JP2019218412A - External composition for skin - Google Patents
External composition for skin Download PDFInfo
- Publication number
- JP2019218412A JP2019218412A JP2019185539A JP2019185539A JP2019218412A JP 2019218412 A JP2019218412 A JP 2019218412A JP 2019185539 A JP2019185539 A JP 2019185539A JP 2019185539 A JP2019185539 A JP 2019185539A JP 2019218412 A JP2019218412 A JP 2019218412A
- Authority
- JP
- Japan
- Prior art keywords
- wax
- component
- skin
- composition
- weight
- 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
- 239000000203 mixture Substances 0.000 title claims abstract description 135
- -1 cyclodextrin compound Chemical class 0.000 claims abstract description 49
- 229920000858 Cyclodextrin Polymers 0.000 claims abstract description 44
- 239000007787 solid Substances 0.000 claims abstract description 33
- 238000002844 melting Methods 0.000 claims abstract description 32
- 230000008018 melting Effects 0.000 claims abstract description 32
- 239000002781 deodorant agent Substances 0.000 claims abstract description 23
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 18
- 239000001993 wax Substances 0.000 claims description 76
- 230000000844 anti-bacterial effect Effects 0.000 claims description 53
- 230000002688 persistence Effects 0.000 claims description 31
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 25
- IJALWSVNUBBQRA-UHFFFAOYSA-N 4-Isopropyl-3-methylphenol Chemical compound CC(C)C1=CC=C(O)C=C1C IJALWSVNUBBQRA-UHFFFAOYSA-N 0.000 claims description 22
- NFIDBGJMFKNGGQ-UHFFFAOYSA-N isopropylmethylphenol Natural products CC(C)CC1=CC=CC=C1O NFIDBGJMFKNGGQ-UHFFFAOYSA-N 0.000 claims description 22
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- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 14
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- RGHNJXZEOKUKBD-SQOUGZDYSA-N D-gluconic acid Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-SQOUGZDYSA-N 0.000 claims description 8
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- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 8
- GLDOVTGHNKAZLK-UHFFFAOYSA-N octadecan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCO GLDOVTGHNKAZLK-UHFFFAOYSA-N 0.000 claims description 8
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- 150000001875 compounds Chemical class 0.000 claims description 6
- NOPFSRXAKWQILS-UHFFFAOYSA-N docosan-1-ol Chemical compound CCCCCCCCCCCCCCCCCCCCCCO NOPFSRXAKWQILS-UHFFFAOYSA-N 0.000 claims description 6
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims description 6
- 229920001155 polypropylene Polymers 0.000 claims description 6
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims description 6
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- UREZNYTWGJKWBI-UHFFFAOYSA-M benzethonium chloride Chemical compound [Cl-].C1=CC(C(C)(C)CC(C)(C)C)=CC=C1OCCOCC[N+](C)(C)CC1=CC=CC=C1 UREZNYTWGJKWBI-UHFFFAOYSA-M 0.000 claims description 5
- 229960001950 benzethonium chloride Drugs 0.000 claims description 5
- WOWHHFRSBJGXCM-UHFFFAOYSA-M cetyltrimethylammonium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+](C)(C)C WOWHHFRSBJGXCM-UHFFFAOYSA-M 0.000 claims description 5
- GHXZTYHSJHQHIJ-UHFFFAOYSA-N Chlorhexidine Chemical compound C=1C=C(Cl)C=CC=1NC(N)=NC(N)=NCCCCCCN=C(N)N=C(N)NC1=CC=C(Cl)C=C1 GHXZTYHSJHQHIJ-UHFFFAOYSA-N 0.000 claims description 4
- RGHNJXZEOKUKBD-UHFFFAOYSA-N D-gluconic acid Natural products OCC(O)C(O)C(O)C(O)C(O)=O RGHNJXZEOKUKBD-UHFFFAOYSA-N 0.000 claims description 4
- 102000016943 Muramidase Human genes 0.000 claims description 4
- 108010014251 Muramidase Proteins 0.000 claims description 4
- 108010062010 N-Acetylmuramoyl-L-alanine Amidase Proteins 0.000 claims description 4
- 229960003260 chlorhexidine Drugs 0.000 claims description 4
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- 235000012208 gluconic acid Nutrition 0.000 claims description 4
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims description 4
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- GOQYKNQRPGWPLP-UHFFFAOYSA-N n-heptadecyl alcohol Natural products CCCCCCCCCCCCCCCCCO GOQYKNQRPGWPLP-UHFFFAOYSA-N 0.000 claims description 4
- 239000003504 photosensitizing agent Substances 0.000 claims description 4
- 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 claims description 3
- HZAXFHJVJLSVMW-UHFFFAOYSA-N 2-Aminoethan-1-ol Chemical compound NCCO HZAXFHJVJLSVMW-UHFFFAOYSA-N 0.000 claims description 3
- QTWJRLJHJPIABL-UHFFFAOYSA-N 2-methylphenol;3-methylphenol;4-methylphenol Chemical compound CC1=CC=C(O)C=C1.CC1=CC=CC(O)=C1.CC1=CC=CC=C1O QTWJRLJHJPIABL-UHFFFAOYSA-N 0.000 claims description 3
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 claims description 3
- 239000004166 Lanolin Substances 0.000 claims description 3
- 240000000111 Saccharum officinarum Species 0.000 claims description 3
- 235000007201 Saccharum officinarum Nutrition 0.000 claims description 3
- XEFQLINVKFYRCS-UHFFFAOYSA-N Triclosan Chemical compound OC1=CC(Cl)=CC=C1OC1=CC=C(Cl)C=C1Cl XEFQLINVKFYRCS-UHFFFAOYSA-N 0.000 claims description 3
- 239000004204 candelilla wax Substances 0.000 claims description 3
- 235000013868 candelilla wax Nutrition 0.000 claims description 3
- 229940073532 candelilla wax Drugs 0.000 claims description 3
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- 239000012185 ceresin wax Substances 0.000 claims description 3
- 229930003836 cresol Natural products 0.000 claims description 3
- 229960000735 docosanol Drugs 0.000 claims description 3
- ZFSXZJXLKAJIGS-UHFFFAOYSA-N halocarban Chemical compound C1=C(Cl)C(C(F)(F)F)=CC(NC(=O)NC=2C=CC(Cl)=CC=2)=C1 ZFSXZJXLKAJIGS-UHFFFAOYSA-N 0.000 claims description 3
- 229950006625 halocarban Drugs 0.000 claims description 3
- IUJAMGNYPWYUPM-UHFFFAOYSA-N hentriacontane Chemical compound CCCCCCCCCCCCCCCCCCCCCCCCCCCCCCC IUJAMGNYPWYUPM-UHFFFAOYSA-N 0.000 claims description 3
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- 229940074146 orange peel wax Drugs 0.000 claims description 3
- WCVRQHFDJLLWFE-UHFFFAOYSA-N pentane-1,2-diol Chemical compound CCCC(O)CO WCVRQHFDJLLWFE-UHFFFAOYSA-N 0.000 claims description 3
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- IYLLULUTZPKQBW-UHFFFAOYSA-N Acrinol Chemical compound CC(O)C(O)=O.C1=C(N)C=CC2=C(N)C3=CC(OCC)=CC=C3N=C21 IYLLULUTZPKQBW-UHFFFAOYSA-N 0.000 claims 1
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Landscapes
- Cosmetics (AREA)
Abstract
Description
本発明は、皮膚外用組成物に関する。より詳細には、抗菌成分の皮膚残存性に優れた皮膚外用組成物に関する。 The present invention relates to a composition for external use on the skin. More specifically, the present invention relates to a composition for external use on skin having excellent skin retentivity of an antibacterial component.
抗菌成分が配合された皮膚外用組成物は、真菌や細菌等を原因とする皮膚の疾患や症状、状態を治療、予防及び／又は改善する目的で有益である。 The skin external composition containing the antibacterial component is useful for treating, preventing and / or improving skin diseases, symptoms and conditions caused by fungi and bacteria.
例えば、腋臭（ワキガとも呼ばれる）等の体臭の原因は、汗に混じった皮脂が過剰増殖した雑菌により分解されて臭いを発生させることが大きな一因とされている。こうした体臭が気になる場合、香水等を使ってマスキングすることもあるが、単純に香水等を使っただけでは、体臭と香水の匂いが混ざり合って不快な臭いを生じさせてしまうこともある。また、香水等でマスキングするだけでは、過剰増殖した雑菌を抑えることはできず、気になる体臭発生の根本原因の解決にはならない。 For example, one of the causes of body odor such as axillary odor (also called wakiga) is that sebum mixed with sweat is decomposed by overgrown bacteria to generate odor. When such body odor is anxious, masking may be performed using perfume, etc., but simply using perfume, etc. may cause unpleasant odor by mixing body odor and perfume odor . Further, simply masking with a perfume or the like cannot suppress the overgrown germs, and does not solve the root cause of anxious body odor.
そこで、腋臭等の気になる体臭を治療、予防及び／又は改善するためのデオドラント剤において、悪臭の原因となる雑菌増殖を抑えることを意図して、抗菌成分を配合した皮膚外用組成物が数多く市販されている。そうした、抗菌成分を配合した皮膚外用組成物では、該外用組成物を塗布・噴霧等して適用した後に、長期にわたり皮膚上に残存してその抗菌効果を発揮させることが望まれる。しかし、皮膚の適用部位や使用状況などによっては、抗菌成分が適用部位から流れ落ちてしまうこともあり抗菌効果の持続が難しい場合もある。例えば、汗をかきやすい部位に適用することを意図した制汗デオドラント剤に抗菌成分を配合した場合、制汗成分では完全に抑えきれず多少なりとも溢れ出た汗によって、皮膚に適用した抗菌成分が洗い流されてしまい、適用部位で所望の抗菌効果を持続し得ない点も懸念されていた。 Therefore, in a deodorant agent for treating, preventing and / or improving anxious body odor such as axillary odor, there are many external skin compositions containing an antibacterial component with the intention of suppressing the growth of various bacteria which cause malodor. It is commercially available. In such a skin external composition containing an antimicrobial component, it is desired that after applying the external composition by applying or spraying, it remains on the skin for a long period of time to exert its antimicrobial effect. However, depending on the application site of the skin, the use condition, and the like, the antibacterial component may flow down from the application site, and it may be difficult to maintain the antibacterial effect. For example, if an antibacterial component is added to an antiperspirant deodorant intended to be applied to a part that is easy to sweat, the antibacterial component applied to the skin is not completely suppressed by the antiperspirant component, but rather overflows to some extent. Was washed away, and there was a concern that the desired antimicrobial effect could not be maintained at the application site.
これまでにも、高い制汗効果、高い抗菌効果、及びそれらの持続性を有し、防臭効果に優れた低刺激性のデオドラント組成物を提供する試みとして、（Ａ）制汗成分と、（Ｂ）特定の２種類のカチオン性界面活性剤と、（Ｃ）ノニオン性抗菌剤と、（Ｄ）多鎖型ノニオン性界面活性剤と、（Ｅ）エタノールとを含有し、特定成分の間での質量比が特定範囲となるようにデオドラント組成物を調製することが提案されている（特許文献１）。しかし、高い抗菌性持続効果を発揮できる、更なる有用な新規の皮膚外用組成物の開発が求められている。 Until now, as an attempt to provide a hypoallergenic deodorant composition having a high antiperspirant effect, a high antibacterial effect, and their persistence, and having an excellent deodorant effect, (A) an antiperspirant component, B) The composition contains two specific cationic surfactants, (C) a nonionic antibacterial agent, (D) a multi-chain nonionic surfactant, and (E) ethanol. It has been proposed to prepare a deodorant composition such that the mass ratio of the deodorant composition falls within a specific range (Patent Document 1). However, there is a need for the development of new and useful new skin external compositions that can exhibit a high antibacterial effect.
本発明は、かかる従来の課題に鑑みてなされたものであり、抗菌成分の皮膚残存性に優れた皮膚外用組成物を提供することを目的とする。 The present invention has been made in view of such conventional problems, and an object of the present invention is to provide a composition for external use on skin having excellent skin persistence of an antibacterial component.
