0.0001 to 1.5 w / v %. [9] The composition according to any one of [1] to [8], further comprising at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride.

[10] The composition according to any one of [1] to [9], further comprising panthenols, menthol, and pyridoxine hydrochloride.

[11] The composition according to any one of [1] to

[10] , further comprising at least one selected from panthenol and pantothenyl ethyl ether, menthol, and pyridoxine hydrochloride.

[12] Further, it contains at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride, When panthenol is contained, the content of panthenol is 1 to 300 parts by mass per 100 parts by mass of component (A), When menthol is contained, the content of menthol is 0.1 to 200 parts by mass per 100 parts by mass of component (A), The composition according to any one of [1] to

[11] , wherein when pyridoxine hydrochloride is contained, the content of pyridoxine hydrochloride is 0.05 to 100 parts by mass per 100 parts by mass of component (A).

[13] The composition according to any one of [1] to

[12] , further comprising 1,3-butylene glycol.

[14] It also contains water, ethanol, and polyhydric alcohol. The composition according to any one of [1] to

[13] , wherein the polyhydric alcohol contains 1,3-butylene glycol in an amount of 20% by mass or more based on the total amount of the polyhydric alcohol.

[15] The composition according to any one of [1] to

[14] , further comprising an acid (for example, at least one acid selected from citric acid, phosphoric acid, and tartaric acid).

[16] The composition according to any one of [1] to

[15] , which has a pH of 5 to 8.

[17] A composition contained in a container, comprising: The composition according to any one of [1] to

[16] , wherein at least a part of the container that comes into contact with the composition is made of polyester.

[18] A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by incorporating (blending, adding) at least one selected from (C) mucopolysaccharides and (D) eucalyptus oil into a composition containing (A) minoxidil and (B) at least one selected from tocopherol and its derivatives.

[19] A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by incorporating (blending, adding) at least one selected from (B) tocopherol and its derivatives into a composition containing (A) minoxidil and at least one selected from (C) mucopolysaccharides and (D) eucalyptus oil.

[20] The method according to

[18] or

[19] , wherein the content of component (A) in the composition is 1 w / v% or more. [twenty one] The method according to any one of

[18] to

[20] , wherein the composition further contains at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride. [twenty two] The method according to any one of

[18] to

[21] , wherein the composition further contains at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride. [Effects of the Invention]

[0010] The present invention provides a composition containing minoxidil (minoxidil-containing composition), which can suppress (ameliorate) discoloration even when it contains minoxidil (and also tocopherol, its derivatives, and specific components). DETAILED DESCRIPTION OF THE INVENTION

[0011] [Composition] The composition of the present invention contains (A) minoxidil and (B) at least one selected from tocopherol and its derivatives, and usually further contains specific components (component (C) and component (D)).

[0012] Minoxidil (including its salts) is a known compound, and may be obtained as a commercially available product, for example, from Tokyo Chemical Industry Co., Ltd. Examples of minoxidil salts include inorganic acid salts such as hydrochloride and sulfate, and organic acid salts such as acetate, citrate, succinate, benzoate, and lactate.

[0013] In the composition, the content (concentration, proportion) of minoxidil (component (A)) may be selected depending on the type of composition, the desired use and function (drug efficacy), etc., and may be selected, for example, from a range of about 0.1 w / v% or more, 0.5 w / v% or more, preferably 1 w / v% or more, more preferably 1.5 w / v% or more, even more preferably 2 w / v% or more, 2.5 w / v% or more, 3 w / v% or more, 3.5 w / v% or more, 4 w / v% or more, 4.5 w / v% or more, etc.

[0014] The upper limit of the minoxidil content in the composition is not limited, but may be selected from a range of, for example, approximately 20 w / v% or less, 15 w / v% or less, preferably 10 w / v% or less, more preferably 8 w / v% or less, and even more preferably 7 w / v% or less, or may be 6 w / v% or less, 5.8 w / v% or less, 5.5 w / v% or less, 5.2 w / v% or less, 5 w / v% or less, etc.

[0015] In addition, these ranges (upper and lower limits) may be appropriately combined to select a range (for example, 0.1 to 10 w / v%, 0.5 to 8 w / v%, 1 to 5 w / v%, etc.; the same applies to ranges hereinafter).

[0016] The specific content of minoxidil in the composition may be, for example, 0.1 to 20 w / v%, 0.2 to 15 w / v%, 0.3 to 12 w / v%, etc., preferably 0.5 to 10 w / v%, more preferably 1 to 5 w / v%, and even more preferably 2 to 5 w / v%.

[0017] It seems that the higher the minoxidil content, the more likely the composition is to become discolored, but in the present invention, discoloration can be efficiently suppressed even when the composition contains a large amount of minoxidil.

[0018] In component (B), examples of tocopherols include α-tocopherol, β-tocopherol, γ-tocopherol, δ-tocopherol, and mixtures thereof. Any of these can be used, but α-tocopherol (or tocopherol containing at least α-tocopherol) may be preferably used.

[0019] Examples of tocopherol derivatives include tocopherol esters [for example, tocopherol organic acid esters (for example, fatty acid esters) such as tocopherol acetate, tocopherol nicotinate, tocopherol succinate, and tocopherol linolenate].

[0020] The component (B) may be used alone or in combination of two or more types.

[0021] Representative examples of component (B) include tocopherol acetate (tocopherol acetate, vitamin E acetate). Therefore, component (B) may contain tocopherol acetate. Such component (B) may be composed solely of tocopherol acetate, as long as it contains tocopherol acetate.

[0022] In the composition, the content (concentration, proportion) of component (B) may be selected depending on the form of the composition, etc., and may be selected, for example, from a range of about 0.0001 w / v% or more, 0.001 w / v% or more, preferably 0.005 w / v% or more, more preferably 0.01 w / v% or more, 0.02 w / v% or more, 0.03 w / v% or more, 0.05 w / v% or more, 0.06 w / v% or more, 0.07 w / v% or more, 0.08 w / v% or more, etc.

[0023] In the composition, the upper limit of the content of component (B) may be selected from a range of, for example, about 10 w / v% or less, and may be 3 w / v% or less, preferably 1 w / v% or less, more preferably 0.5 w / v% or less, or may be 0.3 w / v% or less, 0.2 w / v% or less, 0.15 w / v% or less, 0.12 w / v% or less, 0.1 w / v% or less, 0.09 w / v% or less, 0.08 w / v% or less, etc.

