JP2013525345A - 経皮吸収製剤 - Google Patents
経皮吸収製剤 Download PDFInfo
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- JP2013525345A JP2013525345A JP2013506085A JP2013506085A JP2013525345A JP 2013525345 A JP2013525345 A JP 2013525345A JP 2013506085 A JP2013506085 A JP 2013506085A JP 2013506085 A JP2013506085 A JP 2013506085A JP 2013525345 A JP2013525345 A JP 2013525345A
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- Prior art keywords
- drug
- preparation according
- adhesive layer
- resin
- containing adhesive
- Prior art date
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Abstract
本発明は、薬物含有粘着層、薬物保護層及び剥離層を含む経皮吸収製剤であって、上記薬物含有粘着層は、ロピニロールまたはその塩、ゴム、粘着付与樹脂、酸化防止剤、及び経皮吸収促進剤を含む。また、本発明は、薬物含有粘着層、薬物保護層及び剥離層を含む経皮吸収製剤であって、上記薬物含有粘着層は、ロピニロールまたはその塩、アクリル系粘着剤、結晶化防止剤、及び経皮吸収促進剤を含む経皮吸収製剤を提供する。本発明の経皮吸収製剤をパーキンソン病または下肢静止不能症候群の治療用として使用する場合、初期血中濃度の上昇による副作用が無く、そして薬物の皮膚透過性能に優れている。
Description
Claims (26)
- 薬物含有粘着層、薬物保護層及び剥離層を含む経皮吸収製剤であって、前記薬物含有粘着層は、ロピニロールまたはその塩、ゴム、粘着付与樹脂、酸化防止剤及び経皮吸収促進剤を含むことを特徴とする経皮吸収製剤。
- 薬物含有粘着層、薬物保護層及び剥離層を含む経皮吸収製剤であって、前記薬物含有粘着層は、ロピニロールまたはその塩、アクリル系粘着剤、結晶化防止剤及び経皮吸収促進剤を含むことを特徴とする経皮吸収製剤。
- 前記経皮吸収製剤が、支持層をさらに含むことを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記ロピニロールまたはその塩が、薬物含有粘着層の総重量に対して5〜30重量%含まれることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記ゴムが、スチレン−エチレン−イソプレン−スチレン(styrene−ethylene−isoprene−styrene)共重合体、スチレン−ブタジエン−スチレン(styrene−butadiene−styrene)共重合体、スチレン−ブタジエン(styrene−butadiene)共重合体、スチレン−イソプレン(styrene−isoprene)共重合体、スチレン−イソプレン−スチレン(styrene−isoprene−styrene)共重合体、シリコンゴム、及びポリイソブチレン(polyisobutylene)からなる群から選ばれる少なくとも1つであることを特徴とする請求項1に記載の経皮吸収製剤。
- 前記ゴムが、薬物含有粘着層の総重量に対して10〜50重量%含まれることを特徴とする請求項1に記載の経皮吸収製剤。
- 前記粘着付与樹脂が、ロジングリセリンエステル樹脂、水素添加ロジングリセリンエステル樹脂、ロジンペンタエリスリトールエステル樹脂、水素添加ロジンペンタエリスリトールエステル樹脂、アルファ−メチルスチレン樹脂、炭素数5〜9の脂環式飽和炭化水素樹脂、炭素数5〜9の脂肪族炭化水素樹脂、芳香族炭化水素樹脂、水素添加ジシクロペンタジエン樹脂、テルペン樹脂、クマロンインデン樹脂、及びテルペンフェノール樹脂からなる群から選ばれる少なくとも1つであることを特徴とする請求項1に記載の経皮吸収製剤。
- 前記粘着付与樹脂が、薬物含有粘着層の総重量に対して5〜70重量%含まれることを特徴とする請求項1に記載の経皮吸収製剤。
- 前記酸化防止剤が、ブチル化ヒドロキシトルエン(BHT)、イルガノックス565、イルガノックス1010、イルガノックス1076、亜リン酸系酸化防止剤、及びこれらの混合物のうち一つであることを特徴とする請求項1に記載の経皮吸収製剤。
- 前記酸化防止剤が、薬物含有粘着層の総重量に対して0重量%超過2重量%以下含まれることを特徴とする請求項1に記載の経皮吸収製剤。