本発明者らは、前記課題を解決するために鋭意検討した結果、（Ａ）抗菌成分と共に、（Ｂ）シクロデキストリン系化合物及び（Ｃ）融点が４０℃以上である固形ワックスを組み合わせて配合し、且つ（Ｄ）水の含有量が組成物全体に対して４０重量％以下となるような皮膚外用組成物とすることにより、該外用組成物を皮膚に適用した場合の（Ａ）抗菌成分の残存性が高められることを見出し、本発明を完成するに至った。 The present inventors have conducted intensive studies in order to solve the above-mentioned problems, and as a result, combined with (A) an antibacterial component, (B) a cyclodextrin-based compound and (C) a solid wax having a melting point of 40 ° C. or more. And (D) a skin external composition having a water content of 40% by weight or less based on the whole composition, whereby the (A) antibacterial component when the external composition is applied to the skin The inventors have found that the survivability is improved, and have completed the present invention.
すなわち、本発明は下記に掲げる皮膚外用組成物を提供する。
［項１］ （Ａ）抗菌成分、（Ｂ）シクロデキストリン系化合物、及び（Ｃ）融点が４０℃以上である固形ワックスを含有し、且つ、（Ｄ）水の含有量が組成物全体に対して４０重量％以下である、皮膚外用組成物。
［項２］ （Ａ）成分として、イソプロピルメチルフェノール、塩化ベンザルコニウム、塩化ベンゼトニウム、塩化セチルトリメチルアンモニウム、臭化セチルトリメチルアンモニウム、トリクロサン、トリクロカルバン、サリチル酸、パラベン、クロルヘキシジン及びその塩、リゾチーム及びその塩、アクリノール、エタノール、グルコン酸、アルキルジアミノグリシン及びその塩、ポピドンヨード、ヨウ化カリウム、ヨウ素、クレゾール、感光素１０１号、感光素２０１号、フェノキシエタノール、１，２-ペンタンジオール、ピロクトンオラミン、及びハロカルバンからなる群より選択される少なくとも１種を含む、項１に記載の皮膚外用組成物。
［項３］ （Ｂ）成分として、シクロデキストリン、及びその誘導体、並びにそれらの塩からなる群より選択される少なくとも１種を含有する、項１又は２に記載の皮膚外用組成物。
［項４］ （Ｃ）成分として、パラフィンワックス、マイクロクリスタリンワックス、ポリエチレンワックス、硬化ヒマシ油、ポリプロピレンワックス、（ステアロキシメチコン／ジメチコン）コポリマー、セテアリルメチコン、アルキル（Ｃ３０−４５）セテアリルジメチコンクロスポリマー、カルナウバロウ、キャンデリラワックス、木ロウ、米糠ロウ、ハゼロウ、ウルシロウ、サトウキビロウ、パームロウ、オレンジ果皮ロウ、オレンジ花ロウ、オオバナソケイ花ロウ、クチベニスイセン花ロウ、シロヤマモモ果実ロウ、スイートアカシア花ロウ、チューベロース花ロウ、蜜蝋、サラシミツロウ、鯨蝋、セラック蝋、ラノリン、モンタンワックス、オゾケライト、セレシンワックス、セチルアルコール、ステアリルアルコール、及びベヘニルアルコールからなる群より選択される少なくとも１種を含有する、項１〜３のいずれかに記載の皮膚外用組成物。
［項５］ ２５℃における硬度が０．０５ｋｇｆ以上である、項１〜４のいずれかに記載の皮膚外用組成物。
［項６］ デオドラント剤として用いられる、項１〜５のいずれかに記載の皮膚外用組成物。
［項７］ （Ａ）成分を、組成物全体に対して０．００１重量％以上含有する、項１〜６のいずれかに記載の皮膚外用組成物。
［項８］ （Ｂ）成分を、組成物全体に対して０．１重量％以上含有する、項１〜７のいずれかに記載の皮膚外用組成物。
［項９］ （Ｃ）成分を、組成物全体に対して０．０１重量％以上含有する、項１〜８のいずれかに記載の皮膚外用組成物。
That is, the present invention provides the following external composition for skin.
[Item 1] It contains (A) an antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or more, and (D) a content of water with respect to the whole composition. Composition for external use on the skin, which is 40% by weight or less.
[Item 2] As the component (A), isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium chloride, cetyltrimethylammonium bromide, triclosan, triclocarban, salicylic acid, paraben, chlorhexidine and salts thereof, lysozyme and the like Salts, acrinol, ethanol, gluconic acid, alkyl diaminoglycine and salts thereof, popidone iodine, potassium iodide, iodine, cresol, photosensitizer 101, photosensitizer 201, phenoxyethanol, 1,2-pentanediol, pyroctone olamine, Item 3. The external composition for skin according to Item 1, comprising at least one selected from the group consisting of: and halocarban.
[Item 3] The external composition for skin according to Item 1 or 2, which contains, as the component (B), at least one selected from the group consisting of cyclodextrin, a derivative thereof, and a salt thereof.
[Item 4] As the component (C), paraffin wax, microcrystalline wax, polyethylene wax, hydrogenated castor oil, polypropylene wax, (stearoxymethicone / dimethicone) copolymer, cetearyl methicone, alkyl (C30-45) cetearyl dimethicone cloth Polymer, Carnauba wax, Candelilla wax, Wax wax, Rice bran wax, Hazelau, Urushi wax, Sugarcane wax, Palm wax, Orange peel wax, Orange flower wax, Obanosakei flower wax, Cutis venom flower wax, Whiteberry fruit wax, Sweet acacia flower wax , Tuberose flower wax, beeswax, salami beeswax, spermaceti, shellac wax, lanolin, montan wax, ozokerite, ceresin wax, cetyl alcohol, stearyl alcohol, and behe Item 4. The external skin composition according to any one of Items 1 to 3, which comprises at least one selected from the group consisting of nyl alcohol.
[Item 5] The external skin composition according to any one of Items 1 to 4, which has a hardness at 25 ° C of 0.05 kgf or more.
[Item 6] The composition for external use on skin according to any one of Items 1 to 5, which is used as a deodorant agent.
[Item 7] The external composition for skin according to any one of Items 1 to 6, wherein the component (A) is contained in an amount of 0.001% by weight or more based on the whole composition.
[Item 8] The external composition for skin according to any one of Items 1 to 7, which comprises the component (B) in an amount of 0.1% by weight or more based on the whole composition.
[Item 9] The external composition for skin according to any one of Items 1 to 8, which comprises the component (C) in an amount of 0.01% by weight or more based on the whole composition.
更に本発明は別の観点から、下記に掲げる（Ａ）抗菌成分の皮膚残存性を高める方法をも提供する。
［項１０］ （Ａ）抗菌成分と、（Ｂ）シクロデキストリン系化合物と、（Ｃ）融点が４０℃以上である固形ワックスとを配合し、且つ（Ｄ）水の含有量が組成物全体に対して４０重量％以下となるように皮膚外用組成物を調製することを特徴とする、該外用組成物の（Ａ）成分の皮膚残存性を高める方法。
Further, the present invention also provides a method for enhancing the skin persistence of the following antibacterial component (A) from another viewpoint.
[Item 10] (A) An antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or more, and (D) a water content of the entire composition. A method for improving the skin persistence of the component (A) of the composition for external use, which comprises preparing the composition for external use on the skin so as to be 40% by weight or less.
本発明により、抗菌成分の皮膚残存性に優れた皮膚外用組成物を提供することができる。一実施態様において、本発明の皮膚外用組成物は、適用した抗菌成分が汗などで洗い流されやすい皮膚の部位や状況で用いられることが一般に多い、デオドラント剤などとして好適に用いられ得る。 According to the present invention, it is possible to provide a composition for external use on skin having excellent skin persistence of an antibacterial component. In one embodiment, the composition for external use on the skin of the present invention can be suitably used as a deodorant agent or the like, which is generally used in a skin site or situation where the applied antibacterial component is easily washed away by sweat or the like.
以下、本発明について詳細に説明する。
なお、本明細書中で使用される用語は、特に他を言及しない限り、当該分野で通常用いられる意味で用いられている点が理解されるべきである。
Hereinafter, the present invention will be described in detail.
It should be understood that the terms used in the present specification are used in the meaning commonly used in the art unless otherwise specified.
（１．皮膚外用組成物）
本発明の皮膚外用組成物は、（Ａ）抗菌成分、（Ｂ）シクロデキストリン系化合物、及び（Ｃ）融点が４０℃以上である固形ワックスを含有し、且つ、（Ｄ）水の含有量を組成物全体に対して４０重量％以下とすることを特徴とする。
(1. Skin external composition)
The composition for external use on the skin of the present invention contains (A) an antibacterial component, (B) a cyclodextrin compound, and (C) a solid wax having a melting point of 40 ° C. or more, and has a water content of (D). It is characterized in that it is not more than 40% by weight based on the whole composition.
（Ａ）抗菌成分：
本発明の皮膚外用組成物は、抗菌成分（以下、単に（Ａ）成分ともいう）を含有する。本発明に用いられる抗菌成分とは、殺菌又は静菌作用を発揮して、雑菌（真菌、グラム陽性細菌、グラム陰性細菌等）の増殖を抑えることができる当該分野で公知の任意の成分をいう。具体的には、抗菌成分として、イソプロピルメチルフェノール、トリクロサン、トリクロカルバン、サリチル酸、パラベン等の油溶性抗菌成分；塩化ベンザルコニウム（ベンザルコニウム塩化物ともいう）、塩化ベンゼトニウム（ベンゼトニウム塩化物ともいう）、塩化セチルトリメチルアンモニウム（セチルトリメチルアンモニウム塩化物ともいう）、臭化セチルトリメチルアンモニウム（セチルトリメチルアンモニウム臭化物ともいう）等の四級アンモニウム塩型抗菌成分や、クロルヘキシジン、リゾチーム及びそれらの塩（例えば、塩酸塩、酢酸塩、グルコン酸塩）等を含む、カチオン性抗菌成分；アクリノール、エタノール、グルコン酸、アルキルジアミノグリシン及びそれらの塩（例えば、塩酸塩）等の水溶性抗菌成分；ポピドンヨード、ヨウ化カリウム、ヨウ素等のヨード系抗菌成分；クレゾール、感光素１０１号、感光素２０１号、フェノキシエタノール、１，２-ペンタンジオール、ピロクトンオラミン、ハロカルバン等を挙げることができるが、これらに限定されない。高い皮膚残存性の向上効果が本発明によって得られ易いという観点から、本発明の皮膚外用組成物には、好ましくは油溶性抗菌成分及び／又はカチオン性抗菌成分を使用するのがよく、より好ましくはイソプロピルメチルフェノール、塩化ベンザルコニウム、塩化ベンゼトニウム、塩化セチルトリメチルアンモニウム、臭化セチルトリメチルアンモニウム、塩化リゾチーム（リゾチーム塩酸塩ともいう）、グルコン酸クロルヘキシジン（クロルヘキシジングルコン酸塩ともいう）、塩酸クロルヘキシジン（クロルヘキシジン塩酸塩ともいう）、及び／又は酢酸クロルヘキシジン（クロルヘキシジン酢酸塩ともいう）を使用するのがよく、更に好ましくはイソプロピルメチルフェノール及び／又は塩化ベンザルコニウムを使用するのがよく、特に好ましくはイソプロピルメチルフェノールを使用するのがよい。
(A) Antibacterial component:
The composition for external use on skin of the present invention contains an antibacterial component (hereinafter, also simply referred to as component (A)). The antimicrobial component used in the present invention refers to any component known in the art that can exert a bactericidal or bacteriostatic action and suppress the growth of various bacteria (fungi, gram-positive bacteria, gram-negative bacteria, etc.). . Specifically, as an antibacterial component, an oil-soluble antibacterial component such as isopropylmethylphenol, triclosan, triclocarban, salicylic acid, and paraben; benzalkonium chloride (also called benzalkonium chloride), benzethonium chloride (also called benzethonium chloride) ), Quaternary ammonium salt-type antibacterial components such as cetyltrimethylammonium chloride (also referred to as cetyltrimethylammonium chloride) and cetyltrimethylammonium bromide (also referred to as cetyltrimethylammonium bromide), chlorhexidine, lysozyme and salts thereof (for example, Cationic antimicrobial components including hydrochloride, acetate, gluconate); water-soluble antimicrobial components such as acrinol, ethanol, gluconic acid, alkyldiaminoglycine and salts thereof (eg, hydrochloride); popidone Iodine-based antibacterial components such as sodium chloride, potassium iodide and iodine; cresol, photosensitive element 101, photosensitive element 201, phenoxyethanol, 1,2-pentanediol, pyrocton olamine, halocarban and the like. However, the present invention is not limited to these. From the viewpoint that a high skin persistence improving effect is easily obtained by the present invention, it is preferable to use an oil-soluble antibacterial component and / or a cationic antibacterial component in the composition for external use on the skin of the present invention, more preferably. Are isopropylmethylphenol, benzalkonium chloride, benzethonium chloride, cetyltrimethylammonium chloride, cetyltrimethylammonium bromide, lysozyme chloride (also called lysozyme hydrochloride), chlorhexidine gluconate (also called chlorhexidine gluconate), chlorhexidine hydrochloride (chlorhexidine) Hydrochloride) and / or chlorhexidine acetate (also referred to as chlorhexidine acetate), and more preferably isopropylmethylphenol and / or benzalkonium chloride. And it is preferably to use isopropyl methyl phenol.
