JP2016523979A5 - - Google Patents
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- JP2016523979A5 JP2016523979A5 JP2016525796A JP2016525796A JP2016523979A5 JP 2016523979 A5 JP2016523979 A5 JP 2016523979A5 JP 2016525796 A JP2016525796 A JP 2016525796A JP 2016525796 A JP2016525796 A JP 2016525796A JP 2016523979 A5 JP2016523979 A5 JP 2016523979A5
- Authority
- JP
- Japan
- Prior art keywords
- nicotine
- aerosol
- salicylate
- concentrated aerosol
- meta
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- SNICXCGAKADSCV-JTQLQIEISA-N Nicotine Chemical class CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims description 37
- 229960002715 Nicotine Drugs 0.000 claims description 36
- 229930015196 nicotine Natural products 0.000 claims description 36
- 239000000203 mixture Substances 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000443 aerosol Substances 0.000 description 26
- 239000003814 drug Substances 0.000 description 9
- 229940079593 drugs Drugs 0.000 description 9
- BLUGYPPOFIHFJS-UUFHNPECSA-N (2S)-N-[(2S)-1-[[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C=1SC=CN=1)CC1=CC=CC=C1 BLUGYPPOFIHFJS-UUFHNPECSA-N 0.000 description 6
- 239000007857 degradation product Substances 0.000 description 5
- 239000012458 free base Substances 0.000 description 5
- 230000015572 biosynthetic process Effects 0.000 description 4
- 238000005755 formation reaction Methods 0.000 description 4
- 150000001875 compounds Chemical class 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 239000000758 substrate Substances 0.000 description 2
- IJFXRHURBJZNAO-UHFFFAOYSA-N 3-Hydroxybenzoic acid Chemical compound OC(=O)C1=CC=CC(O)=C1 IJFXRHURBJZNAO-UHFFFAOYSA-N 0.000 description 1
- 206010057852 Nicotine dependence Diseases 0.000 description 1
- 238000001856 aerosol method Methods 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 238000002716 delivery method Methods 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 239000000546 pharmaceutic aid Substances 0.000 description 1
- 230000000391 smoking Effects 0.000 description 1
- 230000005586 smoking cessation Effects 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
Description
本明細書の開示は以下の発明の開示を包含する:
[1]ニコチンのメタ−サリチル酸塩を含むニコチン塩。
[2]下記のものを含む薬物供給用品:
不透過性表面を有する熱伝導性基材;
その表面の少なくとも一部に、ある厚さを有する膜の形態でコートされた、メタ−サリチル酸ニコチンを含むニコチン組成物;および
コートされたニコチン組成物の全部または一部を2秒以内に気化させるのに十分な温度に達する速度で基材に熱を供給するように操作できる熱源;
その際、気化したニコチン組成物は有効量のニコチンを含む;
その際、膜は0.05〜30ミクロンの厚さを有する。
[3]ニコチン組成物がメタ−サリチル酸ニコチンから構成される、[2]に記載の薬物供給用品。
[4]ニコチン組成物が医薬的に許容できる賦形剤を含む、[2]に記載の薬物供給用品。
[5]膜厚が0.1〜30ミクロンである、[2]に記載の薬物供給用品。
[6]メタ−サリチル酸ニコチンを含む医薬組成物であって、その必要がある対象に吸入により投与される組成物。
[7]患者が濃縮エアゾールの形成および送達を作動させた際に3μm未満のMMADおよび5%未満の薬物分解生成物を有する有効量のニコチン濃縮エアゾールが患者に吸入により投与されることを含む禁煙方法。
[8]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[7]に記載の方法。
[9]患者が濃縮エアゾールの形成および送達を作動させた際に0.01〜3μmのMMADおよび5%未満の薬物分解生成物を有するニコチン濃縮エアゾールが患者に吸入により投与されることを含む、ニコチン送達方法。
