JP6845162B2 - ケタミン経皮送達システム - Google Patents
ケタミン経皮送達システム Download PDFInfo
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- JP6845162B2 JP6845162B2 JP2017566151A JP2017566151A JP6845162B2 JP 6845162 B2 JP6845162 B2 JP 6845162B2 JP 2017566151 A JP2017566151 A JP 2017566151A JP 2017566151 A JP2017566151 A JP 2017566151A JP 6845162 B2 JP6845162 B2 JP 6845162B2
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- delivery device
- transdermal delivery
- ketamine
- plasma concentration
- abuse
- Prior art date
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Description
実施例1−5の製剤が以下の表6に開示される。
《分離されていない乱用防止剤を含む経皮送達デバイス》
実施例5は、接着剤薬物マトリックス中に5mgの安息香酸デナトニウム及び200mgのケタミンを含む経皮送達デバイスを調製するように変更された。インビトロ皮膚浸透試験では、(その分子量が大きく(447DA)、融点が高い(170℃)ため、)安息香酸デナトニウムは皮膚に浸透しなかったことが示された。それにも関わらず、ケタミンは優れた皮膚浸透性を示し(24時間で0.8mg/cm2)、これは安息香酸デナトニウムなどの乱用抑止剤の取り込みがケタミンの皮膚浸透に影響を与えなかったことを示している。
《分離層において乱用抑止剤を有する経皮送達デバイス》
実施例7は、分離層中に乱用抑止剤を有する経皮送達デバイスを含む。実施例7で使用される乱用抑止剤は、経皮送達デバイス中のケタミンを抽出及び乱用するのに使用される一般的な溶媒(例えば水及びアルコールなど)と反応するゲル化剤である。接着剤−薬物層及び乱用抑止層の厚さはともに、約2−約5ミルである。実施例7による経皮送達デバイスは、2段階プロセスで調製される。
PolyOx1105、プロピレングリコール及びPEG4000は、乱用防止層を形成するために混合された。3つの成分は水/エタノール溶媒に溶解され、続いて湿潤フィルムが例えば3Mのポリエチレンフィルム、Scotpak 1012などの裏張り層のシート上に直接成型された。湿潤フィルムは次いで、対流空気乾燥オーブンにおいて60℃で30分間乾燥された。乱用防止層のコーティングの厚さは約3ミルである。適切な乱用抑止層組成の例が表9に開示されている。
接着剤薬物マトリックス層は、接着剤薬物マトリックス混合物を直接(ステップ1で調製された)乱用防止層上に流し込むことによって、又は剥離ライナー上に流し込み次いで乱用抑止層にラミネートされることによって調製される。
実施例7による経皮送達デバイスは、乱用防止層においてアポモルヒネ(嘔吐剤)を用いて調製される。乱用者による溶媒抽出の後、嘔吐剤は、注射、吸飲又は吸入された場合に重度の吐き気を引き起こす可能性がある。アポモルヒネは本発明において、好ましくは最終製剤の約0.05−5重量%、最も好ましくは約0.1−2重量%で使用される。
実施例9は、乱用抑止剤がカプサイシンであることを除いて、実施例7に従って調製された。乱用者によって溶媒に溶解された後、カプサイシンを含有するケタミン溶液は、吸飲又は吸入された場合に著しく痛みが強い灼熱感を引き起こし、それによって経皮薬物送達装置の乱用可能性を減少させる。
表11は、それによって乱用抑止剤を本発明の経皮送達デバイスで使用することができる追加の技術を提供する。
本発明の一実施形態は、実施例7に従って調製され、接着剤−薬物層は接着剤及び200mgのケタミンを含み、乱用抑止層は7mgのSLS及び5mgの安息香酸デナトニウムを含むゲル形成剤を含む。
2 接着剤薬物マトリックス
3 剥離ライナー
4 乱用抑止剤
5 薬物
6 乱用抑止層
7 オーバーレイ接着層
Claims (18)
