JP2015535284A - プロピニルアミノインダン経皮組成物 - Google Patents
プロピニルアミノインダン経皮組成物 Download PDFInfo
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- JP2015535284A JP2015535284A JP2015540716A JP2015540716A JP2015535284A JP 2015535284 A JP2015535284 A JP 2015535284A JP 2015540716 A JP2015540716 A JP 2015540716A JP 2015540716 A JP2015540716 A JP 2015540716A JP 2015535284 A JP2015535284 A JP 2015535284A
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- transdermal composition
- composition according
- transdermal
- pressure sensitive
- sensitive adhesive
- Prior art date
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Abstract
Description
35 U.S.C. §119(e)に従って、本出願はUnited States Provisional Application Serial No. 61/722,044, 2012年11月2日出願の出願日に対する優先権を主張し、その開示内容を本明細書に援用する。
前記に概説したように、プロピニルアミノインダン経皮組成物を提供する。本発明の経皮組成物は、対象の皮膚の表面に局所適用した際に、有効薬剤、具体的にはプロピニルアミノインダンを対象に経皮送達するように構成された製剤である。本発明の組成物はプロピニルアミノインダン有効薬剤層を含み、その際、プロピニルアミノインダン有効薬剤層は、その組成物を対象に局所適用した際に対象に療法有効量のプロピニルアミノインダン有効薬剤の複数日間の送達をもたらすように配合される。複数日間の送達とは、組成物を対象の皮膚部位に適用した際に療法有効量を対象に1日以上、たとえば2日以上、たとえば3日以上、たとえば5日以上−これは7日以上、たとえば10日以上を含む−の期間、供給するように層が配合されていることを意味する。療法有効量とは、組成物を対象の皮膚部位にそれの所期の適用期間、適用した際に、たとえば7日間以内の適用で、希望する療法活性をもたらす全身量のプロピニルアミノインダンを供給することを意味する。ある態様において、組成物は目標用量の有効薬剤の送達をもたらす;すなわち、0.5mg/日以上を1週間(すなわち、7日間または168時間)にわたって送達し、これは1.0mg/日以上を1週間にわたって、たとえば10mg/日以上を1週間にわたって送達することを含む。
前記に概説したように、本発明の経皮組成物は、バッキングの表面上に存在する有効薬剤含有マトリックスを含む。着目されるマトリックス層は、感圧接着剤中に存在するある量のプロピニルアミノインダン有効薬剤を含有する。着目されるプロピニルアミノインダンには、次式で記載される化合物が含まれる:
前記にまとめたように、着目される経皮組成物はバッキング(すなわち、支持体層)を含んでもよい。バッキングは、対象の希望する局所位置と密着させることができる程度に柔軟であってよい。バッキングは、有効薬剤を吸収せずかつ有効薬剤を支持体の側から放出させない材料から作成することができる。バッキングは不織布、織布、フィルム(シートを含む)、多孔体、発泡体、紙、フィルムを不織布または織布に積層することにより得られた複合材料、およびその組合わせを含むことができるが、これらに限定されない。
ある態様において、有効薬剤層(すなわち、マトリックス)上に、具体的には、バッキング層が存在する場合にはそれから遠位(すなわち、反対側)の有効薬剤層面に、剥離ライナーを付与する。剥離ライナーは、有効薬剤層の保護を助成する。剥離ライナーは、ポリエチレンコートした上質紙、ポリオレフィンコートしたグラシン紙、ポリエチレンテレフタレート(ポリエステル)フィルム、ポリプロピレンフィルムなどの片側をシリコーン処理で処理することにより作成できる。
所望により、皮膚に適用した際の組成物の接着性を高めるために1以上の粘着性オーバーレイを使用できる。粘着性オーバーレイは、バッキング材料、たとえば多孔質、非孔質、閉鎖性または通気性のバッキング材料上に存在する、接着剤の層を含むことができる。粘着性オーバーレイの寸法は希望する機能性を付与するように選択され、ある場合には、有効薬剤製剤上に適用した際に粘着性オーバーレイが有効薬剤製剤の1以上の側面の外側へある距離広がるように寸法が選択される。ある場合には、粘着性オーバーレイの面積は有効薬剤製剤の面積より5%以上、たとえば10%以上−これは20%以上を含む−大きい。使用に際して、粘着性オーバーレイは患者により、介護者により適用でき、あるいはキットに統合することができる。
