JP2020090452A - Tranexamic acid-containing composition - Google Patents
Tranexamic acid-containing composition Download PDFInfo
- Publication number
- JP2020090452A JP2020090452A JP2018227814A JP2018227814A JP2020090452A JP 2020090452 A JP2020090452 A JP 2020090452A JP 2018227814 A JP2018227814 A JP 2018227814A JP 2018227814 A JP2018227814 A JP 2018227814A JP 2020090452 A JP2020090452 A JP 2020090452A
- Authority
- JP
- Japan
- Prior art keywords
- extract
- acid
- composition
- oil
- tranexamic
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
Links
- GYDJEQRTZSCIOI-LJGSYFOKSA-N tranexamic acid Chemical compound NC[C@H]1CC[C@H](C(O)=O)CC1 GYDJEQRTZSCIOI-LJGSYFOKSA-N 0.000 title claims abstract description 26
- 229960000401 tranexamic acid Drugs 0.000 title claims abstract description 26
- 239000000203 mixture Substances 0.000 title claims description 63
- 239000002253 acid Substances 0.000 claims abstract description 24
- 150000002148 esters Chemical class 0.000 claims abstract description 16
- 239000008247 solid mixture Substances 0.000 claims abstract description 16
- 150000003839 salts Chemical class 0.000 claims abstract description 15
- 125000004442 acylamino group Chemical group 0.000 claims abstract description 14
- 239000007787 solid Substances 0.000 claims description 19
- 239000000843 powder Substances 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 10
- 239000004094 surface-active agent Substances 0.000 claims description 8
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims description 7
- 239000000284 extract Substances 0.000 description 115
- -1 lauryl ester Chemical class 0.000 description 44
- 239000003921 oil Substances 0.000 description 26
- 235000019198 oils Nutrition 0.000 description 26
- 239000002537 cosmetic Substances 0.000 description 19
- 235000014113 dietary fatty acids Nutrition 0.000 description 18
- 239000000194 fatty acid Substances 0.000 description 18
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- 150000007513 acids Chemical class 0.000 description 17
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- 239000006185 dispersion Substances 0.000 description 11
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- 229940024606 amino acid Drugs 0.000 description 9
- 235000001014 amino acid Nutrition 0.000 description 9
- 150000004665 fatty acids Chemical class 0.000 description 9
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 7
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- 239000006097 ultraviolet radiation absorber Substances 0.000 description 7
- 125000004432 carbon atom Chemical group C* 0.000 description 6
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 6
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- DSEKYWAQQVUQTP-XEWMWGOFSA-N (2r,4r,4as,6as,6as,6br,8ar,12ar,14as,14bs)-2-hydroxy-4,4a,6a,6b,8a,11,11,14a-octamethyl-2,4,5,6,6a,7,8,9,10,12,12a,13,14,14b-tetradecahydro-1h-picen-3-one Chemical compound C([C@H]1[C@]2(C)CC[C@@]34C)C(C)(C)CC[C@]1(C)CC[C@]2(C)[C@H]4CC[C@@]1(C)[C@H]3C[C@@H](O)C(=O)[C@@H]1C DSEKYWAQQVUQTP-XEWMWGOFSA-N 0.000 description 4
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- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 description 4
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 description 4
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 4
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- BXWNKGSJHAJOGX-UHFFFAOYSA-N hexadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCO BXWNKGSJHAJOGX-UHFFFAOYSA-N 0.000 description 4
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- 150000001298 alcohols Chemical class 0.000 description 3
- SHGAZHPCJJPHSC-YCNIQYBTSA-N all-trans-retinoic acid Chemical compound OC(=O)\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-YCNIQYBTSA-N 0.000 description 3
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 description 3
- 150000001413 amino acids Chemical class 0.000 description 3
- 125000002511 behenyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 3
- 239000003240 coconut oil Substances 0.000 description 3
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- 229960003720 enoxolone Drugs 0.000 description 3
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 3
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- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 3
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 description 3
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- GHOKWGTUZJEAQD-ZETCQYMHSA-N (D)-(+)-Pantothenic acid Chemical compound OCC(C)(C)[C@@H](O)C(=O)NCCC(O)=O GHOKWGTUZJEAQD-ZETCQYMHSA-N 0.000 description 2
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 description 2
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- ULQISTXYYBZJSJ-UHFFFAOYSA-N 12-hydroxyoctadecanoic acid Chemical compound CCCCCCC(O)CCCCCCCCCCC(O)=O ULQISTXYYBZJSJ-UHFFFAOYSA-N 0.000 description 2
- FPIPGXGPPPQFEQ-UHFFFAOYSA-N 13-cis retinol Natural products OCC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-UHFFFAOYSA-N 0.000 description 2
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- OBETXYAYXDNJHR-UHFFFAOYSA-N 2-Ethylhexanoic acid Chemical compound CCCCC(CC)C(O)=O OBETXYAYXDNJHR-UHFFFAOYSA-N 0.000 description 2
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 description 2
- ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-aminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 description 2
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 description 2
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- 239000011574 phosphorus Substances 0.000 description 1
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- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
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- 239000001233 rosmarinus officinalis l. extract Substances 0.000 description 1
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- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 description 1
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- BTURAGWYSMTVOW-UHFFFAOYSA-M sodium dodecanoate Chemical compound [Na+].CCCCCCCCCCCC([O-])=O BTURAGWYSMTVOW-UHFFFAOYSA-M 0.000 description 1
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- NNMHYFLPFNGQFZ-UHFFFAOYSA-M sodium polyacrylate Chemical compound [Na+].[O-]C(=O)C=C NNMHYFLPFNGQFZ-UHFFFAOYSA-M 0.000 description 1
- YWIVKILSMZOHHF-QJZPQSOGSA-N sodium;(2s,3s,4s,5r,6r)-6-[(2s,3r,4r,5s,6r)-3-acetamido-2-[(2s,3s,4r,5r,6r)-6-[(2r,3r,4r,5s,6r)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2- Chemical compound [Na+].CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 YWIVKILSMZOHHF-QJZPQSOGSA-N 0.000 description 1
- GGXKEBACDBNFAF-UHFFFAOYSA-M sodium;hexadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCC([O-])=O GGXKEBACDBNFAF-UHFFFAOYSA-M 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 235000011069 sorbitan monooleate Nutrition 0.000 description 1
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- 125000002328 sterol group Chemical group 0.000 description 1
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- 239000000454 talc Substances 0.000 description 1
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- 238000012360 testing method Methods 0.000 description 1
- TUNFSRHWOTWDNC-HKGQFRNVSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCC[14C](O)=O TUNFSRHWOTWDNC-HKGQFRNVSA-N 0.000 description 1
- OULAJFUGPPVRBK-UHFFFAOYSA-N tetratriacontyl alcohol Natural products CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCCO OULAJFUGPPVRBK-UHFFFAOYSA-N 0.000 description 1
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- OGIDPMRJRNCKJF-UHFFFAOYSA-N titanium oxide Inorganic materials [Ti]=O OGIDPMRJRNCKJF-UHFFFAOYSA-N 0.000 description 1
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- UJMBCXLDXJUMFB-UHFFFAOYSA-K trisodium;5-oxo-1-(4-sulfonatophenyl)-4-[(4-sulfonatophenyl)diazenyl]-4h-pyrazole-3-carboxylate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)C1=NN(C=2C=CC(=CC=2)S([O-])(=O)=O)C(=O)C1N=NC1=CC=C(S([O-])(=O)=O)C=C1 UJMBCXLDXJUMFB-UHFFFAOYSA-K 0.000 description 1
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- NCYCYZXNIZJOKI-UHFFFAOYSA-N vitamin A aldehyde Natural products O=CC=C(C)C=CC=C(C)C=CC1=C(C)CCCC1(C)C NCYCYZXNIZJOKI-UHFFFAOYSA-N 0.000 description 1
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- 230000037303 wrinkles Effects 0.000 description 1
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- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 1
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Landscapes
- Cosmetics (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Description
本発明は、トラネキサム酸を含有する油性固形組成物に関する。 The present invention relates to an oily solid composition containing tranexamic acid.
