JP7441217B2 - 脱毛または皮膚炎症抑制用組成物 - Google Patents
脱毛または皮膚炎症抑制用組成物 Download PDFInfo
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- JP7441217B2 JP7441217B2 JP2021521802A JP2021521802A JP7441217B2 JP 7441217 B2 JP7441217 B2 JP 7441217B2 JP 2021521802 A JP2021521802 A JP 2021521802A JP 2021521802 A JP2021521802 A JP 2021521802A JP 7441217 B2 JP7441217 B2 JP 7441217B2
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Description
脱毛治療のために現在まで様々な方法が試みられてきたが、外科的方法では頭皮再建術、脱毛部位縮小術及び組織拡張術による頭皮成形術と自己毛髪移植術などがある。前記外科的治療方法は効果面で優れる点があるが、患者の経済的、精神的負担が非常に大きいため、広く利用し難いという短所がある。
この他、様々な治療剤が利用されているが、代表的な外用剤であるミノキシジル(Minoxidil)は毛細管拡張機能があるので、頭皮に塗ることで脱毛を防ぐが、痒み、刺激などの副作用と、脱毛治療におけるアクティブ標的がまだはっきり明かされていないという問題がある。内服薬であるフィナステリド(finasteride)は脱毛を誘発する男性ホルモンDHT(5α‐dihydrotestosterone)の生成抑制作用を有するものであり、6ヶ月~1年程度の服用により、発毛または脱毛抑制効果が表れると知られている。しかし、服用を中止すれば2ヶ月以内に元の状態に戻るという問題点があり、生殖機能障害などの副作用が発生することがあると知られている。
よって、副作用がなく、人体に無害であり、持続的な脱毛抑制効果がある脱毛抑制剤の開発が要求されている実情である。
PTGDSは、プロスタグランジン(Prostaglandin)D2(PGD2)を生成する酵素であって、PGD2は脱毛症のない男性の頭皮より脱毛症がある男性の頭皮でより高い水準で存在することが明らかにされ、脱毛を引き起こす重要な要素として知られている(Garza et al.(2012)Sci.Transl.Med.4、126ra34)。また、PTGDSはPGD2を通じて炎症反応を調節することが明らかになり(R.Rajakariar et al.、PNAS、2007、104、20979‐20984)、炎症反応の媒介物質としてPTGDSの活性を抑制し、炎症反応を阻害することができる。
前記目的を達成するために、本発明の一実施例による脱毛または皮膚炎症抑制用組成物は、アメントフラボン及び柏子仁抽出物、ゲニステイン及びビオカニンAで構成された群から選択された一つ以上の成分を含む。
前記アメントフラボンは、前記組成物の総重量に対して0.1~1,000ppm含有することができる。アメントフラボンは、イワヒバ、カタヒバ、巻柏、扁柏及び銀杏で構成された群から選択された一つ以上から抽出されたものが挙げられる。
前記柏子仁抽出物は前記組成物の総重量に対して10~10,000ppm含有することができる。
ゲニステインは前記組成物の総重量に対して1~1,000ppm含有することができる。ゲニステインは、豆及びイソフラボンで構成された群から選択された一つ以上から抽出したものとすることができる。
前記ビオカニンAは前記組成物の総重量に対して10~1,000ppm含有することができる。ビオカニンAは降真香、豆、ムラサキツメクサ及びイソフラボンで構成された群から選択された一つ以上から抽出したものとすることができる。
前記組成物は、生体内でPTGDSの活性を抑制することができる。前記脱毛または皮膚炎症抑制用組成物は、化粧料を含み、化粧料の剤形は溶液、クリーム、ローション、シャンプー、ヘアトニック、スプレー及びゲルのなかから選択することができる。
前記脱毛または皮膚炎症抑制用組成物は、経皮注射または皮下注射を通して人体に投与することができ、皮膚外用剤または経口投与剤のいずれを選択してもよい。
前記皮膚は毛嚢及び頭皮が含まれる。
