JP5138995B2 - 皮膚貼付用粘着シートおよび経皮吸収製剤 - Google Patents
皮膚貼付用粘着シートおよび経皮吸収製剤 Download PDFInfo
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- JP5138995B2 JP5138995B2 JP2007178677A JP2007178677A JP5138995B2 JP 5138995 B2 JP5138995 B2 JP 5138995B2 JP 2007178677 A JP2007178677 A JP 2007178677A JP 2007178677 A JP2007178677 A JP 2007178677A JP 5138995 B2 JP5138995 B2 JP 5138995B2
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- sensitive adhesive
- pressure
- polymer
- adhesive sheet
- acid
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Landscapes
- Medicinal Preparation (AREA)
Description
ヒドロシリル化架橋を用いた粘着剤が提案されている(例えば、特許文献3)。上記粘着剤では未反応のイソシアネートによる毒性も危惧されなく、また、透湿性が高いため皮膚のムレ等の刺激性が低減された粘着剤が提案されている。しかしながら、上記粘着剤では、皮膚に対する接着力が十分でなく、長時間の皮膚貼付に適さないことがある。特に、生理活性物質の投与を目的とした粘着シートにおいては、皮膚への接着力が低いことは治療効果への影響が懸念される。
(A)末端に少なくとも1個のアルケニル基を有するポリエーテル系重合体
(B)分子中に1〜10個のヒドロシリル基を有する化合物
(C)ヒドロシリル化触媒
からなる混合物を硬化してなり、重合体(A)が少なくとも2種類以上の重合体よりなることを特徴とする皮膚貼付用の粘着シートに関する。
本発明は支持体上に少なくとも一層の粘着剤層が設けられてなる。
が挙げられる。下記式において、R1およびR2は水素原子または炭素数1〜10の炭化水素基であり、好ましくは水素原子またはメチル基である。
(1)H2C=C(R1)−
(2)HC(R2)=CH−
重合体(A)を構成する2種類以上のポリエーテル系重合体は、いずれも、1分子中に平均して少なくとも1個、好ましくは1〜5個、より好ましくは1〜3個、さらに好ましくは1〜2個のアルケニル基を有する。重合体(A)を構成するポリエーテル系重合体1分子中のアルケニル基の数が平均して1個未満では硬化性が不十分になり、また1分子中に含まれるアルケニル基の数が多すぎると網目構造が密になるため、粘着特性が低下する傾向にある。
a)エチレングリコール、ジエチレングリコール、ジプロピレングリコール、プロピレングリコール、ポリエチレングリコール、ポリプロピレングリコール、ブタンジオール、トリエチレングリコール、グリセリンなどの多価アルコール
b)オリーブ油、つばき油、大豆油、ひまし油、ラノリンなどの油脂類
c)オレイン酸などの脂肪酸
d)ポリオキシエチレンヒマシ油、ポリオキシエチレン硬化ヒマシ油、ポリオキシエチレンソルビタンモノラウレート、ポリオキシエチレンソルビタンモノパルミテート、ポリオキシエチレンソルビタンモノステアレート、ポリオキシエチレンソルビタンテトラオレエート、ポリオキシエチレンラウリルエーテル、ポリオキシエチレンラウレート、ソルビタンモノオレエート、ソルビタントリオレエート、ソルビタンセキスオレエート、などの液状界面活性剤
e)カプロン酸メチル、カプリル酸メチル、カプリン酸メチル、ラウリン酸メチル、ミリスチン酸メチル、ステアリン酸メチル、オレイン酸メチル、ラウリン酸エチル、ミリスチン酸エチル、オレイン酸エチル、ミリスチン酸イソプロピル、パルミチン酸イソプロピル、パルミチン酸ブチル、ラウリン酸イソステアリル、パルミチン酸イソステアリル、パルミチン酸オクチル、ステアリン酸オクチル、ミリスチン酸オクチルドデシル、ミリスチン酸イソトリデシル、アジピン酸ジイソプロピル、パルミチン酸オクチル、ステアリン酸オクチル、セバシン酸ジエチル、カプリル酸グリセリド、ペラルゴン酸グリセリド、カプリン酸グリセリド、クエン酸トリエチル、アセチルクエン酸トリブチルなどのその他の脂肪酸エステル
f)流動パラフィン、スクワラン、スクワレンなどの炭化水素
g)エタノール、酢酸エチル、ヂメチルスルホキシド、イソソルビトール、ジメチルデシルスルホキシド、メチルオクチルスルホキシド、ジメチルホルムアミド、ジメチルアセトアミド、N−メチルピロリドン、ドデシルピロリドンなどの有機溶剤
等が挙げられる。これら有機液状成分は必要に応じて1種類以上を混合して用いることができる。
a)天然ゴム、イソプレンゴム、ブタジエンゴム、1,2‐ポリブタジエン、スチレン−ブタジエンゴム、クロロプレンゴム、二トリルゴム、ブチルゴム、エチレン−プロピレンゴム、クロロスルホン化ポリエチレン、アクリルゴム、エピクロルヒドリンゴム、多硫化ゴム、シリコーンゴム、フッ素ゴム、ウレタンゴム、ポリイソブチレンゴム、スチレン−イソプレン−スチレンブロック共重合体(SIS)、スチレン−ブタジエン−スチレンブロック共重合体(SBS)、スチレン−イソブチレン−スチレンブロック共重合体(SIBS)等の合成ゴム
