JP2021154135A - てんかんを処置する方法 - Google Patents
てんかんを処置する方法 Download PDFInfo
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- JP2021154135A JP2021154135A JP2021093227A JP2021093227A JP2021154135A JP 2021154135 A JP2021154135 A JP 2021154135A JP 2021093227 A JP2021093227 A JP 2021093227A JP 2021093227 A JP2021093227 A JP 2021093227A JP 2021154135 A JP2021154135 A JP 2021154135A
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- A61K9/00—Medicinal preparations characterised by special physical form
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- A61K31/33—Heterocyclic compounds
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- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
- A61K31/5513—1,4-Benzodiazepines, e.g. diazepam or clozapine
- A61K31/5517—1,4-Benzodiazepines, e.g. diazepam or clozapine condensed with five-membered rings having nitrogen as a ring hetero atom, e.g. imidazobenzodiazepines, triazolam
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Abstract
Description
この特許文書の開示の一部は、特許権保護の対象である材料を含む。著作権者は、いずれかによる、特許商標庁への特許出願又は記録であると認められる特許文書又は特許開示の複写に対しては異議を唱えないが、それ以外のあらゆる全ての著作権の権利を保有する。
Claims (69)
- 凝縮エアロゾルの形態で投与されるアルプラゾラムの経口投与、
を含む、必要とする対象におけるてんかんを処置するための方法。 - 前記アルプラゾラムが、投与後に15分未満のアルプラゾラム血漿Tmaxを示す、請求項1に記載の方法。
- 前記アルプラゾラムが、投与後に5分未満のアルプラゾラム血漿Tmaxを示す、請求項1に記載の方法。
- 前記アルプラゾラムが、投与後に2分未満のアルプラゾラム血漿Tmaxを示す、請求項1に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも5ng/mLの血漿Cmaxを示す、請求項1に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも12ng/mLの血漿Cmaxを示す、請求項1に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも30ng/mLの血漿Cmaxを示す、請求項1に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも12ng/mLの血漿Cmax及び15分未満のTmaxを示す、請求項1に記載の方法。
- 前記処置が、静脈内投与されたアルプラゾラムで実現される生物学的利用能の約80〜125%である生物学的利用能を実現する、請求項1に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも80重量%が、5ミクロン未満のサイズを有する、請求項1に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも90重量%が、5ミクロン未満のサイズを有する、請求項1に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも50重量%が、2ミクロン未満のサイズを有する、請求項1に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも50重量%が、1ミクロン未満のサイズを有する、請求項1に記載の方法。
- 前記アルプラゾラム凝縮エアロゾルが、実質的に賦形剤不含である、請求項1に記載の方法。
- 前記アルプラゾラム凝縮エアロゾルが、賦形剤不含である、請求項14に記載の方法。
- 前記アルプラゾラムが、てんかん発作の1つ又は複数の症状の開始時に自己投与される、請求項1に記載の方法。
- 前記アルプラゾラムが、てんかん発作の1つ又は複数の症状の開始前に自己投与される、請求項1に記載の方法。
- 前記アルプラゾラムが、てんかん発作の1つ又は複数の症状の開始後に自己投与される、請求項1に記載の方法。
- 前記1つ又は複数の症状が、発作を含む、請求項15〜17に記載の方法。
- 前記処置が、発作を防御し、発作の強度を低下若しくは改善させ、発作の頻度を減少若しくは改善させ、発作の周期を中断させ、そして/又は発作の発生若しくは再発を予防する、請求項1に記載の方法。
- 前記発作が、てんかん発作、ブレークスルー発作、又は他の発作を含む、請求項19に記載の方法。
- 前記発作が、部分(焦点)又は全般発作を含む、請求項20に記載の方法。
- 前記部分発作が、複雑部分発作、単純部分発作、又は1つの脳半球に限定される神経ネットワーク内に起始する発作を含む、請求項21に記載の方法。
- 前記全般発作が、両側性に分布された神経ネットワーク内の幾つかのポイントに起始する、又は部分発作から進展する、請求項21に記載の方法。