本発明において、有効成分として使用するアメントフラボンは、抗酸化作用(Mora A.et al.、Biochem.Pharmacol.、40(4)、pp793‐7、1990)、リンパ球増殖(lymphocyte proliferation)抑制作用(Lee SJ.et al.、Life Sci.、57(6)、pp551‐558、1995)、ホスホリパーゼ(phospholipase)C‐γ1酵素活性抑制作用(Lee HS.et al.、Planta.Med.、1996、62(4)、pp293‐296)、抗‐HIV作用、シクロオキシゲナーゼ(cyclooxygenase)及びリポキシゲナーゼ(lipoxygenase)を抑制することによる抗炎症作用(Kim HP.et al.、Prostaglandins Leukot Essent Fatty Acids、58(1)、pp17‐24、1998)、cAMP‐ホスホジエステラーゼ(cAMP‐phosphodiesterase)抑制作用、ウイルスに対する抗生作用、抗菌作用などについて研究された(Kim HK.et al.、Arch.Pharm.Res.、21(4)、pp406‐410、1998;Lin YM.et al.、Planta.Med.、65(2)、pp120‐125、1999;Krauze‐Baranowska M.et al.、Planta.Med.、65(6)、pp572‐573、1999)。
すなわち、本発明は効果的にPTGDSの活性を抑制して脱毛を引き起こす要素であるPGD2の生成を減少させて脱毛反応を抑制し、皮膚で発生する炎症反応を抑制することができる組成物を提供する。
前記薬学組成物は、アメントフラボンと、柏子仁抽出物、ゲニステイン及びビオカニンAで構成された群から選択された一つ以上の成分とを含む有効成分以外、防腐剤、安定化剤、水和剤または乳化促進剤、浸透圧調節のための塩及び/または緩衝剤などの薬剤学的補助剤、及びその他治療的に有用な物質をさらに含んでもよく、通常の方法によって様々な経口投与剤または非経口投与剤の形態で製剤化することができる。
本発明の一実施例において、前記組成物は化粧料組成物で使われてもよい。前記化粧料組成物には、ラクトコッカスラクチスW‐camellia菌株の湧出物以外、機能性添加物及び一般的化粧料組成物に含まれる成分がさらに含まれてもよい。前記機能性添加物としては、水溶性ビタミン、油溶性ビタミン、高分子ペプチド、高分子多糖、スフィンゴ脂質及び海草エキスからなる群から選択された成分を含むことができる。それ以外に含まれる配合成分としては、乳脂成分、保湿剤、エモリアント剤、界面活性剤、有機及び無機顔料、有機粉体、紫外線吸収剤、防腐剤、殺菌剤、酸化防止剤、植物抽出物、pH調整剤、アルコール、色素、香料、血行促進剤、冷感剤、制汗剤、精製水などが挙げられる。
本発明は、また、脱毛または皮膚炎症抑制方法に関する。前記脱毛または皮膚炎症抑制方法は、前述したような脱毛または皮膚炎症抑制用組成物を脱毛または皮膚炎症がある対象に適用する工程を含む。前記脱毛または皮膚炎症抑制方法は、脱毛または皮膚炎症を予防、改善及び/または治療方法を意味してもよい。
前記脱毛または皮膚炎症抑制用組成物は、皮膚に塗布して適用するものであってもよく、好ましくは、脱毛現象が心配されたり脱毛現象が表れた頭皮、または炎症が心配されたり炎症が表れた皮膚に塗布して適用するものであってもよい。前記組成物を顔に塗布する場合、柚オイルビードの香から心身の安定を得て熟眠を取るためにより有利である。
また、前記脱毛または皮膚炎症抑制用組成物は、1日1回、頭皮または皮膚に塗布すればよい。前記組成物に含まれたアメントフラボンと、柏子仁抽出物、ゲニステイン及びビオカニンAで構成された群から選択された一つ以上の成分との組み合わせがPTGDSの活性を抑制して脱毛を引き起こす要素であるPGD2の生成を減少させて脱毛反応を抑制し、皮膚で発生する炎症反応を抑制させて脱毛または皮膚炎症抑制に有利である。
また、前記脱毛または皮膚炎症抑制用組成物は、1日1回、3週~8週間皮膚へ塗布する時、より改善された脱毛または皮膚炎症抑制効果を示すことができる。前記脱毛または皮膚炎症抑制用組成物は、1日1回皮膚へ適用するだけでも優れた脱毛または皮膚炎症抑制効果を示し、通常、3週以上、好ましくは3週~8週間持続的に使用した時、とても優れる脱毛または皮膚炎症抑制効果を示す。
