JP7365426B2 - 精神障害、行動障害、認知障害を処置するための医薬組成物及び方法 - Google Patents
精神障害、行動障害、認知障害を処置するための医薬組成物及び方法 Download PDFInfo
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Description
[001] 本発明は、実用医学の分野、すなわち、中枢神経系への様々な起源の器質的損傷の場合の精神的、行動的、認知的な障害の症状を軽減する向神経性作用を示す医薬組成物の併用に関する。
[002] アルツハイマー病(AD)は進行性の慢性神経変性疾患であり、通常はゆっくりと始まり、時間の経過とともに徐々に悪化する。アルツハイマー病は、高齢者の認知症の最も一般的な原因である。認知症とは、人の日常生活及び活動に支障をきたす程度の、認知機能(思考、記憶、及び推論)及び行動能力の喪失である。初期の段階では記憶喪失は軽度であるが、後期のADでは、個人は会話を継続し、その環境に反応する能力を失う。未処置の場合、ADは最終的に死に至る。進行の速度は様々であるが、診断後の典型的な平均余命は3~9年である。
[0011] 本発明は、2つの有効成分1つ以上の薬学的に許容される賦形剤を含む、医薬組成物を含む。この医薬組成物は、アゼラスチン又はアゼラスチンの薬学的に許容される塩である第1の有効成分と、メマンチン又はメマンチンの薬学的に許容される塩である第2の有効成分とを含む。
[0017] 本発明の発明者らは、驚くべきことに、活性剤、塩形態のアゼラスチン及び塩形態のメマンチンを含む経口剤形を有する医薬組成物が、精神障害、行動障害、認知障害に罹患している患者を処置するのに適していることを見出した。
[0020] 本明細書で使用される場合、以下の語及び句は、それらが使用される文脈が別の意味を示す場合を除いて、一般に、以下に記載される意味を有することを意図している。
[0039] 79歳、体重51キログラムの女性が後期アルツハイマー病と診断され、メマンチン(10mg)で5年間処置された。しかし、女性の記憶力及び認知能力は悪化し続けた。女性はほとんど何も覚えることができず、数語しか話せなかった。女性は最終的に日常活動及びパーソナルケアで24時間の補助を受けていた。女性は補助を伴っても10歩を超えて歩行することができなかった。この段階で、女性は、12mgのアゼラスチンHCl及び5mgのメマンチンHClを含有する特許請求された医薬組成物の液体経口形態での1日1回の処置を開始した。わずか1ヶ月半後、女性は補助を伴って歩行できた。3ヶ月後、女性は顔及び目の表情があり、数分間話すことができ、軽度の補助のみで歩行できた。処置の6ヶ月後、女性は自由に話し、歌を歌い、独立して歩行することができた。6ヶ月の処置中に、女性の体重は5キログラム増加した。
[0041] 81歳、体重55キログラムの女性が後期アルツハイマー病と診断された。女性は、パーソナルケア、食事、ウォーキングなどの日常活動で24時間体制の補助があった。女性は5語未満しか話すことができず、不規則な睡眠パターンを有していた。女性は、12mgのアゼラスチンHCl及び5mgのメマンチンHClを含有する特許請求された医薬組成物の液体経口形態で処置された。わずか1ヶ月半後、女性の24時間体制の補助は約50%削減された。3ヶ月後、女性は自分で基本的なパーソナルケア活動を行うことができ、10語を超えて話すことができた。
[0043] 77歳、体重66キログラムの男性が後期アルツハイマー病と診断された。男性は数語しか話せなかった。男性は睡眠に困難があった。男性の性格は、非論理的又は非合理的、不安又は過敏、及び攻撃的又は敵対的であると説明された。男性はほとんどの時間非協力的であった。男性は歩行に軽度の補助が必要であった。男性は24時間補助者によって監視されていた。男性は、14mgのアゼラスチンHCl及び5mgのメマンチンHClを含有する医薬組成物の錠剤で処置された。1ヶ月半後、男性の性格は、より理性的であり、敵意なく攻撃性がはるかに少ないと説明された。3ヶ月後、男性は定期的に眠ることができ、24時間体制の補助は必要でなくなった。男性は1分以上話すことができた。
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Claims (13)
- アゼラスチン又はアゼラスチンの薬学的に許容される塩;
メマンチン又はメマンチンの薬学的に許容される塩;及び
1つ以上の薬学的に許容される賦形剤
を含む、アルツハイマー病を処置するための医薬組成物。 - 前記アゼラスチン又は前記アゼラスチンの薬学的に許容される塩が、約1mg~約50mgの範囲の量で前記医薬組成物中に存在する、請求項1に記載の医薬組成物。
- 前記メマンチン又は前記メマンチンの薬学的に許容される塩が、約1mg~約70mgの範囲の量で前記医薬組成物中に存在する、請求項1に記載の医薬組成物。
- 前記アゼラスチン又は前記アゼラスチンの薬学的に許容される塩が、約1mg~約50mgの範囲の量で前記医薬組成物中に存在し;且つ
前記メマンチン又は前記メマンチンの薬学的に許容される塩が、約1mg~約70mgの範囲の量で前記医薬組成物中に存在する、
請求項1に記載の医薬組成物。 - 前記アゼラスチンの薬学的に許容される塩が、アゼラスチン塩酸塩である、請求項2に記載の医薬組成物。
- 前記メマンチンの薬学的に許容される塩が、メマンチン塩酸塩である、請求項3に記載の医薬組成物。
- 前記アゼラスチン塩酸塩が、約2mg~約20mgの範囲の量で存在する、請求項5に記載の医薬組成物。
- 前記アゼラスチン塩酸塩が、約8mg~約16mgの範囲の量で存在する、請求項5に記載の医薬組成物。
- 前記メマンチン塩酸塩が、約2mg~約20mgの範囲の量で存在する、請求項6に記載の医薬組成物。
- 前記医薬組成物が、経口医薬剤形として製剤化される、請求項1に記載の医薬組成物。
- 前記経口医薬剤形が、固体又は液体の形態である、請求項10に記載の医薬組成物。
- 前記アゼラスチン又は前記アゼラスチンの薬学的に許容される塩が、約10mg~約50mgの範囲の量で存在する、請求項1に記載の医薬組成物。
- 前記アゼラスチン又は前記アゼラスチンの薬学的に許容される塩が、前記メマンチン又は前記メマンチンの薬学的に許容される塩の2、3、4、5、6、7、8、9または10倍の量で前記医薬組成物中に存在する;または
前記メマンチン又は前記メマンチンの薬学的に許容される塩が、前記アゼラスチン又は前記アゼラスチンの薬学的に許容される塩の2、3、4、5、6、7、8、9または10倍の量で前記医薬組成物中に存在する、
請求項1に記載の医薬組成物。
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US10966989B2 (en) | 2019-04-12 | 2021-04-06 | LA PharmaTech Inc. | Pharmaceutical compositions and methods for treating mental, behavioral, cognitive disorders |
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