JP2017523206A - ブルトン型チロシンキナーゼ阻害剤の新規製剤 - Google Patents
ブルトン型チロシンキナーゼ阻害剤の新規製剤 Download PDFInfo
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- MSRILKIQRXUYCT-UHFFFAOYSA-M valproate semisodium Chemical compound [Na+].CCCC(C(O)=O)CCC.CCCC(C([O-])=O)CCC MSRILKIQRXUYCT-UHFFFAOYSA-M 0.000 description 1
- 229960000604 valproic acid Drugs 0.000 description 1
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- 229960000653 valrubicin Drugs 0.000 description 1
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- 229960003895 verteporfin Drugs 0.000 description 1
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- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 description 1
- AQTQHPDCURKLKT-JKDPCDLQSA-N vincristine sulfate Chemical compound OS(O)(=O)=O.C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C=O)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 AQTQHPDCURKLKT-JKDPCDLQSA-N 0.000 description 1
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- QDLHCMPXEPAAMD-UHFFFAOYSA-N wortmannin Natural products COCC1OC(=O)C2=COC(C3=O)=C2C1(C)C1=C3C2CCC(=O)C2(C)CC1OC(C)=O QDLHCMPXEPAAMD-UHFFFAOYSA-N 0.000 description 1
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Abstract
Description
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.8重量/重量%のステアリン酸マグネシウムと、を含んでおり、50%活性な噴霧乾燥イブルチニブは約50重量/重量%のポリマーマトリックス内に分散するイブルチニブを含んでおり、ポリマーマトリックスのポリマーはヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である。
a)約52〜約54重量/重量%の20%活性な噴霧乾燥イブルチニブと、
b)約13〜約15重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.4〜約0.6重量/重量%のステアリン酸マグネシウムと、を含み、
20%活性な噴霧乾燥イブルチニブは約20重量/重量%のポリマーマトリックス内に分散するイブルチニブを含んでおり、ポリマーマトリックスのポリマーはヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である。
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.8重量/重量%のステアリン酸マグネシウムと、を含んでおり、50%活性な噴霧乾燥イブルチニブは約50重量/重量%のポリマーマトリックス内に分散するイブルチニブを含む噴霧乾燥イブルチニブ組成物であり、ポリマーマトリックスのポリマーはポリビニルカプロラクタム−ポリビニルアセテート−ポリエチレングリコールのグラフトコポリマー(Soluplus(登録商標))である。
a)約30〜約50重量/重量%の固体分散医薬組成物と、
b)微結晶セルロース、コロイド状二酸化ケイ素、グリコール酸ナトリウムデンプン及びステアリルフマル酸ナトリウムを含む約20〜約25重量/重量%の賦形剤混合物と、
c)約0.2〜約0.8重量/重量%のステアリルフマル酸ナトリウムと、
d)約25〜約35重量/重量%のクロスポビドンと、を含む。
a)約45〜約48重量/重量%の33%活性な噴霧乾燥イブルチニブと、
b)微結晶セルロース、コロイド状二酸化ケイ素、グリコール酸ナトリウムデンプン及びステアリルフマル酸ナトリウムを含む約20〜約25重量/重量%の賦形剤混合物と、
c)約0.2〜約0.8重量/重量%のステアリルフマル酸ナトリウムと、
d)約25〜約35重量/重量%のクロスポビドンと、を含み、
