JP5523708B2 - 親油性かつ/または低皮膚浸透性の活性物質を投与するための経皮治療システム - Google Patents
親油性かつ/または低皮膚浸透性の活性物質を投与するための経皮治療システム Download PDFInfo
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- JP5523708B2 JP5523708B2 JP2008535925A JP2008535925A JP5523708B2 JP 5523708 B2 JP5523708 B2 JP 5523708B2 JP 2008535925 A JP2008535925 A JP 2008535925A JP 2008535925 A JP2008535925 A JP 2008535925A JP 5523708 B2 JP5523708 B2 JP 5523708B2
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Classifications
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- A—HUMAN NECESSITIES
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- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7038—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
- A61K9/7046—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
- A61K9/7053—Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds obtained by reactions only involving carbon to carbon unsaturated bonds, e.g. polyvinyl, polyisobutylene, polystyrene
- A61K9/7061—Polyacrylates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/70—Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
- A61K9/7023—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
- A61K9/703—Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
- A61K9/7084—Transdermal patches having a drug layer or reservoir, and one or more separate drug-free skin-adhesive layers, e.g. between drug reservoir and skin, or surrounding the drug reservoir; Liquid-filled reservoir patches
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/06—Free radical scavengers or antioxidants
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Description
a)テルペン類、
b)環式グルシトールエーテル類、
c)カプリン酸およびカプリル酸および/またはリノール酸の中鎖脂肪酸トリグリセリド類、および
d)比較的長鎖のアルコール類
の異なる1種から選択される液体容器システムにより達成される。
Cオクタノール/C水。
a)テルペン類、
b)環式グルシトールエーテル類、
c)カプリン酸およびカプリル酸および/またはリノール酸のトリグリセリド類、および
d)比較的長鎖のアルコール類
である。
環式グルシトールエーテルとして特に好適なのは、ジメチルイソソルビドである。ソルビトールとも呼ばれるグルシトールは、グルコースの糖アルコールである。
比較的長鎖のアルコール類として用いられるのは、少なくとも8個の炭素原子、好ましくは少なくとも12個の炭素原子の鎖長を有するアルコール類、好ましくは1価アルコール類、特に好ましくは1−ドデカノールである。
a)テルペンとして25重量%のユーカリプトール、
b)環式グルシトールエーテルとして25重量%のジメチルイソソルビド、
c)カプリル酸およびカプリン酸の中鎖脂肪酸トリグリセリドとして35重量%のMiglyol(登録商標) 812、および
d)12個または13個以上の炭素原子の鎖長を有する比較的長鎖のアルコールとして15重量%の1−ドデカノール。
活性物質含有製剤中の活性物質の比率は、合計で0.1〜50重量%、好ましくは5〜25重量%である。
吸収剤は、シクロデキストリン類、ポリビニルピロリドンおよびセルロース誘導体を含む群から選択してもよい。
−用いる制御膜のタイプ、例えばその化学的組成および/または孔径、
−システムを皮膚に付着させる、制御膜の下方で用いる粘着剤層のタイプ、例えば前記粘着剤層の化学的組成および/または層の厚さ、
−液体容器中の吸収剤、例えばシクロデキストリン類、ポリビニルピロリドンまたはセルロース誘導体を用いることにより達成される遅延送達。
表1において一層詳細に特定する粘着剤液体容器システムを製造するために、先ずDuroTak(登録商標)1050タイプ(National Starch, Antwerp)の活性物質非含有ポリアクリレート接着剤溶液またはコロフォニー(Foral(登録商標)85 B)に基づく接着樹脂を加えたエチレンと酢酸ビニルとのコポリマーを、シリコン処理したポリエチレンテレフタレートフィルム上にドクターナイフを用いて300μmの湿潤層の厚さで塗布する。