本発明の皮膚外用組成物では、上記（Ａ）成分のうち、１種のみを単独で用いてもよいし、２種以上を組み合わせて用いてもよい。 In the external composition for skin of the present invention, only one of the above-mentioned components (A) may be used alone, or two or more may be used in combination.
本発明の皮膚外用組成物における（Ａ）成分の含有量は、用途や所望の効果の程度等に応じて適宜設定され得る。一例として、組成物全体に対して、（Ａ）成分が、０．００１重量％以上、好ましくは０．０１重量％以上、より好ましくは０．０５重量％以上とするのがよい。（Ａ）成分の含有量の上限値は特に限定されないが、一例として、組成物全体に対して、１重量％以下とすればよく、好ましくは０．７重量％以下とすればよく、より好ましくは０．５重量％以下とすればよい。本発明によれば、（Ａ）抗菌成分の皮膚残存性が改善されるので、このような範囲であっても十分な抗菌性持続効果を発揮することができる。 The content of the component (A) in the composition for external use on the skin of the present invention can be appropriately set according to the use, the degree of the desired effect, and the like. As an example, the content of the component (A) is preferably 0.001% by weight or more, preferably 0.01% by weight or more, and more preferably 0.05% by weight or more based on the whole composition. Although the upper limit of the content of the component (A) is not particularly limited, it may be, for example, 1% by weight or less, preferably 0.7% by weight or less, more preferably, based on the whole composition. May be 0.5% by weight or less. According to the present invention, since the skin persistence of the antimicrobial component (A) is improved, a sufficient antimicrobial sustaining effect can be exerted even in such a range.
（Ｂ）シクロデキストリン系化合物：
本発明の皮膚外用組成物は更に、シクロデキストリン系化合物（以下、単に（Ｂ）成分ともいう）を含有する。本明細書において、シクロデキストリン系化合物とは、シクロデキストリン、及びその誘導体、並びにそれらの塩からなる群より選択される少なくとも１種をいう。
(B) Cyclodextrin compound:
The external composition for skin of the present invention further contains a cyclodextrin compound (hereinafter, also simply referred to as component (B)). In the present specification, the cyclodextrin-based compound refers to at least one selected from the group consisting of cyclodextrin, a derivative thereof, and a salt thereof.
シクロデキストリンとは、グルコースがα−１，４結合で環状に連なった構造を有する環状オリゴ糖の一種である。シクロデキストリンは、構成するグルコースの数に応じて、α型（α−シクロデキストリン、グルコース６分子）、β型（β−シクロデキストリン、グルコース７分子）、γ型（γ−シクロデキストリン、グルコース８分子）等と呼ばれる。天然には、更に多くの分子のグルコースで構成されるシクロデキストリンも存在することが知られている。また、シクロデキストリンを誘導体化した化合物もこれまでに知られており、本発明にはこのようなシクロデキストリン誘導体を用いてもよい。シクロデキストリン誘導体としては、特に限定はされないが、エステル化誘導体、エーテル化誘導体、スルホニル化誘導体、アミノ化誘導体等を挙げることができ、より具体的には、アルキル化シクロデキストリン（メチル化シクロデキストリン等）、ヒドロキシアルキル化シクロデキストリン（ヒドロキシプロピル化シクロデキストリン等）、スルホアルキル化シクロデキストリン（スルホブチル化シクロデキストリン等）、アミノアルキル化シクロデキストリン（アミノエチル化シクロデキストリン等）、配糖化シクロデキストリン（ガラクトシルシクロデキストリン、マンノシルシクロデキストリン等）等を挙げることができる。本発明に用いられるシクロデキストリン系化合物は、シクロデキストリン又はその誘導体の塩であってもよく、薬学的又は生理学的に許容され得る任意の塩を使用することができる。例えば、有機酸塩［例えば、モノカルボン酸塩（酢酸塩、トリフルオロ酢酸塩、酪酸塩、パルミチン酸塩、ステアリン酸塩等）］；無機酸塩（例えば、塩酸塩、硫酸塩、硝酸塩、臭化水素酸塩、リン酸塩等）；有機塩基との塩（例えば、メチルアミン、トリエチルアミン、トリエタノールアミン、モルホリン、ピペラジン、ピロリジン、トリピリジン、ピコリン等の有機アミンとの塩等）；無機塩基との塩［例えば、アンモニウム塩；アルカリ金属（ナトリウム、カリウム等）、アルカリ土類金属（カルシウム、マグネシウム等）、アルミニウム等の金属との塩等］；等が挙げられるが、これらに限定されない。本発明の皮膚外用組成物では、上記（Ｂ）成分のうち、１種のみを単独で用いてもよいし、２種以上を組み合わせて用いてもよい。 Cyclodextrin is a kind of cyclic oligosaccharide having a structure in which glucose is cyclically connected by α-1,4 bonds. According to the number of glucoses constituting the cyclodextrin, α-type (α-cyclodextrin, 6 molecules of glucose), β-type (7 molecules of β-cyclodextrin, glucose), γ-type (8 molecules of γ-cyclodextrin, glucose) ) And so on. It is known that there are also naturally occurring cyclodextrins composed of more molecules of glucose. Further, a compound obtained by derivatizing cyclodextrin is also known, and such a cyclodextrin derivative may be used in the present invention. The cyclodextrin derivative is not particularly limited, but may be an esterified derivative, an etherified derivative, a sulfonylated derivative, an aminated derivative, and the like. More specifically, an alkylated cyclodextrin (eg, methylated cyclodextrin, etc.) ), Hydroxyalkylated cyclodextrins (such as hydroxypropylated cyclodextrins), sulfoalkylated cyclodextrins (such as sulfobutylated cyclodextrins), aminoalkylated cyclodextrins (such as aminoethylated cyclodextrins), glycosylated cyclodextrins (galactosylcyclo) Dextrin, mannosylcyclodextrin, etc.). The cyclodextrin compound used in the present invention may be a salt of cyclodextrin or a derivative thereof, and any pharmaceutically or physiologically acceptable salt can be used. For example, organic acid salts [eg, monocarboxylates (acetate, trifluoroacetate, butyrate, palmitate, stearate, etc.)]; inorganic acid salts (eg, hydrochloride, sulfate, nitrate, odor) Salts with organic bases (eg, salts with organic amines such as methylamine, triethylamine, triethanolamine, morpholine, piperazine, pyrrolidine, tripyridine, picoline, etc.); inorganic bases and [Eg, ammonium salts; salts with metals such as alkali metals (such as sodium and potassium), alkaline earth metals (such as calcium and magnesium), and aluminum]; and the like, but are not limited thereto. In the external composition for skin of the present invention, only one of the above components (B) may be used alone, or two or more of them may be used in combination.
本発明には、上記のいずれのシクロデキストリン系化合物も用いることができるが、より一層確実に高く本発明の効果を発揮し易いという観点から、好ましくはシクロデキストリン及び／又はその塩が用いられ、より好ましくはシクロデキストリンが用いられ、更に好ましくはα−シクロデキストリン、β−シクロデキストリン、γ−シクロデキストリンが用いられ、特に好ましくはβ−シクロデキストリンが用いられる。 In the present invention, any of the above-mentioned cyclodextrin-based compounds can be used, but from the viewpoint that the effects of the present invention are more easily and more reliably exerted, preferably cyclodextrin and / or a salt thereof are used, More preferably, cyclodextrin is used, further preferably α-cyclodextrin, β-cyclodextrin, and γ-cyclodextrin, and particularly preferably β-cyclodextrin.
本発明の皮膚外用組成物における（Ｂ）成分の含有量は、用途や所望の効果の程度等に応じて適宜設定され得る。一例として、組成物全体に対して、（Ｂ）成分が、０．１重量％以上、好ましくは１重量％以上、より好ましくは３重量％以上とするのがよい。（Ｂ）成分の含有量の上限値は特に限定されないが、一例として、組成物全体に対して、１５重量％以下とすればよく、好ましくは１０重量％以下とすればよく、より好ましくは８重量％以下とすればよい。 The content of the component (B) in the composition for external use on the skin of the present invention can be appropriately set according to the use, the degree of the desired effect, and the like. As an example, the component (B) may be 0.1% by weight or more, preferably 1% by weight or more, and more preferably 3% by weight or more, based on the whole composition. Although the upper limit of the content of the component (B) is not particularly limited, it may be, for example, 15% by weight or less, preferably 10% by weight or less, more preferably 8% by weight, based on the whole composition. % By weight or less.
更に本発明の皮膚外用組成物において、（Ａ）成分の含有量に対する（Ｂ）成分の含有量の比率については、特に限定されないが、より一層効果的に（Ａ）成分の皮膚残存性を向上させ得るという観点から、好ましくは、（Ａ）成分の総量１重量部当たり、（Ｂ）成分の含有量が総量で０．１重量部以上、好ましくは１重量部以上、より好ましくは１０重量部以上となる比率が例示される。（Ａ）成分の含有量に対する（Ｂ）成分の含有量の比率の上限値も特に限定されないが、一例として、（Ａ）成分の総量１重量部あたり、（Ｂ）成分の含有量が総量で１０００重量部以下、好ましくは５００重量部以下、より好ましくは１００重量部以下となる比率を例示することができる。 Furthermore, in the skin external composition of the present invention, the ratio of the content of the component (B) to the content of the component (A) is not particularly limited, but the skin persistence of the component (A) is more effectively improved. From the viewpoint that the component (A) can be obtained, the content of the component (B) is preferably 0.1 part by weight or more, preferably 1 part by weight or more, more preferably 10 parts by weight, per 1 part by weight of the total amount of the component (A). The ratios described above are exemplified. Although the upper limit of the ratio of the content of the component (B) to the content of the component (A) is not particularly limited, for example, the content of the component (B) is 1 part by weight based on the total amount of the component (A). A ratio of 1000 parts by weight or less, preferably 500 parts by weight or less, more preferably 100 parts by weight or less can be exemplified.