トラネキサム酸やその誘導体は、肌荒れや色素沈着を抑制する作用を有することが知られており、化粧料等の皮膚外用組成物に含有させる成分としてよく用いられている(特許文献1,2等)。 Tranexamic acid and its derivatives are known to have an effect of suppressing rough skin and pigmentation, and are often used as a component to be contained in an external composition for skin such as cosmetics (Patent Documents 1 and 2). .
また、油性固形剤型は、油溶性の成分を含有させたり、肌に閉塞性や保湿性を付与したり、スティック状など取扱いしやすい形状にしたりすることができるため、化粧料等で汎用される剤型である。 Further, the oily solid dosage form is commonly used in cosmetics because it can contain an oil-soluble component, can impart occlusive or moisturizing properties to the skin, and can be made into a shape such as a stick that is easy to handle. It is a dosage form.
トラネキサム酸は水溶性であるところ、これを油性固形組成物に含有させるに際しては油性基剤に分散させる態様となる。しかしながら、分散系の組成物においては一般に時間が経つと分散成分が沈降してしまうという問題が存する。
本発明は、このような状況下においてなされたものであり、トラネキサム酸もしくはその誘導体またはその塩を、油性固形組成物に含有させるときに、均一に分散させることを課題とする。
Since tranexamic acid is water-soluble, when it is contained in an oily solid composition, it is dispersed in an oily base. However, in the case of a dispersion type composition, there is a problem that the dispersed components generally settle out over time.
The present invention has been made under such circumstances, and an object thereof is to uniformly disperse tranexamic acid or a derivative thereof or a salt thereof in an oily solid composition.
この様な状況に鑑みて、本発明者らは鋭意努力を重ねた結果、トラネキサム酸もしくはその誘導体またはその塩を、アシルアミノ酸エステルと共に油性固形組成物に含有させることにより、トラネキサム酸もしくはその誘導体またはその塩を均一に分散させることができ、さらに経時的にもその分散安定性が図れることに想到し、本発明を完成させるに至った。
さらに、本発明者らは、トラネキサム酸を含有する油性固形組成物では、時間が経つと硬度が低下することに着目したところ、アシルアミノ酸エステルが共存することにより、経時的な硬度の維持も図れることを見出した。
In view of such a situation, the present inventors have made diligent efforts, and as a result, by incorporating tranexamic acid or a derivative thereof or a salt thereof in an oily solid composition together with an acyl amino acid ester, tranexamic acid or a derivative thereof or The present invention has been completed based on the idea that the salt can be uniformly dispersed and the dispersion stability can be achieved over time.
Furthermore, the present inventors have noted that in an oily solid composition containing tranexamic acid, the hardness decreases with time, and the coexistence of an acylamino acid ester can also maintain the hardness over time. I found that.
すなわち、本発明は以下の通りである。
[1]トラネキサム酸もしくはその誘導体またはその塩と、アシルアミノ酸エステルとを含有する、油性固形組成物。
[2]前記アシルアミノ酸エステルの含有量が、組成物全体の0.1〜10質量%である、[1]に記載の組成物。
[3]さらにソルビタン系界面活性剤を含有する、[1]又は[2]に記載の組成物。
[4]さらに、粉体を含有する、[1]〜[3]のいずれかに記載の組成物。
[5]前記粉体の含有量が、組成物全体の0.5〜40質量%である、[4]に記載の組成物。
[6]固形油脂及び/又は半固形油脂を組成物全体の5質量%以上含む、[1]〜[5]のいずれかに記載の組成物。
[7]皮膚外用剤である、[1]〜[6]のいずれかに記載の組成物。
That is, the present invention is as follows.
[1] An oily solid composition containing tranexamic acid or a derivative thereof or a salt thereof, and an acylamino acid ester.
[2] The composition according to [1], wherein the content of the acyl amino acid ester is 0.1 to 10 mass% of the entire composition.
[3] The composition according to [1] or [2], which further contains a sorbitan surfactant.
[4] The composition according to any one of [1] to [3], which further contains a powder.
[5] The composition according to [4], wherein the content of the powder is 0.5 to 40 mass% of the entire composition.
[6] The composition according to any one of [1] to [5], which contains 5% by mass or more of a solid fat and/or a semisolid fat.
[7] The composition according to any one of [1] to [6], which is an external preparation for skin.
本発明によれば、トラネキサム酸もしくはその誘導体またはその塩の均一分散性が高められた油性固形組成物が提供される。さらに、本発明の油性固形組成物は、経時で硬度が維持される効果やトラネキサム酸類の析出抑制効果をも奏する。 ADVANTAGE OF THE INVENTION According to this invention, the oily solid composition in which the uniform dispersibility of the tranexamic acid or its derivative(s) or its salt was improved is provided. Further, the oily solid composition of the present invention has an effect of maintaining hardness over time and an effect of suppressing precipitation of tranexamic acids.
本発明の組成物は、トラネキサム酸もしくはその誘導体またはその塩(本明細書において「トラネキサム酸類」とも記す)を必須に含有する。
トラネキサム酸は、トランス−4−アミノメチルシクロヘキサン−1−カルボン酸を指す。
The composition of the present invention essentially contains tranexamic acid or a derivative thereof or a salt thereof (also referred to as “tranexamic acids” in the present specification).
Tranexamic acid refers to trans-4-aminomethylcyclohexane-1-carboxylic acid.
トラネキサム酸の誘導体としては、特に限定されないが、エステル体やアミド体等が挙げられ、トラネキサム酸のエステルとしてはトラネキサム酸ラウリルエステル、トラネキサム酸ヘキサデシルエステル、トラネキサム酸セチルエステル等を、トラネキサム酸のアミド体としてはトラネキサム酸メチルアミド等を例示できる。 The derivative of tranexamic acid is not particularly limited, and examples thereof include esters and amides.Examples of the ester of tranexamic acid include lauryl ester of tranexamic acid, hexadecyl ester of tranexamic acid, cetyl ester of tranexamic acid, and amide of tranexamic acid. Examples of the body include tranexamic acid methylamide.
また、トラネキサム酸またはその誘導体の塩としては、ナトリウム塩、カリウム塩等のアルカリ金属塩;カルシウム塩、マグネシウム塩等のアルカリ土類金属塩;亜鉛塩;鉄塩;アンモニウム塩;アルギニン、ヒスチジン、リジン、オルニチン等の塩基性アミノ酸との塩;モノエタノールアミン、ジエタノールアミン、トリエタノールアミン等のアミンとの塩等が挙げられる。これらのうち、ナトリウム塩、カリウム塩、トリエタノールアミン塩、アルギニン塩が、後述する皮膚外用剤の態様とするのに好ましい。 As salts of tranexamic acid or its derivatives, alkali metal salts such as sodium salts and potassium salts; alkaline earth metal salts such as calcium salts and magnesium salts; zinc salts; iron salts; ammonium salts; arginine, histidine, lysine , Salts with basic amino acids such as ornithine; salts with amines such as monoethanolamine, diethanolamine, triethanolamine and the like. Of these, sodium salt, potassium salt, triethanolamine salt, and arginine salt are preferable for the embodiment of the external preparation for skin described below.
