JP2016121092A - Tranexamic acid-containing composition - Google Patents
Tranexamic acid-containing composition Download PDFInfo
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- JP2016121092A JP2016121092A JP2014261913A JP2014261913A JP2016121092A JP 2016121092 A JP2016121092 A JP 2016121092A JP 2014261913 A JP2014261913 A JP 2014261913A JP 2014261913 A JP2014261913 A JP 2014261913A JP 2016121092 A JP2016121092 A JP 2016121092A
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- tranexamic acid
- salt
- inositol
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- 239000000203 mixture Substances 0.000 title claims abstract description 52
- 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 33
- 229960000401 tranexamic acid Drugs 0.000 title claims abstract description 33
- 239000013078 crystal Substances 0.000 claims abstract description 27
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 claims abstract description 20
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 claims abstract description 19
- CDAISMWEOUEBRE-GPIVLXJGSA-N inositol Chemical compound O[C@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](O)[C@@H]1O CDAISMWEOUEBRE-GPIVLXJGSA-N 0.000 claims abstract description 19
- 229960000367 inositol Drugs 0.000 claims abstract description 19
- 150000003839 salts Chemical class 0.000 claims abstract description 17
- 150000005846 sugar alcohols Polymers 0.000 claims abstract description 17
- 238000001556 precipitation Methods 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 9
- 238000000034 method Methods 0.000 claims description 7
- 239000002537 cosmetic Substances 0.000 claims description 6
- 239000002253 acid Substances 0.000 description 13
- 150000007513 acids Chemical class 0.000 description 13
- -1 tranexamic acid lauryl ester Chemical class 0.000 description 7
- 239000002244 precipitate Substances 0.000 description 6
- 239000004615 ingredient Substances 0.000 description 4
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 230000008021 deposition Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 3
- PUPZLCDOIYMWBV-UHFFFAOYSA-N (+/-)-1,3-Butanediol Chemical compound CC(O)CCO PUPZLCDOIYMWBV-UHFFFAOYSA-N 0.000 description 2
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- GSEJCLTVZPLZKY-UHFFFAOYSA-N Triethanolamine Chemical compound OCCN(CCO)CCO GSEJCLTVZPLZKY-UHFFFAOYSA-N 0.000 description 2
- XLOMVQKBTHCTTD-UHFFFAOYSA-N Zinc monoxide Chemical compound [Zn]=O XLOMVQKBTHCTTD-UHFFFAOYSA-N 0.000 description 2
- 239000004480 active ingredient Substances 0.000 description 2
- 230000003110 anti-inflammatory effect Effects 0.000 description 2
- 230000000052 comparative effect Effects 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 159000000000 sodium salts Chemical class 0.000 description 2
- 239000004094 surface-active agent Substances 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- 229940031723 1,2-octanediol Drugs 0.000 description 1
- 229940058015 1,3-butylene glycol Drugs 0.000 description 1
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 description 1
- XPFCZYUVICHKDS-UHFFFAOYSA-N 3-methylbutane-1,3-diol Chemical compound CC(C)(O)CCO XPFCZYUVICHKDS-UHFFFAOYSA-N 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 239000004386 Erythritol Substances 0.000 description 1
- UNXHWFMMPAWVPI-UHFFFAOYSA-N Erythritol Natural products OCC(O)C(O)CO UNXHWFMMPAWVPI-UHFFFAOYSA-N 0.000 description 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-N 0.000 description 1
- ODKSFYDXXFIFQN-BYPYZUCNSA-P L-argininium(2+) Chemical compound NC(=[NH2+])NCCC[C@H]([NH3+])C(O)=O ODKSFYDXXFIFQN-BYPYZUCNSA-P 0.000 description 1
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 description 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 description 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 229920001273 Polyhydroxy acid Polymers 0.000 description 1
- GYDJEQRTZSCIOI-UHFFFAOYSA-N Tranexamic acid Chemical compound NCC1CCC(C(O)=O)CC1 GYDJEQRTZSCIOI-UHFFFAOYSA-N 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 239000006096 absorbing agent Substances 0.000 description 1
