JP5973117B2 - 自己乳化性の活性物質配合物およびこの配合物の使用 - Google Patents
自己乳化性の活性物質配合物およびこの配合物の使用 Download PDFInfo
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Description
i)少なくとも1種の活性物質と、
ii)脂質成分、
iii)結合剤成分、および
iv)適切な場合には、他の添加剤、
を含む配合基剤と、
をベースとする自己乳化性配合物に関する。
i')少なくとも1種の脂質様活性物質および適切な場合には他の活性物質と、
ii')適切な場合には別の脂質成分要素、
iii)結合剤成分、および
iv)適切な場合には他の添加剤、
を含む配合基剤と、
をベースとする自己乳化性配合物に関する。
合成ポリマー、たとえば、ポリビニルラクタム、特に、ポリビニルピロリドン(PVP);ビニルラクタム、たとえば、N-ビニルピロリドン、N-ビニルピペリドンおよびN-ビニル-ε-カプロラクタム、特に、N-ビニルピロリドンと、(メタ)アクリル酸および/または(メタ)アクリル酸エステル、たとえば、長鎖(メタ)アクリレート、具体的には、ステアリル(メタ)アクリレート、四級化されていてもよいジアルキルアミノアルキル(メタ)アクリレート、および無水マレイン酸、ビニルエステル、特に、ビニルアセテート、ビニルホルムアミド、ビニルスルホン酸または四級化ビニルイミダゾールと、のコポリマー;ビニルアセテートとクロトン酸とのコポリマー;部分加水分解ポリビニルアセテート;ポリビニルアルコール;(メタ)アクリル樹脂、たとえば、ポリ(ヒドロキシアルキル(メタ)アクリレート)、ポリ(メタ)アクリレート、アクリレートコポリマー、具体的には、アルキルアクリレートと(メタ)アクリル酸とのコポリマーおよびジメチルアミノエチルアクリレートとメタクリル酸エステルとのコポリマー(たとえば、Eudragitタイプ);ポリアルキレングリコール、たとえば、ポリプロピレングリコールおよびポリエチレングリコール、好ましくは分子量が1,000を超えるもの、特に好ましくは2,000を超えるもの、中でも特に好ましくは4,000を超えるもの(具体的には、ポリエチレングリコール6,000);ポリアルキレンオキシド、たとえば、ポリプロピレンオキシド、特に、ポリエチレンオキシド、好ましくは高分子量のもの、中でも重量平均分子量が100,000よりも大きいもの;メチルメタクリレートとアクリル酸とのコポリマー;ポリアクリルアミド、ポリビニルホルムアミド(適切な場合には、部分的にまたは完全に加水分解されたもの);
変性天然ポリマー、たとえば、変性デンプンおよび変性セルロース、たとえば、セルロースエステル、好ましくは、セルロースエーテル、具体的には、メチルセルロースおよびエチルセルロース、ヒドロキシアルキルセルロース、特に、ヒドロキシプロピルセルロース、ヒドロキシアルキルアルキルセルロース、特に、ヒドロキシプロピルメチルセルロースまたはヒドロキシプロピルエチルセルロース、セルロースフタレート、特に、セルロースアセテートフタレートおよびヒドロキシプロピルメチルセルロースフタレート、デンプン分解生成物、特に、デンプン糖化生成物、具体的には、マルトデキストリン;
天然または主に天然のポリマー、たとえば、ゼラチン、ポリヒドロキシアルカノエート、具体的には、ポリヒドロキシ酪酸およびポリ乳酸、ポリアミノ酸、具体的には、ポリリシン、ポリアスパラギン、ポリジオキサンおよびポリペプチド、およびマンナン、特に、ガラクトマンナン;ならびに
非高分子結合剤、たとえば、ポリオール、たとえば、WO 98/22094およびEP 0 435 450に記載のもの、特に、糖アルコール、具体的には、マルチトール、マンニトール、ソルビトール、セロビイトール(cellobiitol)、ラクチトール、キシリトール、エリトリトールおよびイソマルト(Palatinit)。
iii1) 5〜90重量%、好ましくは10〜50重量%、特に15〜30重量%の少なくとも1種の糖アルコールおよび/または少なくとも1種のデンプン糖化生成物;
iii2) 10〜95重量%、好ましくは50〜90重量%、特に70〜85重量%の少なくとも1種の親水性ポリマー;
iii3)適切な場合には、少なくとも1種の上記のポリマー;
ここで、iii1)、iii2)、およびiii3)の含有量の合計は、結合剤成分の100重量%を構成する。
