JP7026876B2 - 一部がコーティングされた放出制御固形製剤 - Google Patents
一部がコーティングされた放出制御固形製剤 Download PDFInfo
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- JP7026876B2 JP7026876B2 JP2017504225A JP2017504225A JP7026876B2 JP 7026876 B2 JP7026876 B2 JP 7026876B2 JP 2017504225 A JP2017504225 A JP 2017504225A JP 2017504225 A JP2017504225 A JP 2017504225A JP 7026876 B2 JP7026876 B2 JP 7026876B2
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Description
出願番号:201410139563.9
出願日:2014-04-08
発明の名称:新型放出制御錠
1)錠芯を調製するための各組成成分を混合し、I番パンチで一回目のプレスを行って、錠芯を得る工程と、
2)II番パンチに交換し、コーティング層を調製するための各組成成分を混合した後、中金型に充填する工程と、
3)工程1)でプレスした錠芯を中金型の中央に充填し、二回目のプレスを行って、固形製剤を得る工程と
を含み、
前記I番パンチの直径がII番パンチの直径より小さい。
製剤は、1層の徐放層のみを有する単層錠である錠芯と、錠芯外に被覆されたコーティングとを含む。図1に示すように、コアの頂面の一部が、コーティングで被覆されずに固形製剤の表面に露出している。
1、錠芯の原料と添加剤を処方に準じて秤量して、十分に混合した後使用に備え、そして、I番パンチの直径がII番より小さい二種類の規格のパンチを選択する;
製剤は、2層の錠である錠芯と、錠芯外に被覆されたコーティングを含む。図2に示すように、コアの頂面の一部がコーティングで被覆されずに固形製剤の表面に露出している。
1、錠芯の徐放層、錠芯の速放層の原料と添加剤を処方に準じて秤量し、それぞれ十分に混合した後使用に備え、そして、I番パンチの直径がII番より小さい二種類の規格のパンチを選択する;
製剤は、1層の徐放層のみを有する単層錠である錠芯と、錠芯外に被覆されたコーティングとを含む。図1に示すように、コアの頂面の一部がコーティングで被覆されずに固形製剤の表面に露出している。
1、錠芯の原料と添加剤を処方に準じて秤量し、十分に混合した後使用に備え、そして、I番パンチの直径がII番より小さい二種類の規格のパンチを選択する;
製剤は、第1徐放層と第2徐放層からなる2層の錠である錠芯と、錠芯外に被覆されたコーティングとを含む。図3に示すように、コアの頂面の一部がコーティングで被覆されずに固形製剤の表面に露出している。
1、錠芯の第1徐放層、錠芯の第2徐放層の原料と添加剤を処方に準じて秤量して、それぞれ十分に混合した後使用に備え、そして、I番パンチの直径がII番より小さい二種類の規格のパンチを選択する;
実施例5~10の製剤は、実施例1と同様に、コアが単層である(1層の徐放層のみを有する)放出制御製剤である。
本実施例における放出制御製剤のコアが3層(いずれの層も活性成分を含む)であり、不完全なコーティング層にも活性物質が含まれ、最外層のフィルムコーティングにも活性物質が含まれる。図10に示すように、コアの上層薬物含有層の一部がコーティングで被覆されずに固形製剤の表面に露出している。
1、錠芯の上層、中間層、下層の原料と添加剤を処方に準じて秤量し、それぞれ十分に混合した後使用に備え、そして、I番パンチの直径がII番より小さい二種類の規格のパンチを選択する;
<付記>
<項1>
活性薬物と添加剤を含むコアと、徐放・放出制御素材を含み、活性成分を含むか、または含まないコーティング層とからなる放出制御固形製剤において、前記コアの表面がコーティング層で完全に被覆されず、一部が固形製剤の表面に露出していることを特徴とする、放出制御固形製剤。
<項2>
前記コアが1層または複数層であり、前記層が徐放層であり、あるいは速放層と徐放層を共に含み、コアが2層以上である場合、最外層の成分が最初に放出され、第二外層の成分が次に放出され、コアの最内層の成分が最後に放出されるようにそれぞれの層の成分が順次放出される、<項1>に記載の固形製剤。
<項3>