[10]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[9]に記載の方法。
[11]患者が濃縮エアゾールの形成および送達を作動させた際に0.01〜3μmのMMADおよび5%未満の薬物分解生成物を有する有効量のニコチン濃縮エアゾールが患者に吸入により投与されることを含む、ニコチン渇望の処置方法。
[12]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[11]に記載の方法。
[13]患者が濃縮エアゾールの形成および送達を作動させた際に3μm未満のMMADおよび5%未満の薬物分解生成物を有する有効量のニコチン濃縮エアゾールが患者に吸入により投与されることを含む、禁煙を実施する方法。
[14]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[13]に記載の方法。
[15]固体支持体上にコートされたメタ−サリチル酸ニコチンを含む組成物を加熱して蒸気を発生させ、その蒸気を冷却して粒子を含む濃縮エアゾールを形成することにより形成され、その際、粒子が少なくとも50重量%のニコチンおよび5重量%未満の薬物分解生成物を含み、濃縮エアゾールが0.2〜5ミクロンのMMADを有する、ニコチンを送達するためのニコチン濃縮エアゾール。
[16]濃縮エアゾールが1〜3ミクロンのMMADを有する、[15]に記載の濃縮エアゾール。
[17]濃縮エアゾールが1〜10%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[18]濃縮エアゾールが10〜20%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[19]濃縮エアゾールが20〜30%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[20]濃縮エアゾールが30〜40%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[21]濃縮エアゾールが40〜50%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[0009] したがって、本開示の1観点は、メタ−サリチル酸ニコチンを教示する。本開示の1観点は、揮発性メタ−サリチル酸ニコチン化合物を含む化合物を提供し、その化合物は加熱した際に選択的に気化する。
[1]ニコチンのメタ−サリチル酸塩を含むニコチン塩。
[2]下記のものを含む薬物供給用品:
不透過性表面を有する熱伝導性基材;
その表面の少なくとも一部に、ある厚さを有する膜の形態でコートされた、メタ−サリチル酸ニコチンを含むニコチン組成物;および
コートされたニコチン組成物の全部または一部を2秒以内に気化させるのに十分な温度に達する速度で基材に熱を供給するように操作できる熱源;
その際、気化したニコチン組成物は有効量のニコチンを含む;
その際、膜は0.05〜30ミクロンの厚さを有する。
[3]ニコチン組成物がメタ−サリチル酸ニコチンから構成される、[2]に記載の薬物供給用品。
[4]ニコチン組成物が医薬的に許容できる賦形剤を含む、[2]に記載の薬物供給用品。
[5]膜厚が0.1〜30ミクロンである、[2]に記載の薬物供給用品。
[6]メタ−サリチル酸ニコチンを含む医薬組成物であって、その必要がある対象に吸入により投与される組成物。
[7]患者が濃縮エアゾールの形成および送達を作動させた際に3μm未満のMMADおよび5%未満の薬物分解生成物を有する有効量のニコチン濃縮エアゾールが患者に吸入により投与されることを含む禁煙方法。
[8]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[7]に記載の方法。
[9]患者が濃縮エアゾールの形成および送達を作動させた際に0.01〜3μmのMMADおよび5%未満の薬物分解生成物を有するニコチン濃縮エアゾールが患者に吸入により投与されることを含む、ニコチン送達方法。
[10]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[9]に記載の方法。
[11]患者が濃縮エアゾールの形成および送達を作動させた際に0.01〜3μmのMMADおよび5%未満の薬物分解生成物を有する有効量のニコチン濃縮エアゾールが患者に吸入により投与されることを含む、ニコチン渇望の処置方法。
[12]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[11]に記載の方法。
[13]患者が濃縮エアゾールの形成および送達を作動させた際に3μm未満のMMADおよび5%未満の薬物分解生成物を有する有効量のニコチン濃縮エアゾールが患者に吸入により投与されることを含む、禁煙を実施する方法。
[14]ニコチン濃縮エアゾールがメタ−サリチル酸ニコチンを含む、[13]に記載の方法。
[15]固体支持体上にコートされたメタ−サリチル酸ニコチンを含む組成物を加熱して蒸気を発生させ、その蒸気を冷却して粒子を含む濃縮エアゾールを形成することにより形成され、その際、粒子が少なくとも50重量%のニコチンおよび5重量%未満の薬物分解生成物を含み、濃縮エアゾールが0.2〜5ミクロンのMMADを有する、ニコチンを送達するためのニコチン濃縮エアゾール。
[16]濃縮エアゾールが1〜3ミクロンのMMADを有する、[15]に記載の濃縮エアゾール。
[17]濃縮エアゾールが1〜10%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[18]濃縮エアゾールが10〜20%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[19]濃縮エアゾールが20〜30%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[20]濃縮エアゾールが30〜40%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[21]濃縮エアゾールが40〜50%の遊離塩基ニコチンを含む、[15]に記載の濃縮エアゾール。
[0009] したがって、本開示の1観点は、メタ−サリチル酸ニコチンを教示する。本開示の1観点は、揮発性メタ−サリチル酸ニコチン化合物を含む化合物を提供し、その化合物は加熱した際に選択的に気化する。
Claims (2)
- ニコチンのメタ−サリチル酸塩を含むニコチン塩。