充填剤、たとえば、上記の糖アルコール、具体例としては、マンニトール、ソルビトール、キシリトールおよびイソマルト(DE 195 36 394参照)、タルク、スクロース、ラクトース、穀類またはコーンスターチ、ジャガイモ粉。存在する場合、特に、濃度は、混合物の全重量を基準にして、0.02〜50、好ましくは0.20〜20重量%である;
滑沢剤、滑剤および離型剤、たとえば、ステアリン酸のマグネシウム、アルミニウムおよびカルシウム塩、タルクおよびシリコーン、ならびに動物性または植物性の脂肪、特に、水素化された形態のものおよび室温で固体であるもの。これらの脂肪は、好ましくは30℃以上の融点を有する。溶融押出法に関連して技術的に好ましいのは、DE 197 31 277に記載されているC12、C14、C16およびC18脂肪酸のトリグリセリド、または加工性を改良するうえで、DE 195 36 394にイソマルト含有ポリマー/活性物質溶融体の押出と関連して記載されているレシチンである。カルナウバワックスのようなワックスを使用することも可能である。これらの脂肪およびワックスは、単独で、あるいはモノおよび/もしくはジグリセリドまたはホスファチド、特にレシチンと共に、有利に混合することができる。モノおよびジグリセリドは、好ましくは、上記の脂肪酸タイプから誘導される。本発明に従って存在する脂質は、通常、これらの添加剤の機能を担うので、結果として、滑沢剤、滑剤および離型剤は、添加剤として配合物にごく少量添加され、有利にはまったく添加されない。存在する場合、滑沢剤および離型剤の形態の添加剤の合計量は、混合物の全重量を基準にして、好ましくは0.1〜10重量%、特に0.1〜1重量%である;
流動調節剤、たとえば、珪藻土、特に、特許登録名Aerosil(登録商標)を有する高純度二酸化ケイ素。存在する場合、量は、特に、混合物の全重量を基準にして0.1〜5重量%である;
アゾ染料のような染料、有機または無機の顔料あるいは天然源の染料。好ましいのは無機顔料である。存在する場合、濃度は、混合物の全重量を基準にして、0.001〜10、好ましくは0.5〜3重量%である;
安定化剤、たとえば、酸化防止剤、光安定化剤、ヒドロペルオキシド破壊剤、ラジカルスカベンジャー、微生物の攻撃に対する安定化剤;
可塑剤、特に、以下に記載のもの。
i)少なくとも1種の活性物質成分、好ましくは活性医薬成分;
ii)少なくとも1種の不飽和脂肪酸、好ましくは、オレイン酸、リノール酸および/またはリノレン酸、あるいは対応するモノまたはジグリセリドから選択される不飽和脂肪酸;
iii)ポリビニルピロリドン、ビニルピロリドンコポリマー、特にビニルアセテートとのコポリマー、またはセルロース誘導体、特にヒドロキシプロピルセルロースおよびヒドロキシプロピルメチルセルロースから選択される少なくとも1種の結合剤;ならびに
iv)適切な場合には、他の添加剤、たとえば流動調節剤、
を含有する配合物を含む。
i')少なくとも1種の脂質様活性物質、好ましくは油、特に精油;
ii')適切な場合には、1種以上の他の脂質;
iii)少なくとも1種の糖アルコール、特に、マルチトールおよび/またはイソマルト、および少なくとも1種のデンプン糖化生成物、特にマルトデキストリン;ならびに
iv)適切な場合には、他の添加剤、
を含有する配合物を含む。
等重量部のヒドロキシプロピルセルロース(Klucel EF, Agualon)とオレイン酸との混合物を計量混練機(Rheomix, Haake製)により120℃で処理して均一なゴム状溶融体にした。冷却させたところ、水に溶解してエマルジョンを形成する透明な固形塊が得られた。
実施例1と同様にして実験を行ったが、ただし、5分間にわたり100℃の温度で60重量%のKollidon VA-64(BASF)と40重量%のオレイン酸との混合物を処理した。清澄透明な低粘度の溶融体が得られた。またこの溶融体は、室温まで冷却した後(および室温で12ヶ月間保存した後でさえも)、清澄透明であり、しかも依然として塑性変形可能であった。冷却された溶融体は、容易に水中に溶解してエマルジョンを形成した。Mastersizer計器(Malvern, UKから入手)を用いて、この調製物のエマルジョン液滴のサイズを測定した。粒子の90%は35μm未満のサイズを有し、粒子の50%は2μm未満であった。
