JP5925607B2 - 有機化合物のガレヌス製剤 - Google Patents
有機化合物のガレヌス製剤 Download PDFInfo
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- JP5925607B2 JP5925607B2 JP2012129230A JP2012129230A JP5925607B2 JP 5925607 B2 JP5925607 B2 JP 5925607B2 JP 2012129230 A JP2012129230 A JP 2012129230A JP 2012129230 A JP2012129230 A JP 2012129230A JP 5925607 B2 JP5925607 B2 JP 5925607B2
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- 235000019793 magnesium trisilicate Nutrition 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000007909 melt granulation Methods 0.000 description 1
- 239000008185 minitablet Substances 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000003960 organic solvent Substances 0.000 description 1
- 230000003204 osmotic effect Effects 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 239000000813 peptide hormone Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 229920003124 powdered cellulose Polymers 0.000 description 1
- 235000019814 powdered cellulose Nutrition 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 239000003488 releasing hormone Substances 0.000 description 1
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- 238000013341 scale-up Methods 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 229940113147 shellac Drugs 0.000 description 1
- 239000004208 shellac Substances 0.000 description 1
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 description 1
- 235000013874 shellac Nutrition 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 229910000030 sodium bicarbonate Inorganic materials 0.000 description 1
- 235000017557 sodium bicarbonate Nutrition 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 229910001415 sodium ion Inorganic materials 0.000 description 1
- 239000008279 sol Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 238000005507 spraying Methods 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 229940071138 stearyl fumarate Drugs 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 150000008163 sugars Chemical class 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 235000010215 titanium dioxide Nutrition 0.000 description 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 229940078499 tricalcium phosphate Drugs 0.000 description 1
- 229910000391 tricalcium phosphate Inorganic materials 0.000 description 1
- 235000019731 tricalcium phosphate Nutrition 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
- 238000009736 wetting Methods 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical class [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 description 1
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Description
アリスキレンおよび添加剤の好ましい量は、さらに説明的実施例に示す。
・該湿式造粒は、造粒中のアリスキレンの嵩容積を減少させる;
・原体品質の変化への影響が最小限である;
・単位投与形態あたり46重量%を超える高薬剤充填を容易に達成し得る;
・十分な硬さ、破砕性への抵抗性、崩壊時間、溶解速度などの錠剤の製剤が可能である;
・原体の固着性および低い流動性を最小限まで減少させる;
・DPの高加圧の製造工程が達成される;
・再現性のあるDP性能をもたらす製剤および方法のスケールアップが達成される;および
・合理的な貯蔵寿命をもたらす十分な安定性が達成される。
1)活性成分と添加剤を混合し、そして該成分を造粒液と共に造粒し;