[0024] In the composition, the specific content of the component (B) may be, for example, 0.001 to 2 w / v %, preferably 0.005 to 1 w / v %, and more preferably 0.01 to 0.5 w / v %.

[0025] In the composition, the content of component (B) may be, for example, 0.01 to 200 parts by mass, preferably 0.1 to 100 parts by mass, more preferably 1 to 50 parts by mass, and even more preferably 1.6 to 8 parts by mass, per 100 parts by mass of minoxidil (component (A)).

[0026] The composition may contain (C) mucopolysaccharide or (D) eucalyptus oil, or may contain a combination of these [(C) mucopolysaccharide and (D) eucalyptus oil]. By incorporating such component (C) or component (D) in the composition in combination with component (B), discoloration of the minoxidil-containing composition can be efficiently suppressed.

[0027] In particular, according to the investigations of the present inventors, although components (C) and (D) may be factors that cause discoloration (factors that accelerate discoloration) in compositions containing minoxidil, unexpectedly, by combining them with component (B) [component (B) that is also known to be a factor that causes discoloration (factors that accelerate discoloration)], discoloration in compositions containing minoxidil can be efficiently suppressed.

[0028] Examples of component (C) include hyaluronic acid, chondroitin sulfate, heparin, heparinoids, alginic acid, and salts thereof.

[0029] Examples of salts include salts with organic acids [e.g., monocarboxylates (acetate, trifluoroacetate, butyrate, palmitate, stearate, etc.), polycarboxylates (fumarate, maleate, etc.), oxycarboxylates (lactate, tartrate, citrate, succinate, malonate, etc.), organic sulfonates (methanesulfonate, toluenesulfonate, tosylate, etc.)], salts with inorganic acids (e.g., hydrochloride, sulfate, nitrate, hydrobromide, phosphate), salts with organic bases (e.g., salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, picoline, etc.), salts with inorganic bases [e.g., ammonium salts; salts with alkali metals (sodium, potassium, etc.), alkaline earth metals (calcium, magnesium, etc.), aluminum, etc.], and the like.

[0030] Specific salts include sodium hyaluronate, sodium chondroitin sulfate, and the like.

[0031] The component (C) may be used alone or in combination of two or more types.

[0032] Representative examples of component (C) include hyaluronic acid, chondroitin sulfate, heparin, heparin sulfate, heparan sulfate, heparinoids, heparinoids, and salts thereof [particularly, hyaluronic acid and salts of hyaluronic acid (sodium hyaluronate, etc.)].

[0033] Therefore, component (C) may contain at least one selected from hyaluronic acid, chondroitin sulfate, heparin, heparinoids, and salts thereof [particularly, at least one selected from hyaluronic acid and salts of hyaluronic acid (such as sodium hyaluronate)].

[0034] Such component (C) may contain at least one selected from hyaluronic acid, chondroitin sulfate, heparin, heparin-like substances, and salts thereof [particularly, at least one selected from hyaluronic acid and salts of hyaluronic acid (sodium hyaluronate, etc.)], or may consist solely of at least one selected from hyaluronic acid, chondroitin sulfate, heparin, heparin-like substances, and salts thereof [particularly, at least one selected from hyaluronic acid and salts of hyaluronic acid (sodium hyaluronate, etc.)].

[0035] The molecular weight (viscosity average molecular weight) of component (C) is not particularly limited, but may be, for example, 500,000 or more, preferably 800,000 or more, and more preferably 1,000,000 or more, and may be, for example, 3,000,000 or less, preferably 2,500,000 or less, and more preferably 2,000,000 or less. Specifically, the molecular weight (viscosity average molecular weight) of the component (C) may be, for example, 500,000 to 3,000,000, preferably 800,000 to 2,500,000, and more preferably 1,000,000 to 2,000,000. The molecular weight can be measured, for example, according to the Japanese Pharmacopoeia (General Test Methods), Viscosity Measurement Method 1 (Capillary Viscometer Method).

[0036] When the composition contains component (C), the content (concentration, proportion) of component (C) in the composition may be selected depending on the form of the composition, etc., and may be selected, for example, from a range of about 0.00001 w / v% or more, 0.00005 w / v% or more, preferably 0.0001 w / v% or more, and more preferably 0.0005 w / v% or more.

[0037] In the composition, the upper limit of the content of component (C) may be selected, for example, from a range of about 5 w / v% or less, and may be 2 w / v% or less, preferably 0.5 w / v% or less, more preferably about 0.1 w / v% or less, and even more preferably 0.03 w / v% or less.

[0038] In the composition, the specific content of component (C) may be, for example, 0.00001 to 0.2 w / v%, preferably 0.0001 to 0.1 w / v%, more preferably 0.0005 to 0.01 w / v%, and even more preferably 0.001 to 0.003 w / v%.

[0039] When the composition contains component (C), the content of component (C) in the composition may be, for example, 0.00001 to 20 parts by mass, preferably 0.0001 to 10 parts by mass, more preferably 0.001 to 1 part by mass, and even more preferably 0.04 to 0.2 parts by mass per 100 parts by mass of minoxidil (component (A)).

[0040] When the composition contains the component (C), the content of the component (C) in the composition may be, for example, 0.001 to 250 parts by mass, preferably 0.01 to 100 parts by mass, more preferably 0.1 to 10 parts by mass, and even more preferably 0.5 to 5 parts by mass, per 100 parts by mass of the component (B).

[0041] Component (D) may contain cineole (1,8-cineole). In such cases, the content of cineole (1,8-cineole) in component (D) may be preferably 99 w / v% or less (e.g., 50 to 99 w / v%), more preferably 95 w / v% or less (e.g., 60 to 95 w / v%), and even more preferably 90 w / v% or less (e.g., 70 to 90 w / v%).

[0042] When the composition contains component (D), the content (concentration, proportion) of component (D) in the composition may be selected depending on the form of the composition, etc., and may be selected, for example, from a range of about 0.0001 w / v% or more, 0.0005 w / v% or more, preferably 0.001 w / v% or more, more preferably 0.005 w / v% or more, 0.01 w / v% or more, 0.015 w / v% or more, 0.02 w / v% or more, etc.

