JP2013502446A - 1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジンの新規組成物 - Google Patents
1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジンの新規組成物 Download PDFInfo
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- JP2013502446A JP2013502446A JP2012525884A JP2012525884A JP2013502446A JP 2013502446 A JP2013502446 A JP 2013502446A JP 2012525884 A JP2012525884 A JP 2012525884A JP 2012525884 A JP2012525884 A JP 2012525884A JP 2013502446 A JP2013502446 A JP 2013502446A
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Abstract
Description
1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジン臭化水素酸塩(化合物I HBr)を、吸収プロファイル、並びに有害事象の種類及び重症度を調査する5元クロスオーバー研究において健康な志願者に投与した。23人の対象(男性12人及び女性11人)が試験に参加したが、脱落のため、23人の対象全てが5つの処置の全てを受けたわけではない(詳細については下記を参照すること)。
実施例2の錠剤を以下の組成のフィルム被覆配合物で腸溶性被覆する。
化合物Iを薬剤懸濁液としてプラセボペレット(MCC球体−Celphere CP−203)に積層する。薬剤積層ペレットの組成は以下のとおりである。
顆粒は、最初に流動床Aeromatic MP−1によりブレンドし、顆粒化し、乾燥することによって作製した。6w/w%のKlucel EXFの水性懸濁液を、26500gのブレンド(化合物I HBr、マンニトール50c、Avicel PH 101及びデンプングリコール酸ナトリウム(A型))上に噴霧した。
Claims (19)
- 化合物1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジン及びその薬学的に許容される酸付加塩を含み、前記化合物が胃において放出されないように適合されている、経口投与用医薬組成物。
- 持続放出組成物である、請求項1に記載の組成物。
- 遅延放出組成物である、請求項1に記載の組成物。
- pH感受性被覆を含む、請求項3に記載の組成物。
- 腸溶性被覆錠剤である、請求項4に記載の組成物。
- 実質的に各粒子が腸溶性被覆されている多粒子状組成物である、請求項4に記載の組成物。
- 化合物I、マンニトール、微結晶セルロース、デンプングリコール酸ナトリウム、ヒドロキシプロピルセルロース及びステアリン酸マグネシウムを含む錠剤であり、錠剤がメタクリル酸エチルアクリレート(1:1)コポリマーで被覆されている、請求項1に記載の組成物。
- 化合物Iが、1〜50mgの量の1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジンHBrである、請求項1から7のいずれかに記載の組成物。
- 気分障害;大うつ病性障害;全般性不安障害;パニック障害;外傷後ストレス障害:認知機能障害、アルツハイマー病又は不安を伴ううつ病;残存症状を有するうつ病;慢性疼痛;摂食障害又は乱用から選択される疾患を治療する方法であって、請求項1から8のいずれかに記載の医薬組成物の治療有効量を、それを必要とする患者に投与することを含む方法。
- 気分障害;大うつ病性障害;全般性不安障害;パニック障害;外傷後ストレス障害:認知機能障害、アルツハイマー病又は不安を伴ううつ病;残存症状を有するうつ病;慢性疼痛;摂食障害又は乱用から選択される疾患を治療するための経口投与用医薬組成物の製造における1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジン及びその薬学的に許容される酸付加塩の使用であって、前記医薬が、1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジン及びその薬学的に許容される酸付加塩が胃において放出されないように適合されている、使用。
- 前記組成物が、pH感受性被覆で被覆されている錠剤又は多粒子状組成物である、請求項13に記載の使用。
- 前記pH感受性被覆が腸溶性被覆である、請求項14に記載の使用。
- 前記組成物が、化合物Iの放出が小腸において生じるように適合されている、請求項13に記載の使用。
- 前記組成物が、1〜50mgの量の1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジンHBr Iを含む、請求項13から16のいずれかに記載の使用。
- 気分障害;大うつ病性障害;全般性不安障害;パニック障害;外傷後ストレス障害:認知障害、アルツハイマー病又は不安を伴ううつ病;残存症状を有するうつ病;慢性疼痛;摂食障害又は乱用から選択される疾患の治療に使用される化合物1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジン及びその薬学的に許容される酸付加塩であって、前記化合物が胃において放出されないように適合されている経口投与用医薬組成物中にある、化合物1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジン及びその薬学的に許容される酸付加塩。
- 前記組成物が、pH感受性被覆で被覆されている錠剤又は多粒子状組成物である、請求項18に記載の化合物。
- 前記pH感受性被覆が腸溶性被覆である、請求項19に記載の使用。
- 前記組成物が、化合物Iの放出が小腸において生じるように適合されている、請求項18に記載の使用。
- 1〜50mgの量の1−[2−(2,4−ジメチル−フェニルスルファニル)−フェニル]ピペラジンHBr Iである、請求項18から21のいずれかに記載の化合物。
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PCT/DK2010/050216 WO2011023194A2 (en) | 2009-08-24 | 2010-08-23 | New compositions of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine |
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- 2010-08-23 WO PCT/DK2010/050216 patent/WO2011023194A2/en active Application Filing
- 2010-08-23 AU AU2010289022A patent/AU2010289022B2/en not_active Ceased
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2012
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- 2012-02-17 CO CO12028578A patent/CO6612204A2/es not_active Application Discontinuation
- 2012-02-22 CL CL2012000457A patent/CL2012000457A1/es unknown
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2013
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2015
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Patent Citations (4)
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JPH11509539A (ja) * | 1995-07-20 | 1999-08-24 | スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー | パロキセチン制御放出組成物 |
JP2005505585A (ja) * | 2001-10-04 | 2005-02-24 | ハー・ルンドベック・アクチエゼルスカベット | セロトニン再取り込み阻害剤としてのフェニル−ピペラジン誘導体 |
JP2009503057A (ja) * | 2005-08-02 | 2009-01-29 | ルピン・リミテッド | 選択的セロトニン再取り込み阻害剤の新規の制御放出組成物 |
JP2011503125A (ja) * | 2007-11-13 | 2011-01-27 | ハー・ルンドベック・アクチエゼルスカベット | Sert、5−ht3および5−ht1aの組み合わせた活性を有する化合物の治療的使用 |
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