- メタ−サリチル酸ニコチンを含む医薬組成物であって、その必要がある対象に吸入により投与される組成物。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361845333P | 2013-07-11 | 2013-07-11 | |
US61/845,333 | 2013-07-11 | ||
US201462020766P | 2014-07-03 | 2014-07-03 | |
US62/020,766 | 2014-07-03 | ||
PCT/US2014/046288 WO2015006652A1 (en) | 2013-07-11 | 2014-07-11 | Nicotine salt with m eta-salicylic acid |
Related Child Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018162527A Division JP6731982B2 (ja) | 2013-07-11 | 2018-08-31 | メタ−サリチル酸とのニコチン塩 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2016523979A JP2016523979A (ja) | 2016-08-12 |
JP2016523979A5 true JP2016523979A5 (ja) | 2017-08-17 |
JP6397493B2 JP6397493B2 (ja) | 2018-09-26 |
Family
ID=52280631
Family Applications (5)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016525796A Active JP6397493B2 (ja) | 2013-07-11 | 2014-07-11 | メタ−サリチル酸とのニコチン塩 |
JP2018162527A Active JP6731982B2 (ja) | 2013-07-11 | 2018-08-31 | メタ−サリチル酸とのニコチン塩 |
JP2020116222A Active JP7288883B2 (ja) | 2013-07-11 | 2020-07-06 | メタ-サリチル酸とのニコチン塩 |
JP2022043665A Active JP7295300B2 (ja) | 2013-07-11 | 2022-03-18 | メタ-サリチル酸とのニコチン塩 |
JP2022122868A Active JP7309023B2 (ja) | 2013-07-11 | 2022-08-01 | メタ-サリチル酸とのニコチン塩 |
Family Applications After (4)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2018162527A Active JP6731982B2 (ja) | 2013-07-11 | 2018-08-31 | メタ−サリチル酸とのニコチン塩 |
JP2020116222A Active JP7288883B2 (ja) | 2013-07-11 | 2020-07-06 | メタ-サリチル酸とのニコチン塩 |
JP2022043665A Active JP7295300B2 (ja) | 2013-07-11 | 2022-03-18 | メタ-サリチル酸とのニコチン塩 |
JP2022122868A Active JP7309023B2 (ja) | 2013-07-11 | 2022-08-01 | メタ-サリチル酸とのニコチン塩 |
Country Status (8)
Country | Link |
---|---|
US (5) | US9724341B2 (ja) |
EP (2) | EP3019154B1 (ja) |
JP (5) | JP6397493B2 (ja) |
CN (3) | CN111249584B (ja) |
CA (3) | CA3061122C (ja) |
ES (1) | ES2821907T3 (ja) |
HK (1) | HK1224226A1 (ja) |
WO (1) | WO2015006652A1 (ja) |
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2014
- 2014-07-11 EP EP14822991.7A patent/EP3019154B1/en active Active
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- 2014-07-11 JP JP2016525796A patent/JP6397493B2/ja active Active
- 2014-07-11 CN CN201610817592.5A patent/CN107049996B/zh active Active
- 2014-07-11 ES ES14822991T patent/ES2821907T3/es active Active
- 2014-07-11 WO PCT/US2014/046288 patent/WO2015006652A1/en active Application Filing
- 2014-07-11 US US14/904,359 patent/US9724341B2/en active Active
- 2014-07-11 CN CN201480050267.XA patent/CN105530916B/zh active Active
- 2014-07-11 CA CA3006188A patent/CA3006188C/en active Active
- 2014-07-11 EP EP20186522.7A patent/EP3838316B1/en active Active
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2016
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- 2016-11-03 HK HK16112692.8A patent/HK1224226A1/zh unknown
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- 2022-08-22 US US17/893,147 patent/US20220401431A1/en not_active Abandoned
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