JP2008195738A - 経皮グラニセトロン - Google Patents
経皮グラニセトロン Download PDFInfo
- Publication number
- JP2008195738A JP2008195738A JP2008111808A JP2008111808A JP2008195738A JP 2008195738 A JP2008195738 A JP 2008195738A JP 2008111808 A JP2008111808 A JP 2008111808A JP 2008111808 A JP2008111808 A JP 2008111808A JP 2008195738 A JP2008195738 A JP 2008195738A
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- granisetron
- adhesive
- patch
- patch according
- vomiting
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Images
Classifications
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Abstract
【解決手段】接着性パッチが、非酸性求核性部分(但し、該非酸性ヒドロキシル部分は、ヒドロキシメチルアクリレート、ヒドロキシエチルアクリレート、ヒドロキシプロピルアクリレート、ヒドロキシメチルメタクリレート、又は、ヒドロキシエチルメタクリレートによっては提供されない)を含むアクリル接着剤を備える(但し、該接着剤は、側鎖にポリエチレンオキシド又はポリエチレンオキシドモノメチルエーテルを有するアクリル系粘着基剤を含まない)。
【選択図】なし
Description
Porzioら CFS-Theら、2003
求核性モノマーを含む接着剤中にグラニセトロンを導入する可能性を試験するために、この薬物を、4つの異なるNational Starch接着剤中に製剤化した。表1中に列挙されるように、これらの接着剤のうち1つは官能基を有さないポリマーを含み、2つは酸性官能基を有するポリマーを含み、そして4番目はヒドロキシル官能基を含んだ。
実施例1の最良の製剤における薬物安定性を調査した。
ヒトにおけるin vivoでのグラニセトロンの徐放
パッチの調製
グラニセトロンパッチを、以下の様式で調製したコーティング溶液から製造した:
1.DT 387-2287の固体含量を決定し、この接着剤を酢酸エチルで希釈して、49%の規格下限値にした。次いでこの溶液を、15分間にわたってスターラーによって混合した。
2.透明な溶液(約67mg/ml)が得られるまで、グラニセトロン基剤をジメチルアセトアミド(DMA)中に溶解した。
3.上記1から得られた接着剤溶液を、2から得られたグラニセトロン溶液と混合した。
(参考文献)
Claims (30)
- グラニセトロンを含む接着性経皮パッチであって、
更に、非酸性ヒドロキシル部分(但し、該非酸性ヒドロキシル部分は、ヒドロキシメチルアクリレート、ヒドロキシエチルアクリレート、ヒドロキシプロピルアクリレート、ヒドロキシメチルメタクリレート、又は、ヒドロキシエチルメタクリレートによっては提供されない)を含むアクリル接着剤を含み(但し、該接着剤は、側鎖にポリエチレンオキシド又はポリエチレンオキシドモノメチルエーテルを有するアクリル系粘着基剤を含まない)、
生理学的有効量のグラニセトロンが前記接着剤中に装填されている接着性経皮パッチ。 - 前記非酸性ヒドロキシル部分が、適切に選択されたコモノマーによって提供される、請求項1に記載のパッチ。
- 前記選択されたコモノマーが、置換されたアクリレートおよびメタクリレートから選択される、請求項2に記載のパッチ。
- 感圧性である、請求項1乃至3のいずれか一項に記載のパッチ。
- 過半量の主要なアクリレートモノマーを含む、請求項1乃至4のいずれか一項に記載のパッチ。
- 前記主要なアクリレートモノマーが、2-エチルヘキシルアクリレートまたはブチルアクリレートのいずれかである、請求項5に記載のパッチ。
- 約2時間後に薬理学的有効量のグラニセトロンを提供するように適合された、請求項1乃至6のいずれか一項に記載のパッチ。
- 約10重量%までのグラニセトロンを含む、請求項1乃至7のいずれか一項に記載のパッチ。
- 8% w/w未満のグラニセトロンを有する、請求項8に記載のパッチ。
- 約4% w/wを上回るグラニセトロンのレベルを有する、請求項1乃至9のいずれか一項に記載のパッチ。
- 6% w/wと7.7% w/wとの間のグラニセトロンのレベルを有する、請求項8に記載のパッチ。