（Ｃ）固形ワックス：
本発明の皮膚外用組成物は更に、融点が４０℃以上である固形ワックス（以下、単に（Ｃ）成分ともいう）を含有する。本発明に用いられる固形ワックスとは、ろう状の物理的性質（具体的には、耐水性、可塑性、光沢性及び／又は不透明性等）を示し、融点が４０℃以上であって、常温では固形のものをいう。本発明に用いる固形ワックスの融点は、４０℃以上であれば、本発明の効果を奏し得る限り特に限定されないが、通常４０〜１５０℃程度、好ましくは４０〜１３０℃程度、より好ましくは４０〜１００℃程度である。具体的には、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石油由来のワックス；ポリエチレンワックス、硬化ヒマシ油、ポリプロピレンワックス等の合成ワックス；（ステアロキシメチコン／ジメチコン）コポリマー、セテアリルメチコン、アルキル（Ｃ３０−４５）セテアリルジメチコンクロスポリマー等のシリコーンワックス；カルナウバロウ、キャンデリラワックス、木ロウ、米糠ロウ、ハゼロウ、ウルシロウ、サトウキビロウ、パームロウ、オレンジ果皮ロウ、オレンジ花ロウ、オオバナソケイ花ロウ、クチベニスイセン花ロウ、シロヤマモモ果実ロウ、スイートアカシア花ロウ、チューベロース花ロウ等の植物由来のワックス；蜜蝋、サラシミツロウ、鯨蝋、セラック蝋、ラノリン等の動物由来のワックス；モンタンワックス、オゾケライト、セレシンワックス等の鉱物由来のワックス；セチルアルコール（セタノール、パルミチルアルコール等ともいう）、ステアリルアルコール、ベヘニルアルコール等の固形状の高級アルコール；等が挙げられるが、これらに限定されない。本発明の皮膚外用組成物では、上記（Ｃ）成分のうち、１種のみを単独で用いてもよいし、２種以上を組み合わせて用いてもよい。好ましくは、（Ｃ）成分を２種類以上で任意に組み合わせて用いることで、より一層高い本発明の効果が期待できる。
(C) Solid wax:
The composition for external use on the skin of the present invention further contains a solid wax having a melting point of 40 ° C. or higher (hereinafter, also simply referred to as component (C)). The solid wax used in the present invention indicates wax-like physical properties (specifically, water resistance, plasticity, glossiness and / or opacity, etc.), has a melting point of 40 ° C. or more, and It refers to a solid thing. The melting point of the solid wax used in the present invention is not particularly limited as long as the effects of the present invention can be exerted as long as it is 40 ° C or higher, but is usually about 40 to 150 ° C, preferably about 40 to 130 ° C, and more preferably about 40 to 130 ° C. It is about 100 ° C. Specifically, petroleum-derived waxes such as paraffin wax and microcrystalline wax; synthetic waxes such as polyethylene wax, hydrogenated castor oil, and polypropylene wax; (stearyloxymethicone / dimethicone) copolymer, cetearylmethicone, and alkyl (C30-45). ) Silicone waxes such as cetearyl dimethicone crosspolymer; carnauba wax, candelilla wax, wood wax, rice bran wax, hazelau, urushi wax, sugar cane wax, palm wax, orange peel wax, orange flower wax, eucalyptus wax flower, cuticle narcissus flower wax Waxes derived from plants such as yellow wax, peach fruit wax, sweet acacia flower wax, tubellose flower wax; animal-derived waxes such as beeswax, salami beeswax, spermaceti, shellac wax, lanolin; montan (Referred cetanol, also as palmityl alcohol) cetyl alcohol, stearyl alcohol, higher alcohols solid form such as behenyl alcohol; box, ozokerite, waxes derived from mineral such as ceresin wax is like, but not limited to. In the external composition for skin of the present invention, only one of the above components (C) may be used alone, or two or more of them may be used in combination. Preferably, two or more types of the component (C) may be used in any combination, so that a higher effect of the present invention can be expected.
本発明には、上記のいずれの融点が４０℃以上の固形ワックスを用いてもよいが、より一層確実に高い本発明の効果を発揮し易いという観点から、好ましくは、石油由来ワックス、合成ワックス、シリコーンワックス、植物由来ワックス、動物由来ワックス、固形状高級アルコール、及びそれらを含む組合せが用いられ、より好ましくは、石油由来ワックス、合成ワックス、シリコーンワックス、固形状の高級アルコール、及びそれらを含む組合せが用いられ、更に好ましくは、石油由来ワックス、合成ワックス、シリコーンワックス、及びそれらを含む組合せが用いられ、特に好ましくは、合成ワックス、シリコーンワックス、及びそれらを含む組合せが用いられる。具体的には、好ましい（Ｃ）成分として、パラフィンワックス、マイクロクリスタリンワックス、ポリエチレンワックス、硬化ヒマシ油、ポリプロピレンワックス、（ステアロキシメチコン／ジメチコン）コポリマー、セテアリルメチコン、アルキル（Ｃ３０−４５）セテアリルジメチコンクロスポリマー、セチルアルコール、ステアリルアルコール、ベヘニルアルコール、及びそれらを含む組合せを挙げることができ、より好ましくは、パラフィンワックス、マイクロクリスタリンワックス、ポリエチレンワックス、硬化ヒマシ油、ポリプロピレンワックス、（ステアロキシメチコン／ジメチコン）コポリマー、セテアリルメチコン、アルキル（Ｃ３０−４５）セテアリルジメチコンクロスポリマー、及びそれらを含む組合せを挙げることができ、更に好ましくは、パラフィンワックス、マイクロクリスタリンワックス、ポリエチレンワックス、（ステアロキシメチコン／ジメチコン）コポリマー、及びそれらを含む組合せを挙げることができ、特に好ましくは、ポリエチレンワックス、（ステアロキシメチコン／ジメチコン）コポリマー、及びそれらを含む組合せを挙げることができる。 In the present invention, any of the above-mentioned solid waxes having a melting point of 40 ° C. or more may be used. However, from the viewpoint that the effect of the present invention can be more surely enhanced, preferably, a petroleum-derived wax or a synthetic wax is used. , Silicone waxes, plant-derived waxes, animal-derived waxes, solid higher alcohols, and combinations containing them, and more preferably petroleum-derived waxes, synthetic waxes, silicone waxes, solid higher alcohols, and the like. Combinations are used, more preferably petroleum-derived waxes, synthetic waxes, silicone waxes, and combinations containing them, and particularly preferably synthetic waxes, silicone waxes, and combinations containing them. Specifically, preferred components (C) include paraffin wax, microcrystalline wax, polyethylene wax, hydrogenated castor oil, polypropylene wax, (stearyloxymethicone / dimethicone) copolymer, cetearylmethicone, and alkyl (C30-45) cetearyl. Dimethicone crosspolymer, cetyl alcohol, stearyl alcohol, behenyl alcohol, and combinations containing them can be mentioned, and more preferably paraffin wax, microcrystalline wax, polyethylene wax, hydrogenated castor oil, polypropylene wax, (stearoxymethicone / dimethicone) ) Listing copolymers, cetearyl methicone, alkyl (C30-45) cetearyl dimethicone crosspolymers, and combinations comprising them And more preferably paraffin wax, microcrystalline wax, polyethylene wax, (stearoxymethicone / dimethicone) copolymer, and combinations containing them. Particularly preferred are polyethylene wax and (stearoxymethicone / dimethicone). Mention may be made of copolymers and combinations comprising them.
本発明の皮膚外用組成物における（Ｃ）成分の含有量は、用途や所望の効果の程度等に応じて適宜設定され得る。一例として、組成物全体に対して、（Ｃ）成分が、０．０１重量％以上、好ましくは０．１重量％以上、より好ましくは１重量％以上とするのがよい。（Ｃ）成分の含有量の上限値は特に限定されないが、一例として、組成物全体に対して、６０重量％以下とすればよく、好ましくは５０重量％以下とすればよく、より好ましくは４０重量％以下とすることができる。 The content of the component (C) in the composition for external use on the skin of the present invention can be appropriately set according to the use, the degree of the desired effect, and the like. As an example, the content of the component (C) is preferably 0.01% by weight or more, preferably 0.1% by weight or more, and more preferably 1% by weight or more based on the whole composition. Although the upper limit of the content of the component (C) is not particularly limited, it may be, for example, not more than 60% by weight, preferably not more than 50% by weight, more preferably not more than 40% by weight, based on the whole composition. % By weight or less.
更に本発明の皮膚外用組成物において、（Ａ）成分の含有量に対する（Ｃ）成分の含有量の比率については、特に限定されないが、より一層効果的に（Ａ）成分の皮膚残存性を向上させ得るという観点から、好ましくは、（Ａ）成分の総量１重量部当たり、（Ｃ）成分の含有量が総量で１重量部以上、好ましくは１０重量部以上、より好ましくは５０重量部以上となる比率が例示される。（Ａ）成分の含有量に対する（Ｃ）成分の含有量の比率の上限値も特に限定されないが、一例として、（Ａ）成分の総量１重量部あたり、（Ｃ）成分の含有量が総量で１０００重量部以下、好ましくは７５０重量部以下、より好ましくは５００重量部以下となる比率を例示することができる。 Furthermore, in the skin external composition of the present invention, the ratio of the content of the component (C) to the content of the component (A) is not particularly limited, but the skin persistence of the component (A) is more effectively improved. From the viewpoint that the component (A) can be used, the content of the component (C) is preferably 1 part by weight or more, preferably 10 parts by weight or more, more preferably 50 parts by weight or more per 1 part by weight of the total amount of the component (A). The following ratio is exemplified. Although the upper limit of the ratio of the content of the component (C) to the content of the component (A) is not particularly limited, for example, the content of the component (C) is 1 part by weight based on the total amount of the component (A). A ratio of 1000 parts by weight or less, preferably 750 parts by weight or less, more preferably 500 parts by weight or less can be exemplified.
本発明の皮膚外用組成物は更に、粉体を含有することが好ましい。粉体を配合することで、皮膚に適用した際にサラサラした良好な使用感が得られると共に、本発明による抗菌成分の皮膚残存性がより一層効果的に高められる。 It is preferable that the skin external composition of the present invention further contains a powder. By blending the powder, a good smooth feel when applied to the skin can be obtained, and the skin persistence of the antibacterial component according to the present invention can be more effectively enhanced.
本発明に用いられ得る粉体は、薬学的又は生理学的に許容され得る任意の粉体であり得る。具体的には、無水ケイ酸、マイカ、セリサイト、タルク、カオリン、酸化アルミニウム、ケイ酸アルミニウム、ケイ酸アルミニウムマグネシウム、ケイ酸マグネシウム、酸化マグネシウム、炭酸マグネシウム、炭酸マグネシウム、炭酸カルシウム、酸化ジルコニウム、酸化セリウム、炭化珪素、窒化ホウ素等の無機粉体；セルロースパウダー、ポリスチレンパウダー、ナイロンパウダー、ポリエチレンパウダー、ポリプロピレンパウダー、ポリスチレンパウダー等の有機粉体；等を挙げることができるが、これらに限定されない。より効果的に本発明の効果を向上させ得るという観点から、好ましくは無機粉体であり、より好ましくは無水ケイ酸、タルクであり、特に好ましくは無水ケイ酸である。本発明の皮膚外用組成物では、上記の粉体を１種のみで単独で用いてもよいし、２種以上を組み合わせて用いてもよい。 The powder that can be used in the present invention can be any pharmaceutically or physiologically acceptable powder. Specifically, silicic anhydride, mica, sericite, talc, kaolin, aluminum oxide, aluminum silicate, aluminum magnesium silicate, magnesium silicate, magnesium oxide, magnesium carbonate, magnesium carbonate, calcium carbonate, zirconium oxide, oxide Inorganic powders such as cerium, silicon carbide and boron nitride; organic powders such as cellulose powder, polystyrene powder, nylon powder, polyethylene powder, polypropylene powder and polystyrene powder; and the like, but are not limited thereto. From the viewpoint that the effects of the present invention can be more effectively improved, inorganic powders are preferable, silicic anhydride and talc are more preferable, and silicic anhydride is particularly preferable. In the composition for external use on the skin of the present invention, the above powders may be used alone or in combination of two or more.
本発明の皮膚外用組成物に粉体を配合する場合、その含有量は特に限定されないが、組成物全体に対して、好ましくは０．１〜３０重量％、より好ましくは１〜２０重量％、更に好ましくは５〜１５重量％程度とするのがよい。 When a powder is blended into the external composition for skin of the present invention, the content is not particularly limited, but is preferably 0.1 to 30% by weight, more preferably 1 to 20% by weight, based on the whole composition. More preferably, the content is about 5 to 15% by weight.
また、本発明の皮膚外用組成物に粉体を配合する場合、（Ａ）成分の含有量に対する粉体の含有量の比率も特に限定されないが、好ましくは、（Ａ）成分の総量１重量部あたり、粉体の含有量が総量で、１〜１０００重量部、より好ましくは１０〜５００重量部、更に好ましくは２０〜２００重量部程度とするのがよい。 In addition, when a powder is blended into the external composition for skin of the present invention, the ratio of the content of the powder to the content of the component (A) is not particularly limited, but preferably, the total amount of the component (A) is 1 part by weight. The total content of the powder is preferably 1 to 1000 parts by weight, more preferably 10 to 500 parts by weight, and still more preferably about 20 to 200 parts by weight.
