JP5160386B2 - コロイド状二酸化ケイ素を含んでなる医薬組成物 - Google Patents
コロイド状二酸化ケイ素を含んでなる医薬組成物 Download PDFInfo
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Description
− ポリオキシエチレン−ポリオキシプロピレン コポリマーおよびブロックコポリマー、例えばプルロニック(Pluronic)(登録商標)またはポロキサマー(Poloxamer)(登録商標)として商業的に入手可能なもの、例えばH. Fiedler, "Lexikon der Hilfsstoffe fur Pharmazie, Kosmetik und angrenzende Gebiete", Editio Cantor Verlag Aulendorf, Aulendorf, 第4改訂および増補版 (1996)において記載されたもの。その内容を、引用により本明細書の一部とする。好適なポリオキシエチレン−ポリオキシプロピレンブロックコポリマーは、BASF社から商品として入手可能なポロキサマー(登録商標)188である;
a)例えば心臓、肺、心肺同時、肝臓、腎臓、腸、膵臓、インスリン産生細胞、皮膚または角膜移植のための、細胞、組織または器官異種または同種移植拒絶の処置または予防。該医薬組成物は、また、宿主対移植片病、例えば骨髄移植後に時々起きる疾患の予防に適用される;
d)慢性移植片拒絶または再狭窄の処置または予防;
e)癌、過増殖皮膚障害などの処置;
f)感染症、例えば真菌感染症の処置;
g)とりわけステロイドの作用の増強における、炎症の処置または予防;
が挙げられる。
a)
− 器官または組織移植、例えば心臓、腎臓、肝臓、骨髄および皮膚の拒絶、
− 宿主対移植片病、例えば骨髄移植後のもの、
− リウマチ様関節炎、全身性エリテマトーデス、橋本甲状腺炎、多発性硬化症、重症筋無力症、I型糖尿病、およびブドウ膜炎のような自己免疫疾患、
− 免疫介在性疾患の皮膚病変
の予防または処置;
において使用するための抗炎症剤および免疫抑制剤および抗増殖剤として有用である。
分散可能な錠剤は、ステップ(iii)において得られた混合物を打錠することにより得られる。250mgの医薬組成物を、9mmのダイおよび標準的フラットパンチで10.5kNの圧縮力を用いるFette(登録商標)PT 2080ロータリー型打錠機により圧縮する。次いで、得られた錠剤の硬度を、Kraemer 3S錠剤試験デバイスを用いて、該錠剤を破砕するのに必要な力を測定することにより評価する。これらの条件下で製造された錠剤の硬度は、35〜79Nであった。かかる錠剤の崩壊時間は、0.4〜1.4分(24〜84秒)であった。
医薬組成物を上記の通り製造した。分散可能な錠剤を、Fette(登録商標)PT2080ロータリー型打錠機で、7mmのダイおよび標準的フラットパンチにて7.5kNの圧縮力を用いて100mgの医薬製剤を圧縮することにより製造した。これらの条件下で製造された錠剤の硬度は、25〜79Nであった。かかる錠剤の崩壊時間は、1.1〜1.7分(66〜102秒)であった。
Claims (5)
- 40−O−(2−ヒドロキシ)エチル−ラパマイシンの固体分散体、架橋ポリビニルピロリドンを含んでなる崩壊剤およびコロイド状二酸化ケイ素を含む、患者に投与する前に摂取液中に分散させて投与するための分散可能な錠剤の形態である医薬組成物であって、1〜5重量%のコロイド状二酸化ケイ素及び10〜30重量%の架橋ポリビニルピロリドンを含んでなり、錠剤が35〜80Nの硬度および3分以下の崩壊時間を有する、医薬組成物。
- 錠剤が90秒もしくはそれ未満の崩壊時間を有する、請求項1に記載の医薬組成物。
- 錠剤が、250mgの組成物を9mmのダイおよび標準的フラットパンチで8〜11kNの力を用いて圧縮することにより形成されたものである、請求項1または2に記載の医薬組成物。
- 免疫抑制剤または癌処置剤として使用するための、請求項1〜3のいずれかに記載の医薬組成物。
- 請求項1に記載の医薬組成物の製造方法であって、40−O−(2−ヒドロキシ)エチル−ラパマイシンの固体分散体を調製すること、40−O−(2−ヒドロキシ)エチル−ラパマイシンの固体分散体を、架橋ポリビニルピロリドンを含んでなる崩壊剤およびコロイド状二酸化ケイ素と混合して医薬組成物を形成させること、ならびに該医薬組成物を圧縮して分散可能な錠剤を形成させることを含んでなる方法。
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Application Number | Priority Date | Filing Date | Title |
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GB0123400.4 | 2001-09-28 | ||
GBGB0123400.4A GB0123400D0 (en) | 2001-09-28 | 2001-09-28 | Organic compounds |
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JP2003532038A Division JP2005507897A (ja) | 2001-09-28 | 2002-09-27 | コロイド状二酸化ケイ素を含んでなる医薬組成物 |
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JP2009102341A JP2009102341A (ja) | 2009-05-14 |
JP2009102341A5 JP2009102341A5 (ja) | 2011-12-08 |
JP5160386B2 true JP5160386B2 (ja) | 2013-03-13 |
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JP2003532038A Withdrawn JP2005507897A (ja) | 2001-09-28 | 2002-09-27 | コロイド状二酸化ケイ素を含んでなる医薬組成物 |
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CN (3) | CN101912392A (ja) |
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CO (1) | CO5390072A1 (ja) |
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IL (2) | IL160498A0 (ja) |
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PT (2) | PT1432408E (ja) |
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TW (1) | TWI242449B (ja) |
WO (1) | WO2003028705A1 (ja) |
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