72重量%のKollidon VA-64(BASF)と28重量%のオレイン酸との混合物を用いて、実施例2と同様にして実験を行った。冷却された溶融体は同様に透明であったが、実施例2のときほど容易に塑性変形させることはできなかった。冷却された溶融体は、容易に水に溶解してエマルジョンを形成した。Mastersizer計器(Malvern, UKから入手)を用いて、この調製物のエマルジョン液滴のサイズを測定した。粒子の90%は4μm未満のサイズを有し、粒子の50%は0.7μm未満であった。
実施例3と同様にして実験を行ったが、ただし、64重量%のKollidon VA-64(BASF)と、16重量%のオレイン酸と、20重量%のデキストランとの混合物を118℃で処理した。生成した白みを帯びた溶融体は、冷却後、固体になり、0.1M HClにかなり迅速に溶解してエマルジョンを形成した。
実施例4と同様にして実験を行ったが、ただし、70重量%のヒドロキシプロピルセルロース(Klucel EF, Aqualon)と、10重量%オレイン酸と、20重量%のデキストランとからなる混合物を120℃で処理した。生成した白色の溶融体は、冷却後、固体になり、水に溶解してエマルジョンを形成したが、実施例4の場合よりも遅かった。
実施例5と同様にして実験を行ったが、ただし、40重量%のヒドロキシプロピルセルロース(Klucel EF, Aqualon)と、40重量%のステアリン酸と、20重量%のデキストランとからなる混合物を120℃で処理した。生成した白色の溶融体は、冷却粉砕後、比較的容易に水に分散性してエマルジョンを形成した。
実施例1と同様にして実験を行ったが、ただし、70重量%のヒドロキシプロピルセルロース(Klucel EF, Aqualon)と30重量%のステアリン酸とからなる混合物を110℃で処理した。清澄なゴム状溶融体が生成した。冷却したところ、白色固体を形成した。
穏やかに混練しながら、1重量部のオレイン酸を7重量部のKollidon VA-64(BASF)に添加した。数分間混練したところ、わずかに発熱を伴って均一な顆粒が得られた。これを2重量部の活性物質エスプロンと混合した。次に、この顆粒状の混合物に1重量%の高分散シリカ(Aerosil 200)を添加し、次に、この混合物を2軸スクリュー押出機(スクリュー直径16mm)に秤量供給装置を介して計量供給し、そして110℃の温度で押出した。冷却後、生成した清澄な溶融体を水に溶解させてエマルジョンを形成させることができた。
実施例8と同様にして実験を行ったが、ただし、2重量部のパラセタモールを7重量部のKollidon VA-64(BASF)と1重量部のオレイン酸とのあらかじめ顆粒化した混合物と混練した。押出する前に、1重量%のAerosil 200を同様に混合しながら全混合物に添加した。125℃の温度で押出を行い、冷却した溶融体を水に溶解させて微粒子エマルジョンを形成させた。
実施例8と同様にして実験を行ったが、ただし、2重量部のパラセタモールを、6.125重量部のKollidon VA-64(BASF)と0.875重量部のオレイン酸と1重量部のステアリルアルコールとの顆粒状混合物と混練した。押出する前に、1重量%のAerosil 200を同様に混合しながら全混合物に添加した。120℃の温度で押出を行い、冷却した溶融体を水に溶解させて微粒子エマルジョンを形成させた。
K値30を有する2重量%のPVPホモポリマー(Kollidon 30)と70重量%のイソマルトとDE値15を有する18重量%のマルトデキストリン(Cerestar製のC-Pur 01915)とを2軸スクリュー押出機で混合した。10重量%のオレンジ油を側面から計量供給し、連続方式でマトリックス中に組み込んだ。押出後、ホットカットにより混合物を約1mmサイズのペレットに加工した。それぞれのセクションの温度は、39℃、57℃、110℃、89℃および89℃であった。また、ダイの温度は101℃であった。
約80,000の重量平均分子量を有する2重量%のヒドロキシプロピルセルロース(Klucel EF)と70重量%のイソマルトとDE値15を有する18重量%のマルトデキストリン(Cerestar製のC-Pur 01915)とを2軸スクリュー押出機で混合した。10重量%のオレンジ油を側面から計量供給し、連続方式でマトリックス中に組み込んだ。押出後、ホットカットにより混合物を約1mmサイズのペレットに加工した。セクションの温度は、61℃、84℃、120℃、111℃および100℃であった。また、ダイの温度は111℃であった。