[0043] In the composition, the upper limit of the content of component (D) may be selected, for example, from a range of about 20 w / v% or less, and may be 10 w / v% or less, preferably 5 w / v% or less, more preferably 1 w / v% or less, even more preferably 0.3 w / v% or less, or may be 0.2 w / v% or less, 0.1 w / v% or less, 0.05 w / v% or less, etc.

[0044] In the composition, the specific content of component (D) may be, for example, 0.0001 to 1.5 w / v%, preferably 0.001 to 0.5 w / v%, more preferably 0.005 to 0.1 w / v%, and even more preferably 0.01 to 0.03 w / v%.

[0045] When the composition contains component (D), the content of component (D) in the composition may be, for example, 0.0001 to 150 parts by mass, preferably 0.001 to 50 parts by mass, more preferably 0.01 to 10 parts by mass, and even more preferably 0.4 to 2 parts by mass, per 100 parts by mass of minoxidil (component (A)).

[0046] When the composition contains the component (D), the content of the component (D) in the composition may be, for example, 0.01 to 2000 parts by mass, preferably 0.1 to 1000 parts by mass, more preferably 1 to 100 parts by mass, and even more preferably 5 to 50 parts by mass, per 100 parts by mass of the component (B).

[0047] When the composition contains the (C) component and the (D) component, the content of the (C) component in the composition may be, for example, 0.01 to 1000 parts by mass, preferably 0.1 to 100 parts by mass, more preferably 0.3 to 50 parts by mass, and even more preferably 1 to 20 parts by mass, per 100 parts by mass of the (D) component.

[0048] The composition may contain at least one component (sometimes referred to as component (E)) selected from panthenols, menthol (such as l-menthol), and pyridoxine hydrochloride (pyridoxine hydrochloride).

[0049] By incorporating such component (E) in the composition in combination with component (B) (and further with component (C) and / or component (D)), discoloration of the minoxidil-containing composition can be efficiently suppressed.

[0050] In particular, according to the investigations of the present inventors, although such component (E) may be a cause of discoloration (a cause that accelerates discoloration) in compositions containing minoxidil, unexpectedly, by combining it with component (B) [component (B) which is also known to be a cause of discoloration (a cause that accelerates discoloration)], discoloration in compositions containing minoxidil can be efficiently suppressed.

[0051] Moreover, surprisingly, component (E) can be an even greater cause of discoloration in compositions containing minoxidil together with components (C) and (B). However, even in such cases, by combining these with component (B), discoloration in compositions containing minoxidil can be efficiently suppressed.

[0052] Examples of panthenols include panthenol, ethers of panthenol (monoalkyl ethers, etc.) such as pantothenyl ethyl ether, etc. Representative panthenols are panthenol and pantothenyl ethyl ether.

[0053] Component (E) may be used alone or in combination of two or more types.

[0054] When two or more kinds of component (E) are combined, the combination is not particularly limited, but it is preferable to combine at least two kinds selected from panthenols, menthol, and pyridoxine hydrochloride.

[0055] Examples of such combinations include a combination of panthenols (e.g., panthenol and / or panthonyl ethyl ether) and menthol, a combination of panthenols (e.g., panthenol and / or panthonyl ethyl ether) and pyridoxine hydrochloride, a combination of menthol and pyridoxine hydrochloride, and a combination of panthenols (e.g., panthenol and / or panthonyl ethyl ether), menthol, and pyridoxine hydrochloride.

[0056] When the composition contains panthenol, the content (concentration, proportion) of panthenol in the composition may be selected depending on the form of the composition, etc., and may be selected, for example, from a range of about 0.001 w / v% or more, 0.015 w / v% or more, preferably 0.03 w / v% or more, more preferably 0.15 w / v% or more, even more preferably 0.5 w / v% or more, or may be 0.6 w / v% or more, 0.8 w / v% or more, 1 w / v% or more, etc.

[0057] In the composition, the upper limit of the panthenol content may be selected, for example, from a range of about 40 w / v% or less, and may be 20 w / v% or less, preferably 10 w / v% or less, more preferably about 6 w / v% or less, and even more preferably 3 w / v% or less, 2 w / v% or less, 1.5 w / v% or less, 1.2 w / v% or less, etc.

[0058] The specific content of panthenols in the composition may be, for example, 0.01 to 5 w / v%, preferably 0.05 to 4 w / v%, more preferably 0.1 to 3 w / v%, and even more preferably 0.5 to 2 w / v%.

[0059] When the composition contains panthenol, the content of the panthenol in the composition may be, for example, 0.1 to 500 parts by mass, preferably 1 to 300 parts by mass, more preferably 10 to 200 parts by mass, and even more preferably 20 to 100 parts by mass per 100 parts by mass of minoxidil (component (A)).

[0060] When the composition contains panthenol, the content of the panthenol in the composition may be, for example, 1 to 10,000 parts by mass, preferably 50 to 5,000 parts by mass, more preferably 100 to 3,000 parts by mass, and even more preferably 1,000 to 2,000 parts by mass, per 100 parts by mass of component (B).

[0061] When the composition contains component (C) and a panthenol, the content of the panthenol in the composition may be, for example, 10 to 250,000 parts by mass, preferably 100 to 200,000 parts by mass, more preferably 1,000 to 150,000 parts by mass, and even more preferably 10,000 to 100,000 parts by mass per 100 parts by mass of component (C).

[0062] When the composition contains component (D) and panthenol, the content of panthenol in the composition may be, for example, 1 to 25,000 parts by mass, preferably 10 to 20,000 parts by mass, more preferably 100 to 15,000 parts by mass, and even more preferably 1,000 to 10,000 parts by mass, per 100 parts by mass of component (D).

[0063] When the composition contains menthol, the content (concentration, proportion) of menthol in the composition may be selected depending on the embodiment of the composition, etc., and may be selected, for example, from a range of about 0.001 w / v% or more, 0.005 w / v% or more, preferably 0.01 w / v% or more, more preferably 0.05 w / v% or more, even more preferably 0.08 w / v% or more, or may be 0.1 w / v% or more, 0.15 w / v% or more, 0.2 w / v% or more, 0.3 w / v% or more, etc.

[0064] In the composition, the upper limit of the menthol content may be selected from a range of, for example, about 30 w / v% or less, and may be 15 w / v% or less, preferably 10 w / v% or less, more preferably 5 w / v% or less, even more preferably 1.5 w / v% or less, or may be 1.2 w / v% or less, 1 w / v% or less, 0.8 w / v%, 0.5 w / v% or less, etc.