本発明の皮膚外用組成物は更に、液状油分を含んでもよい。液状油分とは、２５℃で液体である油性成分のことをいい、薬学的又は生理学的に許容され得る任意の液状油分であり得る。具体的には、シリコーンオイル、脂肪酸エステル油、炭化水素類、液状高級アルール類等が挙げられるが、これらに限定されない。本発明の皮膚残存性効果をより高度に発揮させることができるという観点から、好ましくは、シリコーンオイルであり、より好ましくは、デカメチルシクロペンタシロキサン、メチルポリシロキサン、メチルフェニルポリシロキサン、ポリエーテル変性シリコーン、オクタメチルトリシロキサン、デカメチルテトラシロキサン、オクタメチルシクロテトラシロキサン、ドデカメチルシクロヘキサシロキサン、メチルハイドロジェンシリコーンであり、より好ましくはデカメチルシクロペンタシロキサン、メチルポリシロキサン、メチルフェニルポリシロキサン、ポリエーテル変性シリコーンであり、更に好ましくはデカメチルシクロペンタシロキサン、メチルポリシロキサンである。本発明の皮膚外用組成物では、上記の液状油分を１種のみで単独で用いてもよいし、２種以上を組み合わせて用いてもよい。 The external composition for skin of the present invention may further contain a liquid oil component. The liquid oil refers to an oily component that is liquid at 25 ° C., and may be any pharmaceutically or physiologically acceptable liquid oil. Specific examples include, but are not limited to, silicone oils, fatty acid ester oils, hydrocarbons, and liquid higher rules. From the viewpoint that the skin persistence effect of the present invention can be exhibited to a higher degree, preferably, it is a silicone oil, more preferably, decamethylcyclopentasiloxane, methylpolysiloxane, methylphenylpolysiloxane, or polyether-modified. Silicone, octamethyltrisiloxane, decamethyltetrasiloxane, octamethylcyclotetrasiloxane, dodecamethylcyclohexasiloxane, methyl hydrogen silicone, more preferably decamethylcyclopentasiloxane, methylpolysiloxane, methylphenylpolysiloxane, poly Ether-modified silicones, more preferably decamethylcyclopentasiloxane and methylpolysiloxane. In the composition for external use on the skin of the present invention, the above-mentioned liquid oils may be used alone or in combination of two or more.
本発明の皮膚外用組成物に液状油分を配合する場合、その含有量は特に限定されないが、組成物全体に対して、好ましくは１〜５０重量％、より好ましくは１０〜４０重量％、更に好ましくは１５〜３５重量％程度とするのがよい。 When a liquid oil component is added to the composition for external use on the skin of the present invention, the content thereof is not particularly limited, but is preferably 1 to 50% by weight, more preferably 10 to 40% by weight, and still more preferably, based on the whole composition. Is preferably about 15 to 35% by weight.
また、本発明の皮膚外用組成物に液状油分を配合する場合、（Ａ）成分の含有量に対する液状油分の含有量の比率も特に限定されないが、好ましくは、（Ａ）成分の総量１重量部あたり、液状油分の含有量が総量で、１０〜１０００重量部、より好ましくは５０〜８００重量部、更に好ましくは１００〜６００重量部程度とするのがよい。 When a liquid oil is blended into the composition for external use on skin of the present invention, the ratio of the content of the liquid oil to the content of the component (A) is not particularly limited, but preferably, the total amount of the component (A) is 1 part by weight. The total content of the liquid oil is preferably about 10 to 1000 parts by weight, more preferably about 50 to 800 parts by weight, and even more preferably about 100 to 600 parts by weight.
本発明の皮膚外用組成物は更に、界面活性剤を含んでもよい。界面活性剤を配合することにより、組成物の製剤的な安定性を高めることができ、本発明の（Ｂ）成分及び（Ｃ）成分による（Ａ）抗菌成分の皮膚残存性向上作用をより効果的に発揮させ易くなる。本発明の皮膚外用組成物に用いられ得る界面活性剤としては、薬学的又は生理学的に許容され得る任意の液状油分であり得る。具体的には、イソステアリルグリセリルエーテル（モノイソステアリルグリセリルエーテル、ジイソステアリルグリセリルエーテル等）、ミリスチルグリセリルエーテル（モノミリスチルグリセリルエーテル、ジミリスチルグリセリルエーテル等）、ラウリルグリセリルエーテル（モノラウリルグリセリルエーテル、ジラウリルグリセリルエーテル等）等のグリセリンアルキルエーテル；ポリオキシエチレン（以下、ＰＯＥという）−オクチルドデシルアルコールやＰＯＥ−２−デシルテトラデシルアルコール等のＰＯＥ−分岐アルキルエーテル；ＰＯＥ−オレイルアルコールエーテルやＰＯＥ−セチルアルコールエーテル等のＰＯＥ−アルキルエーテル；ソルビタンモノオレエート、ソルビタンモノイソステアレート及びソルビタンモノラウレート等のソルビタンエステル；ＰＯＥ−ソルビタンモノオレエート、ＰＯＥ−ソルビタンモノイソステアレート、及びＰＯＥ−ソルビタンモノラウレート等のＰＯＥ−ソルビタンエステル；グリセリンモノオレエート、グリセリンモノステアレート、及びグリセリンモノミリステート等のグリセリン脂肪酸エステル；ＰＯＥ−グリセリンモノオレエート、ＰＯＥ−グリセリンモノステアレート、及びＰＯＥ−グリセリンモノミリステート等のＰＯＥ−グリセリン脂肪酸エステル；ＰＯＥ−ジヒドロコレステロールエステル、ＰＯＥ−硬化ヒマシ油、及びＰＯＥ−硬化ヒマシ油イソステアレート等のＰＯＥ−硬化ヒマシ油脂肪酸エステル；ＰＯＥ−オクチルフェニルエーテル等のＰＯＥ−アルキルアリールエーテル；ＰＯＥ−モノステアリルグリセリルエーテル、ＰＯＥ−モノミリスチルグリセリルエーテル等のＰＯＥ−グリセリンアルキルエーテル；ジグリセリルモノステアレート、デカグリセリルデカステアレート、デカグリセリルデカイソステアレート、及びジグリセリルジイソステアレート等のポリグリセリン脂肪酸エステル等の各種非イオン界面活性剤：あるいはレシチン、水素添加レシチン、サポニン、サーファクチンナトリウム、コレステロール、胆汁酸などの天然由来の界面活性剤等を例示することができる。好ましくは、非イオン界面活性剤であり、より好ましくは、グリセリンアルキルエーテルである。本発明の皮膚外用組成物では、上記の界面活性剤を１種のみで単独で用いてもよいし、２種以上を組み合わせて用いてもよい。 The external composition for skin of the present invention may further contain a surfactant. By adding a surfactant, the formulation stability of the composition can be increased, and the effect of the component (B) and the component (C) of the present invention on the skin persistence of the antimicrobial component (A) can be more effectively improved. It becomes easy to show it. The surfactant that can be used in the external composition for skin of the present invention may be any pharmaceutically or physiologically acceptable liquid oil. Specifically, isostearyl glyceryl ether (monoisostearyl glyceryl ether, diisostearyl glyceryl ether, etc.), myristyl glyceryl ether (monomyristyl glyceryl ether, dimyristyl glyceryl ether, etc.), lauryl glyceryl ether (monolauryl glyceryl ether, Glycerin alkyl ethers such as lauryl glyceryl ether); POE-branched alkyl ethers such as polyoxyethylene (hereinafter referred to as POE) -octyldodecyl alcohol and POE-2-decyltetradecyl alcohol; POE-oleyl alcohol ether and POE-cetyl POE-alkyl ethers such as alcohol ethers; sorbitan monooleate, sorbitan monoisostearate and sorbitan monola Sorbitan esters such as POE-sorbitan monooleate, POE-sorbitan monoisostearate, and POE-sorbitan esters such as POE-sorbitan monolaurate; glycerin monooleate, glycerin monostearate, and glycerin monomyristate Glycerin fatty acid esters such as POE-glycerin monooleate, POE-glycerin monostearate, and POE-glycerin fatty acid esters such as POE-glycerin monomyristate; POE-dihydrocholesterol ester, POE-hardened castor oil, and POE- POE such as hydrogenated castor oil isostearate-fatty acid ester of hydrogenated castor oil; POE-alkyl aryl ether such as octyl phenyl ether; POE-monostearyl POE-glycerin alkyl ethers such as glyceryl ether and POE-monomyristyl glyceryl ether; polyglycerin fatty acid esters such as diglyceryl monostearate, decaglyceryl decastearate, decaglyceryl decaisostearate, and diglyceryl diisostearate; Examples of various nonionic surfactants: lecithin, hydrogenated lecithin, saponin, surfactin sodium, cholesterol, bile acids, and other naturally-derived surfactants. Preferably, it is a nonionic surfactant, and more preferably, it is a glycerin alkyl ether. In the composition for external use on skin of the present invention, one of the above surfactants may be used alone, or two or more thereof may be used in combination.
本発明の皮膚外用組成物に界面活性剤を配合する場合、その含有量は特に限定されないが、組成物全体に対して、好ましくは０．１〜１０重量％、より好ましくは０．５〜５重量％、更に好ましくは１〜２重量％程度とするのがよい。 When a surfactant is incorporated into the composition for external use on the skin of the present invention, the content thereof is not particularly limited, but is preferably 0.1 to 10% by weight, more preferably 0.5 to 5% by weight, based on the whole composition. %, More preferably about 1 to 2% by weight.
また、本発明の皮膚外用組成物に界面活性剤を配合する場合、（Ａ）成分の含有量に対する界面活性剤の含有量の比率も特に限定されないが、好ましくは、（Ａ）成分の総量１重量部あたり、界面活性剤の含有量が総量で、１〜１００重量部、より好ましくは３〜６０重量部、更に好ましくは５〜４０重量部程度とするのがよい。 When a surfactant is added to the composition for external use on the skin of the present invention, the ratio of the content of the surfactant to the content of the component (A) is not particularly limited, but preferably, the total amount of the component (A) is 1%. The total content of the surfactant per part by weight is preferably 1 to 100 parts by weight, more preferably 3 to 60 parts by weight, and still more preferably about 5 to 40 parts by weight.
本発明の皮膚外用組成物は、皮膚への適用後に抗菌成分が特に流れ落ち易い、汗をかきやすい皮膚の部位や状況下で用いられることが想定される。従って、本発明の皮膚外用組成物は、制汗成分も共に配合することが好ましい。制汗成分は、薬学的又は生理学的に許容され得る任意の制汗成分であり得る。具体的には、クロルヒドロキシアルミニウム、パラフェノールスルホン酸亜鉛、酸化亜鉛、塩化アルミニウム、硫酸アルミニウム、ブロモヒドロキシアルミニウム、硫酸アルミニウムカリウム等の収斂作用を有する成分が挙げられるが、これらに限定されない。本発明の（Ｂ）成分及び（Ｃ）成分による（Ａ）抗菌成分の皮膚残存性向上作用をより効果的に発揮させ易いという観点から、好ましくは、クロルヒドロキシアルミニウム、パラフェノールスルホン酸亜鉛が用いられ、より好ましくはクロルヒドロキシアルミニウムが用いられる。本発明の皮膚外用組成物では、上記の制汗成分を１種のみで単独で用いてもよいし、２種以上を組み合わせて用いてもよい。 The composition for external use of the skin of the present invention is assumed to be used under the site or the condition of the skin where the antibacterial component is particularly likely to run off after application to the skin and is easy to sweat. Therefore, it is preferable that the skin external composition of the present invention also contains an antiperspirant component. The antiperspirant component can be any pharmaceutically or physiologically acceptable antiperspirant component. Specific examples include, but are not limited to, components having an astringent action such as chlorohydroxyaluminum, zinc paraphenolsulfonate, zinc oxide, aluminum chloride, aluminum sulfate, bromohydroxyaluminum, and aluminum potassium sulfate. From the viewpoint that the component (B) and the component (C) of the present invention can more effectively exhibit the effect of improving the skin persistence of the antimicrobial component (A), chlorohydroxyaluminum and zinc paraphenol sulfonate are preferably used. And more preferably chlorohydroxyaluminum. In the composition for external use on the skin of the present invention, the above-mentioned antiperspirant component may be used alone or in combination of two or more.
本発明の皮膚外用組成物に制汗成分を配合する場合、その含有量は特に限定されないが、組成物全体に対して、好ましくは０．１〜３０重量％、より好ましくは０．５〜２５重量％、更に好ましくは１〜２０重量％程度とするのがよい。 When the antiperspirant component is added to the composition for external use on skin of the present invention, its content is not particularly limited, but is preferably 0.1 to 30% by weight, more preferably 0.5 to 25% by weight, based on the whole composition. % By weight, more preferably about 1 to 20% by weight.