本発明の組成物におけるトラネキサム酸類の含有量は、特に限定されないが、組成物全体に対して0.01〜5質量%が好ましく、1〜3質量%がより好ましい。かかる範囲で含有させることにより、トラネキサム酸類が発揮する抗炎症(肌荒れ抑制)効果や美白(色素沈着抑制)効果を発揮させやすくなる。 The content of tranexamic acids in the composition of the present invention is not particularly limited, but is preferably 0.01 to 5% by mass, more preferably 1 to 3% by mass, based on the entire composition. By including it in such a range, it becomes easy to exhibit the anti-inflammatory (suppression of skin roughness) effect and the whitening (suppression of pigmentation) effect exhibited by tranexamic acids.
本発明の組成物は、アシルアミノ酸エステルを必須に含有する。
油性固形組成物に該成分をトラネキサム酸類と共に含有させることにより、トラネキサム酸類を組成物に均一に分散させることができ、また経時でもその均一分散性を維持することができる。また、トラネキサム酸類を含有する油性固形組成物においても、経時でも硬度が低下することなく維持することができる。さらに、一般にトラネキサム酸類は析出しやすく、これを含有する化粧料等では保存に難が生じる場合があるところ、アシルアミノ酸エステルの共存により析出を抑制することができる。
The composition of the present invention essentially contains an acyl amino acid ester.
By including the component together with tranexamic acids in the oily solid composition, the tranexamic acids can be uniformly dispersed in the composition, and the uniform dispersibility can be maintained over time. Further, even in an oily solid composition containing tranexamic acids, the hardness can be maintained without deterioration over time. Further, generally, tranexamic acids are liable to be deposited, and cosmetics and the like containing them may be difficult to store. However, the coexistence of an acylamino acid ester can suppress the deposition.
アシルアミノ酸エステルは、アシルアミノ酸とアルコール類とのエステルである。
アシルアミノ酸部分としては、特に限定されないが、N−アシル酸性アミノ酸が好ましく、N−アシルアスパラギン酸又はN−アシルグルタミン酸がより好ましく、N−アシルグルタミン酸がさらに好ましい。これらのアミノ酸構造は光学活性体又はラセミ体のいずれであってもよい。
アシル基としては炭素数8〜22の飽和又は不飽和脂肪酸より誘導されるアシル基であることが望ましく、例えばラウリン酸,パルミチン酸,ステアリン酸,オレイン酸等の単一組成の脂肪酸によるアシル基の他に、ヤシ油脂肪酸,牛脂脂肪酸,硬化牛脂脂肪酸等の天然より得られる混合脂肪酸あるいは合成により得られる脂肪酸(分枝脂肪酸を含む)のアシル基であってもよい。
Acyl amino acid ester is an ester of an acyl amino acid and alcohols.
The acylamino acid moiety is not particularly limited, but N-acyl acidic amino acids are preferable, N-acyl aspartic acid or N-acyl glutamic acid is more preferable, and N-acyl glutamic acid is further preferable. These amino acid structures may be optically active or racemic.
The acyl group is preferably an acyl group derived from a saturated or unsaturated fatty acid having 8 to 22 carbon atoms, for example, an acyl group derived from a fatty acid having a single composition such as lauric acid, palmitic acid, stearic acid, oleic acid. Alternatively, it may be an acyl group of a naturally occurring mixed fatty acid such as coconut oil fatty acid, beef tallow fatty acid, hardened beef tallow fatty acid or the like, or a synthetically obtained fatty acid (including a branched fatty acid).
エステル部分を生成する基としては、特に限定されないが、ステロール、炭素数8〜3
0の液状高級アルキル、もしくはアルケニルアルコール、炭素数12〜38の固形状高級アルキルアルコールなどが好ましく挙げられる。N−アシル酸性アミノ酸エステルの場合、モノエステル体であってもジエステル体であっても構わないが、2つのエステル生成残基のうち少なくとも一方がステロール残基であるジエステル体であることが特に好ましい。ステロールとしては、動物由来のものであっても植物由来のものであってもよく、例えばコレステロール、フィトステロール又はこれらの水添物等を挙げることができる。また、炭素数8〜30の液状高級アルキル、もしくはアルケニルアルコールは炭素数8〜30の天然又は合成脂肪族アルコールでかつ常温で液状を呈するものであり、例えば2−オクチルドデシルアルコール等の分枝アルコール、オレイルアルコール等の不飽和アルコールなどが挙げられる。炭素数12〜38の固形状高級アルキルアルコールは炭素数12〜38の飽和一価アルコールでかつ常温で固形状を呈するもので、例えばセチルアルコール,ベヘニルアルコールなどが挙げられる。
The group that forms an ester moiety is not particularly limited, but is a sterol, a carbon number of 8 to 3
Preferred are liquid higher alkyls of 0 or alkenyl alcohols, solid higher alkyl alcohols having 12 to 38 carbon atoms, and the like. In the case of N-acyl acidic amino acid ester, it may be a monoester or a diester, but it is particularly preferable that at least one of the two ester-forming residues is a sterol residue. .. The sterol may be animal-derived or plant-derived, and examples thereof include cholesterol, phytosterol, and hydrogenated products thereof. Further, the liquid higher alkyl or alkenyl alcohol having 8 to 30 carbon atoms is a natural or synthetic aliphatic alcohol having 8 to 30 carbon atoms and is in a liquid state at room temperature, for example, a branched alcohol such as 2-octyldodecyl alcohol. And unsaturated alcohols such as oleyl alcohol. The solid higher alkyl alcohol having 12 to 38 carbon atoms is a saturated monohydric alcohol having 12 to 38 carbon atoms and is solid at room temperature, and examples thereof include cetyl alcohol and behenyl alcohol.
具体的には、N−ラウロイル−L−グルタミン酸ジ(オクチルドデシル/フィトステリル/ベヘニル)、N−ラウロイル−L−グルタミン酸ジ(フィトステリル/2−オクチルドデシル)、N−ラウロイル−L−グルタミン酸ジ(コレステリル/ベヘニル/オクチルドデシル)、N−ラウロイル−L−グルタミン酸ジ(コレステリル/オクチルドデシル)等を挙げることができる。これらのうち、N−ラウロイルグルタミン酸ジ(オクチルドデシル/フィトステリル/ベヘニル)が特に好ましい。 Specifically, N-lauroyl-L-glutamate di(octyldodecyl/phytosteryl/behenyl), N-lauroyl-L-glutamate di(phytosteryl/2-octyldodecyl), N-lauroyl-L-glutamic acid di(cholesteryl/ Behenyl/octyldodecyl), N-lauroyl-L-glutamate di(cholesteryl/octyldodecyl), and the like. Of these, di-N-lauroyl glutamate (octyldodecyl/phytosteryl/behenyl) is particularly preferred.
これらは一般に市販されており、味の素株式会社より販売されている「エルデュウPS203」、「エルデュウCL−301」、「エルデュウCl−202」、「エルデュウPS−304」、「エルデュウPS−306」などが例示できる。 These are generally commercially available, such as "Eldew PS203", "Eldew CL-301", "Eldew Cl-202", "Eldew PS-304" and "Eldew PS-306" which are sold by Ajinomoto Co., Inc. It can be illustrated.
アシルアミノ酸エステルは一種でも二種以上を任意に組み合わせて用いてもよい。単独で用いてもよいし、2種以上を混合して用いてもよい。
本発明の組成物におけるアシルアミノ酸エステルの含有量は、特に限定されないが、組成物全体に対して0.1〜10質量%が好ましく、2〜8質量%がより好ましい。かかる範囲で含有させることにより、トラネキサム酸類の均一分散性効果や、組成物の経時での硬度維持の効果を発揮させやすくなる。
The acyl amino acid ester may be used alone or in any combination of two or more. They may be used alone or in combination of two or more.
The content of the acylamino acid ester in the composition of the present invention is not particularly limited, but is preferably 0.1 to 10% by mass, more preferably 2 to 8% by mass, based on the entire composition. By including it in such a range, it becomes easy to exert the effect of uniform dispersibility of tranexamic acids and the effect of maintaining the hardness of the composition over time.