33%活性な噴霧乾燥イブルチニブは約33重量/重量%のポリマーマトリックス内に分散するイブルチニブを含む。
a)約30〜約33重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)微結晶セルロース、コロイド状二酸化ケイ素、グリコール酸ナトリウムデンプン及びステアリルフマル酸ナトリウムを含む約20〜約25重量/重量%の、Prosolv(登録商標)EasyTabなどの賦形剤混合物と、
c)約0.2〜約0.8重量/重量%のステアリルフマル酸ナトリウムと、
d)約25〜約35重量/重量%のクロスポビドンと、を含み、
50%活性な噴霧乾燥イブルチニブは約50重量/重量%のポリマーマトリックス内に分散するイブルチニブを含む。
a)約42〜約43%の固体分散イブルチニブ組成物にないイブルチニブ、
b)約4〜約5重量/重量%の界面活性剤SLS(登録商標)と、
c)約45〜約46重量/重量%の微結晶セルロースと、
d)約6〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.4〜約0.5重量/重量%のステアリン酸マグネシウムと、を含む。
本明細書で言及する出版物及び特許出願はすべて、妥当かつ関連する範囲で参照により本明細書に組み込まれる。
他に定義しない限り、本明細書で使用するすべての技術的及び科学的用語は、特許請求されている主題の属する技術の当業者に一般に理解されているのと同じ意味を有する。前述の一般的な説明及び以下の詳細な説明は例示的かつ説明的なものに過ぎず、特許請求されている主題のいずれをも制限するものではないことが理解されるべきである。本出願では別様に特定して記述されない限り、単数の使用は複数を含む。内容が明らかに別様であるとする場合を除いて、明細書及び添付した特許請求の範囲で使用する場合、単数形の「a」、「an」及び「the」は複数の対象を含むことに注意しなければならない。本出願では別様に明記しない限り、「または」の使用は「及び/または」を意味する。更に「含む(including、およびinclude、includes及びincludedなどの他の形態)」の語の使用は限定を表すものではない。
本明細書で用いられる医薬組成物は、化合物1と、他の化学的成分である担体、安定剤、希釈剤、分散剤、懸濁化剤、増粘剤及び/または賦形剤などの混合物を指す。医薬組成物は、対象に対する化合物の投与を促進する。化合物は、単独でまたは混合物の成分として1つ以上の治療薬と組み合わせて用いることができる。
一態様で本発明は、固体分散イブルチニブを含む固体分散医薬組成物を提供する。
別の態様において、本発明は、本明細書に記載される固体分散医薬組成物及び薬学的に許容される賦形剤を含む、固体分散体製剤を提供する。
ラクトースは約5〜約20重量/重量%、約10〜約20重量/重量%または約14〜約19重量/重量%の量で存在し、
微結晶セルロースは約20〜約30重量/重量%、約23〜約28重量/重量%または約24〜約26重量/重量%の量で存在し、
クロスカルメロースナトリウムは約3〜約9重量/重量%、約4〜約8重量/重量%または約5〜約7重量/重量%の量で存在する。
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.8重量/重量%または約0.2〜約0.3重量/重量%のステアリン酸マグネシウムと、を含み、
50%活性な噴霧乾燥イブルチニブは約50重量/重量%のポリマーマトリックス内に分散するイブルチニブを含んでおり、ポリマーマトリックスのポリマーはヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である。
a)約52〜約54重量/重量%の20%活性な噴霧乾燥イブルチニブと、
b)約13〜約15重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.4〜約0.6重量/重量%のステアリン酸マグネシウムと、を含み、
20%活性な噴霧乾燥イブルチニブは約20重量/重量%のイブルチニブをポリマーマトリックス内に分散されて含んでおり、ポリマーマトリックスのポリマーはヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である。
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.8重量/重量%または約0.2〜約0.3重量/重量%のステアリン酸マグネシウムと、を含み、
50%活性な噴霧乾燥イブルチニブは約50重量/重量%のイブルチニブをポリマーマトリックス内に分散されて含む噴霧乾燥イブルチニブ組成物であり、ポリマーマトリックスのポリマーはポリビニルカプロラクタム−ポリビニルアセテート−ポリエチレングリコールのグラフトコポリマー(Soluplus(登録商標))である。
a)約42〜約43重量/重量%のイブルチニブと、
b)約4〜約5重量/重量%の界面活性剤(ラウリル硫酸ナトリウム)SLS(登録商標)と、
c)約45〜約46重量/重量%の微結晶セルロースと、
d)約6〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.4〜約0.5重量/重量%のステアリン酸マグネシウムと、を含む。
