JP2006045117A - アジスロマイシン類を有効成分とする苦味が抑制された安定な組成物 - Google Patents
アジスロマイシン類を有効成分とする苦味が抑制された安定な組成物 Download PDFInfo
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- JP2006045117A JP2006045117A JP2004228370A JP2004228370A JP2006045117A JP 2006045117 A JP2006045117 A JP 2006045117A JP 2004228370 A JP2004228370 A JP 2004228370A JP 2004228370 A JP2004228370 A JP 2004228370A JP 2006045117 A JP2006045117 A JP 2006045117A
- Authority
- JP
- Japan
- Prior art keywords
- arginine
- composition
- bitter taste
- azithromycin
- azithromycins
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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Landscapes
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Abstract
【解決手段】有効成分としてのアジスロマイシン類とL−アルギニンおよび薬剤学的に許容されるキャリアを含む、苦味が抑制された安定な医薬組成物。L−アルギニンは、中核粒子にあってもよいし、コーティング層にあってもよい。
【選択図】なし
Description
アジスロマイシンの苦味を抑制するいくつかの例が知られている(例えば、特許文献2参照。)。この特許においては、アルカリ土類酸化物、アルカリ土類水酸化物またはアルカリ水酸化物が苦味抑制剤として用いられている。
コーティング層にL−アルギニンを含有するアジスロマイシン2水和物組成物(バッチサイズ1000g)を調製した。調製方法を以下に示す。
(1)中核粒子の調製
アジスロマイシン2水和物104.8g、微結晶セルロース(賦形剤)270g、低置換度ヒドロキシプロピルセルロース(結合剤)4g及びヒドロキシプロピルメチルセルロース2910(結合剤)2.5gを造粒機内で混合し、精製水をスプレーしながら造粒した。更に詳しくは、造粒はアジテーター回転速度120回転、ローター回転速度80回転で行った。精製水のスプレー速度は最初の45分間は1760g/minで行い、その後約50分間は800g/minで行った。総造粒時間は95分であった。造粒終点は水分値のモニターと目視確認により行われた。造粒物を乾燥し、篩にかけ、目的とする粒度(105μm−420μm)を有する粒子を得た。得られた粒子を中核粒子として以下のプロセスにおいて用いた。
(2)フィルムコート粒子の調製
水に不溶性であるポリマー(アミノアルキルメタアクリレートコポリマーE(商品名:オイドラギッドE100))40gを54.5%濃度の希釈エタノールに溶解し、被覆用溶液を得た。造粒機内で、上記(1)にて調製した中核粒子に、当該被覆用溶液を噴霧することにより、フィルムコート層で中核粒子を被覆した。得られた粒子を乾燥し、篩にかけて、目的とする粒度(444μm以下)を有するフィルムコート粒子を得た。
(3)シュガーコート粒子の調製
上記(2)で調製したフィルムコート粒子にシュガーコート層を形成した。詳しくは、精製水に白糖を溶解して調製した濃度約50%の白糖溶液を得た。この溶液に、黄色三二酸化鉄(色素)を溶解させた。さらに、この溶液に酸化チタン(遮光剤)20gを分散させ、造粒機内で、(2)にて調製したフィルムコート粒子に、この懸濁溶液を噴霧した。噴霧中、L−アルギニン20gを供給し、パイナップル香料3gとキサンタンガム(粘稠剤)5gも供給した。得られた粒子を乾燥し、篩にかけて、目的とする粒度(708μm以下)を有するシュガーコート粒子を得た。
L−アルギニンをシュガーコート段階ではなく中核粒子の造粒段階で加えた点を除き、実施例1のプロセスと同じプロセスにより、中核粒子にL−アルギニンを含有する組成物を作成する。
L−アルギニンを全く加えなかった点を除き、実施例1のプロセスと同じプロセスにより、比較用のアジスロマイシン2水和物を含む組成物を調製した。
10人のパネリストで苦味比較試験を実施した。上記の実施例1及び実施例3により製造されたアジスロマイシン2水和物製剤を試験に使用した。パネリストの好みを異なる2点で確認した。組成物2gに対して水を2ml滴下して練ったものを検体とした。検体を1分間口に含み、その後吐き出し、口を水ですすいだ。検体を口中に保持していた時点及び口をすすいだ後に感じられた苦味についてパネリストに比較評価してもらった。なお、試験する検体の順序による影響を排除するために、試験はクロスオーバー試験により行い、半数のパネリストと残り半数のパネリストとの間で検体の試験順序を入れ替えた。結果を表1に示す。
上記の試験結果から、本発明の実施例1の組成物は、アジスロマイシン2水和物の苦味発現が効果的に抑制できることが実証された。
このほか、L−アルギニンと同じく有機の塩基性物質である、銅クロロフィリンナトリウムが良好な苦味抑制効果を奏した。
Claims (7)
- L−アルギニン、アジスロマイシン類、および薬剤学的に許容されるキャリアを含む、苦味が抑制された安定な医薬組成物。
- 前記組成物のコーティング層に、L−アルギニンを含有することを特徴とする、請求項1に記載の組成物。
- 前記組成物の中核粒子に、L−アルギニンを含有することを特徴とする、請求項1に記載の組成物。
- L−アルギニンを組成物に加えることにより、アジスロマイシン類を含む組成物の苦味を抑制する方法。
- L−アルギニンを組成物のコーティング層または中核粒子に加えることにより、アジスロマイシン類を含む組成物の苦味を抑制する方法。
- アジスロマイシン類を含む組成物の苦味を抑制するための、L−アルギニンの使用。
- 銅クロロフィリンナトリウム、アジスロマイシン類、および薬剤学的に許容されるキャリアを含む、苦味が抑制された安定な医薬組成物。
