Minoxidil-containing composition

Abstract

Compositions containing minoxidil are provided. The composition contains (A) minoxidil and (B) a polycyclic terpene.

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] According to Patent Document 1, compositions containing minoxidil discolor (over time) even when they further contain tocopherol or its derivatives (such as tocopherol acetate), which are known to have antioxidant properties, and such discoloration can be suppressed by selecting propylene glycol, a specific polyhydric alcohol (specifically, by using only propylene glycol).

[0008] In this situation, the inventors investigated various methods other than the selection of polyhydric alcohols and unexpectedly discovered that discoloration could be suppressed by a specific terpene (terpenes), which is a component completely different from polyhydric alcohols. After further research, they completed the present invention.

[0009] That is, the present invention relates to the following inventions. [1] A composition containing (A) minoxidil and (B) a polycyclic terpene (terpenes). [2] A composition comprising (A) minoxidil, (B) a polycyclic terpene, and (C) at least one member selected from tocopherol and its derivatives. [3] The composition according to [1] or [2], wherein component (B) comprises a bicyclic monoterpene. [4] The composition according to any one of [1] to [3], wherein the component (B) includes at least one selected from cineol, camphor, borneol, isoborneol, and pinene. [5] The composition according to any one of [1] to [4], wherein the component (B) contains cineole. [6] The composition according to any one of [2] to [5], wherein the component (C) contains tocopherol acetate. [7] The composition according to any one of [1] to [6], wherein the content of component (A) is 1 w / v % or more. [8] The composition according to any one of [1] to [7], wherein the content of component (B) is 0.0001 w / v % or more. [9] The composition according to any one of [1] to [8], wherein the content of component (B) is 0.0001 to 150 parts by mass per 100 parts by mass of component (A).

[10] The composition according to any one of [2] to [9], wherein the content of component (C) is 0.001 to 2 w / v %.

[11] The composition according to any one of [2] to

[10] , wherein the content of component (C) is 0.1 to 100 parts by mass per 100 parts by mass of component (A).

[12] The composition according to any one of [2] to

[11] , wherein the content of component (C) is 10 to 100,000 parts by mass per 100 parts by mass of component (B).

[13] A composition comprising (A) minoxidil and (B) a polycyclic terpene, component (B) comprises a bicyclic monoterpene; The content of component (A) is 1 w / v% or more, The content of component (B) is 0.001 w / v% or more, A composition in which the content of component (B) is 0.001 to 50 parts by mass per 100 parts by mass of component (A).

[14] A composition comprising (A) minoxidil, (B) a polycyclic terpene, and (C) at least one selected from tocopherol and derivatives thereof, component (B) comprises a bicyclic monoterpene; The content of component (A) is 1 w / v% or more, The content of component (B) is 0.001 w / v% or more, The content of component (C) is 0.005 to 1 w / v%, The content of component (B) is 0.001 to 50 parts by mass per 100 parts by mass of component (A), A composition in which the content of component (C) is 100 to 10,000 parts by mass per 100 parts by mass of component (B).

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

[14] , further comprising at least one component (D) selected from panthenols, menthol, and pyridoxine hydrochloride.

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

[15] , further comprising panthenols, menthol, and pyridoxine hydrochloride.

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

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

[18] Further, it contains at least one component (D) 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

[17] , 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).

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

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

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

[19] , 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. [twenty one] The composition according to any one of [1] to

[20] , further comprising a polyhydric alcohol, wherein the polyhydric alcohol does not contain propylene glycol or contains propylene glycol in an amount of 30 mass % or less relative to the total amount of the polyhydric alcohol. [twenty two] The composition according to any one of [1] to

[21] , further comprising an acid [for example, at least one acid selected from citric acid, phosphoric acid, tartaric acid, lactic acid, and gluconic acid (particularly, citric acid, phosphoric acid, and tartaric acid)]. [twenty three] The composition according to any one of [1] to

[22] , which has a pH of 5 to 8. [twenty four] A composition contained in a container, comprising: The composition according to any one of [1] to

[23] , wherein at least a part of the container that comes into contact with the composition is made of polyester. [twenty five] A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition by incorporating (blending, adding) (B) a polycyclic terpene into (A) a composition containing minoxidil.