前記コーティング層が圧縮コーティング法で調製されてなる、<項1>に記載の固形製剤。
<項4>
前記コーティング層の素材が水可溶性または水不溶性であり、前記水可溶性のコーティング素材が、ヒドロキシプロピルメチルセルロース、ヒドロキシプロピルセルロースから選ばれる1種または2種であり、前記水不溶性のコーティング素材が、エチルセルロース、セルロースアセテートポリマー、アクリル樹脂から選ばれる1種または複数種であることを特徴とする、<項1>に記載の固形製剤。
<項5>
前記コーティング層の素材が、ポリビニルピロリドン、ラクトース、塩化ナトリウムから選ばれる1種または複数種である水溶性ポロゲンをさらに含むことを特徴とする、<項1>に記載の固形製剤。
<項6>
前記コーティング層の外面に、活性成分を含むか、または含まない、もう1層のコーティングを有する、<項1>~<項5>のいずれか一項に記載の固形製剤。
<項7>
錠剤である<項1>に記載の固形製剤。
<項8>
コアは、1層以上の錠状物からなる錠芯である、<項7>に記載の固形製剤。
<項9>
<項7>または<項8>に記載の固形製剤の調製方法であって、
打錠機でタブレットのプレスを行い、
1)錠芯を調製するための各組成成分を混合し、I番パンチで一回目のプレスを行って、錠芯を得る工程と、
2)II番パンチに交換し、コーティング層を調製するための各組成成分を混合した後、中金型に充填する工程と、
3)工程1)でプレスした錠芯を中金型の中央に充填し、二回目のプレスを行って、固形製剤を得る工程と
を含み、
前記I番パンチの直径がII番パンチの直径より小さい、固形製剤の調製方法。
<項10>
前記工程2)と3)を、
II番パンチに交換した後、工程1)でプレスした錠芯を中金型の中央に充填し、その後、中金型の中で錠芯の周囲に、均一に混合されたコーティング層の組成成分を充填して、二回目のプレスを行うことへ変更する、<項9>に記載の調製方法。
Claims (7)
- コアと、コーティング層とからなる放出制御固形製剤であって、
前記コアが、2層以上であり、それぞれの層が活性薬物と添加剤とを含み、
前記コーティング層が、水溶性ポロゲンと、徐放・放出制御素材とを含み、
前記コーティング層が、活性成分を含むか、または含まず、
前記コアの表面が、前記コーティング層で完全に被覆されず、前記コアの表面の上層の一部が固形製剤の表面に露出しており、
前記コーティング層の前記徐放・放出制御素材が、水不溶性素材であり、前記コーティング層の総量に対して68~78重量%で含まれ、
前記水不溶性素材が、エチルセルロース、セルロースアセテートポリマー、アクリル樹脂からなる群から選ばれる1種または複数種であり、
前記水溶性ポロゲンが、ポリビニルピロリドン、ラクトース、塩化ナトリウムからなる群から選ばれる1種または複数種であり、前記コーティング層の総量に対して20重量%、又は20~30重量%で含まれ、
前記コアと前記コーティング層の重量比が3:5である、ことを特徴とする、放出制御固形製剤。 - 前記コアが3層であり、前記3層中の成分が、上層の成分が最初に放出され、中間層の成分が次に放出され、下層の成分が最後に放出されるようにそれぞれの層の成分が順次放出される、請求項1に記載の固形製剤。
- 前記コーティング層の外面に、活性成分を含むか、または含まない、もう1層のコーティングを有する、請求項1に記載の固形製剤。
- 錠剤である請求項1に記載の固形製剤。
- 前記コーティング層が1種類の活性薬物を含み、前記コアが別の種類の活性薬物を含む、請求項1に記載の固形製剤。
- 請求項4に記載の固形製剤を、打錠機でプレスすることにより調製する方法であって、
1)錠芯を調製するための各組成成分を混合し、I番パンチで一回目のプレスを行って、錠芯を得る工程と、
2)II番パンチに交換し、コーティング層を調製するための各組成成分を混合した後、中金型に充填する工程と、
3)工程1)でプレスした錠芯を中金型の中央に充填し、二回目のプレスを行って、固形製剤を得る工程と
を含み、
前記I番パンチの直径がII番パンチの直径より小さい、固形製剤の調製方法。 - 前記工程2)と3)を、
II番パンチに交換した後、工程1)でプレスした錠芯を中金型の中央に充填し、その後、中金型の中で錠芯の周囲に、均一に混合されたコーティング層の組成成分を充填して、二回目のプレスを行うことへ変更する、請求項6に記載の調製方法。
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