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.3重量/重量%のステアリン酸マグネシウム。
ここで50%活性な噴霧乾燥イブルチニブは約50重量/重量%のポリマーマトリックス内に分散するイブルチニブを含んでおり、ポリマーマトリックスのポリマーはヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である。
a)約52〜約54重量/重量%の20%活性な噴霧乾燥イブルチニブと、
b)約13〜約15重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.4〜約0.6重量/重量%のステアリン酸マグネシウム。
ここで20%活性な噴霧乾燥イブルチニブは約20重量/重量%のポリマーマトリックス内に分散するイブルチニブを含んでおり、ポリマーマトリックスのポリマーはヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である。
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.3重量/重量%のステアリン酸マグネシウム。
ここで50%活性な噴霧乾燥イブルチニブは50重量/重量%のポリマーマトリックス内に分散するイブルチニブを含む噴霧乾燥イブルチニブ組成物であり、ポリマーマトリックスのポリマーはポリビニルカプロラクタム−ポリビニルアセテート−ポリエチレングリコールのグラフトコポリマー(Soluplus(登録商標))である。
a)約30〜約50重量/重量%の本明細書に記載の噴霧乾燥イブルチニブ組成物と、
b)微結晶セルロース、コロイド状二酸化ケイ素、グリコール酸ナトリウムデンプン及びステアリルフマル酸ナトリウムを含む約20〜約25重量/重量%の、Prosolv(登録商標)EasyTabなどの賦形剤混合物と、
c)約0.2〜約0.8重量/重量%のステアリルフマル酸ナトリウムと、
d)約25〜約35重量/重量%のクロスポビドン。
a)約45〜約48重量/重量%の33%活性な噴霧乾燥イブルチニブと、
b)微結晶セルロース、コロイド状二酸化ケイ素、グリコール酸ナトリウムデンプン及びステアリルフマル酸ナトリウムを含む約20〜約25重量/重量%の、Prosolv(登録商標)EasyTabなどの賦形剤混合物と、
c)約0.2〜約0.8重量/重量%のステアリルフマル酸ナトリウムと、
d)約25〜約35重量/重量%のクロスポビドン。
ここで33%活性な噴霧乾燥イブルチニブは約33重量/重量%のポリマーマトリックス内に分散するイブルチニブを含む。いくつかの実施形態では、ポリマーマトリックスのポリマーはポリビニルピロリドン/ビニルアセテートのコポリマーである。いくつかの実施形態において、ポリマーマトリックスのポリマーは比2:1〜1:2、例えば1:1などのポリビニルピロリドン/ビニルアセテートのコポリマー、及びポリビニルカプロラクタム−ポリビニルアセテート−ポリエチレングリコールのグラフトコポリマーの混合物である。
a)約30〜約33重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)微結晶セルロース、コロイド状二酸化ケイ素、グリコール酸ナトリウムデンプン及びステアリルフマル酸ナトリウムを含む約20〜約25重量/重量%の、Prosolv(登録商標)EasyTabなどの賦形剤混合物と、
c)約0.2〜約0.8重量/重量%のステアリルフマル酸ナトリウムと、
d)約25〜約35重量/重量%のクロスポビドン。
ここで50%活性な噴霧乾燥イブルチニブは約50重量/重量%のポリマーマトリックス内に分散するイブルチニブを含む。いくつかの実施形態では、ポリマーマトリックスのポリマーはポリビニルピロリドン/ビニルアセテートのコポリマーである。
一態様では、化合物1を投与することによる患者の治療方法が本明細書に開示される。いくつかの実施形態では、Btkなどのチロシンキナーゼ(複数可)の活性を阻害する方法、またはBtkなどのチロシンキナーゼ(複数可)の阻害により恩恵を受けるであろう、哺乳動物の疾患、障害もしくは状態の治療方法を本明細書において開示し、それは化合物1、または薬学的に許容される塩、薬学的に活性な代謝物、薬学的に許容されるプロドラッグもしくは薬学的に許容される溶媒和物の治療に有効な量を哺乳動物に投与することを含む。
ある特定の実施形態において、血液系腫瘍を治療することを、それを必要とする個人において行う方法を本明細書にて開示しており、個人に化合物1の量を投与することを含む。
ある特定の実施形態において、濾胞性リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性濾胞性リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、CLLまたはSLLを治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性CLLまたはSLLを治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、マントル細胞リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて開示しており、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性マントル細胞リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、辺縁帯B細胞性リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて開示して、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性辺縁帯B細胞性リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示しており、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、MALTを治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性MALTを治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、節性辺縁帯B細胞リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性の節性辺縁帯B細胞リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、脾性辺縁帯B細胞リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性の脾性辺縁帯B細胞リンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、バーキットリンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性のバーキットリンパ腫を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、ワルデンシュトレームマクログロブリン血症を治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性ワルデンシュトレームマクログロブリン血症を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、骨髄腫を治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性骨髄腫を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
ある特定の実施形態において、白血病を治療することを、それを必要とする個人において行う方法を本明細書にて開示し、個人に化合物1の量を投与することを含む。ある特定の実施形態において、再発性または難治性白血病を治療することを、それを必要とする個人において行う方法を本明細書にて更に開示し、個人に化合物1の治療有効量を投与することを含む。
本明細書に記載のBtk阻害剤化合物(すなわち化合物1)は、Btk及びBtkのシステイン481のアミノ酸配列位置と相同である、チロシンキナーゼのアミノ酸配列位置にシステイン残基を有するキナーゼに対して選択的である。Btk阻害剤化合物は、Btkのシステイン481と共有結合を形成し得る(例えば、マイケル反応を介して)。
いくつかの実施形態において、化合物1は非晶質かつ無水である。いくつかの実施形態において、化合物1は非晶質である。いくつかの実施形態において、化合物1は非晶質及び噴霧乾燥形態である。
いくつかの実施形態において、噴霧乾燥形態のイブルチニブが実施例で概説するように調製される。本明細書にて提示する溶媒、温度及び他の反応条件は変化し得る。
本明細書に記載の医薬組成物は、限定されないが経口、非経口(例えば静脈内、皮下、または筋肉内)、口腔内、鼻孔内、直腸または経皮性の投与経路を含む、任意の従来方法を介して哺乳動物へ投与するために製剤することができる。本明細書で使用する場合、「対象」は動物、好ましくはヒト及び非ヒトを含む哺乳動物を意味して使用される。患者及び対象の用語は、どちらも同じ意味で使用され得る。
いくつかの実施形態において、哺乳動物に投与される化合物1の量は300mg/日から、最大1000mg/日である。いくつかの実施形態において、哺乳動物に投与される化合物1の量は420mg/日から最大840mg/日(それを含む)である。いくつかの実施形態において、哺乳動物に投与される化合物1の量は約420mg/日、約560mg/日または約840mg/日である。いくつかの実施形態において、哺乳動物に投与される化合物1の量は約420mg/日である。いくつかの実施形態において、哺乳動物に投与される化合物1の量は約560mg/日である。いくつかの実施形態において、化合物1のAUC0−24は約150〜約3500ng*時間/mLである。いくつかの実施形態において、化合物1のAUC0−24は約500〜約1100ng*時間/mLである。いくつかの実施形態において、化合物1は経口投与される。いくつかの実施形態において、化合物1は1日当たり1回、1日当たり2回または1日当たり3回投与される。いくつかの実施形態において、化合物1は毎日投与される。いくつかの実施形態において、化合物1は1日1回投与される。いくつかの実施形態において、化合物1は2日に1回投与される。いくつかの実施形態において、化合物は維持療法である。