- 裏張り層、接着剤−薬物層、任意の乱用抑止層、及び剥離ライナーを含み、前記接着剤−薬物層は、10−25重量%のケタミン、結晶化防止剤、皮膚浸透促進剤及び感圧接着剤を含む、経皮送達デバイスであって、前記経皮送達デバイスが、約8時間から約168時間の間、0.1−5mg/日/cm2のケタミン浸透速度を提供し、前記結晶化防止剤が、ポリビニルピロリドンコビニルアセテートまたはポリメタクリレートを含み、前記皮膚浸透促進剤が、オレイルオレアート、オレイルアルコール、レブリン酸、及び/又はジエチレングリコールモノエチルエーテルを含み、前記感圧接着剤が、アクリル系感圧接着剤を含む、経皮送達デバイス。
- 約40−60重量パーセントの感圧接着剤、約1−10重量パーセントの皮膚浸透促進剤、及び約5−40重量パーセントの結晶化防止剤を含む、請求項1に記載の経皮送達デバイス。
- 約0.01−10重量パーセントの乱用抑止剤をさらに含む、請求項1に記載の経皮送達デバイス。
- 前記乱用抑止剤が、カプサイシン、アポモルヒネ、デナトニウム、ラウリル硫酸ナトリウム、ゲル形成剤、及びこれらの組み合わせから選択される、請求項3に記載の経皮送達デバイス。
- 前記経皮送達デバイスが、大うつ病性障害を治療するために、1日1回、1週間に2回、又は1週間に1回投与される、請求項1に記載の経皮送達デバイス。
- 前記経皮送達デバイスの投与は、大うつ病性障害を治療するために、約8−168時間にわたって、約10−200ng/mlのケタミン血漿中濃度を提供する、請求項1に記載の経皮送達デバイス。
- 前記経皮送達デバイスの投与は、痛みを治療するために、約8−168時間にわたって、約50−1000ng/mlのケタミン血漿中濃度を提供する、請求項1に記載の経皮送達デバイス。
- 約1日間、約3.5日間、又は約7日間、約0.1−5mg/日/cm2のケタミンを提供する、請求項1に記載の経皮送達デバイス。
- 前記デバイスは約10−300cm2、約100−300cm2、又は約10−100cm2である、請求項1に記載の経皮送達デバイス。
- 前記経皮送達デバイスが、ケタミンの即時放出投与と比較して低減されたCmaxを提供する、請求項1に記載の経皮送達デバイス。
- 約0.4−4000ng/mlのケタミン血漿中濃度を約8−168時間提供する、請求項1に記載の経皮送達デバイス。
- 100ng/ml未満のケタミン血漿中濃度を約8時間から約7日間提供し、即時放出ケタミン製剤からの血漿中濃度と比較してケタミンの有害な副作用を低減する、請求項11に記載の経皮送達デバイス。
- 即時放出ケタミン製剤からの血漿中濃度と比較して低減された経時的血漿中変動を提供する、請求項11に記載の経皮送達デバイス。
- 即時放出製剤からのケタミン血漿中濃度と比較して、
(a)低減されたCmax変動と、
(b)低減された血漿中濃度の変動と、
(c)低減された有害な副作用と、
を提供する、請求項1に記載の経皮送達デバイス。 - Cmaxが、等価投薬量の即時放出ケタミン製剤からのCmaxの約30%以下である、請求項1に記載の経皮送達デバイス。
- 前記ケタミンが、ラセミ、R−エナンチオマー又はS−異性体である、請求項1に記載の経皮送達デバイス。
- 前記皮膚浸透促進剤が、オレイルオレアート及びレブリン酸の組み合わせを含む、請求項1に記載の経皮送達デバイス。
- 前記皮膚浸透促進剤が、オレイルアルコール、レブリン酸及びジエチレングリコールモノエチルエーテルの組み合わせを含む、請求項1に記載の経皮送達デバイス。
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EP3297620A1 (en) | 2018-03-28 |
HK1248578A1 (zh) | 2018-10-19 |
AU2016288188A1 (en) | 2018-01-04 |
CN107847469A (zh) | 2018-03-27 |
US20180353437A1 (en) | 2018-12-13 |
US11191734B2 (en) | 2021-12-07 |
AU2016288188B2 (en) | 2021-08-05 |
KR102299359B1 (ko) | 2021-09-07 |
KR20180021127A (ko) | 2018-02-28 |
CA2987909A1 (en) | 2017-01-05 |
JP2018518498A (ja) | 2018-07-12 |
US20220193000A1 (en) | 2022-06-23 |
EP3297620A4 (en) | 2019-01-09 |
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