また、本発明の皮膚外用組成物に制汗成分を配合する場合、（Ａ）成分の含有量に対する制汗成分の含有量の比率も特に限定されないが、好ましくは、（Ａ）成分の総量１重量部あたり、制汗成分の含有量が総量で、１〜１０００重量部、より好ましくは５〜７００重量部、更に好ましくは１０〜５００重量部程度とするのがよい。 When the antiperspirant component is added to the composition for external use on the skin of the present invention, the ratio of the content of the antiperspirant component to the content of the component (A) is not particularly limited, but preferably, the total amount of the component (A) is 1%. The total amount of the antiperspirant component is preferably 1 to 1000 parts by weight, more preferably 5 to 700 parts by weight, and still more preferably about 10 to 500 parts by weight per part by weight.
本発明の皮膚外用組成物は、更に前述した各成分に加えて、他の有用な作用を付加するため、保湿成分、抗炎症成分、皮脂吸着成分、紫外線散乱成分、紫外線吸収成分、DNA損傷の予防及び／又は修復作用を有する成分、美白成分、細胞賦活化成分、抗酸化成分、老化防止成分、角質柔軟成分、ビタミン類等の各種成分を１種または２種以上組み合わせて配合してもよい。これらの各成分としては、医薬品、医薬部外品、化粧品分野などにおいて使用され得るものであれば特に制限されず、任意のものを適宜選択し使用することができる。 The composition for external use on the skin of the present invention further includes, in addition to the above-mentioned components, other useful effects, a moisturizing component, an anti-inflammatory component, a sebum-adsorbing component, an ultraviolet scattering component, an ultraviolet absorbing component, and a DNA damage component. Various components such as a component having a preventive and / or repairing action, a whitening component, a cell activating component, an antioxidant component, an anti-aging component, a keratin softening component, and vitamins may be used alone or in combination of two or more. . Each of these components is not particularly limited as long as it can be used in the fields of pharmaceuticals, quasi-drugs, cosmetics, and the like, and any components can be appropriately selected and used.
本発明の皮膚外用組成物に、上記のような他の有用成分を配合する場合、その含有量は特に限定されないが、通常０．０１〜１５重量％、好ましくは０．１〜１０重量％、より好ましくは０．３〜５重量％程度とするのがよい。 When the other useful components as described above are added to the external composition for skin of the present invention, the content thereof is not particularly limited, but is usually 0.01 to 15% by weight, preferably 0.1 to 10% by weight, More preferably, the content is about 0.3 to 5% by weight.
また本発明の皮膚外用組成物は、上記各成分に加えて用途あるいは剤形に応じて、医薬品、医薬部外品、又は化粧品などの分野に通常使用される成分を適宜配合して調製され得る。配合できる成分としては、特に制限されないが、例えば、基剤又は担体、香料、酸化防止剤、保存剤、ｐＨ調整剤、キレート剤、安定化剤、刺激軽減剤、防腐剤、着色剤、分散剤等の添加剤を配合することができる。なお、これらの成分は１種単独で、または２種以上を任意に組み合わせて配合することができる。 In addition, the composition for external use on the skin of the present invention can be prepared by appropriately mixing components commonly used in the fields of pharmaceuticals, quasi-drugs, and cosmetics, in addition to the above components, depending on the use or dosage form. . The components that can be blended are not particularly limited, but include, for example, bases or carriers, flavors, antioxidants, preservatives, pH adjusters, chelating agents, stabilizers, stimulants, preservatives, coloring agents, and dispersants. And the like. In addition, these components can be mix | blended individually by 1 type or in combination of 2 or more types arbitrarily.
本発明の皮膚外用組成物は、基剤又は担体として、（Ｄ）水を含んでもよいが、その含有量は組成物全体に対して４０重量％以下とすることを特徴とする。本発明の皮膚外用組成物における（Ｄ）水の含有量が４０重量％を超えると、前述の（Ｂ）成分及び（Ｃ）成分による（Ａ）抗菌成分の皮膚残存性を向上させる効果が得られなくなるので好ましくない。より一層高い本発明の効果が得られやすいという観点から、好ましくは、組成物全体に対する（Ａ）成分の含有量を３０重量％以下、より好ましくは２０重量％以下、更に好ましくは１７重量％以下とするのがよく、特に好ましくは１６重量％以下とするのがよい。本発明の皮膚外用組成物における（Ｄ）水の含有量の下限値は、特に限定されないが、例えば全く含まないとしてもよく、１重量％以上としてもよく、更に２重量％以上としてもよい。 The composition for external use on the skin of the present invention may contain (D) water as a base or a carrier, and its content is 40% by weight or less based on the whole composition. When the content of water (D) in the composition for external use on the skin of the present invention exceeds 40% by weight, the effect of improving the skin persistence of the antibacterial component (A) by the components (B) and (C) is obtained. It is not preferable because it is no longer possible. From the viewpoint that a still higher effect of the present invention can be easily obtained, the content of the component (A) with respect to the entire composition is preferably 30% by weight or less, more preferably 20% by weight or less, and still more preferably 17% by weight or less. And particularly preferably 16% by weight or less. The lower limit of the content of (D) water in the composition for external use on skin of the present invention is not particularly limited, but may be, for example, not contained at all, may be 1% by weight or more, and may be 2% by weight or more.
本発明の皮膚外用組成物に用いられ得る（Ｄ）水以外の基剤又は担体としては、ジプロピレングリコール、１，３−ブチレングリコール、グリセリン、ジグリセリン、ポリエチレングリコール、プロピレングリコール、イソプレングリコールなどの多価アルコール；エチレングリコールモノメチルエーテル、エチレングリコールモノエチルエーテル、エチレングリコールモノプロピルエーテル、ジエチレングリコールモノメチルエーテル、ジエチレングリコールモノエチルエーテル、ジエチレングリコールモノプロピルエーテル、ジエチレングリコールモノブチルエーテル、プロピレングリコールモノエチルエーテル、プロピレングリコールモノプロピルエーテル、ジプロピレングリコールモノエチルエーテル、ジプロピレングリコールモノプロピルエーテルのようなグリコールエーテル；エチルセルロース、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロースのようなセルロース誘導体；ポリビニルピロリドン；カラギーナン；ポリビニルブチラート；ポリエチレングリコール；ジオキサン；ブチレングリコールアジピン酸ポリエステル；ミリスチン酸イソプロピル、ミリスチン酸オクチルドデシル、パルミチン酸イソプロピル、パルミチン酸セチル、イソノナン酸イソノニル、テトラ２−エチルヘキサン酸ペンタエリスリット、ホホバ油のようなエステル類；デキストリン、マルトデキストリンのような多糖類；イソプロパノールのような低級アルコール；等が挙げられるが、これらに限定されない。 Examples of the base or carrier other than water (D) that can be used in the external composition for skin of the present invention include dipropylene glycol, 1,3-butylene glycol, glycerin, diglycerin, polyethylene glycol, propylene glycol, and isoprene glycol. Polyhydric alcohols: 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, dipropylene glycol mono Glycol ethers such as propyl ether; cellulose derivatives such as ethylcellulose, hydroxypropylcellulose and hydroxypropylmethylcellulose; polyvinylpyrrolidone; carrageenan; polyvinylbutyrate; polyethyleneglycol; dioxane; butyleneglycol adipate polyester; isopropyl myristate and octyldodecyl myristate. Esters such as isopropyl palmitate, cetyl palmitate, isononyl isononanoate, pentaerythritol tetra-2-ethylhexanoate, jojoba oil; polysaccharides such as dextrin and maltodextrin; lower alcohols such as isopropanol; But not limited thereto.
香料としては、例えば、天然香料、合成香料、調合香料等が挙げられる。具体的には、炭化水素類、エステル類、エーテル類、ケトン類、アルデヒド類、ラクトン類、フェノール類、アルコール類等が挙げられるが、これらに限定されない。 Examples of the fragrance include a natural fragrance, a synthetic fragrance, and a compounded fragrance. Specific examples include, but are not limited to, hydrocarbons, esters, ethers, ketones, aldehydes, lactones, phenols, alcohols, and the like.
酸化防止剤としては、例えば、ジブチルヒドロキシトルエン、ブチルヒドロキシアニソール、ソルビン酸、亜硫酸ナトリウム、アスコルビン酸、アスコルビン酸誘導体、トコフェロール、トコフェロール誘導体、エリソルビン酸、Ｌ−システイン塩酸塩などが挙げられる。 Examples of the antioxidant include dibutylhydroxytoluene, butylhydroxyanisole, sorbic acid, sodium sulfite, ascorbic acid, ascorbic acid derivatives, tocopherol, tocopherol derivatives, erythorbic acid, L-cysteine hydrochloride, and the like.
ｐＨ調整剤としては、例えば、無機酸（塩酸、硫酸など）、有機酸（乳酸、乳酸ナトリウム、クエン酸、クエン酸ナトリウム、コハク酸、コハク酸ナトリウムなど）、無機塩基（水酸化カリウム、水酸化ナトリウムなど）、有機塩基（トリエタノールアミン、ジイソプロパノールアミン、トリイソプロパノールアミンなど）などが挙げられる。 Examples of the pH adjuster include inorganic acids (such as hydrochloric acid and sulfuric acid), organic acids (such as lactic acid, sodium lactate, citric acid, sodium citrate, succinic acid, and sodium succinate), and inorganic bases (such as potassium hydroxide and hydroxide). Sodium) and organic bases (such as triethanolamine, diisopropanolamine, and triisopropanolamine).
キレート剤としては、例えば、キレート剤としては、エチレンジアミン４酢酸（エデト酸）、エチレンジアミン４酢酸塩（ナトリウム塩（エデト酸ナトリウム：日本薬局方、ＥＤＴＡ−２Ｎａなど）、カリウム塩など）、フィチン酸、グルコン酸、ポリリン酸、メタリン酸などが挙げられる。 Examples of the chelating agent include, as chelating agents, ethylenediaminetetraacetic acid (edetic acid), ethylenediaminetetraacetic acid salt (sodium salt (sodium edetate: Japanese Pharmacopoeia, EDTA-2Na, etc.), potassium salt, etc.), phytic acid, Gluconic acid, polyphosphoric acid, metaphosphoric acid and the like can be mentioned.
安定化剤としては、例えば、ポリアクリル酸ナトリウム、ジブチルヒドロキシトルエン、ビチルヒドロキシアニソールなどが挙げられる。
刺激低減剤としては、例えば、甘草エキス、アルギン酸ナトリウムなどが挙げられる。
Examples of the stabilizer include sodium polyacrylate, dibutylhydroxytoluene, and bitylhydroxyanisole.
Examples of the stimulus reducing agent include licorice extract, sodium alginate and the like.
上記のような添加剤は、１種を単独で、又は２種以上を組み合わせて使用できる。 One of the above additives can be used alone, or two or more can be used in combination.
本発明の皮膚外用組成物は、医薬品、医薬部外品、又は化粧品などの分野で公知の任意の製剤形態で調製され得る。具体的には、固形外用剤、軟膏剤（リニメント剤、パスタ剤、硬膏剤等を含む）、クリーム剤、ジェル剤、乳液剤、懸濁剤、液剤、ミスト剤等の皮膚への適用に適した製剤形態を挙げることができるが、これらに限定されない。好ましくは、乳化工程を含む方法により調製される製剤（乳化製剤ともいう）である。また、より一層確実に高い本発明の効果が得られるという観点から、本発明の皮膚外用組成物は、常温で固体〜半固体の製剤形態であることが好ましく、固形外用剤、軟膏剤、クリーム剤であることがより好ましく、固形外用剤、軟膏剤であることが更に好ましく、とりわけ常温で固体である固形外用剤が好ましい。固形外用剤の形状は特に限定されず、例えば、スティック状（円柱状、楕円柱状、角柱状等）、球状、半球状等の任意の形状であり得る。このような製剤形態は、当業者に周知の任意の方法で調製することができる。 The composition for external use on the skin of the present invention can be prepared in any formulation known in the field of pharmaceuticals, quasi-drugs, cosmetics and the like. Specifically, it is suitable for application to the skin such as solid external preparations, ointments (including liniments, pastes, plasters, etc.), creams, gels, emulsions, suspensions, solutions, mists, etc. However, the present invention is not limited thereto. Preferably, it is a preparation (also referred to as an emulsion preparation) prepared by a method including an emulsification step. In addition, from the viewpoint that the effects of the present invention can be more reliably obtained, the composition for external use on the skin of the present invention is preferably in the form of a solid to semi-solid preparation at room temperature, and a solid external preparation, an ointment, and a cream Agents, more preferably solid external preparations and ointments, and particularly preferably solid external preparations that are solid at room temperature. The shape of the solid external preparation is not particularly limited, and may be, for example, any shape such as a stick (a column, an elliptic column, a prism, etc.), a sphere, a hemisphere, and the like. Such dosage forms can be prepared by any method known to those skilled in the art.