b)ポリジメチルシロキサン、メチルフェニルシロキサン等のポリオルガノシロキサン系ポリマー
c)ポリメチルアクリレート、ポリエチルアクリレート、ポリブチルアクリレート、ポリ2−エチルヘキシルアクリレート等のポリアクリル酸エステル、ポリブチルメタクリレート、ポリエチルメタクリレート、ポリ2−エチルへキシルメタクリレート等のポリメタアクリル酸エステル、アクリル酸・アクリル酸ブチル共重合体等の(メタ)アクリル酸−(メタ)アクリル酸エステル共重合体などのポリアクリレート系ポリマー
d)ポリ塩化ビニル、ポリ塩化ビニリデン、ポリアクリロニトリル等のビニル系ポリマー
e)ナイロン12、ナイロン−6,6等のポリアミド系ポリマー
f)ポリエチレン、ポリプロピレン等のオレフィン系ポリマー
g)アクリル酸デンプン、ポリアクリル酸、ポリアクリル酸ナトリウム、カルボキシメチルセルロース(CMC)、カルボキシメチルセルロースナトリウム(CMCNa)、ポリビニルアルコール(PVA)、ポリビニルピロリドン(PVP)、メチルビニルエーテル無水マレイン酸共重合体、アルギン酸ナトリウム、アルギン酸プロピレングリコールエステル、ペクチン、ザンタンガム、キサンタンガム、ローカストビーンガム、グアーガム、アラビアノガラクタン、ヒアルロン酸ナトリウム等の親水性高分子
等が挙げられる。これら、粘着成分は必要に応じて、1種類以上を適宜組み合わせて混合することができる。
1.β−アドレナリン性作動薬、例えば、アルブテロール、バンブテロール、ビトルテロール、カルブテロール、クレンブテロール、クロルプレナリン、デノパミン、ジオキセテドリン、ドペキサミン、エフェドリン、エピネフリン、エタフェドリン、エチルノルエピネフリン、フェノテロール、ホルモテロール、ヘキソプレナリン、イボパミン、イソエタリン、イソプロテレナール、マブテロール、メタプロテレノール、メトキシフェナミン、オキシフェドリン、ピルブテロール、プレナルテロール、プロカテロール、プロトキロール、レプロテロール、リミテロール、リトドリン、ソテレノール、テルブテロール及びキサモテロール
2.β−アドレナリン性遮断薬、例えば、アセブトロール、アルプレノロール、アモスラロール、アロチノロール、アテノロール、ベフノロール、ベタキソロール、ベバントロール、ビソプロロール、ボピンドロール、ブクモロール、ベフェトロール、ブフラロール、ブニトロロール、ブプラノロール、塩酸ブチドリン、ブトフィロロール、カラゾロール、カルテオロール、カルベジロール、セリプロロール、セタモロール、クロラノロール、ジレバロール、エパノロール、エスモロール、インデノロール、ラベタロール、レボブノロール、メピンドロール、メチプラナロール、メトプロロール、モプロロール、ナドキソロール、ニフェナロール、ニプラジロール、オキシプレノロール、ペンブトロール、ピンドロール、プラクトロール、プロネタロール、プロプラノロール、ソタロール、スルフィナロール、タリノロール、テルタトロール、チモロール、トリプロロール及びキシベノロール
3.鎮痛剤、例えば、クロロブタノール;麻薬性鎮痛剤、例えば、アルフェンタニル、アリルプロジン、アルファプロジン、アニレリジン、ベンジルモルフィン、ベンジトラミド、ブプレノルフィン、ブトルファノール、クロニタゼン、コデイン、臭化メチルコデイン、リン酸コデイン、硫酸コデイン、デソモルフィン、デキストロモラミド、デゾシン、ジアンプロミド、ジヒドロコデイン、エノール酢酸ジヒドロコデイン、ジヒドロモルフィン、ジメノキサドール、ジメフェプタノール、ジメチルチアンブテン、酪酸ジオキサフェチル、ジピパノン、エプタゾシン、エトヘプタジン、エチルメチルチアンブテン、エチルモルフィン、エトニタゼン、フェンタニル、ヒドロコドン、ヒドロモルホン、ヒドロキシペンチジン、イソメタドン、ケトベミドン、レボルファノール、ロフェンタニル、メペリジン、メプタジノール、メタゾシン、塩酸メタドン、メトポン、モルフィネ、モルフィネ誘導体、ミロフィネ、ナルブフィネ、ナルセイン、ニコモルフィネ、ノルレボルファノール、ノルメタドン、ノルモルフィネ、ノルピパノン、阿片、オキシコドン、オキシモルホン、パパベレタム、ペンタゾシン、フェナドキソン、フェナゾシン、フェオペリジン、ピミノジン、ピリトラミド、プロヘプタジン、プロメドール、プロペリジン、プロピラム、プロポキシフェン、スフェンタニル及びチリジン並びに非麻薬性鎮痛剤、例えば、アセトアミノフェン、アセチルサリチルサリチル酸及びアルクロフェナック
4.抗狭心症薬、例えば、アセブトロール、アルプレノロール、アミノダロン、アムロジピン、アロチノロール、アテノロール、ベプリジル、ベバントロール、ブクモロール、ブフェトロール、ブフラロール、ブニトロロール、ブプラノロール、カロゾロール、カルテオロール、カルベジロール、セリプロロール、マレイン酸シネパゼット、ジルチアゼム、エパノロール、フェロジピン、ガロパミル、イモールアミン、インデノロール、二硝酸イソソルビド、イスラジピン、リマプロスト、メピンドロール、メトプロロール、モルシドミン、ナドロール、ニカルジピン、ニフェジピン、ニフェナロール、ニルバジピン、ニプラジロール、ニソルジピン、ニトログリセリン、オキシプレノロール、オキシフェドリン、オザグレル、ペンブトロール、四硝酸ペンタエリスリトール、ピンドロール、プロネタロール、プロプラノロール、ソタロール、テロジリン、チモロール、トリプロロール及びベラパミル