本発明の組成物は、さらにソルビタン系界面活性剤を含有することが、トラネキサム酸類の均一分散性をより向上させる観点から好ましい。
ソルビタン系界面活性剤としては、特に限定されないが、モノステアリン酸ソルビタン、セスキイソステアリン酸ソルビタン、セスキオレイン酸ソルビタン等のソルビタン脂肪酸エステル類;POEソルビタンモノオレエート、モノステアリン酸ポリオキシエチレンソルビタン等のPOEソルビタン脂肪酸エステル類;POE−ソルビットモノラウレート等のPOEソルビット脂肪酸エステル類が挙げられる。これらのうち、ソルビタン脂肪酸エステル類がより好ましく、セスキイソステアリン酸ソルビタンがさらに好ましい。
本発明の組成物におけるソルビタン系界面活性剤の含有量は、特に限定されないが、組成物全体に対して0.1〜5質量%が好ましく、0.5〜3質量%がより好ましい。かかる範囲で含有させることにより、トラネキサム酸類の均一分散性効果をより発揮させやすくなる。
The composition of the present invention preferably further contains a sorbitan-based surfactant from the viewpoint of further improving the uniform dispersibility of tranexamic acids.
The sorbitan-based surfactant is not particularly limited, but sorbitan fatty acid esters such as sorbitan monostearate, sorbitan sesquiisostearate, sorbitan sesquioleate; POE sorbitan monooleate, polyoxyethylene sorbitan monostearate, etc. Sorbitan fatty acid esters; POE-sorbit monolaurate and other POE sorbit fatty acid esters. Of these, sorbitan fatty acid esters are more preferred, and sorbitan sesquiisostearate is even more preferred.
Although the content of the sorbitan surfactant in the composition of the present invention is not particularly limited, it is preferably 0.1 to 5% by mass, more preferably 0.5 to 3% by mass, based on the entire composition. When the content is within such a range, the effect of uniformly dispersing tranexamic acids can be more easily exhibited.
本発明において油性固形組成物とは、実質的に水及び水性成分を含まず、油剤を基材とする固形の化粧料をいう。
ここで、固形とは、半固形も含み、通常は高い粘度を有し流動性が低い状態のものである。例えば、25℃で流動性がないものが好ましい。また、25℃における粘度が20,000Pa・s以上であることが好ましい。かかる剤型であることにより、トラネキサム酸類が、時間が経っても沈降しにくくなり、経時での分散安定性に優れた組成物となり得
る。
また、「実質的に含まない」とは組成物全体に対して好ましくは0.1質量%以下であり、より好ましくは0.01質量%以下であり、さらに好ましくは0.001質量%以下であることをいう。また、水性成分とは例えば25〜65℃のミネラルオイルに懸濁して1時間静置した後にミネラルオイルと相分離する成分をいう。
In the present invention, the oily solid composition refers to a solid cosmetic material which is substantially free of water and an aqueous component and has an oil agent as a base material.
Here, the solid includes a semi-solid and usually has a high viscosity and low fluidity. For example, a material having no fluidity at 25°C is preferable. Further, the viscosity at 25° C. is preferably 20,000 Pa·s or more. With such a formulation, the tranexamic acids are unlikely to settle down over time, and a composition having excellent dispersion stability over time can be obtained.
The term "substantially free" is preferably 0.1% by mass or less, more preferably 0.01% by mass or less, and further preferably 0.001% by mass or less, based on the entire composition. There is something. The aqueous component means, for example, a component suspended in mineral oil at 25 to 65° C., left standing for 1 hour, and then phase-separated from the mineral oil.
本発明の油性固形組成物において基材となり得る油剤としては、通常は固形油脂及び/又は半固形油脂である。固形油脂や半固形油脂を含有させることにより組成物の粘度が大きくなるため、組成物に分散したトラネキサム酸類が、時間が経っても沈降しにくくなり、経時での分散安定性に優れた組成物となり得る。かかる態様は後述のオイルゲル剤型等に好適である。
さらに通常化粧料に用いられる油剤(液状油剤などの流動性のある油剤も含む)も加えられてもよい。
油剤の種類や含有量は特に限定されず、所望の硬度、塗布後の皮膚上での粉末の白さの軽減、皮膚への密着感や塗布時のすべり感などの使用性によって適宜調整してよい。
The oil agent which can serve as a base material in the oily solid composition of the present invention is usually a solid fat and/or a semisolid fat. Since the viscosity of the composition is increased by the inclusion of solid fats and semi-solid fats, tranexamic acids dispersed in the composition is less likely to sediment over time, and a composition excellent in dispersion stability over time Can be. This aspect is suitable for the oil gel formulation and the like described later.
Further, an oil agent (including a fluid oil agent such as a liquid oil agent) usually used in cosmetics may be added.
The type and content of the oil agent are not particularly limited, and may be appropriately adjusted depending on the desired hardness, reduction of whiteness of the powder on the skin after application, usability such as adhesion to the skin and slippage during application. Good.
固形油脂及び/又は半固形油脂の含有量は、組成物全体の5質量%以上が好ましく、8質量%がより好ましく、12質量%以上がさらに好ましい。また、組成物全体の50質量%以下が好ましく、40質量%以下がより好ましく、30質量%以下がさらに好ましい。 The content of solid fats and/or semisolid fats and oils is preferably 5% by mass or more, more preferably 8% by mass, and further preferably 12% by mass or more of the total composition. Moreover, 50 mass% or less of the whole composition is preferable, 40 mass% or less is more preferable, and 30 mass% or less is further preferable.
ここで、固形油脂における固形とは25℃で流動性がないものをいい、半固形油脂における半固形とは1気圧、20℃で応力の存在しない環境では殆ど変形しないが、若干の応力(10〜100g/cm2程度)がかかると変形するものをいう。また、融点が50℃以上のものがより好ましい。
固形油脂及び/又は半固形油脂としては、植物由来のものとして、カルナウバロウ、モクロウ、キャンデリラロウ、コメヌカロウ、シアバター、アフリカマンゴバター等が挙げられ、動物由来のものとして、ミツロウ、シェラックロウ、イボタロウ等が挙げられ、石油由来のものとして、パラフィンワックス、マイクロクリスタリンワックス等の精製ワックスが挙げられ、鉱物由来のものとしてオゾケライト、セレシン、モンタンワックス等の精製ワックスが挙げられる。これらの固形油脂及び/又は半固形油脂は単独で又は2種以上組み合わせて用いることができる。
Here, the solid in the solid fats and oils refers to those that do not have fluidity at 25°C, and the semisolid in the semisolid fats and oils hardly deforms in an environment where there is no stress at 1 atm and 20°C, but some stress (10 (About 100 g/cm 2 ) means that it is deformed. Further, those having a melting point of 50° C. or higher are more preferable.
Examples of solid fats and/or semi-solid fats and oils include plant-derived ones such as carnauba wax, mokuro, candelilla wax, rice bran wax, shea butter, and African mango butter, and animal-derived ones such as beeswax, shellac wax, and ibotaro. Examples thereof include petroleum-derived waxes such as paraffin wax and microcrystalline wax, and mineral-derived waxes such as ozokerite, ceresin and montan wax. These solid fats and/or semisolid fats and oils can be used alone or in combination of two or more kinds.