- 239000012190 activator Substances 0.000 description 1
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 1
- 150000001408 amides Chemical class 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 150000001413 amino acids Chemical class 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 239000003945 anionic surfactant Substances 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 150000001484 arginines Chemical class 0.000 description 1
- 235000019437 butane-1,3-diol Nutrition 0.000 description 1
- 159000000007 calcium salts Chemical class 0.000 description 1
- 239000003093 cationic surfactant Substances 0.000 description 1
- 239000002734 clay mineral Substances 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- ZBCBWPMODOFKDW-UHFFFAOYSA-N diethanolamine Chemical compound OCCNCCO ZBCBWPMODOFKDW-UHFFFAOYSA-N 0.000 description 1
- 229940105990 diglycerin Drugs 0.000 description 1
- GPLRAVKSCUXZTP-UHFFFAOYSA-N diglycerol Chemical compound OCC(O)COCC(O)CO GPLRAVKSCUXZTP-UHFFFAOYSA-N 0.000 description 1
- SZXQTJUDPRGNJN-UHFFFAOYSA-N dipropylene glycol Chemical compound OCCCOCCCO SZXQTJUDPRGNJN-UHFFFAOYSA-N 0.000 description 1
- 229940113120 dipropylene glycol Drugs 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 235000019414 erythritol Nutrition 0.000 description 1
- UNXHWFMMPAWVPI-ZXZARUISSA-N erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 description 1
- 229940009714 erythritol Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 235000011187 glycerol Nutrition 0.000 description 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 150000002505 iron Chemical class 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 239000006210 lotion Substances 0.000 description 1
- 159000000003 magnesium salts Chemical class 0.000 description 1
- 239000000845 maltitol Substances 0.000 description 1
- 235000010449 maltitol Nutrition 0.000 description 1
- VQHSOMBJVWLPSR-WUJBLJFYSA-N maltitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-WUJBLJFYSA-N 0.000 description 1
- 229940035436 maltitol Drugs 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- MGJXBDMLVWIYOQ-UHFFFAOYSA-N methylazanide Chemical compound [NH-]C MGJXBDMLVWIYOQ-UHFFFAOYSA-N 0.000 description 1
- 239000002736 nonionic surfactant Substances 0.000 description 1
- AEIJTFQOBWATKX-UHFFFAOYSA-N octane-1,2-diol Chemical compound CCCCCCC(O)CO AEIJTFQOBWATKX-UHFFFAOYSA-N 0.000 description 1
- 229960003104 ornithine Drugs 0.000 description 1
- WCVRQHFDJLLWFE-UHFFFAOYSA-N pentane-1,2-diol Chemical compound CCCC(O)CO WCVRQHFDJLLWFE-UHFFFAOYSA-N 0.000 description 1
- 230000019612 pigmentation Effects 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920001296 polysiloxane Polymers 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 159000000001 potassium salts Chemical class 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229960004063 propylene glycol Drugs 0.000 description 1
- 235000013772 propylene glycol Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 230000002087 whitening effect Effects 0.000 description 1
- 230000037303 wrinkles Effects 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 150000003751 zinc Chemical class 0.000 description 1
- 239000011787 zinc oxide Substances 0.000 description 1
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組成物、特に化粧料に関する。 The present invention relates to a composition containing tranexamic acid, particularly a cosmetic.
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。 Tranexamic acid and its derivatives are known to have an action 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.
トラネキサム酸は非常に結晶性が強く、化粧料等の組成物がこれを収納した容器の口付近に付着すると、時間が経過するとともに水分が蒸発して硬い結晶が析出する現象が生じることが問題となっている。
従来、かかる問題に対してさまざまな対策がとられてきた。例えば、トラネキサム酸とともに、特定の界面活性剤（特許文献１〜３）や、シリカ被覆酸化亜鉛（特許文献４）や、ポリヒドロキシ酸（特許文献５）を組成物に含有させることで結晶析出を抑制したり、トラネキサム酸を含有する組成物を収納する容器の形状を工夫したりして、上記問題の解決が図られてきている。
Tranexamic acid has a very strong crystallinity, and when a composition such as cosmetics adheres to the vicinity of the mouth of a container in which it is stored, there is a problem that moisture evaporates and a hard crystal precipitates over time. It has become.
