JP2009534441A - ピリジルメチルスルフィニルベンズイミダゾールのための経口速放医薬製剤 - Google Patents
ピリジルメチルスルフィニルベンズイミダゾールのための経口速放医薬製剤 Download PDFInfo
- Publication number
- JP2009534441A JP2009534441A JP2009507049A JP2009507049A JP2009534441A JP 2009534441 A JP2009534441 A JP 2009534441A JP 2009507049 A JP2009507049 A JP 2009507049A JP 2009507049 A JP2009507049 A JP 2009507049A JP 2009534441 A JP2009534441 A JP 2009534441A
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- composition according
- esomeprazole
- carrageenan
- pyridylmethylsulfinylbenzimidazole
- 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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- HBDKFZNDMVLSHM-UHFFFAOYSA-N 2-(pyridin-2-ylmethylsulfinyl)-1h-benzimidazole Chemical compound N=1C2=CC=CC=C2NC=1S(=O)CC1=CC=CC=N1 HBDKFZNDMVLSHM-UHFFFAOYSA-N 0.000 title claims abstract description 20
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 24
- 239000012729 immediate-release (IR) formulation Substances 0.000 title 1
- 239000000679 carrageenan Chemical class 0.000 claims abstract description 29
- 235000010418 carrageenan Nutrition 0.000 claims abstract description 29
- 229920001525 carrageenan Chemical class 0.000 claims abstract description 29
- 229940113118 carrageenan Drugs 0.000 claims abstract description 29
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical class [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 claims abstract description 29
- 239000008188 pellet Substances 0.000 claims abstract description 25
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- 239000000546 pharmaceutical excipient Substances 0.000 claims abstract description 18
- 229960004770 esomeprazole Drugs 0.000 claims abstract description 17
- SUBDBMMJDZJVOS-DEOSSOPVSA-N esomeprazole Chemical compound C([S@](=O)C1=NC2=CC=C(C=C2N1)OC)C1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-DEOSSOPVSA-N 0.000 claims abstract description 17
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- SUBDBMMJDZJVOS-UHFFFAOYSA-N 5-methoxy-2-{[(4-methoxy-3,5-dimethylpyridin-2-yl)methyl]sulfinyl}-1H-benzimidazole Chemical compound N=1C2=CC(OC)=CC=C2NC=1S(=O)CC1=NC=C(C)C(OC)=C1C SUBDBMMJDZJVOS-UHFFFAOYSA-N 0.000 claims description 6
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- MQEUGMWHWPYFDD-JIDHJSLPSA-N magnesium;6-methoxy-2-[(s)-(4-methoxy-3,5-dimethylpyridin-2-yl)methylsulfinyl]-1h-benzimidazole Chemical group [Mg].C([S@](=O)C1=NC2=CC=C(C=C2N1)OC)C1=NC=C(C)C(OC)=C1C MQEUGMWHWPYFDD-JIDHJSLPSA-N 0.000 claims description 5
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- 239000004480 active ingredient Substances 0.000 abstract description 24
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- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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Abstract
Description