本発明の皮膚外用組成物の硬度は、本発明の効果を奏し得る限りにおいて、特に限定されない。一例として、後述の試験例に記載の方法と同様にしてレオメーター（RT-2010D・D−CW、（株）レオテック製等）でφ20mmの円筒形プランジャー（アダプター）を用い進入速度２cm／minで１cm進入させたときの硬度（２５℃）が、０．０５ｋｇｆ以上であることをいい、好ましくは０．１ｋｇｆ以上、より好ましくは０．５ｋｇｆ以上、更に好ましくは１ｋｇｆ以上、なかでも好ましくは２ｋｇｆ以上であることをいう。 The hardness of the external composition for skin of the present invention is not particularly limited as long as the effects of the present invention can be exerted. As an example, the penetration speed is 2 cm / min using a φ20 mm cylindrical plunger (adapter) with a rheometer (RT-2010D / D-CW, manufactured by Leotech Co., Ltd.) in the same manner as described in the test examples described below. The hardness (25 ° C.) when penetrated by 1 cm is 0.05 kgf or more, preferably 0.1 kgf or more, more preferably 0.5 kgf or more, still more preferably 1 kgf or more, and particularly preferably 2 kgf or more. It means that it is above.
本発明の皮膚外用組成物は、抗菌作用を持続的に発揮させることが望まれる任意の場面で使用され得る。具体的には、デオドラント剤等としての用途で用いられ得るが、限定されない。本発明によれば、皮膚に適用した抗菌成分が、汗等で流れ落ちにくくなり、適用した皮膚の部位に長く留まることができ、その抗菌作用を長期にわたり発揮できることが期待できる。かかる観点に鑑みれば、本発明の皮膚外用組成物は、汗をかきやすい皮膚の部位（例えば、腋の下や首筋等）や汗をかきやすい状況（例えば、夏などの暑い時期、激しい運動の前後等）に使用されることが多い、デオドラント剤（なかでも制汗デオドラント剤）として用いられることが好ましい。 The composition for external use on the skin of the present invention can be used in any situation where it is desired to continuously exert an antibacterial action. Specifically, it can be used for applications such as a deodorant agent, but is not limited thereto. ADVANTAGE OF THE INVENTION According to this invention, the antibacterial component applied to the skin becomes hard to flow down by sweat etc., can stay at the site | part of the applied skin for a long time, and it can be expected that the antibacterial effect can be exhibited for a long time. In view of such a viewpoint, the composition for external use of the skin of the present invention can be used for a sweaty skin site (for example, an armpit or a neck muscle) or a sweaty condition (for example, a hot season such as summer, before and after intense exercise, etc.). ), And is preferably used as a deodorant (among others, an antiperspirant deodorant).
本発明の皮膚外用組成物の使用方法は、使用対象の皮膚の状態、年齢、性別や使用する季節等の状況などによって異なるが、抗菌作用を発揮させることが望まれる任意の皮膚の部位に、適量（約０．００１〜０．１ｇ／ｃｍ２程度）を、塗布、噴霧などの当該分野で公知の任意の方法で適用する。本発明の皮膚外用組成物は、１日数回（例えば、１日あたり１〜５回程度）定期的に使用してもよく、抗菌作用を発揮させたいと望むタイミングで不定期で使用してもよい。使用期間も特に制限されず、例えば、数日（例えば、３日程度）〜３ヶ月程度、好ましくは１週間程度〜１ヶ月程度としてもよい。 The method of using the composition for external use of the skin of the present invention varies depending on the condition of the skin to be used, age, gender, seasons of use, and the like, but on any part of the skin where it is desired to exert an antibacterial action, An appropriate amount (about 0.001 to 0.1 g / cm 2 ) is applied by any method known in the art such as coating and spraying. The composition for external use on the skin of the present invention may be used regularly several times a day (for example, about 1 to 5 times a day), or may be used irregularly at a timing when it is desired to exert an antibacterial action. Good. The period of use is not particularly limited, and may be, for example, several days (for example, about three days) to about three months, preferably about one week to about one month.
（２．抗菌成分の皮膚残存性を高める方法）
前述したように、（Ａ）抗菌成分と、（Ｂ）シクロデキストリン系化合物と、（Ｃ）融点が４０℃以上である固形ワックスとを組み合わせて用い、更に（Ｄ）水の配合量を特定範囲内にすることにより、皮膚に適用された（Ａ）抗菌成分の皮膚残存性が高められることが確認されている。
従って、本発明は更に別の観点から、（Ａ）抗菌成分と、（Ｂ）シクロデキストリン系化合物と、（Ｃ）融点が４０℃以上である固形ワックスとを配合し、且つ（Ｄ）水の含有量が組成物全体に対して４０重量％以下となるように皮膚外用組成物を調製することを特徴とする、該外用組成物の（Ａ）成分の皮膚残存性を高める方法をも提供する。なお、本方法において、外用組成物への（Ａ）〜（Ｄ）成分の配合順序等は特に限定されない。また、該方法は、医学的な治療を意図しない美容方法としても実施され得る。
上記方法における（Ａ）〜（Ｄ）成分の種類やその配合割合、その他に配合され得る成分の種類やその配合割合、製剤形態、使用方法等は、上記「（１．皮膚外用組成物）」で記載されたものと同様である。
(2. Method for increasing the skin persistence of antibacterial components)
As described above, (A) an antimicrobial component, (B) a cyclodextrin-based compound, and (C) a solid wax having a melting point of 40 ° C. or more are used in combination, and (D) the amount of water is adjusted to a specific range. It has been confirmed that by setting the content inside, the skin persistence of the antibacterial component (A) applied to the skin is enhanced.
Therefore, the present invention further comprises (A) an antimicrobial component, (B) a cyclodextrin compound, (C) a solid wax having a melting point of 40 ° C. or more, and (D) water from another viewpoint. The present invention also provides a method for enhancing the skin persistence of the component (A) of the external composition, comprising preparing the composition for external use on the skin such that the content is 40% by weight or less based on the whole composition. . In the present method, the order of blending the components (A) to (D) into the external composition is not particularly limited. The method can also be practiced as a cosmetic method that is not intended for medical treatment.
In the above method, the types of the components (A) to (D) and the mixing ratio thereof, the types of the components that can be mixed and the mixing ratio thereof, the formulation, the method of use, and the like are described in the above “(1. External composition for skin)”. Are the same as those described in.
以下に、実施例に基づいて本発明を詳細に説明するが、本発明はこれらの実施例によって限定されるものではない。
（試験例１：抗菌成分の残存性評価）
抗菌成分の塗布部位における残存性を評価するために、以下の試験を行った。
下記表１に示す被験製剤を常法に従い調製した。具体的には、実施例１の被験製剤を例として説明すると、先ず油性成分のみを混合し加熱処理により溶解した油相と、残りの水性成分のみを混合し同様に加温処理して溶解させた水相とをそれぞれ用意し、それらをホモジナイザーで乳化させた後、常温まで冷却することで皮膚外用組成物を調製した。実施例１の製剤の硬度は、レオメーター（RT-2010D・D−CW、（株）レオテック製）により測定した。先ず、レオメーターの測定上限を２ｋｇｆに設定し、円筒形プランジャー（アダプター）φ20mmを設置した。プラ壺（20mL）に実施例１の製剤を擦り切り入れたものを、レオメーターに設置し、アダプター侵入速度を２cm/minとしてプラ壺中の実施例１の製剤に１cm侵入したときの硬度を測定した。その結果、実施例１の製剤の硬度は２ｋｇｆ以上であった。比較例１〜４の製剤も上記と同様にして調製を行った。
(Test Example 1: Evaluation of persistence of antibacterial component)
The following test was performed to evaluate the persistence of the antimicrobial component at the application site.
The test preparations shown in Table 1 below were prepared according to a conventional method. Specifically, the test preparation of Example 1 will be described as an example. First, only the oily component is mixed and dissolved by heat treatment, and only the remaining aqueous component is mixed and similarly heated and dissolved. Each aqueous phase was prepared, emulsified with a homogenizer, and then cooled to room temperature to prepare a skin external composition. The hardness of the preparation of Example 1 was measured with a rheometer (RT-2010D / D-CW, manufactured by Rheotech Co., Ltd.). First, the measurement upper limit of the rheometer was set to 2 kgf, and a cylindrical plunger (adapter) φ20 mm was installed. A preparation prepared by rubbing the preparation of Example 1 into a plastic pot (20 mL) was placed on a rheometer, and the hardness was measured when the adapter penetrated at a rate of 2 cm / min and penetrated 1 cm into the preparation of Example 1 in the plastic pot. did. As a result, the hardness of the preparation of Example 1 was 2 kgf or more. The preparations of Comparative Examples 1 to 4 were also prepared in the same manner as described above.
上記で調製した各被験製剤について、以下の手順で抗菌成分（イソプロピルメチルフェノール）の流出率を評価した。先ず、ＮＥＯカバーグラス（20mm×50mm、松浪硝子工業（株）製）の試験部位（2.4cm×1.5cm）に、上記表１に示す各被験製剤をそれぞれ約25mg塗布した。これを風乾させた後、精製水を10ml入れた遠心管に浸漬させて、約30分間にわたり超音波処理（SONIC CLEANER、アズワン（株）製）を該機器の取扱い説明書に準じて行った。この超音波処理後、浸漬液を２ml採取し、メタノール／水（７：３）混液２mlを加えて混合し、濾過した後、高速液体クロマトグラフィーにて各浸漬液中におけるイソプロピルメチルフェノールを定量した。次いで、各定量値から下式Ｉに従って、イソプロピルメチルフェノールの流出率（％）を算出した。
［式Ｉ］イソプロピルメチルフェノールの流出率（％）＝（各浸漬液中におけるイソプロピルメチルフェノール量／イソプロピルメチルフェノール量〔初期配合量〕）×100
For each of the test preparations prepared above, the outflow rate of the antibacterial component (isopropylmethylphenol) was evaluated by the following procedure. First, about 25 mg of each test preparation shown in Table 1 was applied to a test site (2.4 cm × 1.5 cm) of a NEO cover glass (20 mm × 50 mm, manufactured by Matsunami Glass Industry Co., Ltd.). This was air-dried, immersed in a centrifuge tube containing 10 ml of purified water, and subjected to ultrasonic treatment (SONIC CLEANER, manufactured by AS ONE Corporation) for about 30 minutes according to the instruction manual for the device. After the ultrasonic treatment, 2 ml of the immersion liquid was sampled, 2 ml of a mixed solution of methanol / water (7: 3) was added thereto, mixed, filtered, and then isopropyl methylphenol in each immersion liquid was quantified by high performance liquid chromatography. . Next, the outflow rate (%) of isopropylmethylphenol was calculated from each quantitative value according to the following formula I.