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

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

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

[29] The method according to any one of

[25] to

[28] , wherein the content of component (A) in the composition is 1 w / v % or more.

[30] The method according to any one of

[25] to

[29] , wherein the composition further contains 1,3-butylene glycol and an acid. [Effects of the Invention]

[0010] According to the present invention, it is possible to provide a composition containing minoxidil (minoxidil-containing composition), etc. Even though such a composition contains minoxidil, discoloration can be suppressed (improved).

[0011] Such suppression of discoloration can also be achieved in compositions containing tocopherol or its derivatives (such as tocopherol acetate), and in particular, by combining a specific terpene with tocopherol or its derivatives, discoloration can be further suppressed.

[0012] As mentioned above, tocopherol and its derivatives (such as tocopherol acetate) are known to be components that promote discoloration, so it is surprising that discoloration can be suppressed (especially without the need for propylene glycol), and the effect of further suppressing discoloration by combining it with a specific terpene is even more surprising.

[0013] Furthermore, such suppression of coloration can be achieved without selecting only propylene glycol as the polyhydric alcohol. DETAILED DESCRIPTION OF THE INVENTION

[0014] [Composition] The composition of the present invention contains (A) minoxidil and (B) a polycyclic terpene.

[0015] 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.

[0016] In the composition, the content (concentration, proportion) of minoxidil (component (A), 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.

[0017] 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.

[0018] 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).

[0019] 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%.

[0020] 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.

[0021] Component (B) is a polycyclic terpene (terpenes). Component (B) may be polycyclic, for example, bicyclic to tetracyclic, preferably bicyclic.

[0022] In component (B), examples of the terpene include monoterpenes and terpenes having three or more isoprene structural units (for example, diterpenes, sesquiterpenes, diterpenes, sesterterpenes, triterpenes, and tetraterpenes), and preferably monoterpenes.

[0023] Component (B) (or terpene) may be a terpenoid (or a derivative). Such a terpenoid may have, for example, a hydroxyl group, a carbonyl (ketone) group, an ether group (an ether skeleton), an acid group (e.g., a carboxyl group, a sulfo group), or the like.

[0024] A preferred component (B) is a bicyclic monoterpene. Therefore, component (B) may contain at least a bicyclic monoterpene.

[0025] Specific examples of component (B) include bicyclic monoterpenes such as cineole (1,8-cineole, eucalyptol, limonene oxide), camphor, borneol, isoborneol, and pinene (α-pinene, β-pinene, etc.).

[0026] Component (B) may be used alone or in combination of two or more types.

[0027] Component (B) may be included in the composition as component (B) itself, or may be included in the composition as a mixture containing component (B) [e.g., an extract (essential oil, etc.)] (in the form of a mixture). The mixture [for example, an extract (essential oil, etc.)] can be selected depending on the type of component (B), and examples include mixtures [for example, extracts (essential oil, etc.)] derived from plants (herbs, etc.) such as thyme, cajeput, laurel, ravinsara, sage, basil, peppermint, rosemary, lavender, marjoram, niaouli, cardamom, myrtle, alpinia zerumbet, angelica root, lavandin, lemon verbena, and tea tree. Component (B) may or may not be contained as eucalyptus oil (the composition may or may not contain eucalyptus oil).

[0028] 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, 0.0005 w / v% or more, preferably 0.001 w / v% or more, more preferably 0.005 w / v% or more, or may be 0.01 w / v% or more, 0.015 w / v% or more, 0.02 w / v% or more, etc.

[0029] In the composition, the upper limit of the content of component (B) 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.

[0030] In the composition, the specific content of component (B) 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%.

[0031] In the composition, the content of component (B) 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)).

[0032] The composition of the present invention may contain (C) at least one selected from tocopherol and derivatives thereof.

[0033] By incorporating component (C) in combination with component (B) into the composition, coloration of the composition can be efficiently (for example, more effectively) suppressed.

[0034] In particular, as noted in Patent Document 1, component (C) may be a cause of discoloration (a cause of the progression of discoloration) in compositions containing minoxidil. However, unexpectedly, when combined with component (B), discoloration in compositions containing minoxidil can be efficiently suppressed.

