JP2013541543A - 封入状活性剤を含む皮膚係合部材 - Google Patents
封入状活性剤を含む皮膚係合部材 Download PDFInfo
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- JP2013541543A JP2013541543A JP2013533012A JP2013533012A JP2013541543A JP 2013541543 A JP2013541543 A JP 2013541543A JP 2013533012 A JP2013533012 A JP 2013533012A JP 2013533012 A JP2013533012 A JP 2013533012A JP 2013541543 A JP2013541543 A JP 2013541543A
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- 150000003712 vitamin E derivatives Chemical class 0.000 description 1
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Abstract
Description
本発明の皮膚係合部材は、少なくとも1つの封入状活性剤を含む。一実施形態では、かかる少なくとも1つの封入状活性剤の量は、かかる皮膚係合部材の約0.01重量%〜約50重量%、あるいは約10重量%〜約45重量%、あるいは約15重量%〜約35重量%である。一実施形態では、皮膚係合部材は2つ以上の封入化活性剤を含むが、これはつまり、封入状活性剤と共に含有される冷却剤、並びに/又はナノ粒子及び/若しくはマイクロ粒子の製造に用いられる材料のいずれかが異なることを意味する。
一実施形態では、ナノ粒子及びマイクロ粒子は、米国特許第7,115,282号に概して記載されるナノスフェア及び/又はマイクロスフェアである。用語「粒子」は、固体で、実質的に球形の微粒子の記述を意図する。当然のことながら、本発明の教示に従ってその他の形状を形成することができる。本発明のナノ粒子は本来疎水性である。一実施形態では、ナノ粒子は、約0.01マイクロメートル〜約10マイクロメートル、又は約0.05マイクロメートル〜約5マイクロメートル、又は約0.1マイクロメートル〜約2マイクロメートルの範囲の平均直径を有する。任意の個々の粒子のこの線寸法は、粒子表面上の2点を結んだ最長の直線の長さを表す。
本発明のナノ粒子を形成するのに好適なカプセル材料は、約30℃〜約90℃の範囲の融点を有する不活性で無毒性の疎水性材料である。疎水性材料の例としては、蜜蝋、ラノリン、及びセラックワックスなどの動物ろう、カルナバ、キャンデリラ、サトウキビ、コメヌカ、及びヤマモモワックスなどの植物ろう、パラフィン及び微晶性ワックスを含む石油ワックスなどのミネラルワックス、並びにこれらの混合物などの天然、再生、又は合成ワックスが挙げられる。本発明で使用できるその他の疎水性材料としては、ワックス及びシリコンコポリマー、例えばキャンデリラワックス及びシリコーンコポリマー、オゾケライト(ozokrite)ワックス及びシリコンコポリマー、蜜蝋及びシリコンコポリマーなどが挙げられる。本発明で使用できるその他の疎水性化合物としては、エチルステアレート、イソプロピルミリステート、及びイソプロピルパルミテートなどの脂肪酸エステル、セトステアリルアルコール、セチルアルコール、ステアリルアルコール、及びオレイルアルコールなどの高分子量脂肪族アルコール、固体の硬化ヒマシ油及び植物油、固形パラフィン、硬い脂肪、並びにこれらの混合物が挙げられる。使用できるその他の疎水性化合物としては、好ましくは少なくとも食品グレードの純度を有するトリグリセリドが挙げられ、合成又は天然源からの単離により製造され得る。天然源としては、長鎖トリグリセリド(LCT)源としての動物脂又は植物油、例えば大豆油を挙げてよい。本発明で用いるのに好適なその他のトリグリセリドは、大部分の中程度の長さの脂肪酸(C10〜18)からできており、中鎖トリグリセリド(MCT)と表される。このようなトリグリセリド脂肪酸部分は不飽和又は多価不飽和であってよく、様々な脂肪酸物質を有するトリグリセリドの混合物であってよい。ナノ粒子カプセル材料は、単一の疎水性材料、又は複数の材料の混合物を含んでよい。当業者に周知であるその他好適な疎水性材料は、Bennett F.A.I.C.,「Industrial Waxes」Vol.I and II,Chemical Publishing Company Inc.,1975、及びMartindale,「The Extra Pharmacopoeia」,The Pharmaceutical Press,28th Edition pp.1063〜1072,1982に記載されている。