[0065] The specific menthol content in the composition may be, for example, 0.001 to 5 w / v%, preferably 0.01 to 2.5 w / v%, more preferably 0.05 to 1 w / v%, and even more preferably 0.1 to 0.5 w / v%.

[0066] When the composition contains menthol, the content of menthol in the composition may be, for example, 0.01 to 500 parts by mass, preferably 0.1 to 200 parts by mass, more preferably 1 to 100 parts by mass, and even more preferably 6 to 30 parts by mass, per 100 parts by mass of minoxidil (component (A)).

[0067] When the composition contains menthol, the content of menthol in the composition may be, for example, 0.1 to 10,000 parts by mass, preferably 1 to 5,000 parts by mass, more preferably 10 to 1,000 parts by mass, and even more preferably 100 to 500 parts by mass, relative to 100 parts by mass of the component (B).

[0068] When the composition contains the component (C) and menthol, the content of menthol in the composition may be, for example, 10 to 250,000 parts by mass, preferably 100 to 100,000 parts by mass, more preferably 1,000 to 50,000 parts by mass, and even more preferably 10,000 to 30,000 parts by mass, per 100 parts by mass of the component (C).

[0069] When the composition contains the component (D) and menthol, the content of menthol in the composition may be, for example, 1 to 25,000 parts by mass, preferably 10 to 10,000 parts by mass, more preferably 100 to 5,000 parts by mass, and even more preferably 1,000 to 3,000 parts by mass, per 100 parts by mass of the component (D).

[0070] When the composition contains pyridoxine hydrochloride, the content (concentration, proportion) of pyridoxine hydrochloride in the composition may be selected depending on the form of the composition, etc., and may be selected from a range of, for example, about 0.0001 w / v% or more, 0.0015 w / v% or more, preferably 0.003 w / v% or more, more preferably 0.01 w / v% or more, even more preferably about 0.015 w / v% or more, 0.02 w / v% or more, 0.025 w / v% or more, 0.02 w / v% or more, 0.03 w / v% or more, 0.05 w / v% or more, etc.

[0071] In the composition, the upper limit of the content of pyridoxine hydrochloride may be selected, for example, from a range of about 5 w / v% or less, and may be 2 w / v% or less, preferably 1 w / v% or less, more preferably 0.6 w / v% or less, even more preferably 0.2 w / v% or less, or may be 0.15 w / v% or less, 0.1 w / v% or less, 0.08 w / v% or less, etc.

[0072] The specific content of pyridoxine hydrochloride in the composition may be, for example, 0.0001 to 5 w / v%, preferably 0.003 to 1 w / v%, more preferably 0.01 to 0.5 w / v%, and even more preferably 0.01 to 0.1 w / v%.

[0073] When the composition contains pyridoxine hydrochloride, the content of pyridoxine hydrochloride in the composition may be, for example, 0.001 to 500 parts by mass, preferably 0.05 to 100 parts by mass, more preferably 0.1 to 50 parts by mass, and even more preferably 1 to 5 parts by mass, per 100 parts by mass of minoxidil (component (A)).

[0074] When the composition contains pyridoxine hydrochloride, the content of pyridoxine hydrochloride in the composition may be, for example, 0.01 to 10,000 parts by mass, preferably 0.1 to 3,000 parts by mass, more preferably 1 to 800 parts by mass, and even more preferably 50 to 100 parts by mass per 100 parts by mass of component (B).

[0075] When the composition contains component (C) and pyridoxine hydrochloride, the content of pyridoxine hydrochloride in the composition may be, for example, 1 to 250,000 parts by mass, preferably 10 to 100,000 parts by mass, more preferably 100 to 10,000 parts by mass, and even more preferably 1,000 to 5,000 parts by mass per 100 parts by mass of component (C).

[0076] When the composition contains component (D) and pyridoxine hydrochloride, the content of pyridoxine hydrochloride in the composition may be, for example, 0.1 to 25,000 parts by mass, preferably 1 to 10,000 parts by mass, more preferably 10 to 1,000 parts by mass, and even more preferably 100 to 500 parts by mass per 100 parts by mass of component (D).

[0077] The composition may contain a solvent.

[0078] Examples of the solvent include water, lower alcohols, polyhydric alcohols, and ethers (for example, glycol ethers such as ethylene glycol monomethyl ether, ethylene glycol monoethyl ether, ethylene glycol monopropyl ether, diethylene glycol monomethyl ether, diethylene glycol monoethyl ether, diethylene glycol monopropyl ether, diethylene glycol monobutyl ether, propylene glycol monoethyl ether, propylene glycol monopropyl ether, dipropylene glycol monoethyl ether, and dipropylene glycol monopropyl ether).

[0079] The solvents may be used alone or in combination of two or more.

[0080] The composition may preferably contain at least water, a lower alcohol, and a polyhydric alcohol, as this makes it easier to efficiently obtain the effects of the present invention when combined with the above-mentioned components, and to easily achieve a good balance with other desired performance requirements (e.g., feel during use, solubility of minoxidil or inhibition of precipitation).

[0081] Examples of lower alcohols (mono-ols) include alcohols (mono-ols) having 1 to 4 carbon atoms, such as methanol, ethanol, propanol, isopropyl alcohol, butanol, isobutyl alcohol, s-butyl alcohol, t-butyl alcohol, etc. Preferred lower alcohols include ethanol.

[0082] Therefore, the lower alcohol (composition) may contain at least ethanol (contain it as a lower alcohol).

[0083] In such cases, the content (ratio, concentration) of ethanol relative to the total amount of lower alcohols can be selected from a range of, for example, about 20% by mass or more (e.g., 30% by mass or more), and may be 40% by mass or more (e.g., 50% by mass or more, 60% by mass or more, 70% by mass or more, 80% by mass or more, 90% by mass or more, 100% by mass or more), etc.

[0084] Examples of polyhydric alcohols include propylene glycol, dipropylene glycol, 1,3-butylene glycol, polyethylene glycol (for example, Macrogol 300, Macrogol 400, Macrogol 600, etc.), and glycerin.

[0085] Among these polyhydric alcohols, propylene glycol, 1,3-butylene glycol, and glycerin are included, and 1,3-butylene glycol is particularly preferred, as they can more efficiently achieve the effects of the present invention when combined with the above-mentioned components.