[0035] In component (C), 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.

[0036] 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].

[0037] Component (C) may be used alone or in combination of two or more types.

[0038] A typical example of component (C) is tocopherol acetate (tocopherol acetate, vitamin E acetate). Therefore, component (B) may contain tocopherol acetate. Component (C) may be composed solely of tocopherol acetate, provided that it contains tocopherol acetate.

[0039] When the composition contains component (C), the content (concentration, proportion) of component (C) 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 0.0001 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.

[0040] In the composition, the upper limit of the content of component (C) 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.

[0041] In the composition, the specific content of component (C) 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 %.

[0042] When the composition contains component (C), the content of component (C) in the composition may be, for example, 0.01 to 200 parts by mass, preferably 0.1 to 100 parts by mass, more preferably 0.5 to 50 parts by mass, and even more preferably about 1 to 20 parts by mass, or may be 1.2 to 15 parts by mass, 1.5 to 10 parts by mass, 1.6 to 8 parts by mass, etc., per 100 parts by mass of minoxidil (component (A)).

[0043] When the composition contains component (C), the content of component (C) in the composition may be, for example, 5 to 1,000,000 parts by mass, preferably 10 to 100,000 parts by mass, more preferably 100 to 10,000 parts by mass, and even more preferably 200 to 2,000 parts by mass, per 100 parts by mass of component (B).

[0044] The composition may contain at least one component (sometimes referred to as component (D)) selected from panthenols, menthol (such as l-menthol), and pyridoxine hydrochloride (pyridoxine hydrochloride).

[0045] When such component (D) is contained in the composition in combination with component (B) (and further, component (C)), discoloration of the minoxidil-containing composition can be efficiently suppressed.

[0046] 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.

[0047] Component (D) may be used alone or in combination of two or more types.

[0048] When two or more kinds of component (D) 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.

[0049] Examples of such combinations include a combination of panthenols (e.g., panthenol and / or pantothenyl ethyl ether) and menthol, a combination of panthenols (e.g., panthenol and / or pantothenyl ethyl ether) and pyridoxine hydrochloride, a combination of menthol and pyridoxine hydrochloride, and a combination of panthenols (e.g., panthenol and / or pantothenyl ethyl ether), menthol, and pyridoxine hydrochloride.

[0050] 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.

[0051] 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.

[0052] 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%.

[0053] 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)).

[0054] When the composition contains panthenol, the content of the 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 (B).

[0055] When the composition contains panthenols and component (C), the content of the panthenols 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 (C).

[0056] 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.

[0057] 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.

[0058] 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%.

[0059] 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)).

[0060] When the composition contains 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, relative to 100 parts by mass of component (B).

[0061] When the composition contains menthol and component (C), 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 component (C).

[0062] 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, for example, from a range of 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, 0.03 w / v% or more, 0.05 w / v% or more, etc.

[0063] 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.

[0064] 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%.

[0065] 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)).

[0066] When the composition contains 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 (B).

[0067] When the composition contains pyridoxine hydrochloride and component (C), 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 (C).

[0068] The composition may contain a solvent.

[0069] 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).

[0070] The solvents may be used alone or in combination of two or more.

[0071] 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).

[0072] 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.

[0073] Therefore, the lower alcohol (composition) may contain at least ethanol (contain it as a lower alcohol).

[0074] 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.

[0075] 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.

[0076] 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.

[0077] 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.

[0078] 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.).

[0079] 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.

[0080] 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.

[0081] 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.

[0082] 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].

[0083] On the other hand, propylene glycol does not have to be the only polyhydric alcohol used. In the present invention, by including component (B) (and further component (C) in combination with component (B)), discoloration of the composition (minoxidil) can be efficiently suppressed without using propylene glycol as the only polyhydric alcohol.

[0084] From this viewpoint, in the present invention, a polyhydric alcohol that does not contain propylene glycol may be used as the polyhydric alcohol, or even if it does contain propylene glycol, a polyhydric alcohol that contains propylene glycol in a small proportion [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 alcohol] may also be used.

[0085] 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.

[0086] 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.

[0087] 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%.

[0088] 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.

[0089] 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.

[0090] 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 60 w / v%.