本発明のマイクロ粒子を形成するための感水性材料は、水溶性及び水分散性合成ポリマー及びコポリマー、デンプン誘導体、多糖類、ヒドロコロイド、天然ゴム類、タンパク質、並びにこれらの混合物を含む。
i.ナノ粒子
本発明のナノ粒子中の封入状活性剤は、(1)疎水性材料を融点を超える温度まで加熱して溶解物を形成する工程、(2)かかる活性成分を溶解物中に溶解又は分散する工程、(4)溶解物を水相に乳化する工程、及び(5)分散物を周囲温度まで冷却して微細懸濁液を形成する工程によって調製できる。活性成分を疎水性固体ナノ粒子内に混入できる。ナノ粒子の形成工程において、好ましくは約1重量%〜約80重量%、より好ましくは約1重量%〜約60重量%の活性成分が用いられる。
本発明の封入状活性剤は、(a)第1の活性剤をナノ粒子の疎水性内部に混入する工程、(b)第2の活性剤と、ナノ粒子と、感水性材料とを含む水性混合物を形成する工程、及び(c)本発明の混合物を噴霧乾燥して乾燥粉末組成物を形成する工程によって調製できる。その結果、ナノ粒子をマイクロ粒子構造内に封入できる。第1及び第2の活性剤は同じであっても異なっていてもよく、又はナノ粒子若しくはマイクロ粒子内に活性剤のみが存在する場合もある。
(i)疎水性材料をその材料の融点を超える温度まで加熱して溶解物を形成する工程、
(ii)第1のかかる芳香剤又はフレーバを溶解物中に溶解又は分散する工程、
(iii)第1のかかる活性成分を溶解物中に溶解又は分散する工程、
(iv)第2の活性成分、及びデンプン誘導体、天然ゴム類、ポリビニルアルコール、タンパク質、ヒドロコロイド、又はこれらの混合物などの感湿性材料を水相中に溶解又は分散する工程、
(v)組成物を疎水性材料の融解温度を超えるまで加熱する工程、
(vi)加熱した溶解物を水相と混合して分散物を形成する工程、
(vii)約1マイクロメートル〜約2マイクロメートルの粒径を有する均質な微細分散物が得られるまで、融解温度を超える温度で分散物を高剪断均質化する工程、
(viii)分散物を周囲温度まで冷却する工程、並びに
(ix)乳化された混合懸濁液を噴霧乾燥して乾燥粉末組成物を形成する工程。
局所適用に汎用される様々なスキンケア活性剤(「活性剤」)をナノ粒子及び/又はマイクロ粒子内に存在させてよい。一実施形態では、封入状活性剤は、冷却剤を非限定的に含む1つ以上の活性成分を含有する。好適な冷却剤の非限定例としては、L−メントール、p−メタン−3,8−ジオール、イソプレゴール、メントキシプロパン−1,2,−ジオール、クルクミン、メンチルラクテート(例えばSymriseのFrescolat ML)、ジンゲロール、イシリン、茶木油、メチルサリシレート、樟脳、ペパーミントオイル、N−エチル−p−メンタン−3−カルボキサミド、エチル3−(p−メンタン−3−カルボキサミド)アセテート、2−イソプロピル−N,2,3−トリメチルブチルアミド、メントングリセロールケタール、メントングリセリン(Glyerine)アセタール、Coolact 10、及びこれらの混合物が挙げられる。これら及びその他の冷却剤が周知であり、米国特許出願公開第2008/0300314A1号、米国特許第5,451,404号、及び同第7,482,373号など様々な公表文献に記載されている。更に別の実施形態では、冷却剤は、様々な剃毛補助剤での使用について前述した1つ以上の冷却剤を含む。例えば、米国特許第5,095,619号、同第5,713,131号、同第5,095,619号、同第5,653,971号、同第6,298,558号、同第6,944,952号、及び同第6,295,733号を参照のこと。
皮膚係合は、マトリックス材料中、又は材料上に封入状活性剤を含む。マトリックス材料は、固体ポリマーマトリックス又は皮膚軟化剤の形状であってよい。
一実施形態では、マトリックスは、ポリエチレンオキシド、ポリビニルピロリドン、ポリアクリルアミド、ポリヒドロキシメタクリレート、ポリビニルイミダゾリン、ポリエチレングリコール、ポリビニルアルコール、ポリヒドロキシエチルメタクリレート(polyhydroxyethymethacrylate)、シリコーンポリマー、及びこれらの混合物のうち少なくとも1つを含む水溶性ポリマーを含む。一実施形態では、かかる水溶性ポリマーは、ポリエチレンオキシド、ポリエチレングリコール、及びこれらの混合物からなる群から選択される。