2)得られた顆粒を乾燥させ;
3)乾燥した顆粒を外相賦形剤と混合し;
4)得られた混合物を圧縮して錠剤核としての経口投与形態を形成させ;そして
5)所望により得られた錠剤核をコーティングしてフィルムコート錠を得る。
上記の通り、本核錠剤を所望によりフィルムコートしてよい。
Claims (15)
- 活性成分としてのアリスキレンまたはその薬学的に許容される塩の治療的有効量を含む固体経口投与形製剤であって、該活性成分が経口投与形製剤の重量に基づいて46重量%以上の量で含まれており、錠剤またはフィルムコート錠の形態であり、そしてa)アリスキレンヘミ−フマル酸塩、増量剤、結合剤および崩壊剤を含む内部相と、b)崩壊剤、増量剤、流動促進剤(glidant)および滑剤(lubricant)を含む外部相を有し、
ここで、
増量剤が微結晶性セルロースであって、その量が20〜32重量%であり;
結合剤がポリビニルピロリドンであって、その量が3〜4重量%であり;
崩壊剤が架橋ポリビニルピロリドンであって、その量が13.5〜16重量%であり;
流動促進剤がコロイド状シリカであって、その量が0.4〜0.6重量%であり;そして
滑剤がステアリン酸マグネシウムであって、その量が0.2〜5重量%である、製剤。 - 活性成分が48重量%以上の量で含まれている、請求項1記載の製剤。
- 活性成分が46から60重量%の範囲の量で含まれている、請求項1記載の製剤。
- 活性成分が46から56重量%の範囲の量で含まれている、請求項1記載の製剤。
- 活性成分が全てアリスキレンヘミ−フマル酸塩から成り、単位投与形態あたり75から600mgの範囲の遊離塩基の量で含まれている、請求項1記載の製剤。
- 活性成分が全てアリスキレンヘミ−フマル酸塩から成り、単位投与形態あたり75から300mgの範囲の遊離塩基の量で含まれている、請求項1記載の製剤。
- アリスキレンヘミ−フマル酸塩が、単位投与形態あたり83、166または332mgの量で含まれている、請求項5記載の製剤。
- 製剤がさらにヒドロキシプロピルメチルセルロース、ポリエチレングリコール、ポリビニルピロリドン、ポリビニルピロリドン−ビニルアセテートコポリマー、ポリビニルアルコールおよび糖から選択されるフィルムコーティング材を含むフィルムコートを有する、請求項1〜7のいずれか記載の製剤。
- フィルムコーティング材がヒドロキシプロピルメチルセルロースである、請求項8記載の製剤。
- フィルムコートがさらに色素、染料、二酸化チタン、酸化鉄、タルクおよびポリエチレングリコール3350、4000、6000および8000から選択される添加剤を含む、請求項8または9記載の製剤。
- フィルムコートがヒドロキシプロピルメチルセルロース、酸化鉄色素、二酸化チタン、ポリエチレングリコールおよびタルクを含む、請求項8記載の製剤。
- 高血圧、鬱血性心不全、狭心症、心筋梗塞、アテローム性動脈硬化症、糖尿病性腎症、糖尿病性心筋症(diabetic cardiac myopathy)、腎不全、末梢血管疾患、左室肥大、認知障害、卒中、頭痛および慢性心不全の処置用の、請求項1〜11のいずれか記載の製剤。
- 高血圧、鬱血性心不全、狭心症、心筋梗塞、アテローム性動脈硬化症、糖尿病性腎症、糖尿病性心筋症、腎不全、末梢血管疾患、左室肥大、認知障害、卒中、頭痛および慢性心不全の処置用医薬の製造のための、請求項1〜12のいずれか記載の製剤の使用。
- 請求項1〜12のいずれか記載の製剤の製造法であって:
1)活性成分と内部相賦形剤を混合し、そして該成分を造粒液と共に造粒し;
2)得られた顆粒を乾燥させ;
3)乾燥した顆粒を外部相賦形剤と混合し;そして
4)得られた混合物を圧縮して錠剤核としての経口投与形態を形成させる
ことを含む、方法。 - さらに得られた錠剤核をコーティングしてフィルムコート錠を得る工程を含む、請求項
14記載の方法。
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DE60331849D1 (de) * | 2002-11-05 | 2010-05-06 | Glaxosmithkline Llc | Antibakterielle wirkstoffe |
US20070191487A1 (en) * | 2004-03-17 | 2007-08-16 | Rigassi-Dietrich Petra G | Galenic formulations of organic compounds |
TW200804241A (en) * | 2006-02-24 | 2008-01-16 | Novartis Ag | New salt |
GB0605688D0 (en) | 2006-03-21 | 2006-05-03 | Novartis Ag | Organic compounds |
NZ571251A (en) * | 2006-04-03 | 2011-12-22 | Novartis Ag | Renin inhibitors such as aliskiren for the treatment of rebound hypertension |
GB0612540D0 (en) | 2006-06-23 | 2006-08-02 | Novartis Ag | Galenical formulations of organic compounds |
EP1891937A1 (en) * | 2006-08-25 | 2008-02-27 | Novartis AG | Galenic formulations of aliskiren |
CA2563690C (en) * | 2006-10-12 | 2014-10-07 | Pharmascience Inc. | Pharmaceutical compositions comprising intra- and extra- granular fractions |
US8119841B2 (en) * | 2006-11-07 | 2012-02-21 | Novartis Ag | Crystalline forms of aliskiren hemifumarate |
US20100130616A1 (en) * | 2006-11-09 | 2010-05-27 | Novartis Ag | Salt of aliskiren with orotic acid |
WO2008098992A1 (en) * | 2007-02-16 | 2008-08-21 | Novartis Ag | Use of organic compounds |