[0091] 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.

[0092] 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.

[0093] 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%.

[0094] 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 2 to 15 parts by mass per part by mass of minoxidil (component (A)).

[0095] 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.

[0096] 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, lactic acid, gluconic acid (particularly citric acid, phosphoric acid, tartaric acid), etc. These acids may form hydrates, etc.

[0097] The acids may be used alone or in combination of two or more.

[0098] 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.

[0099] 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 reducing agents, antiseptics, colorants, fragrances, solubilizers, and propellants.

[0100] 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, chamomile oil, ginseng tincture, capsicum tincture, retinol acetate, ascorbic acid, pantothenic acid or a salt thereof (calcium pantothenate, etc.), amino acids (glycine, arginine, etc.), higher fatty acids (isostearic acid, palmitic acid), higher fatty acids (isostearic acid, palmitic acid), Examples of suitable surfactants include alcohols (such as cetanol and stearyl alcohol), thiamine nitrate, cyanocobalamin, biotin, mucopolysaccharides (for example, hyaluronic acid, chondroitin sulfate, heparin, heparin sulfate, heparan sulfate, heparinoids, heparinoids, and salts thereof (such as sodium hyaluronate)), dibutylhydroxytoluene, butylhydroxyanisole, sodium metabisulfite, sodium edetate, ascorbic acid, isopropyl gallate, diisopropyl adipate, isopropyl myristate, cellulose ethers (such as hydroxypropyl methylcellulose), nonionic surfactants (such as polysorbates (such as polysorbate 80), polyoxyethylene hydrogenated castor oil), triethanolamine, diisopropanolamine, triisopropanolamine, potassium hydroxide, sodium hydroxide, and dimethyl ether.

[0101] The other components may be used alone or in combination of two or more.

[0102] 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.

[0103] 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.

[0104] 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.

[0105] 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.

[0106] 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.

[0107] 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.

[0108] 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.

[0109] 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.

[0110] 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 %.

[0111] Examples of polyesters include polyethylene terephthalate (PET), polybutylene terephthalate (PBT), polyethylene naphthalate (PEN), polybutylene naphthalate (PBN), etc. A preferred polyester is polyethylene terephthalate (PET).

[0112] 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.

[0113] 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.

[0114] 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).

[0115] 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 may be a unit-dose type that can be used up in a single use.

[0116] 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.

[0117] 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.

[0118] [method] The composition of the present invention contains (combines) component (A) (minoxidil) and component (B) (polycyclic terpene) [and further, component (C) (at least one selected from tocopherol and its derivatives)], thereby making it possible to suppress (block or prevent) discoloration (progression of discoloration).

[0119] 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.

[0120] Method (a): 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).

[0121] In this method (a), the composition may contain component (C), or component (C) may be contained together with component (B).

[0122] In method (i), the composition may contain components other than components (A) to (C) [for example, component (D), water, a lower alcohol (such as ethanol), a polyhydric alcohol, an acid, other components, etc.].

[0123] 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.

[0124] Specifically, method (A) includes the following methods:

[0125] (A-1) A method of suppressing (blocking, preventing) the (progression of) coloring in a composition by adding component (B) to a composition containing component (A).

[0126] (A-2) A method of suppressing (blocking, preventing) the (progression of) coloring in a composition by adding components (B) and (C) to a composition containing component (A).

[0127] (i-3) A method of suppressing (blocking, preventing) coloration (progression of coloration) in a composition comprising components (A) and (C) by adding component (B).

[0128] Method (ii): A method of suppressing (blocking, preventing) discoloration (progression of discoloration) in a composition containing components (A) and (B) by adding component (C).

[0129] In method (ii), the composition may contain components other than components (A) to (C) [for example, component (D), water, a lower alcohol (such as ethanol), a polyhydric alcohol, an acid, other components, etc.].

[0130] 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. [Example]

[0131] The present invention will be described in more detail below with reference to examples, but the present invention is not limited to these examples.

[0132] [Test example] 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.

[0133] 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., compositions 2 to 3 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.

[0134] 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.

[0135] 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%.

[0136] [Table 1]

[0137] When the control composition 1 was visually observed, it was found to be transparent but slightly yellow in color.