Conventionally, various countermeasures have been taken against such problems. For example, together with tranexamic acid, a specific surfactant (Patent Documents 1 to 3), silica-coated zinc oxide (Patent Document 4), or polyhydroxy acid (Patent Document 5) is contained in the composition to cause crystal precipitation. The solution to the above problem has been attempted by suppressing the shape of the container that contains the composition containing tranexamic acid.
しかしながら、従来トラネキサム酸の結晶析出抑制のためにともに組成物に含有されていた成分では、効果が十分でない場合があったり、組成物の処方や剤型に制限を与えるものだったりして、これらに替わる結晶析出を抑制する方法が望まれている。
このような状況に鑑みて、本発明は時間が経過しても結晶析出しにくいトラネキサム酸及び／又はその誘導体を含有する組成物を提供することを課題とする。
However, the ingredients previously contained in the composition for the purpose of suppressing crystal precipitation of tranexamic acid may not be effective enough, or may limit the formulation and dosage form of the composition. There is a demand for a method of suppressing crystal precipitation instead of.
In view of such a situation, it is an object of the present invention to provide a composition containing tranexamic acid and / or a derivative thereof that hardly precipitates crystals over time.
本発明者らは上記課題を解決するために鋭意研究を行った結果、イノシトール及び多価アルコールをトラネキサム酸もしくはその誘導体またはその塩とともに組成物に含有させることにより、その結晶析出を抑制できることを見出し、本発明を完成するに至った。 As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that crystal precipitation can be suppressed by including inositol and polyhydric alcohol in the composition together with tranexamic acid or a derivative thereof or a salt thereof. The present invention has been completed.
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、イノシトールと、多価アルコールとを含有する組成物（以降、「本発明の組成物」と記す）。
［２］トラネキサム酸もしくはその誘導体またはその塩とイノシトールとの重量比が０．００１：５〜５：０．００１である、［１］に記載の組成物。
［３］トラネキサム酸もしくはその誘導体またはその塩の含有量が０．０１〜４重量％であり、イノシトールの含有量が０．０１〜２．０重量％である、［１］又は［２］に記載の組成物。
［４］多価アルコールの含有量が５〜４０重量％である、［１］〜［３］の何れかに記載の組成物。
［５］皮膚外用剤である、［１］〜［４］の何れかに記載の組成物。
［６］化粧料である、［５］に記載の皮膚外用剤。
［７］トラネキサム酸もしくはその誘導体またはその塩と、イノシトールと、多価アルコールとを混合する工程を含む、トラネキサム酸もしくはその誘導体またはその塩の結晶析出を抑制する方法。
That is, the present invention is as follows.
[1] A composition containing tranexamic acid or a derivative thereof or a salt thereof, inositol, and a polyhydric alcohol (hereinafter referred to as “the composition of the present invention”).
[2] The composition according to [1], wherein the weight ratio of tranexamic acid or a derivative thereof or a salt thereof and inositol is 0.001: 5 to 5: 0.001.
[3] In [1] or [2], the content of tranexamic acid or a derivative thereof or a salt thereof is 0.01 to 4% by weight, and the content of inositol is 0.01 to 2.0% by weight. The composition as described.
[4] The composition according to any one of [1] to [3], wherein the content of the polyhydric alcohol is 5 to 40% by weight.
[5] The composition according to any one of [1] to [4], which is an external preparation for skin.
[6] The external preparation for skin according to [5], which is a cosmetic.
[7] A method for suppressing crystal precipitation of tranexamic acid or a derivative thereof or a salt thereof, comprising a step of mixing tranexamic acid or a derivative thereof or a salt thereof, inositol and a polyhydric alcohol.
本発明により、時間が経過しても結晶が析出しにくいトラネキサム酸もしくはその誘導体またはその塩を含有する組成物が提供される。 According to the present invention, there is provided a composition containing tranexamic acid or a derivative thereof or a salt thereof in which crystals do not easily precipitate over time.