5.抗不整脈薬、例えば、アセブトール、アセカイン、アデノシン、アジマリン、アルプレノロール、アミオダロン、アモプロキサン、アプリンジン、アロチノロール、アテノロール、ベバントロール、トシル酸ブレチリウム、ブブモロール、ブフェトロール、ブナフチン、ブニトロロール、ブプラノロール、塩酸ブチドリン、ブトベンジン、カポベン酸、カラゾロール、カルテオロール、シフェンリン、クロラノロール、ジソピラミド、エンカイニド、エスモロール、フレカイニド、ガロパミル、ヒドロキニジン、インデカイニド、インデノロール、臭化イプラトロピウム、リドカイン、ロラジミン、ロルカイニド、メオベンチン、メチプラノロール、メキシレチン、モリシジン、ナドキソロール、ニフェナロール、オキシプレノロール、ペンブトロール、ピンドロール、ピルメノール、プラクトロール、プラジマリン、塩酸プロカインアミド、プロネタロール、プロパフェノン、プロプラノロール、ピリノリン、硫酸キニジン、キニジン、ソタロール、タリノロール、チモロール、トカイニド、ベラパミル、ビクイジル及びキシベノロール
6.抗うつ薬:二環系、例えば、ビネダリン、カロキサゾン、シタロプラム、ジメタザン、インダルピン、フェンカミン、塩酸インデロキサジン、ネフォパム、ノミフェンシン、オキシトリプタン、オキシペルチン、パロキセチン、セルトラリン、チアゼシム、トラゾドン及びゾメタピン;ヒドラジド/ヒドラジン系、例えば、ベンモキシン、イプロクロジド、イプロニアジド、イソカルボキサジド、ニアラミド、オクタモキシン及びフェネルジン;ピロリドン系、例えば、コチニン、ロリシプリン及びロリプラム;四環系、例えば、マプロチリン、メトラリンドール、ミアンセリン及びオキサプロチリン。三環系、例えば、アジナゾラム、アミトリプチリン、アミトリプチリノキシド、アモキサピン、ブトリプチリン、クロミプラミン、デメキシプチリン、デシプラミン、ジベンゼピン、ジメトラクリン、ドチエピン、ドキセピン、フルアシジン、イミプラミン、イミプラミンN−オキシド、イプリンドール、ロフェプラミン、メリトラセン、メタプラミン、ノルトリプチリン、ノキシプチリン、オピプラモール、ピゾチリン、プロピゼピン、プロトリプチリン、キヌプラミン、チアネプチン及びトリミプラミン;及びその他、例えば、アドラフィニル、ベナクチジン、ブプロピオン、ブタセチン、デアノール、アセグルミン酸デアノール、アセトアミド安息香酸デアノール、ジオキサドロール、エトペリドン、フェバルマメート、フェモキセチン、フェンペンタジオール、フルオキセチン、フルボキサミン、ヘマトポルフィリン、ハイパーシニン、レボファセトペラン、メジホキサミン、ミナプリン、モクロベミド、オキサフロザン、ピベラリン、プロリンタン、ピリスクシデアノール、塩化ルビジウム、スルピリド、スルトプリド、テニロキサジン、トザリノン、トフェナシン、トロキサトン、トラニルシプロミン、L−トリプトファン、リスペリドン、ビロキサジン及びジメルジン
7.抗エストロゲン剤、例えば、酢酸デルマジノン、エタモキシトリフェトール、タモキシフェン及びトレミフェン
8.抗ゴナドトロピン剤、例えば、ダナゾール、ゲストリノン及びパロキシプロピオン
9.抗高血圧剤:アリールエタノールアミン誘導体、例えば、アモスラロール、ブフラロール、ジレバロール、ラベタロール、プロネタロール、ソタロール及びスルフィナロール;アリールオキシプロパノールアミン誘導体、例えば、アセブトロール、アルプレノロール、アロチノロール、アテノロール、ベタキソロール、ベバントロール、ビソプロロール、ボピンドロール、ブニトロロール、ブプラノロール、ブトフィロロール、カラゾロール、カルテゾロール、カルベジロール、セリプロロール、セタモロール、エパノロール、インデノロール、メピンドロール、メチプラノロール、メトプロロール、モプロロール、ナドロール、ニプラジロール、オキシプレノロール、ペンブトロール、ピンドロール、プロプラノロール、タリノロール、テトラオロール、チモロール及びトリプロロール;ベンゾチアジアジン誘導体、例えば、アルチアジド、ベンドロフルメチアジドベンズチアジド、ベンジルヒドロクロロチアジド、ブチアジド、クロロチアジド、クロルタリドン、シクロペンチアジド、シクロチアジド、ジアゾキシド、エピチアジド、エチアジド、フェンクイゾン、ヒドロクロロチアジド、ヒドロフルメチアジド、メチルクロチアジド、メチクラン、メトラゾン、パラフルチジド、ポリチアジド、テトラクロルメチアジド及びトリクロルメチアジド;N−カルボキシアルキル(ペプチド/ラクタム)誘導体、例えば、アラセプリル、カプトプリル、シラザプリル、デラプリル、エナラプリル、エナラプリラット、ホシノプリル、リシノプリル、モベルチプリル、ペリンドプリル、キナプリル及びラミプリル;ジヒドロピリジン誘導体、例えば、アムロジピン、フェロジピン、イスラジピン、ニカルジピン、ニフェジピン、ニルバジピン、ニソルジピン及びニトレンジピン;グアニジン誘導体、例えば、ベタニジン、デブリソクイン、グアナベンズ、グアナクリン、グアナドレル、グアナゾジン、グアネチジン、グアンファシン、グアノクロル、グアノキサベンズ及びグアノキサン;ヒドラジン及びフタラジン系、例えば、ブドララジン、カドララジン、ジヒドララジン、エンドララジン、ヒドラカルバジン、ヒドララジン、フェニプラジン、ピルドララジン及びトドララジン;イミダゾール誘導体、例えば、クロニジン、ロフェキシジン、フェントルアミン、チアメニジン及びトロニジン;四級アンモニウム化合物、臭化アザメトニウム、塩化クロルイソンダミン、ヘキサメトニウム、ビス(硫酸メチル)ペンタシニウム、臭化ペンタメトニウム、酒石酸ペントリニウム、塩化フェナクトピニウム及びメト硫酸トリメチジウナム;キナゾリン誘導体、例えば、アルフゾシン、ブナゾシン、ドキサゾシン、プラソシン、テラゾシン及びトリマゾシン;レセルピン誘導体、ビエタセルピン、デセルピジン、レシンナミン、レセルピン及びシロシンゴピン;スルホンアミド誘導体、例えば、アンブシド、クロパミド、フロセミド、インダパミド、キネタゾン、トリパミド及びキシパミド;及びその他、例えば、アジマリン、γ−アミノ酪酸、ブフェニオード、クロルタリドン、シクレタイン、シクロシドミン、タンニン酸クリプテナミン、フェノルドパム、フロセクイナン、インドラミン、ケタンセリン、メトブタメート、メカミルアミン、メチルドーパ、メチル4−ピリジルケトンチオセミカルバルゾン、メトラゾン、ミノキシジル、ムゾリミン、パルジリン、ペンピジン、ピナシジル、ピペロキサン、プリマペロン、プロトベラトリネス、ラウバシン、レシメトール、リルメニデン、サララシン、ニトロプルシッドナトリウム、チクリナフェン、トリメタファン、カムシレート、チロシナーゼ及びウラピジル
10.抗炎症(非ステロイド系)剤:アミノアリールカルボン酸誘導体、例えば、エンフェナム酸、エトフェナメート、フルフェナム酸、イソニキシン、メクロフェナム酸、メファナム酸、ニフルム酸、タルニフルメート、テロフェナメート及びトルフェナム酸;アリール酢酸誘導体、例えば、アセメタシン、アルクロフェナック、アンフェナック、ブフェキサマック、シンメタシン、クロピラック、ジクロフェナックナトリウム、エトドラック、フェルビナック、フェンクロフェナック、フェンクロラック、フェンクロジン酸、フェンチアザック、グルカメタシン、イブフェナック、インドメタシン、イソフェゾラック、イソキセパック、ロナゾラック、メチアジン酸、オキサメタシン、プログルメタシン、スリンダック、チアラミド、トルメチン及びゾメピラック;アリール酪酸誘導体、例えば、ブマジゾン、ブチブフェン、フェンブフェン及びキセンブシン;アリールカルボン酸誘導体、例えば、クリダナック、ケトロラック及びチノリジン;アリールプロピオン酸誘導体、例えば、アルミノプロフェン、ベノキサプロフェン、ブクロキシ酸、カルプロフェン、フェノプロフェン、フルノキサプロフェン、フルルビプロフェン、イブプロフェン、イブプロキサム、インドプロフェン、ケトプロフェン、ロキソプロフェン、ミロプロフェン、ナプロキセン、オキサプロジン、ピケトプロフェン、ピルプロフェン、プラノプロフェン、プロチジン酸、スプロフェン及びチアプロフェン酸;ピラゾール系、例えば、ジフェナミゾール及びエピリゾール;ピラゾロン系、例えば、アパゾン、ベンズピペリロン、フェプラゾン、モフェブタゾン、モラゾン、オキシフェンブタゾン、フェニブタゾン、ピペブゾン、プロピフェナゾン、ラミフェナゾン、スキシブゾン及びチアゾリノブタゾン;サリチル酸誘導体、例えば、アセタミノサロール、アスピリン、ベノリレート、ブロモサリゲニン、アセチルサリチル酸カルシウム、ジフルニサル、エテルサレート、フェンドサル、ゲンチジン酸、サリチル酸グリコール、サリチル酸イミダゾール、アセチルサリチル酸リシン、メサルアミン、サリチル酸モルホリン、サリチル酸1−ナフチル、オルサラジン、パルサルミド、アセチルサリチル酸フェニル、サリチル酸フェニル、サラセタミド、サリチルアミンo−酢酸、サリチル硫酸、サルサレート及びスルファサラジン;チアジンカルボキサミド系、例えば、ドロキシカム、イソキシカム、ピロキシカム及びテノキシカム;及びその他、例えば、ε−アセトアミドカプロン酸、S−アデノシルメチオニン、3−アミノ−4−ヒドロキシ酪酸、アミキセトリン、ベンダザック、ベンジダミン、ブコローム、ジフェンピラミド、ジタゾール、エモルファゾン、グアヤズレン、ナブメトン、ニメスリド、オルゴテイン、オキサセプロール、パラニリン、ペリソキサール、ピホキシム、プロクアゾン、バルデコキシブ、ケトロラク、プロキサゾール及びテニダップ
11.抗腫瘍剤:2−アミノレブリン酸及びアルキル化剤:スルホン酸アルキル系、例えば、ブスルファン、インプロスルファン及びピポスルファン;アジリジン系、例えば、ベンゾデパ、カルボクオン、メツレデパ及びウレデパ;エチレンイミン及びメチルメラミン系、例えば、アルトレタミン、トリエチレンメラミン、トリエチレンホスホルアミド、トリエチレンチオホスホルアミド及びトリメチロロメラミン;ナイトロジェンマスタード系、例えば、クロルアンブシル、クロルナファジン、シクロホスファミド、エストラムスチン、イホスファミド、メクロルエタミン、塩酸メクロルエタミンオキシド、メルファラン、ノベンビキン、フェネステリン、プレドニムスチン、トロホスファミド及びウラシルマスタード;ニトロソウレア系、例えば、カルムスチン、クロロゾトシン、ホテムスチン、ロムスチン、ニムスチン及びラニムスチン;及びその他、例えば、ダカルバジン、マンノムスチン、ミトブロニトール、ミトラクトール及びピポブロマン;抗生物質、例えば、アクラシノマイシン、アクチノマイシンF1、アントラマイシン、アザセリン、ブレオマイシン、カクチノマイシン、カルビシン、カルジノフィリン、クロモマイシン、ダクチノマイシン、ダウノルビシン、6−ジアゾ−5−オキソ−L−ノルロイシン、ドキソルビシン、エピルビシン、ミトマイシン、マイコフェノール酸、ノガラマイシン、オリボマイシン、ペプロマイシン、プリカマイシン、ポルフィロマイシン、プロマイシン、ストレプトニグリン、ストレプトゾシン、ツベルシジン、ウベニメックス、ジノスタチン及びゾルビシン;