JP6669808B2 - 超低密度肺粉剤 - Google Patents
超低密度肺粉剤 Download PDFInfo
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- JP6669808B2 JP6669808B2 JP2018104193A JP2018104193A JP6669808B2 JP 6669808 B2 JP6669808 B2 JP 6669808B2 JP 2018104193 A JP2018104193 A JP 2018104193A JP 2018104193 A JP2018104193 A JP 2018104193A JP 6669808 B2 JP6669808 B2 JP 6669808B2
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- pharmaceutical composition
- levodopa
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Classifications
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- B65B1/00—Packaging fluent solid material, e.g. powders, granular or loose fibrous material, loose masses of small articles, in individual containers or receptacles, e.g. bags, sacks, boxes, cartons, cans, or jars
- B65B1/20—Reducing volume of filled material
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Description
本出願は、米国特許仮出願第61/724,781号(2012年11月9日出願);米国特許仮出願第61/884,319号;米国特許仮出願第61/884,315号;米国特許仮出願第61/884,436号(すべて、2013年9月30日出願)の利益を主張する。本出願は、米国特許出願第13/679,245号(2012年11月16日出願。現在、米国特許第8,545,878号)の一部継続、および米国特許出願第13/945,160号(2013年7月18日出願)の一部継続である。上記出願の全教示は、参照により本明細書中で援用される。
一実施形態において、本発明は、医薬剤を含有し、約5ミクロン(μm)より大きい中央値幾何学的サイズおよび約0.075g/cm3未満のタップ密度を有する粒子を含む肺送達のための薬学的組成物である。本発明の一態様において、タップ密度は約0.02〜0.075g/cm3である。本発明の別の態様では、タップ密度は約0.02〜0.05g/cm3である。本発明のさらなる態様では、タップ密度は約0.03〜0.06g/cm3である。本発明の一態様では、タップ密度は約0.03〜0.04g/cm3である。本発明の別の態様では、中央値幾何学的サイズは、約5μm〜30μm、5μm〜10μm、7μm〜15μmまたは7μm〜12μmである。
患者にコンパートメントおよび吸入器中で粉剤を提供するステップ(ここで、前記粉剤は医薬剤の粒子を含む);
患者の呼吸作動により粉剤を分散するステップ;
患者の呼吸器系に前記粒子を送達するステップ
を包含する患者の肺系への医薬剤の送達方法であって、粉剤の分散時に、患者の呼吸器系に送達される粒子が、前記コンパートメント中に含有される粒子より小さい中央値幾何学的直径を有する方法である。
レボドパおよびDPPCを室温で30分間、その後、必要量の水およびエタノールを計量し、被覆水性および非被覆有機相供給容器にそれぞれ移す。水性相容器上の被覆物を55℃に設定し、計量水を加熱して52.5℃にして、その後、必要量の塩化ナトリウムおよびL−ドパを水性相容器に付加し、必要量のDPPCを有機相容器に付加して、それらの全てを撹拌により溶解させる。水性供給容器頭隙を、70scfhに保持した窒素でパージする。
レボドパおよびDPPCを室温で30分間、その後、必要量の水およびエタノールを計量し、被覆水性および非被覆有機相供給容器にそれぞれ移す。水性相容器上の被覆物を55℃に設定し、計量水を加熱して52.5℃にして、その後、必要量の塩化ナトリウムおよびL−ドパを水性相容器に付加し、必要量のDPPCを有機相容器に付加して、それらの全てを撹拌により溶解させる。水性供給容器頭隙を、70scfhに保持した窒素でパージする。
VMGD=10.2μm;および
タップ密度=0.033g/cm3。
試料2:同一であるが、しかし充填ロット(60031)で測定したVMGD:
VMGD=8.6μm;および
タップ=0.033g/cm3。
試料1. 0.2の抵抗を有する乾燥粉剤吸入器からの放出粉剤(28.3LPM):
VMGD=9.4μm;および
タップ密度=0.048g/cm3。
試料2. 0.2の抵抗を有する乾燥粉剤吸入器からの放出粉剤(60LPM):
VMGD=8.8μm;および
タップ密度=0.042g/cm3。
Claims (13)
- レボドパの粒子を含む肺送達のための薬学的組成物であって、
前記レボドパの粒子が、
約5μmより大きい幾何学的サイズと、
約0.025g/cm 3 〜約0.050g/cm 3 のタップ密度と、
1.90〜2.90重量%の含水量と
を有する薬学的組成物。 - 前記粒子がリン脂質を含む、請求項1に記載の薬学的組成物。
- 前記粒子が塩を含む、請求項1に記載の薬学的組成物。
- 前記粒子が界面活性剤を含む、請求項1に記載の薬学的組成物。
- 前記粒子が重合体を含む、請求項1に記載の薬学的組成物。
- 前記粒子が糖を含む、請求項1に記載の薬学的組成物。
- 前記粒子が約10m2/gより大きい外表面積を有する、請求項1に記載の薬学的組成物。
- 前記粒子が約15m2/gより大きい外表面積を有する、請求項1に記載の薬学的組成物。
- 前記粒子が約20m2/gより大きい外表面積を有する、請求項1に記載の薬学的組成物。
- 前記粒子が約10m2/g〜約50m2/gの外表面積を有する、請求項1に記載の薬学的組成物。
- 前記粒子が約2.5μm〜5μmの空気動力学径を有する、請求項1に記載の薬学的組成物。
- 請求項1〜11のいずれか一項に記載の薬学組成物を含む、コンパートメント。
- 請求項12のコンパートメントを備える、吸入器。
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Application Number | Priority Date | Filing Date | Title |
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US201261724781P | 2012-11-09 | 2012-11-09 | |
US61/724,781 | 2012-11-09 | ||
US13/679,245 | 2012-11-16 | ||
US13/679,245 US8545878B1 (en) | 2012-11-09 | 2012-11-16 | Capsules containing high doses of levodopa for pulmonary use |
US13/945,160 | 2013-07-18 | ||
US13/945,160 US8685442B1 (en) | 2012-11-09 | 2013-07-18 | Capsules containing high doses of levodopa for pulmonary use |
US201361884436P | 2013-09-30 | 2013-09-30 | |
US201361884315P | 2013-09-30 | 2013-09-30 | |
US201361884319P | 2013-09-30 | 2013-09-30 | |
US61/884,315 | 2013-09-30 | ||
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US61/884,319 | 2013-09-30 |
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