- 前記経皮吸収促進剤が、ポリオキシエチレンモノオレート(polyoxyethylene monooleate)、ポリグリセリルジイソステアレート(polyglyceryl diisostearate)、N−メチル−2−ピロリドン(N−methyl−2−pyrrolidone)、N−カプリリル−2−ピロリドン(N−carprylyl−2−pyrrolidone)、N−ドデシル−2−ピロリドン(N−dodecyl−2−pyrrolidone(lauryl pyrrolidone))、ラウリルアルコール(lauryl alcohol)、グリセロールラウリルアルコール(glycerol lauryl alcohol)、オレイルアルコール(oleyl alcohol)、イソプロピルミリストレート(isopropyl myristrate)、ソルビタンモノオレート(sorbitan mono−oleate)、プロピレンモノラウレート(propylene monolaurate)、プロピレンモノオレート(propylene monooleate)、オレオイルマクロゴールグリセリド(oleoyl macrogolglyceride)、オレイン酸(oleic acid)、ラウロイルマクロゴールグリセリド(lauroyl macrogolglyceride)、リノレオイルマクロゴールグリセリド(linoleoyl macrogolglyceride)、プロピレングリコールカプリレート(Propylene glycol caprylate)、プロピレングリコールカプレート(Propylene glycol caprate)、ソルビタンモノステアレートモノオレート(Sorbitan monostearate monooleate)、グリセロールモノラウレート(glycerol monolaurate)、グリセロールモノオレート(glycerol monooleate)、プロピレングリコールモノラウレート(propyleneglycol monolaurate)、プロピレングリコールモノカプリレート(propyleneglycol monocaprylate)、ソルビタンモノラウレート(sorbitan monolaurate)、ソルビタンモノオレート(sorbitan monooleate)、ラウリルラクテート(lauryl lactate)、カプリルトリグリセリド(caprylic triglyceride)、カプリントリグリセリド(capric triglyceride)、トウモロコシ油PEG−8エステル、トウモロコシ油PEG−6エステル、及びトリアセチンからなる群から選ばれる少なくとも1つであることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記経皮吸収促進剤が、薬物含有粘着層の総重量に対して5〜20重量%含まれることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記アクリル系粘着剤が、官能基を有さないか、或いは−COOH、−OH及び−NH2からなる群から選ばれる少なくとも1つの官能基を含むことを特徴とする請求項2に記載の経皮吸収製剤。
- 前記アクリル系粘着剤が、薬物含有粘着層の総重量に対して30〜90重量%含まれることを特徴とする請求項2に記載の経皮吸収製剤。
- 前記結晶化防止剤が、ポリビニルピロリドン、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、及びエチルセルロースからなる群から1種以上選ばれることを特徴とする請求項2に記載の経皮吸収製剤。
- 前記結晶化防止剤が、薬物含有粘着層の総重量に対して0.1〜20重量%含まれることを特徴とする請求項2に記載の経皮吸収製剤。
- 前記薬物保護層は、ポリエステルフィルム、ポリプロピレンフィルム、ポリエチレンフィルム、ポリアクリロニトリルフィルム、金属が蒸着されたポリエステルフィルム、不織布が張り合わせたポリエステルフィルム、及びこれらの多層化フィルム(multilayered film)からなる群から選ばれることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記剥離層が、ポリエステル、ポリビニルクロリド、ポリビニリデンクロリド、ポリエチレンテレフタレート及びこれらの共重合体からなる群から選ばれるいずれか1つより作られている高分子フィルムをシリコン樹脂またはフッ素樹脂でコーティングすることで形成されるか、あるいは、ポリオレフィン含有上質紙またはグラシン紙をシリコン樹脂またはフッ素樹脂でコーティングすることで形成された剥離紙であることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記支持層が、ポリウレタンフィルム、多孔性フィルム、穿孔フィルム、織物、不織布及びフォーム(foam)からなる群から選ばれたいずれか1つに、アクリル系粘着剤、ゴム系粘着剤、シリコン系粘着剤及びエチレンビニルアセテート(EVA)系粘着剤からなる群から選ばれたいずれか1つを適用することで形成されることを特徴とする請求項3に記載の経皮吸収製剤。
- 前記薬物含有粘着層が、さらに凝集力強化剤を薬物含有粘着層の総重量に対して0.1〜10重量%含むことを特徴とする請求項1に記載の経皮吸収製剤。
- 前記凝集力強化剤が、シリカジメチルシリレートであることを特徴とする請求項20に記載の経皮吸収製剤。