ある特定の場合には、化合物1を別の治療薬と組み合わせて投与することが適切である。
本明細書に記載の治療使用方法での使用のために、製造キット及び物品も本明細書に記載される。そのようなキットはバイアル、チューブなどの容器を1つ以上受け入れるために区分化されているキャリア、パッケージまたは容器を含み、それぞれの容器(複数可)は本明細書に記載の方法で用いる別々の要素のうちの1つを含む。好適な容器には、例えばボトル、バイアル、注射器及び試験管が含まれる。一実施形態において容器は、ガラスまたはプラスチックなどの様々な材料から形成される。
噴霧乾燥混合物溶媒は、総固体重量濃度10%でアセトン中にイブルチニブ及びポリマーを溶解することによって調製された。混合物は、噴霧中の固体凝集塊を回避するため完全に溶解するまで、完全に混合された。適度のイブルチニブ及びポリマー可溶性を提供して、考慮される他の溶媒より好ましい溶媒であったので、アセトンが噴霧乾燥用溶媒として選ばれた。2%または5%の固体重量のイブルチニブと8%または5%のポリマーの溶媒混合物が、ノズルサイズ1.5mm及びノズル圧20psiで速度15ml/分で噴霧乾燥された。注入口温度は70〜80℃の間に設定されて、放出口温度は40〜45℃の間に設定された。乾燥ガス流は35m3/時で維持された。第2の乾燥を40℃のオーブンで約16時間実施して、水分またはアセトンを固体分散粉末から更に除去した。噴霧乾燥は、スクリーニング段階中、広範囲の噴霧乾燥状態及び/または異なる溶媒混合物にわたって、噴霧乾燥チャンバ上の材料の著しい蓄積なしで80〜90%の収率で行われた。
表1:イブルチニブを含む噴霧乾燥(SD)組成物の例
化合物1のキラル純度を、順相HPLCによるLuxセルロース−1キラルカラムを用いて測定した。移動相は、イソプロピルアルコール20%及びヘキサン80%からなる。1−(3−(4−アミノ−3−(4−フェノキシフェニル)−1H−ピラゾロ[3,4−d]ピリミジン−1−イル)ピペリジン−1−イル)プロパ−2−エン−1−オンの鏡像異性体は、260nmで検出される。一実施形態において化合物1はヘキサン:IPA=(7:3)の混合物中に溶解して約0.2mg/mLの濃度を得て、試料のキラル純度を分析する。R鏡像異性体の含量は鏡像異性体ピークのピーク面積正規化によって測定されて、重量対重量パーセントで表される。いくつかの実施形態において、化合物1の試料は、5.0%未満、4.0%未満、3.0%未満、2.0%未満または1.0%未満の(S)−異性体を含む。いくつかの実施形態において、化合物1の試料は、1.0%未満の(S)−異性体を含む。
一実施形態において、ヒトへの投与のための化合物1のカプセル製剤は、以下の成分により調製される。
表2:製剤A
イブルチニブとSoluplusの固体分散中間体(50%活性な噴霧乾燥イブルチニブ)を、ラクトース、微結晶セルロース、クロスカルメロース、二酸化ケイ素及び0.25%ステアリン酸マグネシウムと10分間V−ブレンダで混合した。ブレンド混合物を次いで、サイズ20のメッシュによりスクリーニングした。追加の0.25%ステアリン酸マグネシウムをスクリーニング後のブレンドに添加して、更に3分間混合した。最終的なブレンドをローラー圧密器または単一のプレスステーションを使用してローラー転圧して、リボンまたはスラグを得た。圧縮されたリボンまたはスラグを、造粒機を用いて粉砕して、単一のステーション錠剤プレスを使用して錠剤に圧縮する前にサイズ20でスクリーニングした。
表3:製剤B
*50%活性な噴霧乾燥イブルチニブ
イブルチニブとHPMCAS−Mの固体分散中間体(50%活性な噴霧乾燥イブルチニブ)を、ラクトース、微結晶セルロース、クロスカルメロース、二酸化ケイ素及び0.25%ステアリン酸マグネシウムと10分間V−ブレンダで混合した。ブレンド混合物を次いで、サイズ20のメッシュによりスクリーニングした。追加の0.25%ステアリン酸マグネシウムをスクリーニング後のブレンドに添加して、更に3分間混合した。最終的なブレンドをローラー圧密器または単一のプレスステーションを使用してローラー転圧して、リボンまたはスラグを得た。圧縮されたリボンまたはスラグを、造粒機を用いて粉砕して、単一のステーション錠剤プレスを使用して錠剤に圧縮する前にサイズ20でスクリーニングした。
表4:製剤C
*50%活性な噴霧乾燥イブルチニブ
イブルチニブとHPMCAS−Mの固体分散中間体(20%活性な噴霧乾燥イブルチニブ)を、ラクトース、微結晶セルロース、クロスカルメロース、二酸化ケイ素及び0.25%ステアリン酸マグネシウムと10分間V−ブレンダで混合した。ブレンド混合物を次いで、サイズ20のメッシュによりスクリーニングした。追加の0.25%ステアリン酸マグネシウムをスクリーニング後のブレンドに添加して、更に3分間混合した。最終的なブレンドをローラー圧密器または単一のプレスステーションを使用してローラー転圧して、リボンまたはスラグを得た。圧縮されたリボンまたはスラグを、造粒機を用いて粉砕して、単一のステーション錠剤プレスを使用して錠剤に圧縮する前にサイズ20でスクリーニングした。