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Cited By (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007148772A1 (ja) * | 2006-06-23 | 2007-12-27 | Shionogi & Co., Ltd. | マクロライド系抗生物質の糖類被覆製剤 |
CN100441196C (zh) * | 2006-12-15 | 2008-12-10 | 北京化工大学 | 一种制备微粉化阿奇霉素的方法 |
ES2335334A1 (es) * | 2008-09-23 | 2010-03-24 | Laboratorio Jaer, S.A. | Utilizacion del xilitol para el enmascaramiento gustativo de amargantes en alimentos para animales. |
WO2010034853A1 (es) * | 2008-09-23 | 2010-04-01 | Laboratorio Jaer, S.A. | Utilización de exilitol o sus derivados para el enmascaramiento gustativo de quimioterapicos del grupo del ácido quinolon-o-naftiridoncarboxilico administrados en alimentos destinados a ganado porcino |
JP2010535757A (ja) * | 2007-08-10 | 2010-11-25 | 大塚製薬株式会社 | レバミピドを含有する医薬組成物 |
ES2351643A1 (es) * | 2009-07-27 | 2011-02-09 | Laboratorio Jaer,S.A. | Utilización de xilitol o sus derivados para el enmascaramiento gustativo de quimioterápicos del grupo del ácido quinolon-o-naftiridoncarboxílico administrados en alimentos destinados a ganado porcino. |
JP2012148985A (ja) * | 2011-01-17 | 2012-08-09 | Lintec Corp | シート状製剤 |
JP2014140362A (ja) * | 2012-12-28 | 2014-08-07 | Kao Corp | ジカフェオイルキナ酸類含有飲料 |
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JPH07300420A (ja) * | 1994-04-29 | 1995-11-14 | Pfizer Inc | アジスロマイシン投与法 |
JP2005162733A (ja) * | 2003-12-04 | 2005-06-23 | Pfizer Prod Inc | 少ない副作用しか有さないアジスロマイシン剤形 |
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JPH07300420A (ja) * | 1994-04-29 | 1995-11-14 | Pfizer Inc | アジスロマイシン投与法 |
JP2005162733A (ja) * | 2003-12-04 | 2005-06-23 | Pfizer Prod Inc | 少ない副作用しか有さないアジスロマイシン剤形 |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2007148772A1 (ja) * | 2006-06-23 | 2007-12-27 | Shionogi & Co., Ltd. | マクロライド系抗生物質の糖類被覆製剤 |
CN100441196C (zh) * | 2006-12-15 | 2008-12-10 | 北京化工大学 | 一种制备微粉化阿奇霉素的方法 |
JP2010535757A (ja) * | 2007-08-10 | 2010-11-25 | 大塚製薬株式会社 | レバミピドを含有する医薬組成物 |
KR101551506B1 (ko) * | 2007-08-10 | 2015-09-08 | 오츠카 세이야쿠 가부시키가이샤 | 레바미피드를 함유하는 의약 조성물 |
ES2335334A1 (es) * | 2008-09-23 | 2010-03-24 | Laboratorio Jaer, S.A. | Utilizacion del xilitol para el enmascaramiento gustativo de amargantes en alimentos para animales. |
WO2010034853A1 (es) * | 2008-09-23 | 2010-04-01 | Laboratorio Jaer, S.A. | Utilización de exilitol o sus derivados para el enmascaramiento gustativo de quimioterapicos del grupo del ácido quinolon-o-naftiridoncarboxilico administrados en alimentos destinados a ganado porcino |
ES2351643A1 (es) * | 2009-07-27 | 2011-02-09 | Laboratorio Jaer,S.A. | Utilización de xilitol o sus derivados para el enmascaramiento gustativo de quimioterápicos del grupo del ácido quinolon-o-naftiridoncarboxílico administrados en alimentos destinados a ganado porcino. |
JP2012148985A (ja) * | 2011-01-17 | 2012-08-09 | Lintec Corp | シート状製剤 |
JP2014140362A (ja) * | 2012-12-28 | 2014-08-07 | Kao Corp | ジカフェオイルキナ酸類含有飲料 |
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