- 前記薬物含有粘着層が、厚さが30〜120μmであることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記薬物保護層が、厚さが5〜500μmであることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記剥離層が、厚さが15〜500μmであることを特徴とする請求項1または2に記載の経皮吸収製剤。
- 前記支持層が、厚さが5〜500μmであることを特徴とする請求項3に記載の経皮吸収製剤。
- ロピニロールまたはその塩が、1〜7日間所定の速度で、皮膚で吸収される場合は、前記ロピニロールまたはその塩の透過速度が3〜200μg/cm2/hrであることを特徴とする請求項1または2に記載の経皮吸収製剤。
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JP2015221767A (ja) * | 2014-05-23 | 2015-12-10 | 帝國製薬株式会社 | 経皮投与製剤 |
WO2016052522A1 (ja) * | 2014-09-30 | 2016-04-07 | ニプロ株式会社 | 経皮投与製剤及び包装体 |
JP2017503865A (ja) * | 2014-01-22 | 2017-02-02 | デウン ファーマシューティカル カンパニー リミテッド | ドネペジルまたはその塩を含む経皮吸収システム |
JP2019507142A (ja) * | 2016-02-11 | 2019-03-14 | アイキュア ファーマスーティカル インク. | 経皮投与用紫外線硬化型ハイドロゲル樹脂、ハイドロゲル及びこれを含むカタプラズマ剤 |
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JP5415645B1 (ja) * | 2013-06-28 | 2014-02-12 | 久光製薬株式会社 | 貼付剤の製造方法、貼付剤及び包装体 |
JP2017503865A (ja) * | 2014-01-22 | 2017-02-02 | デウン ファーマシューティカル カンパニー リミテッド | ドネペジルまたはその塩を含む経皮吸収システム |
JP2015221767A (ja) * | 2014-05-23 | 2015-12-10 | 帝國製薬株式会社 | 経皮投与製剤 |
WO2016052522A1 (ja) * | 2014-09-30 | 2016-04-07 | ニプロ株式会社 | 経皮投与製剤及び包装体 |
JP2019507142A (ja) * | 2016-02-11 | 2019-03-14 | アイキュア ファーマスーティカル インク. | 経皮投与用紫外線硬化型ハイドロゲル樹脂、ハイドロゲル及びこれを含むカタプラズマ剤 |
JP2020158514A (ja) * | 2016-02-11 | 2020-10-01 | アイキュア ファーマスーティカル インク. | 経皮投与用紫外線硬化型ハイドロゲルを含むカタプラズマ剤 |
US11382868B2 (en) | 2016-02-11 | 2022-07-12 | Icure Pharmaceutical Inc. | Transdermal UV-curable hydrogel resin, hydrogel curing the same and cataplasm containing the same |
WO2021054257A1 (ja) * | 2019-09-18 | 2021-03-25 | 久光製薬株式会社 | ロピニロール含有貼付剤及びロピニロールの皮膚透過性向上方法 |
JP6908800B1 (ja) * | 2019-09-18 | 2021-07-28 | 久光製薬株式会社 | ロピニロール含有貼付剤及びロピニロールの皮膚透過性向上方法 |
TWI775149B (zh) * | 2019-09-18 | 2022-08-21 | 日商久光製藥股份有限公司 | 含羅匹尼羅之貼附劑及羅匹尼羅之皮膚透過性之提升方法 |
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CN102946873B (zh) | 2015-05-13 |
KR101292768B1 (ko) | 2013-08-05 |
EP2561865A2 (en) | 2013-02-27 |
CN102946873A (zh) | 2013-02-27 |
WO2011132966A2 (ko) | 2011-10-27 |
WO2011132966A3 (ko) | 2012-04-12 |
KR20110118525A (ko) | 2011-10-31 |
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US20130165875A1 (en) | 2013-06-27 |
EP2561865A4 (en) | 2014-05-28 |
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