表5:製剤D
*20%活性な噴霧乾燥イブルチニブ
表6:錠剤 製剤E及びF
*Prosolv(登録商標)EasyTab(JRS PHARMA LP,USA)は、結合剤−充填剤、滑剤、崩壊剤及び滑沢剤、具体的には微結晶セルロース、コロイド状二酸化ケイ素、グリコール酸ナトリウムデンプン及びステアリルフマル酸ナトリウムを含む賦形剤複合物である。
表7:錠剤 製剤G
いくつかの実施形態において、錠剤は表8に記述する成分で調製される。
表8:錠剤製剤の成分
いくつかの実施形態において、錠剤は表9に記述する成分で調製される。
表9−錠剤製剤の成分
カプセル製剤などの従来の製剤と比較して固体分散体製剤の潜在的効果を評価するために、in vivo実験が行われた。
表10−絶食させたビーグル犬への異なるイブルチニブ製剤の単回投与後の平均(%CV)イブルチニブプラズマPKパラメータ(n=7)
Frel:(AUC製剤B、CまたはD/AUC製剤A)*100
**変動係数(CV)値を( )に示す
N/A:該当なし、ND:測定されず
イブルチニブ固体分散錠剤またはカプセルのin vitro溶出試験を、USP<711>装置2を用いてpH6.8の0.05Mリン酸緩衝液900mlと3%(w/v)のポリソルベート20で実行した。パドル速度は0〜60分は75rpmで、60〜75分は250rpmへ増加した。試料は収集時に濾過されて、Pharmacyclics方法による紫外線(UV)検出を伴う無勾配逆相高速液体クロマトグラフィ(HPLC)を使用して分析した。
目的:この実験の目的は、B細胞慢性リンパ性白血病/小リンパ球性リンパ腫/びまん性分化型リンパ性リンパ腫の患者の経口投与化合物1(420mg/日)の安全性及び最適用量を確立することである。
この試験の主要な目的は、マントル細胞リンパ腫(MCL)を有する再発性/難治性対象の化合物1の有効性を評価することである。二次目的は、この母集団の化合物1の一定の毎日の投薬レジメン(カプセル形態で560mg/日)の安全性を評価することである。
目的:この臨床研究試験の目的は、リツキシマブと組み合わせた化合物1が慢性リンパ性白血病(CLL)及び小リンパ球性リンパ腫(SLL)を制御するのを助けることができるのか調べることである。この組み合わせの安全も試験される。
Claims (21)
- 固体分散イブルチニブを含む固体分散医薬組成物であって、イブルチニブが式(I)の化合物である、医薬組成物。
- 前記固体分散イブルチニブが噴霧乾燥イブルチニブ組成物である、請求項1に記載の医薬組成物。
- 前記噴霧乾燥イブルチニブ組成物が1つ以上の溶解促進剤内に分散されているイブルチニブを含む、請求項2に記載の医薬組成物。
- 前記溶解促進剤がポリマーマトリックスであって、前記ポリマーマトリックスが1つ以上のポリマーを含む、請求項3に記載の医薬組成物。
- 前記噴霧乾燥イブルチニブ組成物が、ポリマーマトリックス内に分散された1〜90重量/重量%のイブルチニブを含む、請求項4に記載の医薬組成物。
- 前記ポリマーマトリックス中の前記ポリマーが直鎖ポリマー、架橋ポリマー、コポリマー、グラフトポリマーまたはこれらの任意の組み合わせである、請求項4に記載の医薬組成物。
- 前記ポリマーが約2,000〜約500,000ダルトン、約100,000〜約200,000ダルトン、約200,000〜約300,000ダルトンまたは約400,000〜約500,000ダルトンの範囲の分子量を有する、請求項4に記載の医薬組成物。
- 請求項1に記載の固体分散医薬組成物及び薬学的に許容される担体を含む、固体分散体製剤。
- 前記製剤が液剤または固形剤の形態である、請求項8に記載の固体分散体製剤。
- 前記製剤が粉末、乾燥粉末または凍結乾燥粉末の形態である、請求項9に記載の固体分散体製剤。
- 請求項1に記載の固体分散医薬組成物及び1つ以上の賦形剤を含む、固体分散体製剤。
- 前記賦形剤が約10〜約50重量/重量%の量で存在する、請求項11に記載の固体分散体製剤。
- 前記製剤がラクトース、微結晶セルロース及びクロスカルメロースナトリウムを含んでおり、
前記ラクトースが約5〜約20重量/重量%、約10〜約20重量/重量%または約14〜約19重量/重量%の量で存在し、
前記微結晶セルロースが約20〜約30重量/重量%、約23〜約28重量/重量%または約24〜約26重量/重量%の量で存在し、
前記クロスカルメロースナトリウムが約3〜約9重量/重量%、約4〜約8重量/重量%または約5〜約7重量/重量%の量で存在する、請求項11に記載の固体分散体製剤。 - 前記製剤が1つ以上の滑剤を更に含む、請求項11に記載の固体分散体製剤。
- 前記製剤が1つ以上の滑沢剤を更に含む。請求項11に記載の固体分散体製剤。
- 前記滑沢剤がステアリン酸マグネシウムであり、ステアリン酸マグネシウムが約0.1〜約0.5重量/重量%または約0.2〜約0.3重量/重量%の量で存在する、請求項15に記載の固体分散体製剤。
- 前記製剤が、
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.8重量/重量%のステアリン酸マグネシウムとを含み、