[0086] Therefore, the polyhydric alcohol (composition) may contain (contain as a polyhydric alcohol) at least one selected from propylene glycol, 1,3-butylene glycol, and glycerin.

[0087] In such cases, propylene glycol, 1,3-butylene glycol, and glycerin may each be used alone as a polyhydric alcohol, or in combination (for example, propylene glycol and 1,3-butylene glycol, 1,3-butylene glycol and glycerin, propylene glycol, 1,3-butylene glycol, and glycerin, etc.).

[0088] Among these, the polyhydric alcohol (composition) preferably contains at least 1,3-butylene glycol, and more preferably the polyhydric alcohol (composition as polyhydric alcohol) contains only 1,3-butylene glycol.

[0089] In such cases, the content (ratio, concentration) of 1,3-butylene glycol relative to the total polyhydric alcohol can be selected, for example, from a range of about 5% by mass or more, and may be preferably 10% by mass or more, more preferably 20% by mass or more, and even more preferably 30% by mass or more, or may be 40% by mass or more, 50% by mass or more, 60% by mass or more, 70% by mass or more, 80% by mass or more, 90% by mass or more, 100% by mass, etc.

[0090] When 1,3-butylene glycol is combined with propylene glycol and / or glycerin, the content (ratio, concentration) of 1,3-butylene glycol relative to the total amount of 1,3-butylene glycol, propylene glycol and / or glycerin may be selected, for example, from the range of about 1 to 99% by mass, and may be 10 to 95% by mass, preferably 20 to 90% by mass, more preferably 30 to 85% by mass, and even more preferably 40 to 80% by mass.

[0091] When the polyhydric alcohol (composition) contains at least one selected from propylene glycol, 1,3-butylene glycol, and glycerin, the polyhydric alcohol (the composition as the polyhydric alcohol) may contain other polyhydric alcohols (polyhydric alcohols other than propylene glycol, 1,3-butylene glycol, and glycerin), but it is preferable that the composition does not contain other polyhydric alcohols or contains only a small amount of other polyhydric alcohols [for example, 30% by mass or less (for example, 20% by mass or less, 10% by mass or less, 5% by mass or less) of the total polyhydric alcohols].

[0092] When the composition contains water, the water content (proportion, concentration) in the composition may be, for example, 1 w / v% or more, preferably 5 w / v% or more, more preferably 10 w / v% or more, even more preferably 15 w / v% or more, or may be 18 w / v% or more, 20 w / v% or more, etc.

[0093] In the composition, the upper limit of the water content may be selected, for example, from a range of about 80 w / v% or less, and may be 60 w / v% or less, preferably 50 w / v% or less, more preferably 40 w / v% or less, even more preferably 30 w / v% or less, or may be 25 w / v% or less, 22 w / v% or less, etc.

[0094] The specific water content in the composition may be, for example, 1 to 60 w / v%, preferably 3 to 50 w / v%, more preferably 5 to 40 w / v%, and even more preferably 10 to 30 w / v%.

[0095] When the composition contains a lower alcohol (particularly, ethanol), the content (proportion, concentration) of the lower alcohol in the composition may be, for example, 3 w / v% or more, preferably 10 w / v% or more, more preferably 15 w / v% or more, even more preferably 20 w / v% or more, or may be 25 w / v% or more, 30 w / v% or more, 35 w / v% or more, 40 w / v% or more, etc.

[0096] In the composition, the upper limit of the content of lower alcohols (particularly ethanol) may be selected from a range of, for example, about 90 w / v% or less, and may be 80 w / v% or less, preferably 70 w / v% or less, more preferably 60 w / v% or less, even more preferably 55 w / v% or less, or may be 50 w / v% or less, 45 w / v% or less, etc.

[0097] The specific content of the lower alcohol in the composition may be, for example, 10 to 80 w / v%, preferably 20 to 70 w / v%, more preferably 30 to 65 w / v%, and even more preferably 40 to 55 w / v%.

[0098] When the composition contains a polyhydric alcohol, the content (proportion, concentration) of the polyhydric alcohol in the composition may be, for example, 0.1 w / v% or more, preferably 2 w / v% or more, more preferably 5 w / v% or more, even more preferably 10 w / v% or more, or may be 12 w / v% or more, 15 w / v% or more, etc.

[0099] In the composition, the upper limit of the polyhydric alcohol content may be selected, for example, from a range of approximately 60 w / v% or less, and may be 50 w / v% or less, preferably 40 w / v% or less, more preferably 35 w / v% or less, even more preferably 30 w / v% or less, or may be 25 w / v% or less, 20 w / v% or less, etc.

[0100] The specific content of the polyhydric alcohol in the composition may be, for example, 0.1 to 60 w / v%, preferably 1 to 40 w / v%, more preferably 3 to 35 w / v%, and even more preferably 5 to 30 w / v%.

[0101] When the composition contains a polyhydric alcohol (or at least one selected from propylene glycol, 1,3-butylene glycol, and glycerin), the content of the polyhydric alcohol (or at least one selected from propylene glycol, 1,3-butylene glycol, and glycerin) may be, for example, 0.01 to 100 parts by mass, preferably 0.1 to 50 parts by mass, more preferably 1 to 30 parts by mass, and even more preferably 3 to 15 parts by mass per part by mass of minoxidil (component (A)).

[0102] The composition may contain an acid. The acid may be used for purposes such as adjusting the pH and efficiently achieving desired performance requirements (e.g., solubility or inhibition of precipitation of minoxidil). Meanwhile, according to the studies of the present inventors, compositions containing minoxidil may be prone to discoloration depending on the type of acid or the type of acid used. However, the present invention can efficiently inhibit discoloration even when such an acid is used.

[0103] The acid may be either an inorganic acid or an organic acid, and examples thereof include citric acid, phosphoric acid, lactic acid, hydrochloric acid, acetic acid, sulfuric acid, nitric acid, tartaric acid, maleic acid, malic acid, gluconic acid, etc. Preferred acids include citric acid, phosphoric acid, tartaric acid, etc. These acids may form hydrates, etc.

[0104] The acids may be used alone or in combination of two or more.

[0105] The composition may contain other components (components other than those mentioned above) as needed, provided that the effects of the present invention are not impaired.

