JP2007505830A5 - - Google Patents

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JP2007505830A5
JP2007505830A5 JP2006525902A JP2006525902A JP2007505830A5 JP 2007505830 A5 JP2007505830 A5 JP 2007505830A5 JP 2006525902 A JP2006525902 A JP 2006525902A JP 2006525902 A JP2006525902 A JP 2006525902A JP 2007505830 A5 JP2007505830 A5 JP 2007505830A5
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composition according
particles
composition
hydrophobic amino
mucus
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JP4913595B2 (ja
JP2007505830A (ja
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Priority claimed from GBGB0321611.6A external-priority patent/GB0321611D0/en
Priority claimed from GBGB0327723.3A external-priority patent/GB0327723D0/en
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Description

投与効率は乾燥粉末配合物の微粒子の割合(FPF)に非常に依存し、さまざまな賦形剤を加えて、非常に充分なFPFが得られることを確実にする必要がある。
子の割合(FPF)はEDで割ったFPDとして通常定義し、パーセンテージとして表す。本明細書では、EDのFPFはFPF(ED)と呼び、FPF(ED)=(FPD/ED)×100%として計算する。
子の割合(FPF)はMDで割ったFPDとして定義し、パーセンテージとして表すこともできる。本明細書では、MDのFPFはFPF(MD)と呼び、FPF(MD)=(FPD/MD)×100%として計算する。
好ましくは、添加剤物質は抗接着性物質であり、それは粒子間の凝集性を低下させる傾向があり、微粒子が吸入デバイスの内側表面に付着した状態になるのも妨げる。添加剤物質は減摩剤または流動促進剤であり、吸入器中での医薬組成物のより良い流れを与えることが有利である。このように使用される添加剤物質は、通常は必ずしも抗接着剤または減摩剤と呼ぶことはできないが、それらは粒子間の凝集性を低下させる効果、または粉末の流れを改善する効果を有する。添加剤物質は力制御物質(FCA)と呼ばれることが多く、これらは通常はより良い用量再現性および充分な細粒の割合をもたらす。
一般に、乾燥粉末配合物に含まれる添加剤物質の最適量は、添加剤物質および活性剤の化学組成および他の性質、ならびに存在する場合は担体粒子などの他の粒子の性質に依存するであろう。一般に、添加剤物質の有効性は、組成物の細粒の割合に関して測定する。
粉末の処理を試験するために、Monohalerおよび20mgの粉末を充填したカプセルを使用して作業を行い、前に説明した方法で迅速なTSIに移した。この試験は60lpmのTSI流速、および約5μmのカットオフを使用した。
さらに、5μm未満の大きさを有する粒子の質量の割合粒径データから得て、FPFとして表す。

Claims (30)