EP1972335A1 (en) * | 2007-03-23 | 2008-09-24 | Krka | Solid dosage forms comprising aliskiren and pharmaceutically acceptable salts thereof |
US20090082458A1 (en) * | 2007-09-26 | 2009-03-26 | Protia, Llc | Deuterium-enriched aliskiren |
AU2008309058B2 (en) * | 2007-09-28 | 2012-08-09 | Novartis Ag | Galenical formulations of Aliskiren and Valsartan |
MY148266A (en) * | 2007-09-28 | 2013-03-29 | Novartis Ag | Galenical formulations of aliskiren |
MX2010003439A (es) * | 2007-09-28 | 2010-04-21 | Novartis Ag | Combinacion farmaceutica de aliskiren y valsartan. |
JP2011503185A (ja) | 2007-11-13 | 2011-01-27 | テバ ファーマシューティカル インダストリーズ リミティド | ヘミフマル酸アリスキレンの多形形態及びその調製プロセス |
EP2062874B1 (en) | 2007-11-20 | 2014-12-17 | KRKA, tovarna zdravil, d.d., Novo mesto | Process and intermediates for the preparation of aliskiren |
JP2011522829A (ja) * | 2008-06-06 | 2011-08-04 | テバ ファーマシューティカル インダストリーズ リミティド | 固体状のアリスキレン遊離塩基 |
EP2143425A1 (de) * | 2008-07-11 | 2010-01-13 | Ratiopharm GmbH | Direktverpresste Aliskiren-Tabletten |
US20100093603A1 (en) * | 2008-07-17 | 2010-04-15 | Kenneth Baker | Use of organic compounds |
JO3239B1 (ar) * | 2008-09-22 | 2018-03-08 | Novartis Ag | تركيبات جالينية من مركبات عضوية |
US9026212B2 (en) | 2008-09-23 | 2015-05-05 | Incube Labs, Llc | Energy harvesting mechanism for medical devices |
AR073651A1 (es) * | 2008-09-24 | 2010-11-24 | Novartis Ag | Formulaciones galenicas de compuestos organicos |
SI2189442T1 (sl) | 2008-11-20 | 2015-03-31 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Postopek in intermediati za pripravo aliskirena |
CN102300558A (zh) * | 2009-01-28 | 2011-12-28 | 诺瓦提斯公司 | 有机化合物的盖伦制剂 |
EP2340820A1 (en) | 2009-12-16 | 2011-07-06 | KRKA, tovarna zdravil, d.d., Novo mesto | Moisture-activated granulation process |
WO2010089105A2 (en) | 2009-02-05 | 2010-08-12 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Moisture-activated granulation process |
EP2216020A1 (en) | 2009-02-05 | 2010-08-11 | KRKA, tovarna zdravil, d.d., Novo mesto | Moisture-activated granulation process |
AR075880A1 (es) | 2009-03-20 | 2011-05-04 | Novartis Ag | Formulaciones galenicas de compuestos organicos que comprenden alisquireno y valsartan. uso. metodo. |
KR20110129482A (ko) | 2009-03-20 | 2011-12-01 | 노파르티스 아게 | 알리스키렌을 포함하는 제약 조성물 |
JP2010280601A (ja) * | 2009-06-04 | 2010-12-16 | Suntory Holdings Ltd | キシロオリゴ糖高含有錠剤 |
WO2011028919A2 (en) | 2009-09-03 | 2011-03-10 | Teva Pharmaceutical Industries Ltd. | Solid forms of aliskiren hemifumarate and processes for preparation thereof |
EP2382967A1 (de) | 2010-04-21 | 2011-11-02 | ratiopharm GmbH | Aliskiren in Form einer festen Dispersion |
US20110268797A1 (en) | 2010-04-30 | 2011-11-03 | Sanovel IIac Sanayi Ve Ticaret Anonim Sirketi | Multicoated aliskiren formulations |
US20130129791A1 (en) * | 2010-05-04 | 2013-05-23 | Mahmut Bilgic | Preparations of effervescent formulations comprising second and third generation cephalosporin and uses thereof |