本発明の組成物において基材となり得る他の油剤としては、さらに通常化粧料に用いられる油剤(液状油剤などの流動性のある油剤も含む)も挙げられる。
かかる他の油剤としては、マカデミアナッツ油、アボカド油、トウモロコシ油、オリーブ油、ナタネ油、ゴマ油、ヒマシ油、サフラワー油、綿実油、ホホバ油、ヤシ油、パーム油、液状ラノリン、硬化ヤシ油、硬化油、モクロウ、硬化ヒマシ油、ミツロウ、キャンデリラロウ、カルナウバロウ、イボタロウ、ラノリン、還元ラノリン、硬質ラノリン、ホホバロウ等のオイル、ワックス類;流動パラフィン、スクワラン、プリスタン、オゾケライト、パラフィン、セレシン、ワセリン、マイクロクリスタリンワックス等の炭化水素類;オレイン酸、イソステアリン酸、ラウリン酸、ミリスチン酸、パルミチン酸、ステアリン酸、ベヘン酸、ウンデシレン酸等の高級脂肪酸類;セチルアルコール、ステアリルアルコール、イソステアリルアルコール、ベヘニルアルコール、オクチルドデカノール、ミリスチルアルコール、セトステアリルアルコール等の高級アルコール等;イソオクタン酸セチル、ミリスチン酸イソプロピル、イソステアリン酸ヘキシルデシル、アジピン酸ジイソプロピル、セバチン酸ジ−2−エチルヘキシル、乳酸セチル、リンゴ酸ジイソステアリル、ジ−2−エチルヘキサン酸エチレングリコール、ジカプリン酸ネオペンチルグリコール、ジ−2−ヘプチルウンデカン酸グリセリン、トリ−2−エチルヘキサン酸グリセリン、トリ−2−エチルヘキサン酸トリメチロールプロパン、トリイソステアリン酸トリメチロールプロパン、テトラ−2−エチルヘキサン酸ペンタンエリトリット等の合成エステル油類
;アミノ変性ポリシロキサン、ポリエーテル変性ポリシロキサン、アルキル変性ポリシロキサン、フッ素変性ポリシロキサン等の変性ポリシロキサン等の前記のシリコーンに分類されないシリコーン油等の油剤類が挙げられる。
Examples of other oil agents that can serve as a base material in the composition of the present invention include oil agents that are usually used in cosmetics (including fluid oil agents such as liquid oil agents).
Such other oil agents include macadamia nut oil, avocado oil, corn oil, olive oil, rapeseed oil, sesame oil, castor oil, safflower oil, cottonseed oil, jojoba oil, coconut oil, palm oil, liquid lanolin, hardened coconut oil, hardened oil. Oils, waxes such as, syrup, hydrogenated castor oil, beeswax, candelilla wax, carnauba wax, ivota wax, lanolin, reduced lanolin, hard lanolin, jojoba wax; liquid paraffin, squalane, pristane, ozokerite, paraffin, ceresin, vaseline, microcrystalline Hydrocarbons such as waxes; higher fatty acids such as oleic acid, isostearic acid, lauric acid, myristic acid, palmitic acid, stearic acid, behenic acid, undecylenic acid; cetyl alcohol, stearyl alcohol, isostearyl alcohol, behenyl alcohol, octyldodeca Higher alcohols such as norol, myristyl alcohol and cetostearyl alcohol; cetyl isooctanoate, isopropyl myristate, hexyldecyl isostearate, diisopropyl adipate, di-2-ethylhexyl sebacate, cetyl lactate, diisostearyl malate, di- Ethylene glycol 2-ethylhexanoate, neopentyl glycol dicaprate, glycerin di-2-heptylundecanoate, glyceryl tri-2-ethylhexanoate, trimethylolpropane tri-2-ethylhexanoate, trimethylolpropane triisostearate, Synthetic ester oils such as penta-2-ethylhexanoic acid pentane erythritol; Not classified into the above silicones such as amino-modified polysiloxane, polyether-modified polysiloxane, alkyl-modified polysiloxane, fluorine-modified polysiloxane and other modified polysiloxane Oil agents such as silicone oil may be mentioned.
本発明の組成物は、さらに粉体を含有することが好ましい。粉体を含有させることにより組成物の粘度が大きくなるため、組成物に分散したトラネキサム酸類が、時間が経っても沈降しにくくなり、経時での分散安定性に優れた組成物となり得る。かかる態様は後述のオイルゲル剤型等に好適である。
粉体の含有量は、組成物全体の0.5〜40質量%が好ましく、1〜30質量%がより好ましい。
The composition of the present invention preferably further contains a powder. Since the viscosity of the composition is increased by including the powder, the tranexamic acids dispersed in the composition are less likely to settle over time, and the composition can be excellent in dispersion stability over time. This aspect is suitable for the oil gel formulation and the like described later.
The content of the powder is preferably 0.5 to 40% by mass, more preferably 1 to 30% by mass, based on the entire composition.
粉体類としては、表面を処理されていてもよい、シリカ(無水ケイ酸)、マイカ、タルク、カオリン、合成雲母、炭酸カルシウム、炭酸マグネシウム、酸化アルミニウム、硫酸バリウム等の粉体類、ベントナイト、ヘクトライト等の粘土鉱物、表面を処理されていてもよい、ベンガラ、黄酸化鉄、黒酸化鉄、酸化コバルト、群青、紺青、酸化チタン、酸化亜鉛の無機顔料類、表面を処理されていてもよい、雲母チタン、魚燐箔、オキシ塩化ビスマス等のパール剤類、レーキ化されていてもよい赤色202号、赤色228号、赤色226号、黄色4号、青色404号、黄色5号、赤色505号、赤色230号、赤色223号、橙色201号、赤色213号、黄色204号、黄色203号、青色1号、緑色201号、紫色201号、赤色204号等の有機色素類、ポリエステル末、ポリアミド末、ポリエチレン末、ポリメタクリル酸メチル、ナイロン粉末、オルガノポリシロキサンエラストマー等の有機粉体類、が挙げられる。
また、その形状は、特に限定されないが、一般に化粧料等の皮膚外用剤に用いられる球状、半球状、板状などが挙げられ、また多孔性であってもよい。
また、その粒子径は、一般に化粧料等の皮膚外用剤に用いられる程度であればよいが、とくに煙霧状の微細な粒子径(例えば5nm〜20nm)が好ましい。
これらのうち、本発明においては、組成物の分散安定性の観点から、煙霧状シリカ(フュームドシリカ)が特に好ましく挙げられ、市販品を用いてもよい。
As the powder, the surface may be treated, silica (anhydrous silicic acid), mica, talc, kaolin, synthetic mica, calcium carbonate, magnesium carbonate, aluminum oxide, barium sulfate, etc. powder, bentonite, Clay minerals such as hectorite, which may be surface-treated, red iron oxide, yellow iron oxide, black iron oxide, cobalt oxide, ultramarine blue, navy blue, titanium oxide, inorganic pigments of zinc oxide, which may be surface-treated Good, pearl agents such as mica titanium, fish phosphorus foil, bismuth oxychloride, etc., red 202, red 228, red 226, yellow 4, blue 404, yellow 5 and red, which may be laked. Organic dyes such as 505, red 230, red 223, orange 201, red 213, yellow 204, yellow 203, blue 1, green 201, purple 201 and red 204, polyester powder , Polyamide powder, polyethylene powder, polymethylmethacrylate, nylon powder, organic powders such as organopolysiloxane elastomer, and the like.
The shape is not particularly limited, and examples thereof include spheres, hemispheres, and plates that are generally used for external preparations for skin such as cosmetics, and may be porous.
The particle size may be such that it is generally used for external preparations for skin such as cosmetics, but a fine particle size in the form of fumes (for example, 5 nm to 20 nm) is particularly preferable.
Of these, fumed silica (fumed silica) is particularly preferable in the present invention from the viewpoint of dispersion stability of the composition, and commercially available products may be used.
