JP2019504095A - 引湿性が改善されたカルベジロール速放性製剤{Carvedilol immediate release formulation having improved madescent} - Google Patents
引湿性が改善されたカルベジロール速放性製剤{Carvedilol immediate release formulation having improved madescent} Download PDFInfo
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- JP2019504095A JP2019504095A JP2018540450A JP2018540450A JP2019504095A JP 2019504095 A JP2019504095 A JP 2019504095A JP 2018540450 A JP2018540450 A JP 2018540450A JP 2018540450 A JP2018540450 A JP 2018540450A JP 2019504095 A JP2019504095 A JP 2019504095A
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- polyvinyl alcohol
- carvedilol
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- 229960004195 carvedilol Drugs 0.000 title claims abstract description 37
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- 239000012729 immediate-release (IR) formulation Substances 0.000 title claims abstract description 13
- 238000002360 preparation method Methods 0.000 claims abstract description 38
- 239000011247 coating layer Substances 0.000 claims abstract description 31
- 235000014113 dietary fatty acids Nutrition 0.000 claims abstract description 30
- 239000000194 fatty acid Substances 0.000 claims abstract description 30
- 229930195729 fatty acid Natural products 0.000 claims abstract description 30
- -1 fatty acid ester Chemical class 0.000 claims abstract description 19
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- 239000000203 mixture Substances 0.000 claims description 11
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- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical group [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
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- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 description 1
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- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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Abstract
Description
を含む。本発明において、薬剤学的に許容される塩は、患者に対して比較的非毒性でかつ無害な濃度で使用され、この塩の有する副作用が薬効成分の有益な効果を低下させない任意の有機または無機付加塩を示す。
た積層体も適用することができる。
下記表1のような組成により、カルベジロール、粉砕白糖、マンニトール、乳糖水和物、クロスポビドンおよび軽質無水ケイ酸を混合した後、ポビドンを精製水に溶解させて得たポビドン液によって顆粒化した。顆粒化産物を乾燥および整粒した後、クロスポビドン
、軽質無水ケイ酸およびステアリン酸マグネシウムと混合した後に打錠(圧縮)して比較例1〜3の裸錠を製造した。比較例3の裸錠は、さらにヒドロキシプロピルメチルセルロース、酸化チタンおよびポリエチレングリコール400を下記表1の量で含むコーティング分散液でコーティングしてコーティング錠を製造した。
実施例1〜8のコーティング錠は、比較例1と2の裸錠を、下記の表2に示した成分を含むコーティング分散液で、フィルムコーティング率(%)に対応する量でコーティングすることによって製剤した。
実施例1〜8のコーティング錠、比較例1〜2の裸錠および比較例3のコーティング錠を「大韓薬典」の一般試験法中の溶出試験法第2法に従って毎分90回転で溶出試験を行った。試験開始から30分後、紫外吸光光度計を用いて285nm波長でカルベジロールの放出率を算出した。その結果を下記表3に示した。試験液は、pH4.5クエン酸緩衝液1000mLである。
下記の保管条件に応じて包装されていない実施例1〜8のコーティング錠、比較例1〜2の裸錠および比較例3のコーティング錠を保管し、その外観を確認した。
*保管条件:加速保管条件(40±2℃/相対湿度75±5%)
Claims (8)