別の実施形態では、マトリックス材料は少なくとも1つの皮膚軟化剤を含む。一実施形態では、皮膚軟化剤は疎水性である。特定の実施形態では、組成物は、25℃で流体を形成し得る1つ以上の皮膚軟化剤から本質的になってよい。皮膚軟化剤が流体状の場合、流体は好ましくは以下に開示するような皮膚係合リザーバ内に含有される。そのような実施形態では、組成物の粘度に応じて可変的な開口部寸法を利用し、使用中の皮膚軟化剤の分配を制御してよい。
一実施形態では、皮膚係合部材は更に担体を含み、マトリックス材料及び封入状活性剤は、担体中に含有及び/又は担体上に存在できる。上述のように、マトリックス材料は、固体ポリマーマトリックス又は固体若しくは非固体状の皮膚軟化剤であってよい。担体は、マトリックス材料及び封入状活性剤が適用されるトレーの形状であってよく、又は担体は、マトリックス及び封入された材料を少なくとも部分的に含有する保持構造を形成してよい。一実施形態では、担体は、米国特許第6,298,558号、及び同第7,581,318号に開示されるシースなどのリザーバを形成する。マトリックス材料が流体状の皮膚軟化剤を含む場合、担体は好ましくは、皮膚軟化剤の分配を制御するための1つ以上の分配開口部を有するシースである。皮膚係合部材の構成に関するとき、本明細書で定義される重量パーセントは、特に定めがない限り、担体ではなく開示される皮膚係合部材の構成要素に基づいて決定される。
i.任意の冷却剤
マトリックス材料は、未封入の不揮発性冷却剤又は皮膚鎮静剤のシクロデキストリンとの包接錯体を、好ましくは皮膚係合部材の最大約25重量%、最も好ましくは10〜20重量%の量で含んでもよい。本明細書で用いるとき「未封入」とは、追加の活性剤が封入体の外側に存在し、マトリックス材料の残部内に分散されていることを意味する。不揮発性冷却剤とは、皮膚において生理学的冷却効果を有し、メントールより揮発性がかなり低い薬剤を意味する。好ましくは、不揮発性冷却剤は、熱重量分析(例えば、Dupontの951 Thermogravimetric Analyzerを1分あたり20℃の温度上昇で用いて)にかけると、160℃の温度において初期重量の少なくとも50%、より好ましくは160℃の温度において初期重量の少なくとも80%、最も好ましくは175℃の温度において初期重量の少なくとも50%を保持するものである。
除毛装置は通常、除毛ヘッドと、除毛ヘッドが取り付けられるハンドル、つまり把持部とを含む。除毛装置は、手動又は電動であってよく、湿式及び/又は乾燥用途で用いてよい。除毛ヘッドは、除毛装置が脱毛器具と共に使用される場合は幅広いこすり落とし表面を含み得、又は装置が剃毛かみそりである場合はかみそりカートリッジを含み得る。除毛ヘッドは、交換可能であり得る、又はカートリッジ連結構造体に枢動可能に接続され得る。一態様では、カートリッジ連結構造体は、除毛ヘッドを解除可能に係合するために少なくとも1つのアームを含む。
本発明の皮膚係合部材は、射出成形、加圧成形、含浸、スプレーコーティング、カレンダー工法、及び押出成形などの任意の適当な方法で作製されてよいが、後者が好ましい。ストリップの構成成分の全ては、成形又は押出成形の前にブレンドされる。最良の結果として、構成成分は乾燥していることが好ましい。
図1及び図2を参照すると、かみそりカートリッジ14はハウジング16を含み、このハウジング16は3枚のブレード18、フィン付きエラストマーガード20、及びカートリッジの皮膚係合部分(この場合ではキャップ)上に配置された皮膚係合部材22を含む。皮膚係合部材22は2層を有するように示され、第1の層はマトリックス及び本発明の封入状活性剤であってよく、第2の層は従来の剃毛補助剤であってよく、又はその逆であってよい。皮膚係合部材は、カートリッジ後部の開口部に中に好ましくは固定される(接着剤、嵌合具、又は溶融結合により)。図3に示す皮膚係合部材32は、皮膚係合部材32が全体的に均質な組成物、及び均一でわずかに湾曲した上部平面を有すること以外は、皮膚係合部材22と同様である。この種の皮膚係合部材も、楔型状断面(図4の要素42に示す)又は任意のその他所望の形状で作製できる。皮膚係合部材は、サンドイッチ構成又は図4の要素52に示すようなシース/コア構成など、2つ以上の層で構成してもよい。
b)ポリスチレン731G HIPS(Nova Chemicals)