ビンポセチン含有液体容器システムについての参照として、マトリックスTTSを、BASFからの中分子量および高分子量ポリイソブチレンであるOppanol(登録商標)B 10およびOppanol(登録商標)B 100を、種々の混合比で、特定の沸点を有するタイプ80/110のガソリンに溶解し、その後この中に2重量%のビンポセチンおよびエンハンサーとして17重量%の乳酸ラウリルを分散させることにより調製した。30分間攪拌することにより、接着剤溶液中の活性物質結晶の均一な分布が達成された。これに続いて、超音波浴中で10〜15分間分散体をガス抜きした。
モクソニジンを投与するための粘着剤液体容器システムを、例1〜4について示した方法に従って、活性物質非含有ポリアクリレート接着剤溶液を塗布および乾燥し、その後これを、制御膜としての厚さ35μmのポリウレタンフィルム(Opraflex(登録商標)、Lohmann)を積層して被覆することにより製造した。ポリエステルフィルムを、制御膜上に配置し、特別な密封マスクで密封して、25mmの直径を有する円形の容器を有する袋を形成した。
モクソニジン含有液体容器システムについての比較例として、すでにモクソニジンの経皮投与のために最適化されている透過エンハンサーを有するTTSからなるマトリックスTTSを製造した。
ペルゴリドを投与するための粘着剤液体容器システムを、例1〜4について示した方法に従って、活性物質非含有ポリアクリレート接着剤溶液を塗布および乾燥し、その後これを、制御膜として作用する厚さ35μmのポリウレタンフィルム(Opraflex(登録商標)、Lohmann)を積層して被覆することにより製造した。ポリエステルフィルムを、制御膜上に配置し、特別な密封マスクで密封して、25mmの直径を有する円形の容器を有する袋を形成した。
ペルゴリド含有液体容器システムについての比較例として、すでにペルゴリドの経皮投与のために最適化されている透過エンハンサーを有するTTSからなるマトリックスTTSを製造した。
前述のシステムの透過速度を、改良Franz拡散セルを用いた「ヒト表皮」のインビトロ拡散モデルで決定した。すべての場合において、0.1%のNaN3を加えたリン酸緩衝液(pH5.5)を、保存剤として用いた。
QSS=定常状態の血漿レベル、単位ng/ml、
JSS=インビトロ皮膚流量、単位μg/cm2×時、
A=システムの有効放出表面積、単位cm2、および
Cl=クリアランス(浄化速度、ある活性物質の単位時間あたりの血漿の量)、単位l/時、ビンポセチンについての数値は、Kobayashi, D.ら、Biol. Pharm. Bull., 16, (1993), 254-258から採用。
Claims (16)
- ビンポセチン、モクソニジン、ペルゴリドおよびこれらの薬学的に許容し得る塩を含む群から選択される活性物質を投与するための経皮治療システムであって、該活性物質が、多成分エンハンサー系中に溶解または懸濁した形態で存在し、前記エンハンサー系が以下の4種の成分a)〜d):
a)モノテルペン、
b)環式グルシトールエーテル、
c)カプリン酸およびカプリル酸の中鎖脂肪酸トリグリセリドならびに/あるいはリノール酸の中鎖脂肪酸トリグリセリド、および
d)8個以上の炭素原子の鎖長を有する長鎖のアルコール
からなることを特徴とする、前記経皮治療システム。 - エンハンサー成分が、多成分エンハンサー系に対して、最低の用量で用いる成分の比率が少なくとも10重量%であり、最も高い用量の成分の比率が最大で40重量%である混合比で存在することを特徴とする、請求項1に記載の経皮治療システム。
- 活性物質の含量が、活性物質含有製剤に対して0.1〜50重量%であることを特徴とする、請求項1または2に記載の経皮治療システム。
- 活性物質の含量が、活性物質含有製剤に対して5.0〜25.0重量%であることを特徴とする、請求項1または2に記載の経皮治療システム。
- 活性物質および全エンハンサー成分が、液体容器中に存在することを特徴とする、請求項1〜4のいずれかに記載の経皮治療システム。
- 液体容器が、エンハンサー成分および活性物質の放出を制御する制御膜を含むことを特徴とする、請求項5に記載の経皮治療システム。
- 制御膜が、ポリエチレン、ポリプロピレン、シリコーン、ポリウレタンおよびエチレンと酢酸ビニルとのコポリマーを含む群から選択されるポリマーからなることを特徴とする、請求項6に記載の経皮治療システム。
- 液体容器システムが、制御膜の下に位置する粘着剤層を含み、ここで、前記粘着剤層の粘着剤が、シリコーン、アクリレート、ポリイソブチレンおよびエチレンと酢酸ビニルとのコポリマーからなる群から選択され、前記コポリマーは、接着樹脂を加えることにより接着性としてあることを特徴とする、請求項6に記載の経皮治療システム。
- 制御膜の下に位置する粘着剤層が、活性物質の放出を制御し、前記膜が、その層の厚さによってその制御効果を発揮することを特徴とする、請求項8に記載の経皮治療システム。
- エチレンと酢酸ビニルとのコポリマーをベースとする、接着樹脂が加えられた粘着剤層が、エチレン対酢酸ビニルの比率によってその制御効果を発揮することを特徴とする、請求項8に記載の経皮治療システム。
- 多成分エンハンサー系を含む活性物質製剤を含み、および
活性物質製剤が、増粘剤の意味での追加の補助物質を含むことを特徴とする、請求項1〜10のいずれかに記載の経皮治療システム。 - 多成分エンハンサー系を含む活性物質製剤を含み、および
活性物質製剤が、増粘剤の意味での追加の補助物質を含み、これが、鉱油、羊毛脂、ポリアクリル酸、高分子ポリエチレングリコールおよび高分散二酸化ケイ素を含む群から選択されることを特徴とする、請求項1〜10のいずれかに記載の経皮治療システム。 - 多成分エンハンサー系を含む活性物質製剤を含み、および
活性物質製剤が、溶液、分散体、懸濁液、ペーストまたはゲルとして存在することを特徴とする、請求項1〜12のいずれかに記載の経皮治療システム。 - 多成分エンハンサー系を含む活性物質製剤を含み、および