- カルベジロールを有効成分として含む速放性製剤であって、前記製剤は表面に形成されたコーティング層を含み、前記コーティング層はポリビニルアルコール、ポリビニルアルコール−ポリエチレングリコール共重合体、メタクリル酸−エチルアクリレート共重合体、ワックス、脂肪酸および脂肪酸エステルからなる群より選択される少なくとも1種の成分を含む製剤。
- カルベジロールを有効成分として含む速放性製剤であって、前記製剤は表面に形成されたコーティング層を含み、前記コーティング層はヒドロキシプロピルメチルセルロース、ポリビニルアルコール、ポリビニルアルコール−ポリエチレングリコール共重合体、メタクリル酸−エチルアクリレート共重合体、ワックス、脂肪酸および脂肪酸エステルからなる群より選択される少なくとも2種の異なる成分を含む製剤。
- 前記コーティング層は、ヒドロキシプロピルメチルセルロースおよびポリビニルアルコールの中から選択されるいずれか1つ、並びにポリビニルアルコール−ポリエチレングリコール共重合体、メタクリル酸−エチルアクリレート共重合体、ワックス、脂肪酸および脂肪酸エステルの中から選択されるいずれか1つを含む、請求項2に記載の製剤。
- 前記コーティング層は、ポリビニルアルコールおよび脂肪酸エステル、ポリビニルアルコールおよびポリビニルアルコール−ポリエチレングリコール共重合体、ポリビニルアルコールおよびメタクリル酸−エチルアクリレート共重合体、ヒドロキシプロピルメチルセルロースおよび脂肪酸、またはヒドロキシプロピルメチルセルロースおよびワックスを含む、請求項2に記載の製剤。
- 前記コーティング層は、前記製剤の全体重量に対して1〜10質量%の重量で用いられている、請求項1または請求項2に記載の製剤。
- 希釈剤、崩壊剤、結合剤および滑沢剤からなる群より選択される少なくとも1つの添加剤を含む、請求項1または請求項2に記載の製剤。
- pH4.5クエン酸緩衝液において30分以内にカルベジロールが65%以上放出される、請求項1または請求項2に記載の製剤。
- 引湿性を防止する請求項1〜6のいずれか1つに記載の製剤。
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KR1020160015177A KR102158339B1 (ko) | 2016-02-05 | 2016-02-05 | 인습성이 개선된 카르베딜롤 속방성 제제 |
KR10-2016-0015177 | 2016-02-05 | ||
PCT/KR2017/000811 WO2017135627A1 (en) | 2016-02-05 | 2017-01-24 | Carvedilol immediate release formulation having improved madescent |
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JP2019504095A true JP2019504095A (ja) | 2019-02-14 |
JP6684915B2 JP6684915B2 (ja) | 2020-04-22 |
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US (1) | US20190038564A1 (ja) |
EP (1) | EP3411020A4 (ja) |
JP (1) | JP6684915B2 (ja) |
KR (1) | KR102158339B1 (ja) |
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Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001513752A (ja) * | 1996-09-12 | 2001-09-04 | ロシュ ダイアグノスティクス ゲゼルシャフト ミット ベシュレンクテル ハフツング | 迅速崩壊ペレット |
JP2007512350A (ja) * | 2003-11-25 | 2007-05-17 | エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド | カルベジロール組成物の治療および送達方法 |
JP2008504322A (ja) * | 2004-06-30 | 2008-02-14 | ビーエーエスエフ アクチェンゲゼルシャフト | 粉末形態にあり、凝離傾向がなく、かつポリビニルアルコール−ポリエーテルグラフト共重合体に基づく、特定の物理的安定性及び低い表面粗さを特徴とする急速分散性微粒子フィルムコーティング組成物 |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
IL136028A0 (en) * | 1997-11-12 | 2001-05-20 | Boehringer Mannheim Pharm Corp | Novel oral dosage form for carvedilol |
DE69910188T2 (de) | 1998-04-09 | 2004-06-17 | Roche Diagnostics Gmbh | Arzneiformen enthaltend carvedilol |
US6448323B1 (en) * | 1999-07-09 | 2002-09-10 | Bpsi Holdings, Inc. | Film coatings and film coating compositions based on polyvinyl alcohol |
US20010036959A1 (en) | 2000-04-03 | 2001-11-01 | Gabel Rolf Dieter | Carvedilol-hydrophilic solutions |
IN191028B (ja) | 2001-05-17 | 2003-09-13 | Sun Pharmaceutical Ind Ltd | |
WO2004096182A1 (en) | 2003-04-30 | 2004-11-11 | Ranbaxy Laboratories Limited | Extended release matrix tablets of carvedilol |