製品である経皮組成物の使用方法は、着目される標的状態、たとえば後記の有用性のセクションに記載する標的状態に対して対象を処置するために、有効量のプロピニルアミノインダン組成物を対象に投与することを含む。“処置する”または“処置”とは、対象が罹患している状態に関連する症状を少なくとも抑制または改善することを意味し、その際、抑制および改善は、処置される状態に関連するパラメーター、たとえば症状の大きさを、少なくとも低減することを表わすために広い意味で用いられる。したがって、処置には、その状態が完全に阻害され、たとえば発生が阻止され、または停止し、たとえば終止し、これにより対象がもはやその状態を経験しない状況も含まれる。したがって、処置にはある状態の阻止および管理が共に含まれる。
本発明の経皮組成物は、プロピニルアミノインダン、たとえばラサギリンを経皮投与することが対象に有益となるいずれかの用途に有用である。ラサギリンおよび/またはそれの塩類は、多種多様な疾病状態、たとえば下記の処置に有用であるが、それらに限定されない:パーキンソン病、アルツハイマー病、記憶障害、発作、ならびに他の障害、たとえばU.S. Pat. No.: 5,387,612; 5,453,446; 5,457,133; 5,668,181; 5,576,353; 5,532,415; 5,599,991; 5,786,390; 5,519,061; 5,891,923; 5,744,500および6,316,504に記載のもの;それらの内容を本明細書に援用する。処置とは、少なくとも対象が罹患している状態に関連する症状の改善を達成することを意味し、その際、改善は、処置される状態に関連するパラメーター、たとえば症状の大きさを、少なくとも低減することを表わすために広い意味で用いられる。したがって、処置には、病的状態または少なくともそれと関連する症状が完全に阻害され、たとえば発生が阻止され、または停止し、たとえば終止し、これにより対象がもはやその状態または少なくともその状態を特徴づける症状に罹患しない状況も含まれる。
本明細書に記載する特定の方法を実施する際に使用するためのキットも提供される。特定の態様において、キットは前記に述べた1以上の経皮組成物を含む。特定の態様において、キットは前記に述べた粘着性オーバーレイを含む。ある態様において、キットは多層、たとえば薬物を含有する層、ならびに薬物および他の賦形剤を含有しても含有しなくてもよい層を含む。2以上の組成物を含む特定のキットにおいて、組成物は個別にパッケージされてもいてよく、あるいは共通の容器内に存在してもよい。
A.有効薬剤レザバー層の作成
有機溶剤中における、混合物の各成分の原液(一般に、酢酸エチル、メタノール、および/またはエタノール中における30〜60重量%の固形分)を混和し、続いて混合処理することにより、配合物を調製した。均一な混合物が形成されると、この溶液を剥離ライナー(シリコーン処理した2〜3ミルのポリエステルシート)上にキャストし、65℃〜80℃で10〜90分間乾燥させた。これらの粘着フィルムをPETバッキングに積層した。
ヒトの死体皮膚を用い、上皮層(epidermal layer)(角質層および表皮(epidermis))を全厚皮膚から皮膚膜として分離した。アーチパンチで約2.0cm2の最終直径に試料を打ち抜いた。剥離ライナーを取り除き、このシステムを表皮/角質層の上に、薬物接着剤層を角質層に向けて配置した。接着剤層と角質層が良好に接触するように、穏やかな圧力をかけた。フランツセル(Franz cell)のドナー側とレセプター側を互いにクランプで留め、pH6.5のリン酸緩衝液を含有するレセプター溶液をフランツセルに添加した。実験期間中、セルを33℃に保持した。レセプター溶液の試料を規則的間隔で採取し、有効薬剤濃度をHPLCにより測定した。シンク条件を維持するために、取り出したレセプター溶液の代わりに新鮮な溶液を入れた。時間に対するレシーバーコンパートメント内の薬物累積量のプロットの傾きから、フラックスを計算した。
C.1 メシル酸ラサギリンをアクリレート系接着剤中に含有する種々の経皮製剤のフラックス
前記の一般法を用いて、異なる量のラサギリン、Duro−tak(登録商標) 87−2353、87−2052および/または87−9301のうち1種類以上、ならびにEudragit E POを含有する一連の経皮システムを作成した;詳細を次表に示す。さらに、Gelva 7883(アクリレート ビニルアセテート)を用いた1種類の製剤を作成した。ヒトの死体皮膚を通るフラックスを測定し、結果を図2Aおよび2Bにグラフで提示する。
安定性を下記に従って判定した。メシル酸ラサギリン被験パッチを4cm2サイズで作成し、ポリアクリロニトリル(PAN)材料製パウチに入れた。これらのパッチを室温、30℃および40℃の温度のチャンバー(湿度制御なし)に貯蔵した。用いたパウチ材料はDia Nipponから購入された。
メシル酸ラサギリンの経口製剤(1mg Azilect(登録商標)錠)と比較した2種類の7日用経皮パッチ製剤の薬物動態の測定を、ゲッチンゲン(Gottingen)系ミニブタで実施した。
Claims (20)
- 経皮組成物であって、