抗代謝剤:葉酸類縁体、例えば、デノプテリン、メソトレキセート、プテロプテリン及びトリメトレキセート;プリン類縁体、例えば、フルダラビン、6−メルカプトプリン、チアミプリン及びチオグアナイン;及びピリミジン類縁体、例えば、アンシタビン、アザシチジン、6−アザウリジン、カルモフール、シタラビン、ドキシフルリジン、エノシタビン、フロキシウリジン、フルロオウラシル及びテガフール;酵素、例えば、L−アスパラギナーゼ;及びその他、例えば、アセグラトン、アンサクリン、ベストラブシル、ビサントレン、カルボプラチン、シスプラチン、デホファミド、デメコルシン、ジアジクオン、エルホルニチン、酢酸エリプチニウム、エトグルシド、エトポシド、硝酸ガリウム、ヒドロキシウレア、インターフェロン−α、インターフェロン−β、インターフェロン−γ、インターロイキン−2、レンチナン、ロニダミン、ミトグアゾン、ミトキサントロン、モピダモール、ニトラクリン、ペントスタチン、フェナメット、ピラルビシン、ポドフィリン酸、2−エチチドラジド、プロカルバテニポシド、テヌアゾン酸、トリアジクオン、2,2′,2″−トリクロロトリエチルアミン、ウレタン、ビンブラスチン、ビンクリスチン及びビンデシン;抗腫瘍(ホルモン性)剤:アンドロゲン系、例えば、カルステロン、プロピオン酸ドロモスタノロン、エピチオスタノール、メピチオスタン及びテストラクトン;抗副腎系、例えば、アミノグルテチミド、ミトタン及びトリロスタン;抗アンドロゲン系、例えば、フルタミド及びニルタミド;及び抗エストロゲン系、例えば、タモキシフェン及びトレミフェン
12.抗パーキンソン剤、例えば、アマンタジン、ベンセラジド、ビエタナウチン、ビペリデン、ブロモクリプチン、ブジピン、カルビドーパ、デプレニル、デキセチミド、ジエタジン、ドロキシドーパ、エトプロパジン、エチルベンズヒドラミン、レボドーパ、ナキサゴリド、ペルゴリド、ピロヘプチン、プリジノール、プロジピン、テルグリド、チグロイジン及び塩酸トリヘキシフェニジル
13.抗前立腺肥大症剤、例えば、カプロン酸ゲストノロン、メパルトリシン
14.抗精神病薬:ブチロフェノン系、例えば、ベンペリドール、ブロムペリドール、ドロペリドール、フルアニゾン、ハロペリドール、メルペロン、モペロン、ピパンペロン、スニペロン、チミペロン及びトリフルペリドール;フェノチアジン系、例えば、アセトフェナジン、ブタペラジン、カルフェナジン、クロルプロエタジン、クロルプロマジン、クロスピラジン、シアメマジン、ジキシラジン、フルフェナジン、イミクロパジン、メパジン、メソリダジン、メトキシプロマジン、メトフェナゼート、オキサフルマジン、ペラジン、ペリシアジン、ペリメタジン、ペルフェナジン、ピペラセタジン、ピポチアジン、プロクロルペラジン、プロマジン、スルホリダジン、チオプロパゼート、チオリダジン、トリフルオペラジン及びトリフルプロマジン;チオキサンテン系、例えば、クロルプロチキセン、クロペンチキソール、フルペンチキソール及びチオチキセン;他の三環系、例えば、ベンズキナミド、カルピプラミン、クロカプラミン、クロマクラン、クロチアピン、クロザピン、オピプラモール、プロチペンジル、テトラベナジン及びゾテピン;及びその他、例えば、アリザプリド、アミスルプリド、ブラメート、フルスピリレン、モリンドン、ペンフルリドール、ピモジド、スピリレン及びスルピリド
15.鎮痙剤、例えば、アリベンドール、アンブセタミド、アミノプロマジン、アポアトロピン、硫酸メチルベボニウム、ビエタミベリン、ブタベリン、臭化ブトロピウム、臭化N−ブチルスコポルアンモニウム、カロベリン、臭化シメトロピウム、シンナメドリン、クレボプリド、臭酸コニイン、塩酸コニイン、ヨウ化シクロニウム、ジフェメリン、ジイソプロミン、酪酸ジオキサフェチル、臭化ジポニウム、ドロフェニン、臭化エメプロニウム、エタベリン、フェクレミン、フェナラミド、フェノベリン、フェンピプラン、臭化フェンピベリニウム、臭化フェントニウム、フラボキセート、フロプロピオン、グルコン酸、グアイアクタミン、ヒドラミトラジン、ヒメクロモン、レイオピロール、メベベリン、モキサベリン、ナフィベリン、オクタミラミン、オクタベリン、ペンタピペリド、塩酸フェナマシド、フロログルシノール、臭化ピナベリウム、ピペリレート、塩酸ピポキソラン、プラミベリン、臭化プリフィニウム、プロペリジン、プロピバン、プロピロマジン、プロザピン、ラセフェミン、ロシベリン、スパスモリトール、ヨウ化スチロニウム、スルトロポニウム、ヨウ化チエモニウム、臭化チキジウム、チロプラミド、トレピブトン、トリクロミル、トリホリウム、トリメブチン、N,N−1−トリメチル−3,3−ジフェニルプロピルアミン、トロペンジル、塩化トロスピウム及び臭化キセニトロピウム
16.抗不安薬:アリールピペラジン系、例えば、ブスピロン、ゲピロン及びイプサピロン;ベンゾジアゼピン誘導体、例えば、アルプラゾラム、ブロマゼパム、カマゼパム、クロルジアゼポキシド、クロバザム、クロラゼペート、コチアゼパム、クロキサゾラム、ジアゼパム、エチルロフラゼペート、エチゾラム、フルイダゼパム、フルタゾラム、フルトプラゼパム、ハラゼパム、ケタゾラム、ロラゼパム、ロキサピン、メダゼパム、メタクラゼパム、メキサゾラム、ノルダゼパム、オキサゼパム、オキサゾラム、ピナゼパム、プラゼパム及びトフィソパム;カルバメート系、例えば、シクラルバメート、エミルカメート、ヒドロキシフェナメート、メプロバメート、フェンプロバメート及びチバメート;及びその他、例えば、アルピデン、ベンゾクタミン、カプトジアミン、クロルメザノン、エチホキシン、フルオレゾン、グルタミン酸、ヒドロキシジン、メクロラルウレア、メフェノキサロン、オキサナミド、フェナグリコドール、スリクロン