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（以降「トラネキサム酸類」とも記す）と、イノシトールと、多価アルコールとを含有する。 The composition of the present invention contains tranexamic acid or a derivative thereof or a salt thereof (hereinafter also referred to as “tranexamic acids”), inositol, and a polyhydric alcohol.
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。
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。
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に適用するのに好ましい。
Tranexamic acid refers to trans-4-aminomethylcyclohexane-1-carboxylic acid.
The derivative of tranexamic acid is not particularly limited, and examples thereof include esters and amides. Examples of tranexamic acid esters include tranexamic acid lauryl ester, tranexamic acid hexadecyl ester, tranexamic acid cetyl ester, and the like. Examples of the body include tranexamic acid methylamide.
Examples of salts of tranexamic acid or its derivatives include alkali metal salts such as sodium salt and potassium salt; alkaline earth metal salts such as calcium salt and magnesium salt; zinc salt; iron salt; ammonium salt; arginine, histidine, lysine And salts with basic amino acids such as ornithine; salts with amines such as monoethanolamine, diethanolamine and triethanolamine. Of these, sodium salts, potassium salts, triethanolamine salts, and arginine salts are preferable for application to a skin external preparation described later.
イノシトールは、１，２，３，４，５，６−シクロヘキサンヘキサオールの９種類の異性体を総じて指す。 Inositol generally refers to nine isomers of 1,2,3,4,5,6-cyclohexanehexaol.
本発明の組成物においてトラネキサム酸類とイノシトールとの重量比は、好ましくは０．００１：５〜５：０．００１であり、より好ましくは０．０１：３〜４：０．０１であり、さらに好ましくは０．１：２〜２：０．１である。このような範囲で組成物中に共存することにより、トラネキサム酸類の結晶析出が抑制されやすい。 In the composition of the present invention, the weight ratio of tranexamic acids to inositol is preferably 0.001: 5 to 5: 0.001, more preferably 0.01: 3 to 4: 0.01, Preferably it is 0.1: 2 to 2: 0.1. By coexisting in the composition in such a range, crystal precipitation of tranexamic acids is easily suppressed.
本発明の組成物において、トラネキサム酸類の含有量は好ましくは組成物全量に対して０．０１〜４重量％であり、より好ましくは０．１〜３重量％であり、さらに好ましくは１〜２重量％である。含有量が４重量％より大きいと時間の経過によりトラネキサム酸類の結晶析出が抑制され難くなる場合があり、また含有量が０．０１重量％より小さいと組成物においてトラネキサム酸の作用、例えば美白作用や抗炎症作用が発揮されにくい場合があり、所望の効果が得られ難くなることがある。
また、本発明の組成物において、イノシトールの含有量は好ましくは組成物全量に対して０．０１〜２．０重量％であり、より好ましくは０．１〜０．９重量％であり、さらに好ましくは０．２〜０．７重量％である。含有量が２重量％より大きいと、結晶析出抑制効果が頭打ちになるほか、時間の経過によりイノシトール自体の結晶が析出する場合があり、また含有量が０．０１重量％より小さいとトラネキサム酸類の結晶析出を抑制できない場合がある。
In the composition of the present invention, the content of tranexamic acids is preferably 0.01 to 4% by weight, more preferably 0.1 to 3% by weight, further preferably 1 to 2% based on the total amount of the composition. % By weight. If the content is more than 4% by weight, crystal precipitation of tranexamic acids may be difficult to be suppressed over time, and if the content is less than 0.01% by weight, the action of tranexamic acid in the composition, for example, whitening effect. In some cases, the anti-inflammatory action is difficult to be exhibited, and it may be difficult to obtain a desired effect.
In the composition of the present invention, the content of inositol is preferably 0.01 to 2.0% by weight, more preferably 0.1 to 0.9% by weight, based on the total amount of the composition. Preferably it is 0.2-0.7 weight%. If the content is greater than 2% by weight, the effect of suppressing crystal precipitation reaches its peak, and inositol crystals may precipitate over time, and if the content is less than 0.01% by weight, tranexamic acids Crystal precipitation may not be suppressed.