前記脱毛または皮膚炎症抑制用組成物の1回適用量は、脱毛または皮膚炎症を経験している対象の状態、睡眠障害度合い、塗布面積及び組成物の形態によって異なるが、通常25mg~150mgとすることができ、前記1回適用量の範囲内で適宜調節して塗布することができる。
<実施例1~3>
精製水1000mlに、アメントフラボンに加え、柏子仁抽出物、ゲニステイン及びビオカニンAで構成された群から選択された一つ以上の成分を添加した後、撹拌した。具体的な有効成分の含量を表1に示す。
比較例の組成物は、実施例1~3で利用した同一な有効成分を単独で使用するが、成分含量が10倍になるように製造した。具体的には、精製水1000mlにアメントフラボン、柏子仁抽出物、ゲニステイン及びビオカニンAのうちの1種を添加した後、撹拌する。具体的な有効成分の含量は表1のとおりである。
PTGDSに酵素反応の基質であるプロスタグランジンH2(PGH2)を処理してプロスタグランジンD2(PGD2)を生成するが、実施例1~実施例3で製造された組成物を一緒に投入した後、PGD2の生成減少量を測定してPTGDS活性抑制効果を確認した。
前記PGD2の生成量測定は、酵素結合免疫吸着測定法(ELISA)によって測定した。酵素結合免疫吸着測定法(ELISA)の実施は以下の工程で行われた。
(a)実施例1~3を固体基質の表面にコーティングする工程、
(b)PTGDSと前記PGH2を反応させる工程、
(c)前記工程(b)の結果物を酵素が結合された二次抗体と反応させる工程及び
(d)前記酵素の活性をELISA readerで410nmでの吸光度測定を通じて示す工程を含む。
本発明の実施例1~3によって製造された組成物100mg、ラクトース400mg、とうもろこし澱粉400mg及びステアリン酸マグネシウム2mgを混合した後、通常の錠剤の製造方法にしたがって打錠して錠剤を製造した。
<剤形例2>カプセル剤
本発明の実施例1~3によって製造された組成物100mg、ラクトース400mg、とうもろこし澱粉400mg及びステアリン酸マグネシウム2mgを混合した後、通常のカプセル剤の製造方法にしたがってゼラチンカプセルに充填してカプセル剤を製造した。
<剤形例3>顆粒剤
本発明の実施例1~3によって製造された組成物50mg、無水結晶葡萄糖250mg及び澱粉550mgを混合し、流動層顆粒機を利用して顆粒に成形した後、袋に充填した。
<剤形例4>ドリンク剤
本発明の実施例1~3によって製造された組成物50mg、葡萄糖10g、クエン酸0.6g及び液相オリゴ糖25gを混合した後、精製水300mlを加えて各ボトルに200mlずつ充填した後、130℃で4~5秒間殺菌してドリンク剤を製造した。
Claims (10)
- アメントフラボン(Amentoflavone)と、
柏子仁抽出物と、
を含む脱毛または皮膚炎症抑制用組成物。 - 前記アメントフラボンは、前記組成物の総重量に対して0.1ないし1,000ppm含有される請求項1に記載の脱毛または皮膚炎症抑制用組成物。
- 前記アメントフラボンは、イワヒバ、カタヒバ、巻柏、扁柏及び銀杏で構成された群から選択された一つ以上から抽出されたものである請求項1に記載の脱毛または皮膚炎症抑制用組成物。
- 前記柏子仁抽出物は、前記組成物の総重量に対して10ないし10,000ppm含有される請求項1に記載の脱毛または皮膚炎症抑制用組成物。
- 前記組成物は、生体内でPTGDS(Prostagladin D2 Synthase)の活性を抑制するものである請求項1に記載の脱毛または皮膚炎症抑制用組成物。
- 前記脱毛または皮膚炎症抑制用組成物は化粧料である請求項1に記載の脱毛または皮膚炎症抑制用組成物。
- 前記化粧料の剤形は、溶液、クリーム、ローション、シャンプー、ヘアトニック、スプレー及びゲルの中で選択される請求項6に記載の脱毛または皮膚炎症抑制用組成物。
- 前記脱毛または皮膚炎症抑制用組成物は、経皮注射または皮下注射を通じて人体に投与されるものである請求項1に記載の脱毛または皮膚炎症抑制用組成物。
- 前記脱毛または皮膚炎症抑制用組成物は、皮膚外用剤または経口投与剤である請求項1に記載の脱毛または皮膚炎症抑制用組成物。
- 前記皮膚は毛嚢及び頭皮を含む請求項1に記載の脱毛または皮膚炎症抑制用組成物。
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