- 室温および常圧での1ヶ月間の保存の後に結晶化が観察されない、請求項1乃至11のいずれか一項に記載のパッチ。
- 化学的に誘発された嘔吐の処置又は予防のための、請求項1乃至12のいずれか一項に記載のパッチ。
- 前記嘔吐が急性である、請求項13に記載のパッチ。
- 前記嘔吐が遅延性である、請求項13に記載のパッチ。
- 分割化学療法に付随する嘔吐の処置又は予防のための、請求項1から12のいずれか一項に記載のパッチ。
- 術後の悪心および嘔吐の処置又は予防のための、請求項1から12のいずれか一項に記載のパッチ。
- 化学療法により誘発された悪心及び嘔吐の処置又は予防のための、請求項1から12のいずれか一項に記載のパッチ。
- 放射線療法に付随する悪心及び嘔吐の処置又は予防のための、請求項1から12のいずれか一項に記載のパッチ。
- 分割癌療法に付随する悪心及び嘔吐の処置又は予防のための、請求項1から12のいずれか一項に記載のパッチ。
- 掻痒、線維筋痛およびそれに付随する疼痛、偏頭痛、不安、認識障害および精神病性障害、鬱病、精神分裂病、産後鬱病における精神病、過敏性腸症候群、アルコール中毒症、閉塞性睡眠時呼吸障害、乗り物酔い、アルツハイマー病などの認識機能の喪失、尿失禁、ジスキネジア、全身性エリテマトーデス、薬物性の掻痒、早期射精、摂食障害、強迫性障害、胃運動障害、慢性疲労症候群、消化不良ならびにコカイン依存症から選択される状態の処置または予防のための、請求項1から12のいずれか一項に記載のパッチ。
- 前記接着剤に、3% w/wと12% w/wとの間のグラニセトロンが装填されている、請求項1乃至21のいずれか一項に記載のパッチ。
- 前記接着剤に、4% w/wと10% w/wとの間のグラニセトロンが装填されている、請求項22に記載のパッチ。
- 前記接着剤に、5% w/wと8% w/wとの間のグラニセトロンが装填されている、請求項22に記載のパッチ。
- 可塑剤も浸透促進剤も導入していない、請求項1乃至24のいずれか一項に記載のパッチ。
- 6% w/wのグラニセトロンの接着剤充填量で、前記接着剤が10cm2と100cm2との間の表面積を有する、請求項1乃至25のいずれか一項に記載のパッチ。
- 前記接着剤が15cm2と50cm2との間の表面積を有する、請求項26に記載のパッチ。
- 5−HT3レセプター活性に関連する嘔吐の処置又は予防のための医薬品の製造におけるグラニセトロンの使用であって、
前記医薬品が、患者の皮膚に施される、請求項1乃至20及び22乃至27のいずれか一項に記載の接着性経皮パッチである使用。 - 化学療法により誘発された悪心及び嘔吐の処置又は予防のための医薬品の製造におけるグラニセトロンの使用であって、
前記医薬品が、患者の皮膚に施される、請求項1乃至20及び22乃至27のいずれか一項に記載の接着性経皮パッチである使用。 - 掻痒、線維筋痛及びそれに付随する疼痛、偏頭痛、不安、認識障害及び精神病性障害、鬱病、精神分裂病、産後鬱病における精神病、過敏性腸症候群、アルコール中毒症、閉塞性睡眠時呼吸障害、乗り物酔い、アルツハイマー病等の認識機能の喪失、尿失禁、ジスキネジア、全身性エリテマトーデス、薬物性の掻痒、早期射精、摂食障害、強迫性障害、胃運動障害、慢性疲労症候群、消化不良並びにコカイン依存症から選択される状態の処置又は予防のための医薬品の製造におけるグラニセトロンの使用であって、
前記医薬品が、患者の皮膚に施される、請求項1乃至12及び21乃至27のいずれか一項に記載の接着性経皮パッチである使用。
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
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GBGB0302662.2A GB0302662D0 (en) | 2003-02-05 | 2003-02-05 | Transdermal granisetron |
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JP2006502225A Division JP4146486B2 (ja) | 2003-02-05 | 2004-02-05 | 経皮グラニセトロン |
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JP2008111808A Pending JP2008195738A (ja) | 2003-02-05 | 2008-04-22 | 経皮グラニセトロン |
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