EP1691789B1 (en) | 2003-11-25 | 2017-12-20 | SmithKline Beecham (Cork) Limited | Carvedilol free base, salts, anhydrous forms or solvate thereof, corresponding pharmaceutical compositions, controlled release formulations, and treatment or delivery methods |
WO2006044202A2 (en) * | 2004-10-19 | 2006-04-27 | State Of Oregon Acting By And Through The State Board Of Higher Education On Behalf Of Oregon State University | Enteric coated compositions that release active ingredient(s) in gastric fluid and intestinal fluid |
US20080292695A1 (en) * | 2006-12-01 | 2008-11-27 | Kristin Arnold | Carvedilol forms, compositions, and methods of preparation thereof |
EP2167048B1 (en) * | 2007-05-30 | 2016-10-26 | Wockhardt Limited | A novel tablet dosage form |
WO2009110004A1 (en) * | 2008-03-04 | 2009-09-11 | Lupin Limited | Stable pharmaceutical compositions qf carvedilol |
AU2010248060A1 (en) * | 2009-05-12 | 2011-10-27 | Bpsi Holdings, Llc. | Enhanced moisture barrier immediate release film coating systems and substrates coated therewith |
US20110229564A1 (en) * | 2010-03-22 | 2011-09-22 | Amneal Pharmaceuticals, L.L.C. | Pharmaceutical Compositions Of Carvedilol Salts And Process For Preparation Thereof |
KR102241487B1 (ko) | 2013-02-20 | 2021-04-16 | 주식회사 종근당 | 제어방출 펠릿으로 된 약제학적 조성물 |
CA2933202C (en) * | 2014-01-21 | 2022-05-31 | Jason Teckoe | Immediate release film coatings containing medium chain glycerides and substrates coated therewith |
-
2016
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2017
- 2017-01-24 WO PCT/KR2017/000811 patent/WO2017135627A1/en active Application Filing
- 2017-01-24 US US16/075,399 patent/US20190038564A1/en not_active Abandoned
- 2017-01-24 JP JP2018540450A patent/JP6684915B2/ja active Active
- 2017-01-24 EP EP17747672.8A patent/EP3411020A4/en not_active Withdrawn
- 2017-01-24 CN CN201780010145.1A patent/CN108601742A/zh active Pending
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2001513752A (ja) * | 1996-09-12 | 2001-09-04 | ロシュ ダイアグノスティクス ゲゼルシャフト ミット ベシュレンクテル ハフツング | 迅速崩壊ペレット |
JP2007512350A (ja) * | 2003-11-25 | 2007-05-17 | エスビー・ファルムコ・プエルト・リコ・インコーポレイテッド | カルベジロール組成物の治療および送達方法 |
JP2008504322A (ja) * | 2004-06-30 | 2008-02-14 | ビーエーエスエフ アクチェンゲゼルシャフト | 粉末形態にあり、凝離傾向がなく、かつポリビニルアルコール−ポリエーテルグラフト共重合体に基づく、特定の物理的安定性及び低い表面粗さを特徴とする急速分散性微粒子フィルムコーティング組成物 |
Non-Patent Citations (1)
Title |
---|
ASIAN JOURNAL OF PHARMACEUTICAL AND CLINICAL RESEARCH, vol. 2, no. 3, JPN6019026271, 2009, pages 39 - 43, ISSN: 0004071356 * |
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KR102158339B1 (ko) | 2020-09-21 |
CN108601742A (zh) | 2018-09-28 |
WO2017135627A1 (en) | 2017-08-10 |
EP3411020A4 (en) | 2019-10-16 |
KR20170093589A (ko) | 2017-08-16 |
US20190038564A1 (en) | 2019-02-07 |
EP3411020A1 (en) | 2018-12-12 |
JP6684915B2 (ja) | 2020-04-22 |
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