c)Polyox Coag,N750及びCarbowax 4600G(Dow Chemical)
d)ポリカプロラクトンCAPA 6505(Solvay)
e)(押出成形後のL−メントール)×100/(押出成形前のL−メントール)によって値を決定する。
Claims (14)
- 除毛装置(14)に使用される皮膚係合部材(22)であって、
a.水溶性ポリマー、皮膚軟化剤、及びこれらの混合物のうち少なくとも1つを含むマトリックスと、
b.前記皮膚係合部材の0.01重量%〜50重量%の量の封入状活性剤であって、マイクロ粒子内に封入された少なくとも1つのナノ粒子を含み、前記ナノ粒子が疎水性材料を含む外殻を含み、前記マイクロ粒子が感水性材料を含む外殻を含む、封入状活性剤と、
を含み、
前記ナノ粒子及び前記マイクロ粒子のうち少なくとも1つがスキンケア活性剤を含み、前記マイクロスフェアが2.0マイクロメートル〜100マイクロメートルの寸法を有し、前記少なくとも1つのナノスフェアが0.01マイクロメートル〜5マイクロメートルの寸法を有する、皮膚係合部材。 - 前記少なくとも1つのスキンケア活性剤が、L−メントール、p−メタン−3,8−ジオール、イソプレゴール、メントキシプロパン−1,2,−ジオール、クルクミン、メンチルラクテート(例えばSymriseのFrescolat ML)、ジンゲロール、イシリン、茶木油、メチルサリシレート、樟脳、ペパーミントオイル、N−エチル−p−メンタン−3−カルボキサミド、エチル3−(p−メンタン−3−カルボキサミド)アセテート、2−イソプロピル−N,2,3−トリメチルブチルアミド、メントングリセロールケタール、メントングリセリンアセタール、Coolact 10、及びこれらの混合物からなる群から選択される冷却剤を含む、請求項1又はその任意の従属請求項に記載の皮膚係合部材。
- 前記冷却剤が、1:4〜4:1の範囲の重量比のメントール及びメンチルラクテートの混合物である、請求項2又はその任意の従属請求項に記載の皮膚係合部材。
- 前記疎水性材料が、アルキル化ポリビニルピロリジン、硬化ヒマシ油、硬化植物油、固形パラフィン、固形脂肪、トリグリセリド、及びこれらの混合物からなる群から選択される、請求項1〜3のいずれか一項に記載の皮膚係合部材。
- 前記感水性材料が、水溶性及び水分散性合成ポリマー及びコポリマー、デンプン誘導体、多糖類、ヒドロコロイド、天然ゴム、タンパク質、並びにこれらの混合物のうち1つ以上を含む、請求項1〜4のいずれか一項に記載の皮膚係合部材。
- 前記感水性材料が、75%〜100%の加水分解度を有するポリビニルアルコールを含む、請求項7又はその任意の従属請求項に記載の皮膚係合部材。
- 前記疎水性材料が、アルキル化ポリビニルピロリジン、硬化ヒマシ油、硬化植物油、固形パラフィン、固形脂肪、トリグリセリド、及びこれらの混合物からなる群から選択され、前記感水性材料が、水溶性及び水分散性合成ポリマー及びコポリマー、デンプン誘導体、多糖類、ヒドロコロイド、天然ゴム、タンパク質、並びにこれらの混合物のうち1つ以上を含み、前記マイクロスフェアが、約2.0マイクロメートル〜約100マイクロメートルの寸法を有し、前記少なくとも1つのナノスフェアが、約0.01マイクロメートル〜約5マイクロメートルの寸法を有する、請求項1〜6のいずれか一項に記載の皮膚係合部材。
- 前記マトリックスの前記水溶性ポリマーが、ポリエチレンオキシド、ポリビニルピロリドン、ポリアクリルアミド、ポリヒドロキシメタクリレート、ポリビニルイミダゾリン、ポリエチレングリコール、ポリビニルアルコール、ポリヒドロキシエチルメタクリレート、シリコーンポリマー、及びこれらの混合物のうち少なくとも1つを含む、請求項1〜7のいずれか一項に記載の皮膚係合部材。
- 前記水溶性ポリマーの量が、前記固体ポリマーマトリックスの約50重量%〜約100重量%の量である、請求項8又はその任意の従属請求項に記載の皮膚係合部材。
- 前記マトリックスが、ポリエチレン、ポリプロピレン、ポリスチレン、高耐衝撃性ポリスチレン、ブタジエンスチレンコポリマー、ポリアセタール、アクリロニトリル−ブタジエンスチレンコポリマー、エチレンビニルアセテートコポリマー、及びこれらの混合物のうち少なくとも1つを含む非水溶性ポリマーを更に含む、請求項1〜9のいずれか一項に記載の皮膚係合部材。
- 前記非水溶性ポリマーが、前記固体ポリマーマトリックスの少なくとも35重量%の量で存在する、請求項10又はその任意の従属請求項に記載の皮膚係合部材。