1つまたは複数のグリコサミノグリカンおよび疎水性アミノ酸を含む、粘液の浄化を促進するための組成物であって、肺吸入用の乾燥粉末であり、2% w/w以上の疎水性アミノ酸を含む、組成物
症を低下させることができる、請求項1に記載の組成物。
1つまたは複数の更なる粘液活性剤を含む、請求項1または2に記載の組成物。
1つまたは複数の粘液活性剤が粘液内の架橋を減少させ、粘液を希釈する、請求項1から3のいずれか一項に記載の組成物。
グリコサミノグリカンがヘパリンおよび/またはヘパリノイドである、請求項1に記載の組成物。
ヘパリノイドがダナパロイドナトリウム、またはデルマタン硫酸である、請求項5に記載の組成物。
ヘパリノイドがヘパリン、デルマタン硫酸およびコンドロイチン硫酸を含む、請求項5に記載の組成物。
硫酸化グリコサミノグリカン、ポリ硫酸グリコサミノグリカン化合物、または硫酸化ムコ多糖を含む、請求項1から7のいずれか一項に記載の組成物。
50%と99%の間の微粒子の割合を前記微粒子の割合が、5μm未満の空気力学的粒径を有する粒子の質量割合である、請求項1に記載の組成物。
疎水性アミノ酸が50%w/wまでの量で含まれる、請求項1に記載の組成物。
疎水性アミノ酸がロイシンである、請求項1から10のいずれかに記載の組成物。
10μm未満の空気力学的質量中央径を有するグリコサミノグリカンの粒子を含む、請求項1から11のいずれかに記載の組成物。
子が2〜5μmの空気力学的質量中央径を有する、請求項12に記載の組成物。
20μm以上の粒径を有する担体粒子をさらに含、請求項1から13のいずれか一項に記載の組成物。
治療において使用するための、請求項1から14のいずれか一項に記載の医薬組成物。
肺疾患を治療するための、請求項15に記載の医薬組成物。
肺疾患が粘液の分泌過多または粘液の異常な粘弾性を伴う、請求項16に記載の医薬組成物。
肺疾患が慢性気管支炎、急性喘息、のう胞性線維症(CF)、慢性閉塞性肺疾患(COPD)または気管支拡張である、請求項16または17に記載の医薬組成物。
請求項1から14のいずれか一項に記載の組成物を治療有効量含む、肺疾患を治療するための医薬
1つまたは複数のグリコサミノグリカンを噴霧乾燥することを含む、請求項1から14のいずれか一項に記載の組成物中で使用するための粒子を生成する方法。
噴霧乾燥が、制御された速度で動く小滴を生成するための手段を含む噴霧乾燥機の使用を含む、請求項20に記載の方法。
小滴の生成地点から5mmにおける小滴の速度が20m/s未満である、請求項21に記載の方法。
噴霧乾燥機が超音波ネブライザーを含む、請求項21または22に記載の方法。
1つまたは複数のグリコサミノグリカン疎水性アミノ酸と同時に噴霧乾燥する、請求項20から23のいずれか一項に記載の方法。
請求項1から14のいずれか一項に記載の組成物中で使用するための粒子を生成する方法であって、空気または圧縮ガスまたは流体の存在下で1つまたは複数のグリコサミノグリカンの粒子をジェットミリングすることを含む方法。
疎水性アミノ酸の存在下で粒子をジェットミリングする、請求項25に記載の方法。
0.1バールと3バールの間の入口圧力でジェットミリングを行う、請求項25または26に記載の方法。
3バールと12バールの間の入口圧力でジェットミリングを行う、請求項25から27のいずれか一項に記載の方法。
少なくとも90体積%の活性粒子がジェットミリングの前に直径20μm未満である、請求項25から28のいずれか一項に記載の方法。
生成する乾燥粒子の90%がレーザー回折によって測定して10μm未満の大きさを有する、請求項20から29のいずれか一項に記載の方法。
JP2006525902A 2003-09-15 2004-09-15 肺疾患を治療するための粘液活性剤 Expired - Fee Related JP4913595B2 (ja)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
GB0321611.6 2003-09-15
GBGB0321611.6A GB0321611D0 (en) 2003-09-15 2003-09-15 Pharmaceutical compositions
GBGB0327723.3A GB0327723D0 (en) 2003-09-15 2003-11-28 Pharmaceutical compositions
GB0327723.3 2003-11-28
PCT/GB2004/003932 WO2005025540A2 (en) 2003-09-15 2004-09-15 Mucoactive agents for treating a pulmonary disease

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JP2011243533A Division JP2012031204A (ja) 2003-09-15 2011-11-07 肺疾患を治療するための粘液活性剤

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JP2007505830A JP2007505830A (ja) 2007-03-15
JP2007505830A5 true JP2007505830A5 (ja) 2011-08-04
JP4913595B2 JP4913595B2 (ja) 2012-04-11

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JP2011243533A Pending JP2012031204A (ja) 2003-09-15 2011-11-07 肺疾患を治療するための粘液活性剤

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US (2) US7928089B2 (ja)
EP (2) EP1663151A2 (ja)
JP (2) JP4913595B2 (ja)
KR (1) KR20060082865A (ja)
CN (1) CN1874757B (ja)
AU (1) AU2004271778B2 (ja)
BR (1) BRPI0414425A (ja)
CA (1) CA2538399A1 (ja)
GB (1) GB0327723D0 (ja)
IL (1) IL173987A0 (ja)
NO (1) NO20061254L (ja)
NZ (1) NZ545550A (ja)
RU (1) RU2363448C2 (ja)
SG (1) SG146649A1 (ja)
WO (1) WO2005025540A2 (ja)

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