活性物質製剤がさらに、遅延放出の意味での制御要素を含むことを特徴とする、請求項1〜13のいずれかに記載の経皮治療システム。 - 多成分エンハンサー系を含む活性物質製剤を含み、および
活性物質製剤がさらに、遅延放出の意味での制御要素を含み、前記制御要素が、シクロデキストリン、ポリビニルピロリドンおよびセルロース誘導体を含む群から選択されることを特徴とする、請求項1〜13のいずれかに記載の経皮治療システム。 - 多成分エンハンサー系が、以下の組成:
a)25重量%のユーカリプトール、
b)25重量%のジメチルイソソルビド、
c)35重量%のミグリオール(登録商標)タイプ812、および
d)15重量%の1−ドデカノール
を有することを特徴とする、請求項1〜15のいずれかに記載の経皮治療システム。
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DE102005050431A DE102005050431A1 (de) | 2005-10-21 | 2005-10-21 | Transdermales therapeutisches System zur Verabreicherung lipophiler und/oder wenig hautpermeabler Wirkstoffe |
DE102005050431.0 | 2005-10-21 | ||
PCT/EP2006/009570 WO2007045352A1 (de) | 2005-10-21 | 2006-10-04 | Transdermales therapeutisches system zur verabreichung lipophiler und/oder wenig hautpermeabler wirkstoffe |
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EP (1) | EP1937227B1 (ja) |
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Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE102005050431A1 (de) * | 2005-10-21 | 2007-04-26 | Lts Lohmann Therapie-Systeme Ag | Transdermales therapeutisches System zur Verabreicherung lipophiler und/oder wenig hautpermeabler Wirkstoffe |
US8906967B2 (en) * | 2007-09-11 | 2014-12-09 | Dsm Ip Assets B.V. | Sesquiterpenes and derivatives thereof for use as feed additives |
EP2547323B1 (en) | 2010-03-17 | 2016-01-27 | Novaliq GmbH | Pharmaceutical composition for treatment of increased intraocular pressure |
CA2834855C (en) | 2011-05-25 | 2020-12-29 | Novaliq Gmbh | Topical pharmaceutical composition based on semifluorinated alkanes |
MX363182B (es) | 2012-09-12 | 2019-03-13 | Novaliq Gmbh | Composiciones que comprenden mezclas de alcanos semifluorados. |
AU2013314303B2 (en) | 2012-09-12 | 2018-01-18 | Novaliq Gmbh | Semifluorinated alkane compositions |
EP2944324A1 (de) | 2014-05-13 | 2015-11-18 | LTS LOHMANN Therapie-Systeme AG | Verwendung von semifluorierten Alkanen in transdermalen therapeutischen Systemen |
EP3495023B1 (en) | 2015-09-30 | 2020-04-22 | Novaliq GmbH | Semifluorinated compounds and their compositions |
KR20190057338A (ko) | 2016-09-23 | 2019-05-28 | 노바리크 게엠베하 | 시클로스포린을 포함하는 안과 조성물 |
PL3338768T3 (pl) | 2016-12-20 | 2020-05-18 | Lts Lohmann Therapie-Systeme Ag | Transdermalny system terapeutyczny zawierający asenapinę |
CA3047354A1 (en) | 2016-12-20 | 2018-06-28 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine and polysiloxane or polyisobutylene |
AU2018253944B2 (en) | 2017-04-21 | 2022-09-15 | Dermaliq Therapeutics, Inc. | Iodine compositions |
CA3067938A1 (en) | 2017-06-26 | 2019-01-03 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine and silicone acrylic hybrid polymer |