17.カルシウム調節剤、例えば、カルシフェジオール、カルシトニン、カルシトリオール、クロドロン酸、ジヒドロタキステロール、エルカトニン、エチドロン酸、イプリフラボン、パミドロン酸、パラチロイドホルモン及び酢酸テリパラチド
18.強心剤、例えば、アセフィリン、アセチルジギチトキシン、2−アミノ−4−ピコリン、アンリノン、ベンフロジルセミコハク酸塩、ブクラスデシン、セルベロシド、カンホタミド、コンバラトキシン、シマリン、デノパミン、デスラノシド、ジタリン、ジギタリス、ジギトキシン、ジゴキシン、ドブタミン、ドーパミン、ドペキアミン、エノキシモン、エリスロフレイン、フェナルコミン、ギタリン、ギトキシン、グリコシアミン、ヘプタミノール、ヒドラスチニン、イボパミン、ラノトジセス、メタミバム、ミルリノン、ネリイホリン、オレアンドリン、ウーアバイン、オキシフェドリン、プレナルテロール、プロシラリジン、レシブホゲニン、シラレン、シラレニン、ストロファンチン、スルマゾール、テオブロミン及びキサモテロール
19.キレート化剤、例えば、デフェロジミン、ジチオカルブナトリウム、エデト酸カルシウム二ナトリウム、エデト酸二ナトリウム、エデト酸ナトリウム、エデト酸三ナトリウム、ペニシルアミン、ペンテン酸カルシウム三ナトリウム、ペンテクチン酸、スクシメール及びトリエンチン
20.ドーパミンレセプター作動薬、例えば、ブロモクリプチン、ドペキサミン、フェノルドパム、イボパミン、リスリド、ナキサゴリド及びペルゴリド
21.酵素誘導物質(肝)、例えば、フルメシノール
22.エストロゲン:非ステロイド系エストロゲン、例えば、ベンゼストロール、ブロパロエストロール、クロロトリアニセン、ジエネストロール、ジエチルスチルベストロール、ジプロピオン酸ジエチルスチルベストロール、ジメストロール、ホスフェストロール、ヘキセストロール、メタレンストリル及びメテストロール;及びステロイド系エストロゲン、例えば、コルポルモン、接合エストロゲンホルモン、エクイレニン、エクイリン、エストラジオール、安息香酸エストラジオール、17β−シピオン酸エストラジオール、エストリオール、エストロン、エチニルエストラジオール、メストラノール、メキセストロール、ミタトリエンジオール、酪酸クロベタゾン、キネストラジオール及びキネストロール
23.グルココルチコイド、例えば、21−アセトキシプレフネノロン、アアルクロメタゾン、アルゲストン、アミシノニド、ベクロメタゾン、ベタメタゾン、ブデソニド、クロロプレドニゾン、クロベタソール、ブロベタゾン、クロコルトロン、クロプレドノール、コルチコステロン、コルチゾン、コルチバゾール、デフラザコルト、デソニド、デソキシメタゾン、デキサメタゾン、ジフロラゾン、ジフルコルトロン、ジフルプレドネート、エノキソロン、フルアザコルト、フルクロロニド、フルメタゾン、フルニソリド、フルオシノロンアトニド、フルオシノニド、フルオコルチンブチル、フルオコルトロン、フルオロメトロン、酢酸フルペロロン、酢酸フルプレドニデン、フルプレドニゾロン、フルランドレノリド、ホルモコルタル、ハルシノニド、ハロメタゾン、酢酸ハロプレドン、ヒドロコルタメート、ヒドロコルチゾン、酢酸ヒドロコルチゾン、リン酸ヒドロコルチゾン、21−コハク酸ヒドロコルチゾンナトリウム、テブト酸ヒドロコルチゾン、マジプレドン、メドリゾン、メプレドニゾン、メチオルプレドニゾロン、フラン酸モメタゾン、パラメタゾン、プレドニカルベート、プレドニゾロン、21−ジエチルアミノ酢酸プレドニゾロン、リン酸プレドニゾンナトリウム、コハク酸プレドニゾロンナトリウム、21−m−スルホ安息香酸プレドニゾロンナトリウム、21−ステアロイルグルコール酸プレドニゾロン、テブト酸プレドニゾロン、21−トリメチル酢酸プレドニゾロン、プレドニゾン、プレドニバル、プレドニリデン、21−ジエチルアミノ酢酸プレドニリデン、チキソコルタール、トリアンシノロン、トリアンシノロンアセトニド、トリアンシノロンベネトニド及びトリアンシノロンヘキサセトニド
24.ミネラルコルチコイド、例えば、アルドステロン、デオキシコルチコステロン、酢酸デオキシコルチコステロン及びフルドロコルチゾン
25.モノアミンオキシダーゼ阻害剤、例えば、デプレニル、イプロクロジド、イプロニアジド、イソカルボキサジド、モクロベミド、オクトモキシン、パルギリン、フェネルジン、フェノキシプロパジン、ピバリルベンズヒドラジン、プロジピン、トロキサトン及びトラニルシプロミン
26.筋弛緩剤(骨格)、例えば、アフロクアロン、アルクロニウム、ベシル酸アトラクリウム、バクロフェン、ベンゾクタミン、塩化ベンゾキノニウム、C−カレバッシン、カリソプロドール、クロルメザノン、カルバミン酸クロルフェネシン、クロルプロエタジン、クロゾキサゾン、クラレ、シクラルバメート、シクロベンザプリン、ダントロレン、臭化デカメトニウム、ジアゼパム、エペリゾン、臭化ファザジニウム、フルメトラミド、トリエトヨウ化ガラミン、臭化ヘキサカルバコリン、臭化ヘキサフルオレニウム、イドロシラミド、硫酸メチルラウエキシウム、レプトダクチリン、メマンチン、メフェネシン、メフェノキサロン、メタキサロン、メトカルバモール、ヨウ化メトクリン、ニメタゼパム、オルフェナドリン、臭化パンクロニウム、フェンプロバメート、フェニラミドール、臭化ピペクリウム、プロモキソラン、硫酸キニン、スチラメート、臭化スクシニルコリン、塩化スクシニルコリン、ヨウ化スクシニルコリン、臭化スキセトニウム、テトラゼパム、チオコルキコシド、チザニジン、トルペリゾン、塩化ツボクラリン、臭化ベクロニウム、メシル酸プリジノール及びゾキソラミン