本発明の油性固形組成物は、オイルゲル剤型であることが好ましい。
本発明の組成物がオイルゲル剤型である場合は、前述の固形油脂や半固形油脂に加えて又は替えて、油性ゲル化剤を含有することが好ましい。油性ゲル化剤を含有することで組成物の粘度が大きくなるため、組成物に分散したトラネキサム酸類が、時間が経っても沈降しにくくなり、経時での分散安定性に優れた組成物となり得る。
ここで油性ゲル化剤とは、油剤等の油性成分と相溶性のあるゲル化剤をいい、特に限定されないが、12−ヒドロキシステアリン酸、パルミチン酸デキストリン、(パルミチン
酸/オクタン酸)デキストリン、ジブチルラウロイルグルタミド、ジメチコンクロスポリ
マー等を例示できる。
油性ゲル化剤の含有量は、組成物全体の0.5〜20質量%が好ましく、2〜15質量%がより好ましく、3〜10質量%がさらに好ましい。
The oily solid composition of the present invention is preferably in the form of oil gel.
When the composition of the present invention is in the form of oil gel, it is preferable to contain an oily gelling agent in addition to or in place of the above-mentioned solid fat and oil or semi-solid fat and oil. Since the viscosity of the composition is increased by containing the oily gelling agent, the tranexamic acids dispersed in the composition are unlikely to settle down over time, and the composition may have excellent dispersion stability over time. ..
Here, the oily gelling agent refers to a gelling agent that is compatible with an oily component such as an oily agent, and is not particularly limited, but 12-hydroxystearic acid, dextrin palmitate, (palmitic acid/octanoic acid) dextrin, dibutyl Examples include lauroyl glutamide and dimethicone crosspolymer.
The content of the oily gelling agent is preferably 0.5 to 20% by mass, more preferably 2 to 15% by mass, and even more preferably 3 to 10% by mass of the entire composition.
本発明の組成物は、トラネキサム酸類の、経時での組成物中の分散安定性が高いものである。具体的には、例えば、40℃で1日間静置した後、該化合物の沈降が目視により認められないことをいう。あるいは、40℃で1日間静置した後、組成物の上方95v/v
%中と下方95v/v%中との該化合物の濃度の差が、好ましくは10%以内、より好ま
しくは5%以内、さらに好ましくは0.5%以内である。
The composition of the present invention has high dispersion stability of tranexamic acids in the composition over time. Specifically, it means that no precipitation of the compound is visually observed after standing at 40° C. for 1 day. Alternatively, after standing at 40° C. for 1 day, the composition above 95 v/v
The difference in the concentration of the compound between% and lower 95 v/v% is preferably within 10%, more preferably within 5%, even more preferably within 0.5%.
本発明の組成物は、前述の通りトラネキサム酸類は抗炎症(肌荒れ抑制)効果や美白(色素沈着抑制)効果を発揮し得るため、皮膚外用剤に好適に利用でき、化粧料への適用がより好ましい。なお、化粧料には医薬部外品が含まれる。 The composition of the present invention, as described above, tranexamic acids can exhibit anti-inflammatory (suppression of skin roughness) and whitening (suppression of pigmentation) effects, and thus can be suitably used as an external preparation for skin and more suitable for application to cosmetics. preferable. The cosmetics include quasi-drugs.
本発明の組成物においては、かかる成分以外に、通常の皮膚外用剤で使用される任意成分を本発明の効果を損なわない限りにおいて任意に含有することができる。この様な任意成分としては、各種有効成分、油性成分、他の界面活性剤、多価アルコール、増粘剤、紫外線吸収剤等が挙げられる。 In addition to such components, the composition of the present invention may optionally contain optional components used in ordinary skin external preparations as long as the effects of the present invention are not impaired. Examples of such optional ingredients include various active ingredients, oily ingredients, other surfactants, polyhydric alcohols, thickeners, and ultraviolet absorbers.
有効成分としては、他の美白成分、シワ改善成分、他の抗炎症成分、動植物由来の抽出物等が挙げられる。
他の美白成分としては、一般的に化粧料に用いられているものであれば特に限定はない。例えば、4−n−ブチルレゾルシノール、アスコルビン酸グルコシド、3−О−エチルアスコルビン酸、アルブチン、エラグ酸、コウジ酸、リノール酸、ニコチン酸アミド、5,5'−ジプロピルビフェニル−2,2'−ジオール、5'−アデニル酸二ナトリウム、ト
ラネキサム酸セチル、4−メトキシサリチル酸カリウム塩、ハイドロキノン、パントテン酸等が挙げられる。
Examples of the active ingredient include other whitening ingredients, wrinkle-improving ingredients, other anti-inflammatory ingredients, extracts derived from plants and animals, and the like.
Other whitening ingredients are not particularly limited as long as they are generally used in cosmetics. For example, 4-n-butyl resorcinol, ascorbic acid glucoside, 3-O-ethylascorbic acid, arbutin, ellagic acid, kojic acid, linoleic acid, nicotinic acid amide, 5,5′-dipropylbiphenyl-2,2′- Examples thereof include diol, 5'-adenylate disodium salt, cetyl tranexamic acid, 4-methoxysalicylic acid potassium salt, hydroquinone, and pantothenic acid.
シワ改善成分としては、一般的に化粧料に用いられているものであれば特に限定はない。例えば、ニコチン酸アミド、ビタミンA又はその誘導体(レチノール、レチナール、レチノイン酸、トレチノイン、イソトレチノイン、レチノイン酸トコフェロール、パルミチン酸レチノール、酢酸レチノール等)、ウルソール酸ベンジルエステル、ウルソール酸リン酸エステル、ベツリン酸ベンジルエステル、ベンジル酸リン酸エステルが挙げられる。 The wrinkle improving component is not particularly limited as long as it is generally used in cosmetics. For example, nicotinic acid amide, vitamin A or a derivative thereof (retinol, retinal, retinoic acid, tretinoin, isotretinoin, tocopherol retinoic acid, retinol palmitate, retinol acetate, etc.), ursolic acid benzyl ester, ursolic acid phosphoric acid ester, betulinic acid. Examples thereof include benzyl ester and benzyl phosphate.
他の抗炎症成分としては、クラリノン、グラブリジン、グリチルリチン酸、グリチルレチン酸、パントテニルアルコール等が挙げられ、好ましくは、グリチルリチン酸及びその塩、グリチルレチン酸アルキル及びその塩、並びに、グリチルレチン酸及びその塩である。 Other anti-inflammatory components include clarinone, glabridin, glycyrrhizinic acid, glycyrrhetinic acid, pantothenyl alcohol and the like, preferably glycyrrhizinic acid and its salts, alkyl glycyrrhetinic acid and its salts, and glycyrrhetinic acid and its salts. is there.