ES2821528T3 (es) | 2012-11-14 | 2021-04-26 | Grace W R & Co | Composiciones que contienen un material biológicamente activo y un óxido inorgánico no ordenado |
CN103099793B (zh) * | 2013-02-06 | 2015-07-15 | 中国人民解放军第二军医大学 | 片剂及其制备方法 |
CN103536576B (zh) * | 2013-10-15 | 2015-07-01 | 海南卫康制药(潜山)有限公司 | 阿利吉仑组合物胶囊 |
RU2545833C1 (ru) * | 2013-12-03 | 2015-04-10 | Государственное бюджетное образовательное учреждение высшего профессионального образования "Санкт-Петербургская государственная химико-фармацевтическая академия" Министерства здравоохранения Российской Федерации (ГБОУ ВПО СПХФА Минздрава России) | Фармацевтическая композиция с антиишемической и антиоксидантной активностью и способ ее получения |
CA2937365C (en) | 2016-03-29 | 2018-09-18 | F. Hoffmann-La Roche Ag | Granulate formulation of 5-methyl-1-phenyl-2-(1h)-pyridone and method of making the same |
Family Cites Families (15)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US3039922A (en) * | 1959-08-17 | 1962-06-19 | Carter Prod Inc | Method of administering tablets having decongestant and anti-histaminic activity |
MY119161A (en) * | 1994-04-18 | 2005-04-30 | Novartis Ag | Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities |
DE19820801A1 (de) * | 1998-05-09 | 1999-11-25 | Gruenenthal Gmbh | Orale Arzneiformen mit reproduzierbarer Wirkstofffreisetzung von Gatifloxacin oder pharmazeutisch verwendbaren Salzen oder Hydraten |
ATE404178T1 (de) * | 1999-02-10 | 2008-08-15 | Pfizer Prod Inc | Vorrichtung mit matrixgesteuerter wirkstofffreisetzung |
US6264983B1 (en) * | 1999-09-16 | 2001-07-24 | Rhodia, Inc. | Directly compressible, ultra fine acetaminophen compositions and process for producing same |
CA2420055C (en) | 2000-08-25 | 2010-06-01 | Takeda Chemical Industries, Ltd. | Fibrinogen-lowering agent |
US8168616B1 (en) | 2000-11-17 | 2012-05-01 | Novartis Ag | Combination comprising a renin inhibitor and an angiotensin receptor inhibitor for hypertension |
US7316819B2 (en) * | 2001-03-08 | 2008-01-08 | Unigene Laboratories, Inc. | Oral peptide pharmaceutical dosage form and method of production |
EP1250921A1 (en) * | 2001-04-21 | 2002-10-23 | BOEHRINGER INGELHEIM INTERNATIONAL GmbH | Fast disintegrating meloxicam tablet |
JP2003015880A (ja) * | 2001-06-29 | 2003-01-17 | Toshiba Corp | 携帯情報端末およびアドインプログラム起動方法 |
JP2005509631A (ja) | 2001-10-18 | 2005-04-14 | ノバルティス アクチエンゲゼルシャフト | At1−レセプターアンタゴニストと心臓血管薬から形成される塩 |
US20030114389A1 (en) * | 2001-11-13 | 2003-06-19 | Webb Randy Lee | Combination of organic compounds |
US20050182042A1 (en) * | 2002-05-17 | 2005-08-18 | Feldman David L. | Pharmaceutical composition comprising a renin inhibitor, a calcium channel blocker and a diuretic |
US20050147629A1 (en) * | 2002-06-28 | 2005-07-07 | Jutta Riedl | Pharmaceutical formulation comprising non-peptide renin inhibitor and surfactant |
US20040002520A1 (en) * | 2002-07-01 | 2004-01-01 | Soderlund Patrick L. | Composition and method for cessation of Nicotine cravings |
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