- 前記マトリックス材料が皮膚軟化剤を含む、請求項1〜11のいずれか一項に記載の皮膚係合部材。
- 前記マトリックスが、ジブロックコポリマー、トリブロックコポリマー、マルチブロックコポリマー、ラジアルブロックコポリマー、ランダムブロックコポリマー、及びこれらの混合物からなる群から選択されるブロックポリマーを更に含む、請求項12又はその任意の従属請求項に記載の皮膚係合部材。
- 前記皮膚係合部材が、かみそりカートリッジに取り付けられている、請求項1〜13のいずれか一項に記載の皮膚係合部材。
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- 2011-10-11 SG SG10201508416VA patent/SG10201508416VA/en unknown
- 2011-10-11 BR BR112013007584A patent/BR112013007584A2/pt not_active IP Right Cessation
- 2011-10-11 KR KR1020157027131A patent/KR20150117713A/ko not_active Application Discontinuation
- 2011-10-11 CN CN2011800490128A patent/CN103260587A/zh active Pending
- 2011-10-11 RU RU2013114212/15A patent/RU2537231C1/ru not_active IP Right Cessation
- 2011-10-11 WO PCT/US2011/055740 patent/WO2012051166A2/en active Application Filing
- 2011-10-11 SG SG2013025754A patent/SG189294A1/en unknown
- 2011-10-11 CN CN201710937346.8A patent/CN107669496A/zh active Pending
- 2011-10-11 PL PL11773630T patent/PL2627303T3/pl unknown
- 2011-10-11 KR KR1020137009175A patent/KR20130073962A/ko active Application Filing
- 2011-10-11 EP EP11773630.6A patent/EP2627303B1/en active Active
- 2011-10-11 MX MX2013003979A patent/MX2013003979A/es active IP Right Grant
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Also Published As
Publication number | Publication date |
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EP2627303A2 (en) | 2013-08-21 |
MX2013003979A (es) | 2013-05-28 |
KR20130073962A (ko) | 2013-07-03 |
SG10201508416VA (en) | 2015-11-27 |
RU2537231C1 (ru) | 2014-12-27 |
SG189294A1 (en) | 2013-05-31 |
CN107669496A (zh) | 2018-02-09 |
CN103260587A (zh) | 2013-08-21 |
BR112013007584A2 (pt) | 2016-07-26 |
RU2013114212A (ru) | 2014-11-20 |
KR20150117713A (ko) | 2015-10-20 |
US20120087981A1 (en) | 2012-04-12 |
PL2627303T3 (pl) | 2017-03-31 |
WO2012051166A2 (en) | 2012-04-19 |
EP2627303B1 (en) | 2016-08-31 |
JP5551321B2 (ja) | 2014-07-16 |
WO2012051166A3 (en) | 2013-06-27 |
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