動植物由来の抽出物としては、一般的に化粧料に用いられているものであれば特に限定はない。例えば、アケビエキス、アスナロエキス、アスパラガスエキス、アボカドエキス、アマチャエキス、アーモンドエキス、アルニカエキス、アロエエキス、アロニアエキス、アンズエキス、イチョウエキス、インドキノエキス、ウイキョウエキス、ウドエキス、エイジツエキス、エゾウコギエキス、エンメイソウエキス、オウゴンエキス、オウバクエキス、オウレンエキス、オタネニンジンエキス、オトギリソウエキス、オドリコソウエキス、オレンジエキス、カキョクエキス、カッコンエキス、カモミラエキス、カロットエキス、カワラヨモギエキス、カンゾウエキス、キウイエキス、キューカンバーエキス、グアバエキス、クジンエキス、クチナシエキス、クマザサエキス、クララエキス、クルミエキス、グレープフルーツエキス、黒米エキス、クロレラエキス、クワエキス、ケイケットウエキス、ゲットウヨウエキス、ゲンチアナエキス、ゲンノショウコエキス、紅茶エキス、ゴボウエキス、コメエキス、コメ発酵エキス、コメヌカ発酵エキス、コメ胚芽油、コケモモエキス、サルビアエキス、サボンソウエキス、ササエキス、サンザシエキス、サンシャエキス、サンショウエキス、シイタケエキス、ジオウエキス、シコンエキス、シソエキス、シナノキエキス、シモツケソウエキス、シャクヤクエキス、ショウキョウエキス、ショウブ根エキス、シラカバエキス、スギナエキス、ステビアエキス、ステビア発酵物、セイヨウキズタエキス、セイヨウサンザシエキス、セイヨウニワトコエキス、セイヨウノコギリソウエキス、セイヨウハッカエキス、セージエキス、ゼニアオイエキス、センキュウエキス、センブリエキス、ソウハクヒエキス、ダイオウエキス、ダイズエキス、タイソウエキス、タイムエキス、タンポポエキス、茶エキス、チョウジエキス、チンピエキス、甜茶エキス、トウガラシエキス、トウキエキス、トウキンセンカエキス、トウニンエキス、トウヒエキス、ドクダミエキス、トマトエキス、納豆エキス、ニンジンエキス、ニンニクエキス、ノバラエキス、ハイビスカスエキス、バクモンドウエキス、ハスエキス、パセリエキス、バーチエキス、ハマメリスエキス、ヒキオコシエキス、ヒノキエキス、ビワエキス
、フキタンポポエキス、フキノトウエキス、ブクリョウエキス、ブッチャーブルームエキス、ブドウエキス、ブドウ種子エキス、ヘチマエキス、ベニバナエキス、ペパーミントエキス、ボダイジュエキス、ボタンエキス、ホップエキス、マツエキス、マヨナラエキス、マロニエエキス、ミズバショウエキス、ムクロジエキス、メリッサエキス、モズクエキス、モモエキス、ヤグルマギクエキス、ユーカリエキス、ユキノシタエキス、ユズエキス、ユリエキス、ヨクイニンエキス、ヨモギエキス、ラベンダーエキス、緑茶エキス、リンゴエキス、ルイボス茶エキス、レイシエキス、レタスエキス、レモンエキス、レンギョウエキス、レンゲソウエキス、ローズエキス、ローズマリーエキス、ローマカミツレエキス、ローヤルゼリーエキス、ワレモコウエキス等のエキスが好ましいものとして挙げられる。
The extract derived from animals and plants is not particularly limited as long as it is generally used in cosmetics. For example, akebi extract, asunaro extract, asparagus extract, avocado extract, armature extract, almond extract, arnica extract, aloe extract, aronia extract, apricot extract, ginkgo extract, indoquino extract, fennel extract, udo extract, age extract, eleuthero extract. , Crassulaceae extract, Scutellaria extract, Scutellaria extract, Scutellaria extract, Panax ginseng extract, Hypericum perforatum extract, Stinkweed extract, Orange extract, Kakigoku extract, Cuckoo extract, Chamomile extract, Carrot extract, Kawamura Yomogi extract, Kanzo extract, Kiwi extract, Cucumber extract, Guava extract, Kujin extract, Gardenia extract, Kumazasa extract, Clara extract, Walnut extract, Grapefruit extract, Black rice extract, Chlorella extract, Mulberry extract, Cake extract, Gett extract, Gentiana extract, Gentian ginger extract, Black tea extract, Burdock extract, Rice extract, Fermented rice extract, fermented rice bran extract, rice germ oil, cowberry extract, salvia extract, saponsou extract, sasa extract, hawthorn extract, sangsha extract, salamander extract, shiitake extract, dio extract, shikon extract, perilla extract, linden extract, spirea extract, peony root. Extract, ginger extract, ginger root extract, birch extract, horse mackerel extract, stevia extract, stevia fermented product, hawthorn extract, hawthorn extract, hawthorn extract, halibut extract, hazelnut extract, sage extract, mallow extract, senkyu Extract, assembly extract, sow extract, rhubarb extract, soybean extract, turmeric extract, thyme extract, dandelion extract, tea extract, clove extract, chimpi extract, black tea extract, capsicum extract, spruce extract, daffodil extract, spruce extract, spruce extract, duckweed extract , Tomato extract, natto extract, carrot extract, garlic extract, nobara extract, hibiscus extract, bakumondou extract, lotus extract, parsley extract, birch extract, hamamelis extract, Hikiokoshi extract, cypress extract, loquat extract, coltsfoot extract, butterbur extract, butterbur extract , Butcher bloom extract, grape extract, grape seed extract, loofah extract, safflower extract, peppermint extract, bo Daiju extract, button extract, hop extract, pine extract, mayonnaise extract, horse chestnut extract, hornwort extract, sorghum extract, melissa extract, mozuku extract, peach extract, cornflower extract, eucalyptus extract, yukinoshita extract, yuzu extract, lily extract, yokuinin extract, mugwort extract, lavender extract. Extracts such as green tea extract, green tea extract, apple extract, rooibos tea extract, litchi extract, lettuce extract, lemon extract, forsythia extract, astragalus extract, rose extract, rosemary extract, Roman chamomile extract, royal jelly extract, and oleander extract are preferred. Can be mentioned.
他の界面活性剤としては、脂肪酸セッケン(ラウリン酸ナトリウム、パルミチン酸ナトリウム等)、ラウリル硫酸カリウム、アルキル硫酸トリエタノールアミンエーテル等のアニオン界面活性剤類、塩化ステアリルトリメチルアンモニウム、塩化ベンザルコニウム、ラウリルアミンオキサイド等のカチオン界面活性剤類、ベタイン系界面活性剤(アルキルベタイン、アミドベタイン、スルホベタイン等)、イミダゾリン系両性界面活性剤(2−ココイル−2−イミダゾリニウムヒドロキサイド−1−カルボキシエチロキシ2ナトリウム塩等)、アシルメチルタウリン等の両性界面活性剤類、
セスキイソステアリン酸ポリグリセリル、グリセリン脂肪酸エステル類(モノステアリン酸グリセリル等)、プロピレングリコール脂肪酸エステル類(モノステアリン酸プロピレングリコール等)、硬化ヒマシ油誘導体、グリセリンアルキルエーテル、POEグリセリン脂肪酸エステル類(POE−グリセリンモノイソステアレート等)、POE脂肪酸エステル類(ポリエチレングリコールモノオレート、POEジステアレート等)、POEアルキルエーテル類(POE2−オクチルドデシルエーテル等)、POEアルキルフェニルエーテル類(POEノニルフェニルエーテル等)、プルロニック型類、POE・POPアルキルエーテル類(POE・POP2−デシルテトラデシルエーテル等)、テトロニック類、POEヒマシ油・硬化ヒマシ油誘導体(POEヒマシ油、POE硬化ヒマシ油等)、ショ糖脂肪酸エステル、アルキルグルコシド等の非イオン界面活性剤類、等が挙げられる。
Other surfactants include fatty acid soaps (sodium laurate, sodium palmitate, etc.), anionic surfactants such as potassium lauryl sulfate, triethanolamine ether alkylsulfate, stearyltrimethylammonium chloride, benzalkonium chloride, lauryl. Cationic surfactants such as amine oxide, betaine-based surfactants (alkylbetaine, amidobetaine, sulfobetaine, etc.), imidazoline-based amphoteric surfactants (2-cocoyl-2-imidazolinium hydroxide-1-carboxyethyl ester) Roxy disodium salt, etc.), amphoteric surfactants such as acylmethyl taurine,
Polyglyceryl sesquiisostearate, glycerin fatty acid esters (glyceryl monostearate, etc.), propylene glycol fatty acid esters (propylene glycol monostearate, etc.), hydrogenated castor oil derivative, glycerin alkyl ether, POE glycerin fatty acid esters (POE-glycerin mono) Isostearate, etc.), POE fatty acid esters (polyethylene glycol monooleate, POE distearate, etc.), POE alkyl ethers (POE2-octyldodecyl ether, etc.), POE alkylphenyl ethers (POE nonylphenyl ether, etc.), pluronic types , POE/POP alkyl ethers (POE/POP2-decyl tetradecyl ether, etc.), Tetronics, POE castor oil, hydrogenated castor oil derivatives (POE castor oil, POE hydrogenated castor oil, etc.), sucrose fatty acid ester, alkyl glucoside Nonionic surfactants such as and the like.