K値30を有する2重量%のPVPホモポリマー(Kollidon 30)と53重量%のイソマルトとDE値15を有する35重量%のマルトデキストリン(Cerestar製のC-Pur 01915)とを2軸スクリュー押出機で混合した。10重量%のオレンジ油を側面から計量供給し、連続方式でマトリックス中に組み込んだ。押出後、ホットカットにより混合物を約1mmサイズのペレットに加工した。セクションの温度は、52℃、64℃、110℃、92℃および91℃であった。また、ダイの温度は104℃であった。
Claims (10)
- i)0.1〜50重量%の、少なくとも1種の活性物質を含む活性成分、
ii)6〜60重量%の、少なくとも1種の脂質を含み、50℃を超えない融点を有する脂質成分、および
iii)20〜93.9重量%の、ポリビニルピロリドン、ビニルピロリドン/ビニルアセテートコポリマー、ヒドロキシアルキルセルロース、ヒドロキシアルキルアルキルセルロース、セルロースフタレートおよび(メタ)アクリル樹脂から選択される少なくとも1種の結合剤を含む結合剤成分、
を含む自己乳化性固形配合物であって、
前記脂質成分が、12を超えないHLBを有し、
前記脂質成分の含有量が、前記結合剤成分を基準にして、40重量%を超えず、
前記配合物が、前記脂質成分および前記結合剤成分を含む分子分散体を含み、
前記配合物が、本質的に前記活性物質の結晶を含まない、
前記配合物。 - 本質的に前記活性物質の結晶および前記脂質の結晶を含まない、請求項1に記載の配合物。
- 前記活性物質が、水に対して低い溶解度を有する、請求項1に記載の配合物。
- 前記脂質成分が、30℃よりも低い融点を有する、請求項1に記載の配合物。
- 前記脂質成分の含有量が、前記結合剤成分を基準にして、25重量%を超えない、請求項1に記載の配合物。
- 前記結合剤が、ヒドロキシプロピルセルロース、ヒドロキシプロピルメチルセルロース、またはビニルピロリドン/ビニルアセテートコポリマーである、請求項1に記載の配合物。
- 成分i)、ii)、およびiii)を含む可塑性混合物の溶融押出により得られる、請求項1に記載の配合物。
- 前記結合剤が、ビニルピロリドン/ビニルアセテートコポリマーである、請求項1に記載の配合物。
- 前記活性物質が、活性医薬成分である、請求項8に記載の配合物。
- 前記脂質が、モノグリセリド、ジグリセリドまたはトリグリセリドである、請求項8に記載の配合物。
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- 2001-05-29 EP EP01957809A patent/EP1284716B1/de not_active Revoked
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Also Published As
Publication number | Publication date |
---|---|
PT1284716E (pt) | 2007-03-30 |
US8470347B2 (en) | 2013-06-25 |
WO2001091727A3 (de) | 2002-05-10 |
US20120225953A1 (en) | 2012-09-06 |
EP1284716A2 (de) | 2003-02-26 |
US20110123652A1 (en) | 2011-05-26 |
JP2003534369A (ja) | 2003-11-18 |
US20140135388A1 (en) | 2014-05-15 |
CA2408915A1 (en) | 2002-11-13 |
WO2001091727A2 (de) | 2001-12-06 |
CA2408915C (en) | 2010-07-27 |
US20040013697A1 (en) | 2004-01-22 |
SI1284716T1 (sl) | 2007-08-31 |
EP1284716B1 (de) | 2006-11-02 |
ES2275705T3 (es) | 2007-06-16 |
CY1105968T1 (el) | 2011-04-06 |
DE50111376D1 (de) | 2006-12-14 |
ATE344019T1 (de) | 2006-11-15 |
AU2001279631A1 (en) | 2001-12-11 |
DK1284716T3 (da) | 2007-03-05 |
DE10026698A1 (de) | 2001-12-06 |
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