US11723861B2 (en) | 2017-09-27 | 2023-08-15 | Novaliq Gmbh | Ophthalmic compositions comprising latanoprost for use in the treatment of ocular diseases |
US11896559B2 (en) | 2017-10-04 | 2024-02-13 | Novaliq Gmbh | Opthalmic compositions comprising F6H8 |
CA3101420A1 (en) | 2018-06-20 | 2019-12-26 | Lts Lohmann Therapie-Systeme Ag | Transdermal therapeutic system containing asenapine |
CA3111870C (en) | 2018-09-27 | 2022-04-12 | Novaliq Gmbh | Topical sunscreen formulation |
ES2974839T3 (es) | 2018-10-12 | 2024-07-01 | Novaliq Gmbh | Composición oftálmica para el tratamiento de la enfermedad de ojos secos |
Family Cites Families (24)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE3564073D1 (en) * | 1984-06-23 | 1988-09-08 | Beiersdorf Ag | Self-adhesive plaster |
DE3423328A1 (de) | 1984-06-23 | 1986-01-02 | Beiersdorf Ag, 2000 Hamburg | Selbstklebendes pflaster |
CA2062828C (en) * | 1990-04-24 | 1996-04-16 | Osafumi Hidaka | Pharmaceutical plasters |
DE4341444C2 (de) * | 1993-12-04 | 1996-03-14 | Lohmann Therapie Syst Lts | Wirkstoffhaltiges Pflaster und Verfahren zu seiner Herstellung |
TW304167B (ja) * | 1995-01-30 | 1997-05-01 | Lilly Co Eli | |
US6572879B1 (en) * | 1995-06-07 | 2003-06-03 | Alza Corporation | Formulations for transdermal delivery of pergolide |
KR970064620A (ko) * | 1996-03-05 | 1997-10-13 | 임성기 | 사이클로스포린-함유 외용약제 조성물 |
US6019988A (en) * | 1996-11-18 | 2000-02-01 | Bristol-Myers Squibb Company | Methods and compositions for enhancing skin permeation of drugs using permeation enhancers, when drugs and/or permeation enhancers are unstable in combination during long-term storage |
DE19701059C2 (de) * | 1997-01-15 | 2000-12-21 | Lohmann Therapie Syst Lts | Acetylsalicylsäure enthaltendes transdermales therapeutisches System mit Resorptionsverstärkung |
JPH11189546A (ja) * | 1997-12-25 | 1999-07-13 | Saitama Daiichi Seiyaku Kk | 経皮吸収促進剤 |
KR100383252B1 (ko) * | 1998-12-17 | 2003-07-16 | 주식회사 삼양사 | 부프레놀핀을함유하는경피투여조성물및이를포함하는패취 |
JP2001064205A (ja) * | 1999-06-25 | 2001-03-13 | Dai Ichi Seiyaku Co Ltd | 製剤組成物 |
AU3104301A (en) * | 2000-01-20 | 2001-07-31 | Noven Pharmaceuticals, Inc. | Compositions and methods to effect the release profile in the transdermal administration of active agents |
DE10019171A1 (de) | 2000-04-07 | 2001-10-18 | Schering Ag | Zusammensetzungen zur Verwendung als Penetrationsverstärker in transdermalen Formulierungen für hoch lipophile Wirkstoffe |
DE10019311A1 (de) * | 2000-04-19 | 2001-10-31 | Lohmann Therapie Syst Lts | Transdermale therapuetische Systeme zur Applikation von Moxonidin |
DE10033853A1 (de) * | 2000-07-12 | 2002-01-31 | Hexal Ag | Transdermales therapeutisches System mit hochdispersem Siliziumdioxid |