[Formula I] Outflow rate (%) of isopropylmethylphenol = (amount of isopropylmethylphenol in each immersion liquid / amount of isopropylmethylphenol [initial blending amount]) x 100
この結果を上記表１の最下欄に示す。上記結果から明らかなように本試験条件下において、（Ｂ）シクロデキストリンも（Ｃ）融点が４０℃以上である固形ワックス（パラフィン〔融点：５５℃〕、ポリエチレンワックス〔融点：７５〜９０℃〕、精製マイクロクリスタリンワックス〔融点：７０〜８５℃〕、（ステアロキシメチコン／ジメチコン）コポリマー〔融点：４０〜５０℃〕）も含まない比較例３の被験製剤は、塗布したイソプロピルメチルフェノールが約８６％も流出してしまう。そして、この比較例３の被験製剤に（Ｂ）成分のみ又は（Ｃ）成分のみを加えた比較例１、２の被験製剤では、イソプロピルメチルフェノールの流出率はやや抑えられたものの、まだ十分とは言えない。一方、全く予想外のことに、（Ａ）イソプロピルメチルフェノールと共に、（Ｂ）シクロデキストリン及び（Ｃ）融点が４０℃以上である固形ワックスを組み合わせて配合することにより、（Ａ）抗菌成分の残存率が高度に向上することが明らかとなった。そして、（Ｃ）融点が４０℃以上である固形ワックスに替えて、常温で液体のワックス（流動パラフィン）を使用し、（Ａ）抗菌成分と（Ｂ）シクロデキストリンを組み合わせて用いた場合には、本発明のような高い残存性は認められなかった（比較例４）。 The results are shown in the lowermost column of Table 1 above. As is clear from the above results, under the test conditions, (B) cyclodextrin is also (C) solid wax having a melting point of 40 ° C. or more (paraffin [melting point: 55 ° C.]), polyethylene wax [melting point: 75 to 90 ° C.] , Purified microcrystalline wax [melting point: 70-85 ° C.] and (Stearoxymethicone / dimethicone) copolymer [melting point: 40-50 ° C.] did not contain about 86 of isopropylmethylphenol applied. % Will be leaked. In the test preparations of Comparative Examples 1 and 2 in which only the component (B) or only the component (C) was added to the test preparation of Comparative Example 3, although the outflow rate of isopropylmethylphenol was slightly suppressed, it was still insufficient. I can't say. On the other hand, completely unexpectedly, the combination of (A) isopropyl methylphenol, (B) cyclodextrin and (C) a solid wax having a melting point of 40 ° C. or more is combined to form (A) residual antibacterial component. It was found that the rate improved significantly. When (C) a wax that is liquid at normal temperature (liquid paraffin) is used instead of the solid wax having a melting point of 40 ° C. or more, and (A) an antibacterial component and (B) cyclodextrin are used in combination, However, high persistence as in the present invention was not observed (Comparative Example 4).
（参考試験例１：抗菌成分の残存性評価）
抗菌成分の塗布部位における残存性について更に評価するために、以下の試験を行った。
下記表２に示す液体の形状の被験製剤を、上記試験例１と同様にして、常法により調製した。次いで上記試験例１と同様の手順で、超音波処理を行い、処理後の浸漬液中に含まれるイソプロピルメチルフェノールを定量して、イソプロピルメチルフェノール流出率（％）を算出した。
The following test was conducted to further evaluate the persistence of the antibacterial component at the application site.
Test preparations in the form of liquids shown in Table 2 below were prepared in the same manner as in Test Example 1 by a conventional method. Next, ultrasonic treatment was performed in the same procedure as in Test Example 1, and isopropyl methylphenol contained in the immersion liquid after the treatment was quantified to calculate the isopropyl methyl phenol outflow rate (%).
この結果を上記表２の最下欄に示す。上記結果に示されるように、（Ｄ）水を約６０重量％含有する液状の皮膚外用組成物とした場合には、（Ａ）抗菌成分と共に、（Ｂ）シクロデキストリン系化合物及び（Ｃ）融点が４０℃以上の固形ワックスを組み合わせて配合しても、イソプロピルメチルフェノールの流出率は高く、本発明のような塗布部位における優れた残存性は認められなかった。 The results are shown in the lowermost column of Table 2 above. As shown in the above results, when (D) a liquid external composition for skin containing about 60% by weight of water, (A) an antimicrobial component, (B) a cyclodextrin compound, and (C) a melting point However, even when a solid wax of 40 ° C. or more was combined, the outflow rate of isopropylmethylphenol was high, and excellent persistence at the application site as in the present invention was not observed.
（試験例２：抗菌成分の残存性評価）
抗菌成分の塗布部位における残存性について更に評価するために、以下の試験を行った。
下記表３に示す被験製剤を、上記試験例１と同様にして、常法により調製した。実施例の各被験製剤について、上記試験例１と同様の測定条件下でレオメーター（RT-2010D・D-CW、（株）レオテック製）により硬度（２５℃）を測定したところ、実施例２の製剤は２ｋｇｆ以上、実施例３の製剤は２ｋｇｆ以上、実施例４の製剤は０．５９ｋｇｆ、実施例５の製剤は０．１４ｋｇｆ、実施例６の製剤は２ｋｇｆ以上であった。次いで上記試験例１と同様の手順で、超音波処理を行い、処理後の浸漬液中に含まれる抗菌成分（イソプロピルメチルフェノール）を定量して、上記式Ｉによりイソプロピルメチルフェノール流出率（％）を算出した。
The following test was conducted to further evaluate the persistence of the antibacterial component at the application site.
The test preparations shown in Table 3 below were prepared in the same manner as in Test Example 1 by a conventional method. The hardness (25 ° C.) of each of the test preparations of the examples was measured with a rheometer (RT-2010D / D-CW, manufactured by Reotech Co., Ltd.) under the same measurement conditions as in Test Example 1 above. The formulation of Example 3 was 2 kgf or more, the formulation of Example 3 was 2 kgf or more, the formulation of Example 4 was 0.59 kgf, the formulation of Example 5 was 0.14 kgf, and the formulation of Example 6 was 2 kgf or more. Next, ultrasonic treatment was performed in the same procedure as in Test Example 1, and the antibacterial component (isopropylmethylphenol) contained in the immersion liquid after the treatment was quantified. Was calculated.
この結果を上記表３の最下欄に示す。上記結果に示されるように、本試験例においても、（Ａ）イソプロピルメチルフェノールと共に、（Ｂ）シクロデキストリン及び（Ｃ）融点が４０℃以上である固形ワックス（パラフィン〔融点：５５℃〕、ポリエチレンワックス〔融点：７５〜９０℃〕、精製マイクロクリスタリンワックス〔融点：７０〜８５℃〕、（ステアロキシメチコン／ジメチコン）コポリマー〔融点：４０〜５０℃〕、セチルアルコール〔融点：４６〜５５℃〕）を組み合わせて配合し、且つ（Ｄ）水の含有量を４０重量％以下とすることにより、上記試験例１の結果と同様に優れた（Ａ）イソプロピルメチルフェノール残存性が認められた（実施例２〜６）。 The results are shown in the lowermost column of Table 3 above. As shown in the above results, in this test example, together with (A) isopropylmethylphenol, (B) cyclodextrin and (C) solid wax having a melting point of 40 ° C. or more (paraffin [melting point: 55 ° C.]), polyethylene Wax [melting point: 75-90 ° C], Purified microcrystalline wax [melting point: 70-85 ° C], (Stearoxymethicone / dimethicone) copolymer [melting point: 40-50 ° C], cetyl alcohol [melting point: 46-55 ° C] ) And the content of water (D) of 40% by weight or less, excellent (A) isopropylmethylphenol persistence was observed in the same manner as in the results of Test Example 1 (executed). Examples 2-6).
（試験例３：抗菌成分の残存性評価）
抗菌成分の塗布部位における残存性について更に評価するために、以下の試験を行った。
下記表４に示す実施例７の被験製剤を、上記試験例１と同様にして、常法により調製した。この実施例７の製剤の硬度（２５℃）を、上記試験例１と同様の測定条件下でレオメーター（RT-2010D・D-CW、（株）レオテック製）を用いて測定したところ、２ｋｇｆ以上であった。比較例６〜７の製剤も上記と同様にして調製を行った。
次に、上記試験例１と同様にＮＥＯカバーグラス（24mm×50mm、松浪硝子工業（株）製）の試験部位（2.4cm×1.5cm）に、下記表４に示す各被験製剤をそれぞれ約25mg塗布した。これを風乾させた後、精製水を10ml入れた遠心管に浸漬させて、約15分間にわたり超音波処理（SONIC CLEANER、アズワン（株）製）を該機器の取扱い説明書に準じて行った。この超音波処理後、浸漬液を２ml採取し、これに有機溶媒を約２ml加えて10分間振とうした。次いで、この振とう処理後の混合液から２mlを採取し、メタノール／水混液を加えて混合し、濾過した後、高速液体クロマトグラフィーにて各浸漬液中における塩化ベンザルコニウム（ベンザルコニウム塩化物）を定量した。次いで、各定量値から下式ＩＩに従って、塩化ベンザルコニウムの流出率（％）を算出した。
［式ＩＩ］塩化ベンザルコニウムの流出率（％）＝（各浸漬液中における塩化ベンザル
コニウム量／塩化ベンザルコニウム量〔初期配合量〕）×100
The following test was conducted to further evaluate the persistence of the antibacterial component at the application site.
The test preparations of Example 7 shown in Table 4 below were prepared in the same manner as in Test Example 1 by a conventional method. The hardness (25 ° C.) of the preparation of Example 7 was measured using a rheometer (RT-2010D / D-CW, manufactured by Reotech Co., Ltd.) under the same measurement conditions as in Test Example 1 above. That was all. The preparations of Comparative Examples 6 and 7 were also prepared in the same manner as described above.
Next, in the same manner as in Test Example 1, about 25 mg of each test preparation shown in Table 4 below was placed on a test site (2.4 cm × 1.5 cm) of a NEO cover glass (24 mm × 50 mm, manufactured by Matsunami Glass Co., Ltd.). Applied. This was air-dried, immersed in a centrifuge tube containing 10 ml of purified water, and subjected to ultrasonic treatment (SONIC CLEANER, manufactured by AS ONE Corporation) for about 15 minutes according to the instruction manual for the device. After the ultrasonic treatment, 2 ml of the immersion liquid was collected, and about 2 ml of an organic solvent was added thereto, followed by shaking for 10 minutes. Next, 2 ml of the mixed solution after the shaking treatment was collected, mixed with a mixed solution of methanol and water, filtered, and then subjected to benzalkonium chloride (benzalkonium chloride) in each immersion liquid by high performance liquid chromatography. Was determined. Next, the outflow rate (%) of benzalkonium chloride was calculated from each quantitative value according to the following formula II.
[Formula II] Outflow rate (%) of benzalkonium chloride = (amount of benzalkonium chloride / amount of benzalkonium chloride in each immersion liquid [initial blending amount]) × 100
この結果を上記表４の最下欄に示す。（Ａ）抗菌成分として、イソプロピルメチルフェノールに代えて、塩化ベンザルコニウムについて塗布部位における残存性を評価したところ、塩化ベンザルコニウムの流出率は、（Ｃ）融点が４０℃以上である固形ワックス（パラフィン〔融点：５５℃〕、ポリエチレンワックス〔融点：７５〜９０℃〕、精製マイクロクリスタリンワックス〔融点：７０〜８５℃〕、（ステアロキシメチコン／ジメチコン）コポリマー〔融点：４０〜５０℃〕）を組み合わせ、且つ（Ｄ）水の含有量を４０重量％以下にすることでも流出率はかなり抑えられたものの（比較例６）、これに更に（Ｂ）シクロデキストリンを組み合わせることにより、塩化ベンザルコニウムの流出率をより一層効果的に抑制できることが認められた（実施例７）。シクロデキストリンの配合による塗布部位残存性の向上はこれまで知られておらず、このような本発明の残存性向上効果は予想外であった。 The results are shown in the lowermost column of Table 4 above. (A) When benzalkonium chloride was used as an antibacterial component in place of isopropylmethylphenol to evaluate the survivability at the application site, the outflow rate of benzalkonium chloride was (C) solid wax having a melting point of 40 ° C. or higher. (Paraffin [melting point: 55 ° C], polyethylene wax [melting point: 75-90 ° C], purified microcrystalline wax [melting point: 70-85 ° C], (stearoxymethicone / dimethicone) copolymer [melting point: 40-50 ° C]) By combining (B) and cyclodextrin (B) with cyclodextrin, the outflow rate was considerably suppressed by combining (D) with a water content of 40% by weight or less. It was confirmed that the outflow rate of the nickel could be more effectively suppressed (Example 7). Up to now, the improvement of the application site persistence by the addition of cyclodextrin has not been known, and such an effect of improving the persistence of the present invention was unexpected.
以下に本発明の製剤処方例を示す。処方例１〜７は全て、硬度（２５℃）が２ｋｇｆ以上である固形の制汗デオドラント剤である。
Hereinafter, formulation examples of the present invention are shown. Formulation Examples 1 to 7 are all solid antiperspirant deodorants having a hardness (25 ° C.) of 2 kgf or more.
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