[0106] Examples of such ingredients include hair growth ingredients, vasodilators, blood circulation promoting ingredients, angiogenesis promoting factors, moisturizing ingredients, anti-inflammatory ingredients, antibacterial ingredients, vitamins, peptides or derivatives thereof, amino acids or derivatives thereof, cell activating ingredients, anti-aging ingredients, keratin softening or keratin dissolving ingredients, whitening ingredients, astringent ingredients, vasodilating ingredients, antihistamine ingredients, antioxidant ingredients, metabolic activators, refreshing agents, excipients, solubilizers, animal and vegetable oils, gelling agents, adhesives, fragrances, antioxidants, surfactants, thickeners, preservatives, pH adjusters, stabilizers, irritation reducers, antiseptics, colorants, fragrances, solubilizers, etc.

[0107] Specific examples of other ingredients include spiranolactone, 6-benzylaminopurine, Swertia japonica extract, adenosine, capsaicinoid, pentadecanoic acid glyceride, keratinocyte growth factor (KGF; FGF-7), diphenhydramine or a salt thereof (diphenhydramine hydrochloride, etc.), isothipendyl hydrochloride, guaiazulene, urea, salicylic acid or a salt thereof, chlorhexidine gluconate, isopropylmethylphenol, piroctone olamine, hinokitiol, glycyrrhizinate, glycyrrhetinic acid, ginseng extract (Panax ginseng Extract, etc.), carpronium chloride, benzyl nicotinate, Swertia japonica extract, Panax ginseng tincture, Capsicum tincture, retinol acetate, ascorbic acid, thiamine nitrate, cyanocobalamin, biotin, dibutylhydroxytoluene, sodium metabisulfite, sodium edetate, ascorbic acid, isopropyl gallate, diisopropyl adipate, isopropyl myristate, triethanolamine, diisopropanolamine, triisopropanolamine, potassium hydroxide, sodium hydroxide, etc.

[0108] The other components may be used alone or in combination of two or more.

[0109] The form of the composition is not particularly limited, and examples thereof include a liquid, suspension, emulsion, cream, gel, liniment, lotion, aerosol, ointment, etc. Among these, a liquid, suspension, emulsion, lotion, or aerosol is preferred, and a liquid, lotion, or aerosol is more preferred.

[0110] When the composition contains an oily base and an aqueous base (for example, a cream, emulsion, ointment, aerosol, etc.), it may be either a W / O type or an O / W type, but an O / W type is preferred in terms of its pleasant feel when used.

[0111] The composition can be produced, for example, by mixing the components in accordance with or in accordance with the General Provisions of the Japanese Pharmacopoeia. The composition can also be incorporated into cosmetic compositions such as lotions, creams, skin lotions, emulsions, foams, shampoos, rinses, conditioners, hair tonics, hair creams, and hair liquids.

[0112] The pH of the composition (for example, pH at 15 to 35°C, 15 to 25°C, or 20°C) may be selected from a range of 4 or higher, and may be preferably 5 or higher, more preferably 5.5 or higher, even more preferably 5.8 or higher, or may be 5.9 or higher, 6 or higher, etc. The pH of the composition may be selected from a range of 9 or lower, and may be preferably 8 or lower, more preferably 7.5 or lower, even more preferably 7 or lower, or may be less than 7, 6.9 or lower, 6.8 or lower, 6.7 or lower, 6.6 or lower, 6.5 or lower, etc.

[0113] Specific examples of the pH of the composition include 5 to 8, preferably 5.3 to 7.8, more preferably 5.5 to 7.5, and even more preferably 6 to 7.

[0114] At this pH, minoxidil can be dissolved efficiently (and scalp irritation can be avoided). Meanwhile, according to the inventors' investigations, compositions containing minoxidil may be prone to discoloration at the above pH, but the present invention can efficiently inhibit discoloration even at this pH.

[0115] The container into which the composition is filled is not particularly limited, and a container of a shape and material appropriately selected depending on the purpose of use, the form of the composition, etc. can be used.

[0116] The material of the container (main body, cap, discharge member, inner plug, sealing member, etc.) may be selected appropriately depending on the type of the composition, etc.

[0117] Examples of such materials include resins or polymers (e.g., polyethylene, polypropylene, polyester, polystyrene, polyvinyl chloride, ABS resin, ethylene-vinyl alcohol resin, acrylonitrile-styrene resin, epoxy resin, polyamide-imide resin, etc.), metals (aluminum, etc.), glass, etc. A laminate using these materials (resins, etc.) may also be used as the material for the container. Among these, it is preferable to use a resin containing polyester as the main component as the material for the container. Here, the main component refers to the material that is contained in the largest amount among the materials for the container, and the content may be preferably 50 to 100 mass %, more preferably 80 to 100 mass %.

[0118] Examples of polyesters include polyethylene terephthalate (PET), polybutylene terephthalate (PBT), polyethylene naphthalate (PEN), polybutylene naphthalate (PBN), etc. A preferred polyester is polyethylene terephthalate (PET).

[0119] Furthermore, at least a portion of the container that comes into contact with the composition may be made of a polyester such as polyethylene terephthalate. By storing the composition in a container in this manner, the effects of the present invention can be efficiently achieved (in particular, the solubility or inhibition of precipitation of minoxidil and the inhibition of discoloration can be efficiently achieved or in a well-balanced manner). In such a case, it is particularly preferable that the entire portion of the container that comes into contact with the composition is (substantially) made of a polyester such as polyethylene terephthalate.

[0120] The container containing the composition is composed of a main body, a cap, a discharge member, an inner plug, a sealing member, etc., and it is preferable that at least the portion of each of these components that comes into contact with the composition is made of polyester. Specifically, for example, if the container main body has a laminated structure, it is preferable that the innermost layer that comes into contact with the topical composition is made of polyester. It is more preferable that all of the components that come into contact with the topical composition among the multiple components that make up the container are made of polyester, and it is even more preferable that all of the components that make up the container are made of polyester.

[0121] Although the container may vary depending on its material, it is preferably an injection blow-molded container (a container molded by injection blow molding). By storing the composition in a container in this manner, the effects of the present invention can be efficiently achieved (in particular, the solubility or suppression of precipitation of minoxidil and the suppression of discoloration can be efficiently achieved or in a well-balanced manner).

[0122] The container may be a multi-dose type that can be used multiple times (for example, 30 to 360 times, preferably 60 to 240 times), or a unit-dose type that can be used up in a single use.