本発明の組成物における多価アルコールの含有量としては、組成物全量に対して５〜４０重量％が好ましく、７〜３５重量％がより好ましく、１０〜３０重量％がさらに好まし
い。これによりトラネキサム酸類の結晶がより析出されにくくなる。
本明細書において、多価アルコールはイノシトール以外のものを指す。そのような多価アルコールとしては特に限定されないが、皮膚外用剤に一般的に使用されるものが好ましい。例えば、ソルビトール、グリセリン、ジグリセリン、ポリエチレングリコール、１，３−ブチレングリコール、エリスリトール、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、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を例示できる。本発明の組成物には、多価アルコールを好ましくは１種又は２種以上、より好ましくは２種以上を本発明の組成物に含有させ、さらに好ましくは価数の異なる２種以上を組み合わせて含有させる。
As content of the polyhydric alcohol in the composition of this invention, 5 to 40 weight% is preferable with respect to the composition whole quantity, 7 to 35 weight% is more preferable, and 10 to 30 weight% is further more preferable. Thereby, the crystals of tranexamic acids are less likely to be precipitated.
In this specification, polyhydric alcohol refers to things other than inositol. Although it does not specifically limit as such a polyhydric alcohol, What is generally used for a skin external preparation is preferable. For example, sorbitol, glycerin, diglycerin, polyethylene glycol, 1,3-butylene glycol, erythritol, xylitol, maltitol, propylene glycol, dipropylene glycol, isoprene glycol, 1,2-pentanediol, 2,4-hexylene glycol 1,2-hexanediol, 1,2-octanediol and the like. The composition of the present invention preferably contains one or more polyhydric alcohols, more preferably two or more polyhydric alcohols in the composition of the present invention, and more preferably a combination of two or more different valences. Contain.
本発明の組成物は、通常、水を含有する。トラネキサム酸の結晶が析出しにくいことから組成物のｐＨは５〜７の範囲であることが好ましく、皮膚外用剤に適用する際の刺激低減の観点からｐＨは５．５〜６．５の範囲であることがより好ましいが、特に限定されない。 The composition of the present invention usually contains water. The pH of the composition is preferably in the range of 5 to 7 because tranexamic acid crystals are difficult to precipitate, and the pH is in the range of 5.5 to 6.5 from the viewpoint of reducing irritation when applied to an external preparation for skin. Although it is more preferable, it is not specifically limited.
また、本発明の組成物は、その効果を損なわない限りにおいて、その他の任意成分を含有することができる。
任意成分としては、通常皮膚外用剤に配合し得る成分であれば特に限定されず、他の界面活性剤（カチオン性界面活性剤、アニオン性界面活性剤、非イオン性界面活性剤、シリコーン系界面活性剤等）、各種有効成分、油性成分、ｐＨ調整剤、増粘剤、紛体類、紫外線吸収剤、有機変性粘土鉱物等が挙げられる。
有効成分としては、シワ改善成分、抗炎症成分、動植物由来の抽出物等が挙げられ、１種のみを含有させてもよく、２種以上含有されていてもよい。
Moreover, the composition of this invention can contain another arbitrary component, unless the effect is impaired.
The optional component is not particularly limited as long as it is a component that can be usually added to a skin external preparation, and other surfactants (cationic surfactant, anionic surfactant, nonionic surfactant, silicone-based interface) Activators, etc.), various active ingredients, oily ingredients, pH adjusters, thickeners, powders, ultraviolet absorbers, organically modified clay minerals, and the like.
Examples of the active ingredient include a wrinkle improving ingredient, an anti-inflammatory ingredient, an extract derived from animals and plants, and the like, and only one kind may be contained, or two or more kinds may be contained.
本発明の組成物の剤形としては、ローション、エマルション（水中油型、油中水型）、クリーム等特に限定されず、任意の態様を採用できる。 The dosage form of the composition of the present invention is not particularly limited, such as lotion, emulsion (oil-in-water type, water-in-oil type), cream and the like, and any mode can be adopted.
本発明の組成物は、定法に従って製造することができる。すなわち、組成物に含有させる成分を任意の方法で混合すればよい。 The composition of this invention can be manufactured in accordance with a conventional method. That is, what is necessary is just to mix the component contained in a composition by arbitrary methods.