AU2001282064B2 (en) * | 2000-08-03 | 2007-02-01 | Antares Pharma Ipl Ag | Novel composition for transdermal and/or transmucosal administration of active compounds that ensures adequate therapeutic levels |
DE10128685A1 (de) * | 2001-06-13 | 2002-12-19 | Beiersdorf Ag | Selbstklebendes, wirkstoffhaltiges Matrixpflaster auf Basis von Polyurethangelen |
US20050100588A1 (en) | 2001-06-13 | 2005-05-12 | Beiersdorf Ag | Self-adhesive matrix plaster containing an active ingredient and based on polyurethane gels |
JP2003063954A (ja) * | 2001-08-24 | 2003-03-05 | Saitama Daiichi Seiyaku Kk | リザーバー型貼付剤 |
US20040126415A1 (en) * | 2002-11-21 | 2004-07-01 | Lu Guang Wei | Dermal delivery of a water-soluble selective cyclooxygenase-2 inhibitor |
DE10256774A1 (de) | 2002-12-05 | 2004-06-24 | Lts Lohmann Therapie-Systeme Ag | Transmucosale und transdermale Arzneimittel mit verbesserter Wirkstoffresorption |
DE102004062614B4 (de) * | 2004-12-24 | 2011-12-29 | Lts Lohmann Therapie-Systeme Ag | Transdermales therapeutisches System mit aktivierbarer Übersättigung und kontrollierter Permeationförderung sowie Verfahren zu dessen Herstellung |
DE102005050431A1 (de) * | 2005-10-21 | 2007-04-26 | Lts Lohmann Therapie-Systeme Ag | Transdermales therapeutisches System zur Verabreicherung lipophiler und/oder wenig hautpermeabler Wirkstoffe |
-
2005
- 2005-10-21 DE DE102005050431A patent/DE102005050431A1/de not_active Withdrawn
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2006
- 2006-10-04 DE DE502006003488T patent/DE502006003488D1/de active Active
- 2006-10-04 ES ES06806011T patent/ES2326043T3/es active Active
- 2006-10-04 JP JP2008535925A patent/JP5523708B2/ja active Active
- 2006-10-04 WO PCT/EP2006/009570 patent/WO2007045352A1/de active Application Filing
- 2006-10-04 EP EP06806011A patent/EP1937227B1/de active Active
- 2006-10-04 AT AT06806011T patent/ATE428410T1/de not_active IP Right Cessation
- 2006-10-04 US US12/083,888 patent/US8309120B2/en active Active
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Also Published As
Publication number | Publication date |
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US20120316520A1 (en) | 2012-12-13 |
ATE428410T1 (de) | 2009-05-15 |
US9486417B2 (en) | 2016-11-08 |
JP2009512645A (ja) | 2009-03-26 |
EP1937227A1 (de) | 2008-07-02 |
EP1937227B1 (de) | 2009-04-15 |
DE102005050431A1 (de) | 2007-04-26 |
ES2326043T3 (es) | 2009-09-29 |
DE502006003488D1 (de) | 2009-05-28 |
US20090169601A1 (en) | 2009-07-02 |
WO2007045352A1 (de) | 2007-04-26 |
US8309120B2 (en) | 2012-11-13 |
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