[0123] The method of using the composition varies depending on the condition of the hair, scalp, age, sex, etc. of the user, but may be, for example, as follows. That is, an appropriate amount (e.g., 0.5 to 2 g or 0.5 to 2 mL) may be applied to the skin (e.g., scalp) several times a day (e.g., 1 to 5 times, preferably 1 to 3 times). The topical composition may be applied to the skin (e.g., scalp) so that the daily dose of minoxidil is, for example, 1 to 1000 mg. The application method may be painting or spraying, depending on the dosage form. The application period may be, for example, 7 days or more, until a sufficient hair growth effect is obtained, for example, within 6 months, but at least within 4 months.

[0124] The composition may generally be a topical composition. Such a composition (external composition) may be suitably used, typically for hair growth (a composition for hair growth). Hair growth may mean a composition having one or more of the following effects: hair growth, hair growth promotion, hair care, and hair loss prevention.

[0125] [method] The composition of the present invention contains (combines) component (A) (minoxidil), component (B) (at least one selected from tocopherol and its derivatives), and a specific component (e.g., component (C), component (D), or even component (E)), thereby making it possible to suppress (block or prevent) discoloration (progression of discoloration).

[0126] Therefore, the present invention also includes, for example, the following inventions corresponding to the embodiments of such compositions. Note that in the following inventions, the order of blending (the order of inclusion) of each component is not particularly limited.

[0127] Method (a): A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by incorporating (blending, adding) at least one selected from component (C) and component (D) into a composition containing component (A) and component (B).

[0128] In this method (i), the composition may contain component (E), or may contain component (E) together with at least one selected from component (C) and component (D).

[0129] In the method (i), the composition may contain components other than the components (A) to (E) [for example, water, lower alcohols (such as ethanol), polyhydric alcohols, acids, other components, etc.].

[0130] In the method (a), the types, proportions, amounts of the various components, and the like, including preferred embodiments, are the same as those of the above-mentioned composition.

[0131] Specifically, method (A) includes the following methods:

[0132] (i-1) A method of suppressing (blocking, preventing) coloration (progression of coloration) in a composition comprising component (A) and component (B) by adding component (C).

[0133] (A-2) A method of suppressing (blocking, preventing) coloration (progression of coloration) in a composition comprising component (A) and component (B) by adding component (D).

[0134] (i-3) A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by adding component (C) and component (D) to a composition containing component (A) and component (B).

[0135] (i-4) A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (B), and (E) by adding component (C).

[0136] (i-5) A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (B), and (E) by adding component (D).

[0137] (i-6) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (B), and (E), by adding components (C) and (D).

[0138] (i-7) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising component (A) and component (B) by adding component (C) and component (E).

[0139] (i-8) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising component (A) and component (B) by adding component (D) and component (E).

[0140] (i-9) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by adding components (C), (D), and (E) to a composition containing components (A) and (B).

[0141] Method (ii): A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by incorporating (blending, adding) component (B) into a composition containing component (A) and at least one selected from component (C) and component (D).

[0142] In this method (ii), the composition may contain component (E), or component (E) may be contained together with component (B).

[0143] In the method (ii), the composition may contain components other than the components (A) to (E) [for example, water, lower alcohols (such as ethanol), polyhydric alcohols, acids, other components, etc.].

[0144] In the method (ii), the types, proportions, amounts of the various components, and the like, including preferred embodiments, are the same as those of the above-mentioned composition.

[0145] Specifically, method (b) includes the following methods:

[0146] (ii) A method of suppressing (blocking or preventing) coloration (progression of coloration) in a composition comprising component (A) and component (C) by adding component (B).

[0147] (ii) A method of suppressing (blocking or preventing) coloration (progression of coloration) in a composition comprising component (A) and component (D) by adding component (B).

[0148] (Ro-3) A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (C), and (D) by adding component (B).

[0149] (Ro-4) A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (C), and (E) by adding component (B).

[0150] (Ro-5) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (D), and (E) by adding component (B).

[0151] (Ro-6) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (C), (D), and (E) by adding component (B).

[0152] (Ro-7) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by adding component (B) and component (E) to a composition containing component (A) and component (C).

[0153] (Ro-8) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by adding component (B) and component (E) to a composition containing component (A) and component (D).

[0154] (Ro-9) A method for suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition comprising components (A), (C), and (D), by adding components (B) and (E). [Example]

[0155] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0156] [Test Example 1] Compositions shown in the table below were prepared according to conventional methods. The composition was filled into 30 mL containers at 26.5 mL each, sealed, and left to stand in an incubator at 65°C for 19 days.

[0157] The absorbance (420 nm) of the composition after standing was measured, and the ratio (A2 / A1, the ratio when absorbance A1 is set to 1) of the absorbance A2 of the composition containing each component (i.e., composition 2 in the table) to the absorbance A1 of the composition not containing each component (control composition, i.e., composition 1 in the table) was calculated.

[0158] The absorbance was measured as follows. The absorbance of purified water was used as the blank value, and the absorbance of the target formulation was measured using a spectrophotometer (AS ONE ASV11D-H) in a 10 mm glass cell at a wavelength of 420 nm.

[0159] The results are shown in the table. In the table, the units of each component in the composition are "w / v%" (or "g / 100mL"), and the "remaining amount" of absolute ethanol indicates the proportion that, when combined with other components, amounts to 100w / v%. The sodium hyaluronate used had a molecular weight (viscosity average molecular weight) of approximately 1 to 2 million.

[0160] [Table 1]

[0161] When the control composition 1 was visually observed, it was found to be transparent but yellow in color. On the other hand, as described below, when a composition (composition 7) which was the same as composition 1 but did not contain sodium hyaluronate was visually observed, it was transparent but only slightly yellow in color.

[0162] As is clear from the above results, when sodium hyaluronate was added to a composition containing minoxidil, coloring progressed (composition 1 vs. composition 7), but surprisingly, when tocopherol acetate was added in combination, the absorbance decreased (composition 1 vs. composition 2).

[0163] [Test Example 2] In the same manner as in Test Example 1, the compositions shown in the table below (Compositions 3 to 6) were prepared, the absorbance (420 nm) of each composition was measured, and the absorbance ratio was calculated.

[0164] Therefore, in this test example, the absorbance of composition 3 was designated as A1, and the absorbances of the other compositions (compositions 4 to 6) were designated as A2.