27.麻薬拮抗薬、例えば、アミフェナゾール、シクラゾシン、レバロルファン、ナジド、ナルムフェン、ナロルフィン、ジニコチン酸ナロルフィン、ナロキソン及びナルトレキソン
28.プロゲストーゲン、例えば、アリルエストレノール、アナゲストン、酢酸クロルマジノン、酢酸デルマジノン、デメゲストン、デソゲストレル、ジメチステロン、ジドロゲステロン、エチステロン、エチノジオール、酢酸フルロゲストン、ゲストデン、カプロン酸ゲストノロン、ハロプロゲステロン、17−ヒドロキシ−16−メチレンプロゲステロン、17α−ヒドロキシプロゲステロン、カプロン酸17α−ヒドロキシゲステロン、リネストレノール、メドロゲストン、メドロキシプロゲステロン、酢酸メゲストロール、メレンゲストロール、ノルエチンドロン、ノルエチノドレル、ノルゲステロン、ノルゲスチメート、ノルゲストレル、ノルゲストリエノン、ノルビニステロン、ペンタゲストロン、プロゲステロン、プロメゲストン、キンゲストロン及びトレンゲストン及びそのエステル
29.血管拡張剤(冠動脈)、例えば、アモトリフェン、ベンダゾール、ヘミスクシン酸ベンフロジル、ベンジオダロン、クロアシジン、クロモナール、クロベンフロール、クロニトレート、ジラゼップ、ジピリダモル、ドロプレニラミン、エフロキセート、エリトリトール、四硝酸エリトリチル、エタフェノン、フェンジリン、フロレジル、ガングレフェン、ヘキセストロールビス(β−ジエチルアミノエチルエーテル)、ヘキソベンジン、トシル酸イトラミン、ケリン、リドフラジン、六硝酸マンニトール、メジバジン、ニコランジル、ニトログリセリン、四硝酸ペンタエリトリトール、ペントリニトロール、ペルヘキシリン、ピメフィリン、プレニラミン、硝酸プロパチル、ピリドフィリン、トラピジル、トリクロミル、トリメタジジン、リン酸トロルニトレート及びビスナジン及び末梢血管拡張剤、例えば、ニコチン酸アルミニウム、バメタン、ベンシクラン、ベタヒスチン、ブラジキニン、ブロビンカミン、ブホニオード、ブフロメジル、ブタラミン、セチエジル、シクロニケート、シネパジド、シンナリジン、シクランデレート、ジクロル酢酸ジイソプロピルアミン、エレドイシン、フェノキシジル、フルナリシン、ヘロニケート、イフェンプロジル、ナイアシン酸イノシトール、イソキシスプリン、カリジン、カリクレイン、モキシシリテ、ナフロニル、ニカメテート、ニセルゴリン、ニコフラノース、ニコチニルアルコール、ニリドリン、ペンチフィリン、ペントキシフィリン、ピリベジル、プロタグランジンE1、スロクチジル及びナイアシン酸キサンチナール
30.ベンゾジアゼピン拮抗薬、例えば、フルマゼニル
31.気管支拡張剤:エフェドリン誘導体、例えば、アルブテロール、バンブテロール、ビトルテロール、カルブテロール、クレンブテロール、クロルプレナリン、ジオキセテドリン、エフェドリン、エピニフリン、エプロジノール、エタフェドリン、エチルノルエピネフリン、フェノテロール、ヘキソプレナリン、イソエタリン、イソプロテレノール、マブテロール、メタプロテレノール、N−メチルエフェドリン、ピルブテロール、プロカテロール、プロトキロール、レプロテロール、リミテロール、ソテレノール、テルブタリン及びツロブテロール;四級アンモニウム化合物、例えば、硫酸メチルベボニウム、臭化クルトロピウム、臭化イプラトロピウム及び臭化オキシトロピウム;キサンチン誘導体、例えば、アセフィリン、アセフィリンピペラジン、アンブフィリン、アミノフィリン、バミフィリン、コリンテオフィリネート、ドキソフィリン、ダイフィリン、エンプロフィリン、エタミフィリン、エトフィリン、グアイチリン、プロキシフィリン、テオブロミン、1−テオブロミン酢酸及びテオフィリン;及びその他、例えば、フェンスピリド、メジバジン、メトキシフェナミン及びトレトキノール
32.その他、オキシブチニンなどの失禁治療薬、リセドロネートなどの骨粗鬆症治療薬、酢酸ケトフェチンなどの抗ヒスタミン治療薬、トルブタミドなどの糖尿病治療薬、コルヒチンなどの通風治療薬
等が挙げられる。これらは必要に応じて二種類以上併用することができる。
苛性アルカリを用いた重合法により、数平均分子量3000のオキシプロピレン重合体グリコールを得た。特開平5−117521号公報の合成例1の方法に準じ、そのオキシプロピレン重合体グリコールを開始剤として複合金属シアン化物錯体触媒(亜鉛ヘキサシアノコバルテート)を用いてプロピレンオキシドを重合し、数平均分子量28000の重合物を得た。この重合物に対して、ナトリウムメチラートの28%メタノール溶液と塩化アリルを使用して末端をアリル基に変換した後、脱塩精製して、1分子中に概ね2個のアリル基末端を有するポリオキシアルキレン重合体(重合体A−1)を得た。得られた重合体のアリル末端基量は0.12mmol/gであった。
特開平5−117521号公報の合成例1の方法に準じ、苛性アルカリを用いた重合法により、数平均分子量3000のオキシプロピレン重合体グリコールを得た。このオキシプロピレン重合体グリコールとアルカリとジハロメタンとを分子鎖延長反応に供し、さらに、塩化アリルにより末端をアリル基に変化した後、脱塩精製することで重合体A−2を得た。この重合体の、GPCによる数平均分子量は13800であり、1分子中有するアリル末端は概ね1個であった。重合体A−2の重量あたりのアリル末端基量は0.12mmol/gであった。