本発明の組成物は、時間が経過してもトラネキサム酸の結晶が析出しにくいという効果がある。具体的には、組成物をポンプ容器に収納して数回吐出した後に４０℃で１日静置しても、トラネキサム酸の結晶が析出しない。そのため、組成物の処方の安定性や取扱い性に優れる。 The composition of the present invention is effective in that crystals of tranexamic acid are difficult to precipitate over time. Specifically, tranexamic acid crystals do not precipitate even when the composition is stored in a pump container and discharged several times, and then allowed to stand at 40 ° C. for one day. Therefore, the stability of the formulation of the composition and the handleability are excellent.
本発明の組成物は、皮膚外用剤として好ましく利用できる。特に、化粧料（医薬部外品を含む）が好ましい。 The composition of the present invention can be preferably used as a skin external preparation. In particular, cosmetics (including quasi drugs) are preferable.
本発明は、別の態様として、トラネキサム酸類の析出を抑制する方法をも提供する。すなわち、トラネキサム酸類と、イノシトールと、多価アルコールとを混合する工程を含む、トラネキサム酸類の結晶析出を抑制する方法である。
本方法において、トラネキサム酸類、イノシトール、及び多価アルコールに係る説明は、前述の本発明の組成物における説明に準じる。
As another aspect, the present invention also provides a method for suppressing precipitation of tranexamic acids. That is, it is a method for suppressing crystal precipitation of tranexamic acids, including a step of mixing tranexamic acids, inositol, and polyhydric alcohol.
In the present method, the description relating to tranexamic acids, inositol, and polyhydric alcohol is in accordance with the above description of the composition of the present invention.
以下、本発明を実施例により更に詳細に説明するが、本発明は、その要旨を超えない限り、以下の実施例に限定されるものではない。 EXAMPLES Hereinafter, although an Example demonstrates this invention still in detail, this invention is not limited to a following example, unless the summary is exceeded.
表１に示す成分を常法に従って混合し、実施例１〜４及び比較例１〜２の組成物を作製
した。
The components shown in Table 1 were mixed according to a conventional method to prepare compositions of Examples 1 to 4 and Comparative Examples 1 and 2.
＜試験例＞
実施例１〜４及び比較例１〜２の各組成物を、ポンプ容器に収納して数回吐出した後に４０℃で１日静置した後に、結晶の析出の程度を観察し、以下の４段階で評価した。結果は表１に合わせて示す。この結果より、イノシトールと多価アルコールとを組み合わせてトラネキサム酸類と混合することにより、トラネキサム酸類の結晶析出が抑制できることが分かる。
◎・・・まったく結晶の析出がみられない
○・・・吐出口の一部に、結晶の析出がみられる
△・・・吐出口全体に、結晶の析出がみられる
×・・・吐出口全体に、はげしく結晶の析出がみられる
<Test example>
Each composition of Examples 1 to 4 and Comparative Examples 1 to 2 was stored in a pump container and discharged several times, and then allowed to stand at 40 ° C. for 1 day, and then the degree of crystal precipitation was observed. Rated by stage. The results are shown in Table 1. From this result, it can be seen that crystal precipitation of tranexamic acids can be suppressed by combining inositol and polyhydric alcohol and mixing with tranexamic acids.
◎ ・ ・ ・ No crystal deposition is observed ○ ・ ・ ・ Crystal deposition is observed in a part of the discharge port △ ・ ・ ・ Crystal deposition is observed in the entire discharge port × ・ ・ ・ Discharge port There is a sharp precipitation of crystals throughout.
本発明により、本発明により、時間が経過しても結晶析出しにくいトラネキサム酸及び／又はその誘導体を含有する組成物が提供されるため、産業上非常に有用である。 According to the present invention, a composition containing tranexamic acid and / or a derivative thereof which hardly precipitates crystals over time is provided by the present invention, which is very useful industrially.
Claims (7)
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| JP2014261913A JP2016121092A (en) | 2014-12-25 | 2014-12-25 | Tranexamic acid-containing composition |
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