実施例1ならびに比較例AおよびBにより製造したペレットを、それぞれパドル法によりpH8.6、100rpmおよび37±0.5℃で撹拌し、所定の時間後に、300nmの分光光度計で吸光度を測定し(Perkin Elmer Lambda 15)、参照溶液と比較することにより、溶解した活性成分の量を決定する。
製造例4:エソメプラゾールマグネシウム二水和物を、以下に示す量のリン酸二カルシウム、カラギーナンおよびステアリン酸マグネシウムと、Colette社のミキサー中、10分間混合する。混合物を、Korsch社の、ディスク径2.5mmの同心打錠装置(concentric tabletting apparatus)でミニ錠にプレスする。実施例5〜8のミニ錠を、同様に製造する。
実施例4〜8および比較例C〜Eにより製造したミニ錠を、それぞれパドル法によりpH8.6、100rpmおよび37±0.5℃で撹拌し、所定の時間後に、300nmの分光吸光度を測定し(Perkin Elmer Lambda 15)、参照溶液と比較することにより、溶解した活性成分の量を決定する。
Claims (17)
- 場合により置換された2−(ピリジルメチルスルフィニル)−1H−ベンズイミダゾールおよびカラギーナンを含む固体経口投与形態の医薬組成物。
- ピリジルメチルスルフィニルベンズイミダゾールが、オメプラゾール、エソメプラゾール、パントプラゾール、ランソプラゾールまたはラベプラゾールであることを特徴とする、請求項1記載の医薬組成物。
- ピリジルメチルスルフィニルベンズイミダゾールが、エソメプラゾールであることを特徴とする、請求項1記載の医薬組成物。
- ピリジルメチルスルフィニルベンズイミダゾールが、非晶質形態のエソメプラゾールであることを特徴とする、請求項1記載の医薬組成物。
- ピリジルメチルスルフィニルベンズイミダゾールが、エソメプラゾールマグネシウム塩二水和物であることを特徴とする、請求項1記載の医薬組成物。
- ピリジルメチルスルフィニルベンズイミダゾールが、エソメプラゾールマグネシウム塩三水和物であることを特徴とする、請求項1記載の医薬組成物。
- 固体経口投与形態が、ペレット、錠剤、ミニ錠、またはカプセルであることを特徴とする、請求項1〜6のいずれか1項記載の医薬組成物。
- 固体経口投与形態が、ペレットであることを特徴とする、請求項7記載の医薬組成物。
- 固体経口投与形態が、ミニ錠であることを特徴とする、請求項7記載の医薬組成物。
- 1種以上の賦形剤を更に含有することを特徴とする、請求項1〜9のいずれか1項記載の医薬組成物。
- 賦形剤として、6.0を超えるpH値の緩衝混合物を含むことを特徴とする、請求項1〜10のいずれか1項記載の医薬組成物。
- エソメプラゾール10〜40%およびカラギーナン5〜50%を含む、請求項3〜11のいずれか1項記載の医薬組成物。
- エソメプラゾール25〜35%およびカラギーナン9〜20%を含む、請求項3〜12のいずれか1項記載の医薬組成物。
- 5以上のpH値のみで溶解するポリマーでコートされていることを特徴とする、請求項1〜13のいずれか1項記載の医薬組成物。
- 請求項1〜13のいずれか1項記載のペレットまたはミニ錠を含む、5以上のpH値のみで溶解するポリマーでコートされている、カプセルまたは錠剤の形態の医薬組成物。
- 5以上のpH値のみで溶解するポリマー層の下に、安定化中間層を含むことを特徴とする、請求項14または15記載の医薬組成物。
- 抗潰瘍剤として、そしてホ乳類、特にヒトの胃酸の過剰産生に関与する疾患の予防および処置のために使用される、請求項1〜16のいずれか1項記載の医薬組成物。
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
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CH00673/06A CH698658B1 (de) | 2006-04-24 | 2006-04-24 | Orale pharmazeutische Formulierung mit schneller Freisetzung für Pyridylmethylsulfinyl-Benzimidazole. |
CH00673/06 | 2006-04-24 | ||
PCT/EP2007/053942 WO2007122212A1 (en) | 2006-04-24 | 2007-04-23 | Oral rapid release pharmaceutical formulation for pyridylmethylsulfinyl-benzimidazoles |
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JP2009534441A true JP2009534441A (ja) | 2009-09-24 |
JP5211040B2 JP5211040B2 (ja) | 2013-06-12 |
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JP2009507049A Expired - Fee Related JP5211040B2 (ja) | 2006-04-24 | 2007-04-23 | ピリジルメチルスルフィニルベンズイミダゾールのための経口速放医薬製剤 |
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US (1) | US20090068261A1 (ja) |
EP (1) | EP2012754B1 (ja) |
JP (1) | JP5211040B2 (ja) |
CA (1) | CA2648538C (ja) |
CH (1) | CH698658B1 (ja) |
ES (1) | ES2424865T3 (ja) |
PT (1) | PT2012754E (ja) |
WO (1) | WO2007122212A1 (ja) |
Cited By (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20190091879A (ko) * | 2018-01-29 | 2019-08-07 | 주식회사 종근당 | 에스오메프라졸 및 탄산수소나트륨을 포함하는 안정한 약제학적 조성물 |
US11759428B2 (en) | 2018-01-29 | 2023-09-19 | Chong Kun Dang Pharmaceutical Corp. | Pharmaceutical formulation comprising esomeprazole and sodium bicarbonate |