[0165] [Table 2]

[0166] When the control composition 3 was visually observed, it was found to be transparent but yellowish in color, whereas when the composition 3 (composition 7) which did not contain eucalyptus oil was visually observed as described below, it was found to be transparent but only slightly yellowish in color.

[0167] As is clear from the above results, when eucalyptus oil was added to a composition containing minoxidil, coloring progressed (comparison between composition 3 and composition 7), and when sodium hyaluronate was further added, the absorbance increased (comparison between composition 3 and composition 4). However, surprisingly, when tocopherol acetate was added in combination, the absorbance decreased (comparison between composition 3 and composition 5, comparison between composition 4 and composition 6).

[0168] In particular, it was extremely surprising to find that, although the combination of eucalyptus oil and sodium hyaluronate significantly increased absorbance (comparison between Composition 3 and Composition 4), the addition of tocopherol acetate suppressed the increase in absorbance to a level equal to or greater than that achieved when eucalyptus oil was used alone (comparison between Composition 5 and Composition 6).

[0169] [Test Example 3] In the same manner as in Test Example 1, the compositions shown in the table below (Compositions 7 to 10) were prepared, and the absorbance (420 nm) A2 of each composition was measured. The ratio (A2 / A1, the ratio when the absorbance A1 is set to 1) to the absorbance A1 of the target composition (i.e., composition 7 in the table) was calculated. When the control composition 7 was visually observed, it was found to be transparent but only slightly yellow in color.

[0170] [Table 3]

[0171] As is clear from the above results, the absorbance increased with the incorporation of pantothenyl ethyl ether, menthol, and pyridoxine hydrochloride (comparison between Composition 7 and Composition 8), and the absorbance increased further with the incorporation of sodium hyaluronate and eucalyptus oil (comparison between Composition 8 and Composition 9). However, surprisingly, the absorbance decreased with the incorporation of tocopherol acetate (comparison between Composition 9 and Composition 10).

[0172] In particular, although the absorbance increases significantly when pantothenyl ethyl ether, menthol, and pyridoxine hydrochloride, or a combination of these with eucalyptus oil and sodium hyaluronate, is blended (comparison between Composition 7 and Compositions 8 and 9), the addition of tocopherol acetate significantly reduces the absorbance compared to when pantothenyl ethyl ether, menthol, and pyridoxine hydrochloride, or a combination of these with eucalyptus oil and sodium hyaluronate, is not blended (comparison between Composition 7 and Composition 10), which was extremely surprising.

[0173] [Experimental Example] The compositions shown in the table below were prepared in the same manner as above. Note that the compositions of Experimental Examples 1 and 5 were stored in metal aerosol containers. In each composition, the pH was 6.0 to 7.0, and the unit of the proportion (concentration) of each component was g / 100 mL. The coloring (absorbance) of the composition showed the same tendency as above.

[0174] [Table 4]

[0175] [Table 5]

[0176] [Table 6] [Industrial Applicability]

[0177] The composition of the present invention can be used as a composition for hair growth or hair development (such as a composition for external use).

Claims

1. A composition comprising (A) minoxidil, (B) at least one member selected from tocopherol and its derivatives, and (C) a mucopolysaccharide.

2. A composition comprising (A) minoxidil, (B) at least one selected from tocopherol and its derivatives, and (D) eucalyptus oil.

3. A composition comprising (A) minoxidil, (B) at least one selected from tocopherol and its derivatives, (C) mucopolysaccharide, and (D) eucalyptus oil.

4. The composition of any one of claims 1 to 3, wherein component (B) comprises tocopherol acetate.

5. 4. The composition according to claim 1, wherein component (C) comprises at least one selected from the group consisting of hyaluronic acid, chondroitin sulfate, heparin, heparinoids, and salts thereof.

6. The composition according to any one of claims 1 to 3, wherein the content of component (A) is 1 w / v % or more, and the content of component (B) is 0.1 to 100 parts by mass per 100 parts by mass of component (A).

7. The composition according to claim 1 or 3, wherein the content of component (C) is 0.00001 to 0.2 w / v %.

8. The composition according to claim 2 or 3, wherein the content of component (D) is 0.0001 to 1.5 w / v %.

9. The composition according to any one of claims 1 to 3, further comprising at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride.

10. The composition according to any one of claims 1 to 3, further comprising panthenols, menthol, and pyridoxine hydrochloride.

11. The composition according to any one of claims 1 to 3, further comprising at least one selected from panthenol and pantothenyl ethyl ether, menthol, and pyridoxine hydrochloride.

12. Further, it contains at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride, When panthenol is contained, the content of panthenol is 1 to 300 parts by mass per 100 parts by mass of component (A), When menthol is contained, the content of menthol is 0.1 to 200 parts by mass per 100 parts by mass of component (A), 4. The composition according to claim 1, wherein when pyridoxine hydrochloride is contained, the content of pyridoxine hydrochloride is 0.05 to 100 parts by mass per 100 parts by mass of component (A).

13. The composition according to any one of claims 1 to 3, further comprising 1,3-butylene glycol.

14. It also contains water, ethanol, and polyhydric alcohol. The composition according to any one of claims 1 to 3, wherein the polyhydric alcohol contains 1,3-butylene glycol in an amount of 20 mass% or more based on the total amount of the polyhydric alcohol.

15. The composition according to any one of claims 1 to 3, further comprising at least one acid selected from citric acid, phosphoric acid, and tartaric acid.

16. The composition according to any one of claims 1 to 3, having a pH of 5 to 8.

17. A composition contained in a container, comprising:

4. The composition according to claim 1, wherein at least a part of the container that comes into contact with the composition is made of polyester.

18. A method for suppressing discoloration in a composition comprising (A) minoxidil and (B) at least one selected from tocopherol and its derivatives, by adding at least one selected from (C) mucopolysaccharides and (D) eucalyptus oil.

19. A method for suppressing discoloration in a composition by adding (B) at least one selected from tocopherol and its derivatives to a composition containing (A) minoxidil and at least one selected from (C) mucopolysaccharides and (D) eucalyptus oil.

20. The method according to claim 18 or 19, wherein the content of component (A) in the composition is 1 w / v % or more.

21. 20. The method of claim 18 or 19, wherein the composition further comprises at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride.

22. 20. The method according to claim 18 or 19, wherein the composition further comprises at least one component (E) selected from panthenols, menthol, and pyridoxine hydrochloride.

Citation Information

Patent Citations

  • Composition for external use

    JP2018048124A