(A)下記のものを含むマトリックス:
(i)プロピニルアミノインダン;および
(ii)下記のものを含む感圧接着剤:
(a)ペンダント官能基を欠如したアクリレートコポリマー;および
(a)カチオン性アクリルコポリマー;ならびに
(B)バッキング
を含む組成物。 - プロピニルアミノインダンがラサギリンである、請求項1に記載の経皮組成物。
- ラサギリンが遊離塩基として存在する、請求項2に記載の経皮組成物。
- ラサギリンが塩として存在する、請求項2に記載の経皮組成物。
- 塩がメシル酸ラサギリンである、請求項4に記載の経皮組成物。
- 感圧接着剤がDuroTak(登録商標) 87−9301と同一または実質的に同一である、請求項5に記載の経皮組成物。
- 感圧接着剤がGelva(登録商標) 7883と同一または実質的に同一である、請求項5に記載の経皮組成物。
- 感圧接着剤がマトリックスの75重量%から90重量%までの範囲の量で存在する、請求項1〜7のいずれか1項に記載の経皮組成物。
- カチオン性アクリルコポリマーがアミノ化メタクリレートコポリマーである、請求項1〜8のいずれか1項に記載の経皮組成物。
- アミノ化メタクリレートコポリマーが、メタクリル酸ジエチルアミノエチル、メタクリル酸ブチルおよびメタクリル酸メチルのコポリマーである、請求項9に記載の経皮組成物。
- アミノ化メタクリレートコポリマーが次式:
- 組成物がさらに、−COOH官能基を含む第2の感圧接着剤を含む、請求項1〜11のいずれか1項に記載の経皮組成物。
- 第2の感圧接着剤がマトリックスの2重量%から10重量%までの範囲の量で存在する、請求項12に記載の経皮組成物。
- マトリックスが促進剤を含む、前記請求項のいずれか1項に記載の経皮組成物。
- 経皮組成物が長期間にわたるプロピニルアミノインダンの療法フラックスを示す、前記請求項のいずれか1項に記載の経皮組成物。
- マトリックスが単層構造を有する、前記請求項のいずれか1項に記載の経皮組成物。
- 組成物がさらに剥離ライナーを含む、前記請求項のいずれか1項に記載の経皮組成物。
- 組成物が貯蔵安定性である、前記請求項のいずれか1項に記載の経皮組成物。
- 対象の皮膚表面に、請求項1〜18のいずれか1項に記載の経皮組成物を、長期間にわたるプロピニルアミノインダンの療法フラックスを達成するのに十分な様式で適用することを含む方法。
- 請求項1〜18のいずれか1項に記載の経皮組成物を2以上含むキット。
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IL238381A0 (en) | 2015-06-30 |
EP2914249A1 (en) | 2015-09-09 |
SG11201502681WA (en) | 2015-05-28 |
KR101856515B1 (ko) | 2018-05-10 |
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TW201431571A (zh) | 2014-08-16 |
MX2015004858A (es) | 2015-07-21 |
EA031621B1 (ru) | 2019-01-31 |
AR093329A1 (es) | 2015-06-03 |
NZ706590A (en) | 2016-02-26 |
US9827207B2 (en) | 2017-11-28 |
US9205061B2 (en) | 2015-12-08 |
EA201590489A1 (ru) | 2016-02-29 |
HK1207558A1 (en) | 2016-02-05 |
CN104797245B (zh) | 2018-05-04 |
KR20150059177A (ko) | 2015-05-29 |
CA2887705A1 (en) | 2014-05-08 |
AU2013338243A1 (en) | 2015-04-23 |
US10918607B2 (en) | 2021-02-16 |
BR112015007872A2 (pt) | 2017-07-04 |
KR20170091791A (ko) | 2017-08-09 |
US20140127281A1 (en) | 2014-05-08 |
CA2887705C (en) | 2018-07-24 |
US20160051489A1 (en) | 2016-02-25 |
IL238381B (en) | 2019-12-31 |
TWI543782B (zh) | 2016-08-01 |
CN104797245A (zh) | 2015-07-22 |
EP2914249A4 (en) | 2016-05-11 |
US20140186422A1 (en) | 2014-07-03 |
JP6050896B2 (ja) | 2016-12-21 |
AU2013338243B2 (en) | 2016-09-29 |
MX366649B (es) | 2019-07-17 |
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