[0138] As is clear from the above results, when a bicyclic terpene (1,8-cineole) was added to a composition containing minoxidil, the absorbance decreased (comparison between Composition 1 and Composition 2), and unexpectedly, when a bicyclic terpene was added in combination with tocopherol acetate, the absorbance decreased even further (comparison between Composition 1 and Compositions 2-3).

[0139] Since none of the compositions uses propylene glycol as a polyhydric alcohol, it was found that the absorbance can be reduced (discoloration suppressed) without necessarily selecting propylene glycol. Furthermore, it was found that by combining tocopherol acetate with a bicyclic terpene, not only was the increase in absorbance (discoloration) suppressed, but the absorbance was also reduced (discoloration suppressed) [and moreover, the absorbance was reduced (discoloration suppressed) even compared to when only a bicyclic terpene was used].

[0140] [Experimental Example] The compositions shown in the table below were prepared in the same manner as above. 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.

[0141] [Table 2]

[0142] [Table 3]

[0143] [Table 4] [Industrial Applicability]

[0144] 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 and (B) a polycyclic terpene.

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

3. 3. The composition of claim 1 or 2, wherein component (B) comprises a bicyclic monoterpene.

4. 3. The composition according to claim 1, wherein component (B) comprises at least one selected from cineol, camphor, borneol, isoborneol, and pinene.

5. The composition of claim 1 or 2, wherein component (B) comprises cineole.

6. The composition of claim 2 wherein component (C) comprises a tocopherol acetate.

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

8. 3. The composition according to claim 1, wherein the content of component (B) is 0.0001 w / v % or more.

9. 3. The composition according to claim 1, wherein the content of component (B) is 0.0001 to 150 parts by mass per 100 parts by mass of component (A).

10. The composition according to claim 2, wherein the content of component (C) is 0.001 to 2 w / v %.

11. The composition according to claim 2, wherein the content of component (C) is 0.1 to 100 parts by mass per 100 parts by mass of component (A).

12. 3. The composition according to claim 1, wherein the content of component (C) is 10 to 100,000 parts by mass per 100 parts by mass of component (B).

13. A composition comprising (A) minoxidil and (B) a polycyclic terpene, component (B) comprises a bicyclic monoterpene; The content of component (A) is 1 w / v% or more, The content of component (B) is 0.001 w / v% or more, The content of component (B) is 0.001 to 50 parts by mass per 100 parts by mass of component (A).

14. A composition comprising (A) minoxidil, (B) a polycyclic terpene, and (C) at least one selected from tocopherol and derivatives thereof, component (B) comprises a bicyclic monoterpene; The content of component (A) is 1 w / v% or more, The content of component (B) is 0.001 w / v% or more, The content of component (C) is 0.005 to 1 w / v %, The content of component (B) is 0.001 to 50 parts by mass per 100 parts by mass of component (A), The content of component (C) is 100 to 10,000 parts by mass per 100 parts by mass of component (B).

15. The composition according to claim 1, 2, 13 or 14, further comprising 1,3-butylene glycol.

16. It also contains water, ethanol, and polyhydric alcohol. The composition according to claim 1, 2, 13 or 14, 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.

17. 15. The composition according to claim 1, 2, 13 or 14, further comprising at least one acid selected from citric acid, phosphoric acid and tartaric acid.

18. 15. The composition of claim 1, 2, 13 or 14, having a pH of 5 to 8.

19. A composition contained in a container, comprising:

15. The composition according to claim 1, 2, 13 or 14, wherein at least a part of the container that comes into contact with the composition is made of polyester.

20. A method for suppressing discoloration in a composition by adding (B) a polycyclic terpene to a composition containing (A) minoxidil.

21. A method for suppressing discoloration in a composition by adding (B) a polycyclic terpene and (C) at least one selected from tocopherol and its derivatives to a composition containing (A) minoxidil.

22. A method for suppressing discoloration in a composition comprising (A) minoxidil and (C) at least one selected from tocopherol and its derivatives, by incorporating (B) a polycyclic terpene into the composition.

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

24. The method of any one of claims 20 to 23, wherein the composition further comprises 1,3-butylene glycol and an acid.

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