下記式(4)で表されるメチルハイドロジェンシリコーン(式中、xは平均5である)に白金触媒存在下、全ヒドロシリル基量の0.5当量のα−メチルスチレンを添加し、1分子中に平均2.5個のヒドロシリル基を有する化合物(化合物B)を得た。この化合物のヒドロシリル基含有量は3.2mmol/gであった。
重合体(A−1)70重量部、重合体(A−2)30重量部に対して、化合物(B)を2.3重量部、ヒドロシリル化触媒である白金−1,3−ジビニル−1,1,3,3−テトラメチルジシロキサン錯体(3重量%白金イソプロパノール溶液)0.1重量部、マレイン酸ジメチル0.03重量部、を十分に混合して粘着剤組成物を得た。この粘着剤組成物をポリエステルフィルム(厚さ25μm)上に硬化後の厚みが50μmになるよう塗布したのち、130℃で5分間加熱し、本発明の貼付剤を得た。
重合体(A−1)90重量部、重合体(A−2)10重量部に対して、化合物(B)を2.1重量部、ヒドロシリル化触媒である白金−1,3−ジビニル−1,1,3,3−テトラメチルジシロキサン錯体(3重量%白金イソプロパノール溶液)0.1重量部、マレイン酸ジメチル0.03重量部、を十分に混合して粘着剤組成物を得た。この粘着剤組成物をポリエステルフィルム(厚さ25μm)上に硬化後の厚みが50μmになるよう塗布したのち、130℃で5分間加熱し、本発明の貼付剤を得た。
重合体(A−1)50重量部、重合体(A−2)50重量部に対して、化合物(B)を3.8重量部、ヒドロシリル化触媒である白金−1,3−ジビニル−1,1,3,3−テトラメチルジシロキサン錯体(3重量%白金イソプロパノール溶液)0.1重量部、マレイン酸ジメチル0.03重量部、を十分に混合して粘着剤組成物を得た。この粘着剤組成物をポリエステルフィルム(厚さ25μm)上に硬化後の厚みが50μmになるよう塗布したのち、130℃で5分間加熱し、本発明の貼付剤を得た。
重合体(A−1)100重量部に対して、化合物(B)を2.3重量部、ヒドロシリル化触媒である白金−1,3−ジビニル−1,1,3,3−テトラメチルジシロキサン錯体(3重量%白金イソプロパノール溶液)0.1重量部、マレイン酸ジメチル0.03重量部、を十分に混合して粘着剤組成物を得た。この粘着剤組成物をポリエステルフィルム(厚さ25μm)上に硬化後の厚みが50μmになるよう塗布したのち、130℃で5分間加熱し、貼付剤を得た。
重合体(A−1)100重量部に対して、化合物(B)を3.6重量部、ヒドロシリル化触媒である白金−1,3−ジビニル−1,1,3,3−テトラメチルジシロキサン錯体(3重量%白金イソプロパノール溶液)0.1重量部、マレイン酸ジメチル0.03重量部、を十分に混合して粘着剤組成物を得た。この粘着剤組成物をポリエステルフィルム(厚さ25μm)上に硬化後の厚みが50μmになるよう塗布したのち、130℃で5分間加熱し、貼付剤を得た。
幅25mmに裁断した帯状の各製剤サンプルをSUS304の板に貼付し、重さ2kgのゴムローラーを速度2m/minの条件で1往復させて密着させた後、1時間放置した。各テープをSUS304板から300mm/minの速度にて180°の角度で剥がす際の応力を接着強さの測定値とした。
幅25mmに裁断した帯状の各製剤サンプルをSUS304の板に貼付し、それを水平に固定した後、サンプルの一端を折り曲げ、鉛直方向に錘をぶら下げる。1時間後に剥離しない最大の重量を固定力とする。
幅25mm長さ10cmに裁断した帯状の各製剤サンプルを30°の角度に設置し、SUS304製のボールを滑走距離10cmで転がし、JIS Z 0237に準ずる傾斜式ボールタック試験を行った。粘着剤上で静止した最大のボールNo.をボールタックNo.とする。
Claims (8)
- 支持体上に粘着剤組成物層が形成された皮膚貼付用の粘着シートであって、該粘着剤組成物層が
(A)末端に少なくとも1個のアルケニル基を有するポリエーテル系重合体
(B)分子中に1〜10個のヒドロシリル基を有する化合物
(C)ヒドロシリル化触媒
からなる混合物を硬化してなり、
重合体(A)が、末端に1個のアルケニル基を有するポリエーテル系重合体と、末端に2個以上のアルケニル基を有するポリエーテル系重合体を含む、2種類以上の重合体より構成されることを特徴とする皮膚貼付用の粘着シート。 - 重合体(A)のポリエーテル系重合体がポリオキシプロピレンであることを特徴とする請求項1に記載の粘着シート。
- サイズ排除クロマトグラフィーで測定した重合体(A)のポリスチレン換算数平均分子量が3000〜50000である請求項1または2に記載の粘着シート。
- 重合体(A)を構成する末端に1個のアルケニル基を有するポリエーテル系重合体の含有分率が0.1%〜70%であることを特徴とする請求項1〜3のいずれかに記載の粘着シート。
- ヒドロシリル化触媒(C)が白金−ビニルシロキサン錯体であることを特徴とする、請求項1〜4のいずれかに記載の粘着シート。
- 粘着剤組成物層が、さらに、
(D)有機液状成分
を含有する混合物を硬化してなることを特徴とする請求項1〜5のいずれかに記載の粘着シート。 - 液状成分(D)が脂肪酸エステルであることを特徴とする請求項1〜6のいずれかに記載の粘着シート。
- 請求項1〜7のいずれかに記載の粘着シートに、生理活性物質を含有してなる経皮吸収製剤。
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