多価アルコールとしては、ポリエチレングリコール、グリセリン、1,3−ブチレングリコール、エリスリトール、ソルビトール、キシリトール、マルチトール、プロピレングリコール、ジプロピレングリコール、ジグリセリン、イソプレングリコール、1,2−ペンタンジオール、2,4−ヘキシレングリコール、1,2−ヘキサンジオール、1,2−オクタンジオール等が挙げられる。 Polyhydric alcohols include polyethylene glycol, glycerin, 1,3-butylene glycol, erythritol, sorbitol, xylitol, maltitol, propylene glycol, dipropylene glycol, diglycerin, isoprene glycol, 1,2-pentanediol, 2,4. -Hexylene glycol, 1,2-hexanediol, 1,2-octanediol and the like.
増粘剤としては、グアーガム、クインスシード、カラギーナン、ガラクタン、アラビアガム、ペクチン、マンナン、デンプン、キサンタンガム、カードラン、メチルセルロース、ヒドロキシエチルセルロース、カルボキシメチルセルロース、メチルヒドロキシプロピルセルロース、コンドロイチン硫酸、デルマタン硫酸、グリコーゲン、ヘパラン硫酸、ヒアルロン酸、ヒアルロン酸ナトリウム、トラガントガム、ケラタン硫酸、コンドロイチン、ムコイチン硫酸、ヒドロキシエチルグアガム、カルボキシメチルグアガム、デキストラン、ケラト硫酸、ローカストビーンガム、サクシノグルカン、カロニン酸,キチン、キトサン、カルボキシメチルキチン、寒天、ポリビニルアルコール、ポリビニルピロリドン、カルボキシビニルポリマー、アルキル変性カルボキシビニルポリマー、ポリアクリル酸ナトリウム、ポリエチレングリコール等が挙げられる。 As the thickener, guar gum, quince seed, carrageenan, galactan, gum arabic, pectin, mannan, starch, xanthan gum, curdlan, methyl cellulose, hydroxyethyl cellulose, carboxymethyl cellulose, methyl hydroxypropyl cellulose, chondroitin sulfate, dermatan sulfate, glycogen, Heparan sulfate, hyaluronic acid, sodium hyaluronate, tragacanth gum, keratan sulfate, chondroitin, mucoitin sulfate, hydroxyethyl guar gum, carboxymethyl guar gum, dextran, keratosulfate, locust bean gum, succinoglucan, caronic acid, chitin, chitosan, carboxymethyl Examples thereof include chitin, agar, polyvinyl alcohol, polyvinylpyrrolidone, carboxyvinyl polymer, alkyl-modified carboxyvinyl polymer, sodium polyacrylate, polyethylene glycol and the like.
紫外線吸収剤としては、パラアミノ安息香酸系紫外線吸収剤、アントラニル酸系紫外線吸収剤、サリチル酸系紫外線吸収剤、桂皮酸系紫外線吸収剤、ベンゾフェノン系紫外線吸収剤、糖系紫外線吸収剤、2−(2'−ヒドロキシ−5'−t−オクチルフェニル)ベンゾ
トリアゾール、4−メトキシ−4'−t−ブチルジベンゾイルメタン等の紫外線吸収剤類
、等が挙げられる。
As the ultraviolet absorber, para-aminobenzoic acid type ultraviolet absorber, anthranilic acid type ultraviolet absorber, salicylic acid type ultraviolet absorber, cinnamic acid type ultraviolet absorber, benzophenone type ultraviolet absorber, sugar type ultraviolet absorber, 2-(2 Examples thereof include ultraviolet absorbers such as'-hydroxy-5'-t-octylphenyl)benzotriazole and 4-methoxy-4'-t-butyldibenzoylmethane.
本発明の組成物は、前記必須成分、好ましい成分、任意成分などを常法に従って処理することにより製造することができる。 The composition of the present invention can be produced by treating the above-mentioned essential components, preferred components, optional components and the like according to a conventional method.
以下に、実施例を挙げて、本発明について更に詳細に説明を加えるが、本発明がかかる実施例にのみ限定されないことは言うまでもない。 Hereinafter, the present invention will be described in more detail with reference to Examples, but it goes without saying that the present invention is not limited to such Examples.
<製造例>
下記の表1に示す処方に従い、乳化剤形の皮膚外用剤を製造した。すなわち、成分ロを95℃にて加熱溶解させ、混合した。さらに95℃下で3000rpm1分間ディスパーを用いて撹拌しながら、前記混合物に成分イを添加した。その後脱泡を行い、容器に充填し、冷却固化させ、油性固形化粧料を得た。
<Production example>
An emulsifier type external preparation for skin was produced according to the formulation shown in Table 1 below. That is, the component B was heated and melted at 95° C. and mixed. Further, Component A was added to the above mixture while stirring with a disper at 3000 rpm for 1 minute at 95°C. After that, defoaming was performed, the mixture was filled in a container, and solidified by cooling to obtain an oily solid cosmetic.
<試験例>
(1)分散安定性の評価
調製した各油性固形化粧料を40℃で1日間静置した後、トラネキサム酸の沈降の有無を目視により観察し、均一に分散している場合に分散安定性が○、わずかに沈降が認めらるが凝視しないとわからない場合に分散性が△、沈降が認められた場合に分散安定性が×と評価した。結果を表1に併せて示す。
<Test example>
(1) Evaluation of Dispersion Stability After the prepared oily solid cosmetics were allowed to stand at 40° C. for 1 day, the presence or absence of sedimentation of tranexamic acid was visually observed, and the dispersion stability was confirmed when they were uniformly dispersed. ◯, dispersibility was evaluated as Δ when slight sedimentation was observed but not observed without staring, and dispersion stability was evaluated as x when sedimentation was observed. The results are also shown in Table 1.
(2)硬度の評価
調製した各油性固形化粧料を0℃から40℃まで24時間で変化させるよう設定したエイジングボックスに1ヶ月間放置した後、さらに20℃の恒温室に2時間放置し、その後カードメーター(アイテクノエンジニアリング株式会社製)を用いて硬度を測定した。調製直後の硬度を100%とした場合の3ヶ月放置後の硬度を維持率とした。硬度の経時での維持率が80%以上の場合は○、51〜79%の場合は△、経時での変化が50%以下の場合は×と評価した。結果を表1に併せて示す。
(2) Evaluation of Hardness Each of the prepared oily solid cosmetics was left for 1 month in an aging box set to change from 0°C to 40°C in 24 hours, and then left in a thermostatic chamber at 20°C for 2 hours, Then, the hardness was measured using a card meter (manufactured by Aitechno Engineering Co., Ltd.). The hardness after leaving for 3 months when the hardness immediately after preparation was 100% was defined as the maintenance rate. When the hardness retention rate was 80% or more, it was evaluated as ◯, when 51 to 79% was evaluated as Δ, and when the change with time was 50% or less, it was evaluated as x. The results are also shown in Table 1.
(3)トラネキサム酸析出評価
調製した各油性固形化粧料を40℃で1ヵ月静置し、油性固形化粧料の表面にトラネキサム酸の析出の有無を目視で確認した。結果を表1に併せて示す。
(3) Evaluation of precipitation of tranexamic acid Each prepared oily solid cosmetic was allowed to stand at 40°C for 1 month, and the presence or absence of precipitation of tranexamic acid was visually confirmed on the surface of the oily solid cosmetic. The results are also shown in Table 1.
本発明は、化粧料などの皮膚外用剤に応用できる。 The present invention can be applied to skin external preparations such as cosmetics.
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