- 前記対象が、発作の前駆症状又は前兆期にある患者である場合の、前記アルプラゾラム凝縮エアロゾルの投与を含む、請求項1に記載の方法。
- 患者が、感覚的前兆又は体験的前兆を主観的に経験している場合の投与を含む、請求項24に記載の方法。
- 前記感覚的前兆が、体性感覚的、視覚的、聴覚的、臭覚的、味覚的、胃部又は頭部前兆を含む、請求項25に記載の方法。
- 前記体験的前兆が、感情的、記憶的、幻覚的、又は錯覚的前兆を含む、請求項25に記載の方法。
- 前記対象が、群発性若しくは急性反復性発作、長期の焦点部分発作、又は若年ミオクロニーてんかんの患者である、請求項1に記載の方法。
- 前記処置が、静脈内投与されたアルプラゾラムで実現される生物学的利用能の約80〜125%である生物学的利用能を実現する、請求項1に記載の方法。
- 前記効果が、アルプラゾラムの吸入の15分以内に最大になる、請求項29に記載の方法。
- 前記効果が、アルプラゾラムの吸入の5分以内に最大になる、請求項30に記載の方法。
- 前記効果が、アルプラゾラムの吸入の2分以内に最大になる、請求項32に記載の方法。
- てんかん様活性が、アルプラゾラムの吸入の15分以内に存在しない、請求項1に記載の方法。
- てんかん様活性が、アルプラゾラムの吸入後少なくとも6時間、存在しない、請求項1に記載の方法。
- 凝縮エアロゾルの形態で投与されるアルプラゾラムの経口投与、
を含む、対象における発作を処置するための方法。 - 前記アルプラゾラムが、投与後に15分未満のアルプラゾラム血漿Tmaxを示す、請求項36に記載の方法。
- 前記アルプラゾラムが、投与後に5分未満のアルプラゾラム血漿Tmaxを示す、請求項36に記載の方法。
- 前記アルプラゾラムが、投与後に2分未満のアルプラゾラム血漿Tmaxを示す、請求項36に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも5ng/mLの血漿Cmaxを示す、請求項36に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも12ng/mLの血漿Cmaxを示す、請求項36に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも30ng/mLの血漿Cmaxを示す、請求項36に記載の方法。
- 前記アルプラゾラムが、経口投与後に少なくとも12ng/mLの血漿Cmax及び15分未満のTmaxを示す、請求項36に記載の方法。
- 前記処置が、静脈内投与されたアルプラゾラムで実現される生物学的利用能の約80〜125%である生物学的利用能を実現する、請求項35に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも80重量%が、5ミクロン未満のサイズを有する、請求項35に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも90重量%が、5ミクロン未満のサイズを有する、請求項35に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも50重量%が、2ミクロン未満のサイズを有する、請求項35に記載の方法。
- 前記アルプラゾラムエアロゾル粒子の少なくとも50重量%が、1ミクロン未満のサイズを有する、請求項35に記載の方法。
- 前記アルプラゾラム凝縮エアロゾルが、実質的に賦形剤不含である、請求項35に記載の方法。
- 前記アルプラゾラム凝縮エアロゾルが、賦形剤不含である、請求項47に記載の方法。
- 前記アルプラゾラムが、前記発作の1つ又は複数の症状の開始時に自己投与される、請求項35に記載の方法。
- 前記アルプラゾラムが、前記発作の1つ又は複数の症状の開始前に自己投与される、請求項35に記載の方法。
- 前記アルプラゾラムが、前記発作の1つ又は複数の症状の開始後に自己投与される、請求項35に記載の方法。
- 前記処置が、発作を防御し、発作の強度を低下若しくは改善させ、発作の頻度を減少若しくは改善させ、発作の周期を中断させ、そして/又は発作の発生若しくは再発を予防する、請求項35に記載の方法。
- 前記発作が、てんかん発作、ブレークスルー発作、又は他の発作を含む、請求項35に記載の方法。
- 前記発作が、部分(焦点)又は全般発作を含む、請求項35に記載の方法。
- 前記部分発作が、複雑部分発作、単純部分発作、又は1つの脳半球に限定される神経ネットワーク内に起始する発作を含む、請求項54に記載の方法。
- 前記全般発作が、両側性に分布された神経ネットワーク内の幾つかのポイントに起始する、又は部分発作から進展する、請求項54に記載の方法。
- 前記対象が、発作の前駆症状又は前兆期にある対象である場合の、前記アルプラゾラム凝縮エアロゾルの投与を含む、請求項35に記載の方法。
- 対象が、感覚的前兆又は体験的前兆を主観的に経験している場合の投与を含む、請求項57に記載の方法。
- 前記感覚的前兆が、体性感覚的、視覚的、聴覚的、臭覚的、味覚的、胃部又は頭部前兆を含む、請求項58に記載の方法。
- 前記体験的前兆が、感情的、記憶的、幻覚的、又は錯覚的前兆を含む、請求項58に記載の方法。
- 前記対象が、群発性若しくは急性反復性発作、長期の焦点部分発作、又は若年ミオクロニーてんかんの患者である、請求項35に記載の方法。
- 前記処置が、静脈内投与されたアルプラゾラムで実現される生物学的利用能の約80〜125%である生物学的利用能を実現する、請求項35に記載の方法。
- 前記効果が、アルプラゾラムの吸入の15分以内に最大になる、請求項62に記載の方法。
- 前記効果が、アルプラゾラムの吸入の5分以内に最大になる、請求項63に記載の方法。
- 前記効果が、アルプラゾラムの吸入の2分以内に最大になる、請求項64に記載の方法。
- 発作活性が、アルプラゾラムの吸入の15分以内に存在しない、請求項1に記載の方法。
- 発作活性が、アルプラゾラムの吸入後少なくとも6時間、存在しない、請求項1に記載の方法。
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