前記50%活性な噴霧乾燥イブルチニブが、ポリマーマトリックス内に分散された約50重量/重量%のイブルチニブを含んでおり、前記ポリマーマトリックス中の前記ポリマーがヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である、請求項11に記載の固体分散体製剤。 - 前記製剤が、
a)約52〜約54重量/重量%の20%活性な噴霧乾燥イブルチニブと、
b)約13〜約15重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.4〜約0.6重量/重量%のステアリン酸マグネシウムとを含み、
前記20%活性な噴霧乾燥イブルチニブが、ポリマーマトリックス内に分散された約20重量/重量%のイブルチニブを含んでおり、前記ポリマーマトリックス中の前記ポリマーがヒドロキシプロピルメチルセルロースアセテートサクシネート(HPMCAS)である、請求項11に記載の固体分散体製剤。 - 前記製剤が、
a)約49〜約51重量/重量%の50%活性な噴霧乾燥イブルチニブと、
b)約16〜約18重量/重量%のラクトースと、
c)約24〜約26重量/重量%の微結晶セルロースと、
d)約5〜約7重量/重量%のクロスカルメロースナトリウムと、
e)約0.8〜約1.2重量/重量%のコロイド状二酸化ケイ素と、
f)約0.2〜約0.8重量/重量%のステアリン酸マグネシウムとを含み、
前記50%活性な噴霧乾燥イブルチニブが、ポリマーマトリックス内に分散された約50重量/重量%のイブルチニブを含んでおり、前記ポリマーマトリックス中の前記ポリマーがポリビニルカプロラクタム−ポリビニルアセテート−ポリエチレングリコールグラフトコポリマー(Soluplus(登録商標))である、請求項11に記載の固体分散体製剤。 - 疾患の治療を、そのような治療を必要な患者において行う方法であって、治療に有効な量の請求項1に記載の医薬組成物を患者に投与することを含む、前記方法。
- 癌を治療する方法であって、治療に有効な量の請求項1に記載の医薬組成物を、それを必要とする患者に投与することを含む、前記方法。
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- 2015-08-07 MX MX2017001671A patent/MX2017001671A/es unknown
- 2015-08-07 RU RU2017106795A patent/RU2017106795A/ru not_active Application Discontinuation
- 2015-08-07 AU AU2015300798A patent/AU2015300798A1/en not_active Abandoned
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- 2015-08-07 SG SG11201700849XA patent/SG11201700849XA/en unknown
- 2015-08-07 CA CA2955747A patent/CA2955747A1/en not_active Abandoned
- 2015-08-07 KR KR1020177004064A patent/KR20170033358A/ko not_active Withdrawn
- 2015-08-07 BR BR112017002231-1A patent/BR112017002231A2/pt not_active Application Discontinuation
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2016
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EP3193877A1 (en) | 2017-07-26 |
CN106573002A (zh) | 2017-04-19 |
US20170079981A1 (en) | 2017-03-23 |
RU2017106795A (ru) | 2018-09-07 |
WO2016022942A1 (en) | 2016-02-11 |
AU2015300798A1 (en) | 2017-02-02 |
KR20170033358A (ko) | 2017-03-24 |
CA2955747A1 (en) | 2016-02-11 |
US20160038496A1 (en) | 2016-02-11 |
US9545407B2 (en) | 2017-01-17 |
MX2017001671A (es) | 2017-07-04 |
BR112017002231A2 (pt) | 2018-07-17 |
SG11201700849XA (en) | 2017-03-30 |
EP3193877A4 (en) | 2018-04-04 |
IL250085A0 (en) | 2017-03-30 |
US20180028537A1 (en) | 2018-02-01 |
RU2017106795A3 (ja) | 2019-04-12 |
US20190282578A1 (en) | 2019-09-19 |
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