Families Citing this family (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN102666403A (zh) * | 2009-11-19 | 2012-09-12 | 日本曹达株式会社 | 压载水的还原处理方法 |
US20130064891A1 (en) * | 2010-05-21 | 2013-03-14 | Ashok Sahoo | Pharmaceutical compositions of nsaid and acid inhibitor |
WO2017145146A1 (en) | 2016-02-25 | 2017-08-31 | Dexcel Pharma Technologies Ltd. | Compositions comprising proton pump inhibitors |
US10076494B2 (en) | 2016-06-16 | 2018-09-18 | Dexcel Pharma Technologies Ltd. | Stable orally disintegrating pharmaceutical compositions |
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JP2004521955A (ja) * | 2001-07-09 | 2004-07-22 | キュレーターズ・オブ・ザ・ユニバーシティ・オブ・ミズーリ | 新規置換ベンズイミダゾール製剤およびその使用方法 |
JP2004522796A (ja) * | 2001-03-09 | 2004-07-29 | アストラゼネカ・アクチエボラーグ | H+,k+−atpアーゼ阻害剤を含む微粒子の製造方法 |
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US5777102A (en) * | 1993-04-06 | 1998-07-07 | Grindsted Products A/S (Danisco) | Carrageenan-containing product and a method of producing same |
SE9301489D0 (sv) * | 1993-04-30 | 1993-04-30 | Ab Astra | Veterinary composition |
US6228400B1 (en) * | 1999-09-28 | 2001-05-08 | Carlsbad Technology, Inc. | Orally administered pharmaceutical formulations of benzimidazole derivatives and the method of preparing the same |
SI1341524T1 (sl) * | 2000-12-07 | 2012-02-29 | Nycomed Gmbh | Farmacevtski pripravek v obliki paste, ki obsega kislinsko labilno učinkovino |
EP1402900A1 (en) * | 2001-06-11 | 2004-03-31 | Takeda Chemical Industries, Ltd. | Medicinal compositions |
US20030175360A1 (en) * | 2002-02-22 | 2003-09-18 | Renzo Luzzatti | Symptomatic relief of gastrointestinal disorders |
WO2004002982A2 (en) * | 2002-06-27 | 2004-01-08 | Dr. Reddy's Laboratories Limited | A process for preparation of optically pure or optically enriched sulfoxide compounds, including amorphous esomeprazole and salts thereof |
WO2005004921A1 (en) * | 2003-07-11 | 2005-01-20 | Astrazeneca Ab | Solid composition comprising a proton pump inhibitor |
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2006
- 2006-04-24 CH CH00673/06A patent/CH698658B1/de not_active IP Right Cessation
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2007
- 2007-04-23 CA CA2648538A patent/CA2648538C/en not_active Expired - Fee Related
- 2007-04-23 JP JP2009507049A patent/JP5211040B2/ja not_active Expired - Fee Related
- 2007-04-23 PT PT77283992T patent/PT2012754E/pt unknown
- 2007-04-23 ES ES07728399T patent/ES2424865T3/es active Active
- 2007-04-23 US US12/298,083 patent/US20090068261A1/en not_active Abandoned
- 2007-04-23 EP EP07728399.2A patent/EP2012754B1/en active Active
- 2007-04-23 WO PCT/EP2007/053942 patent/WO2007122212A1/en active Application Filing
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JP2004522796A (ja) * | 2001-03-09 | 2004-07-29 | アストラゼネカ・アクチエボラーグ | H+,k+−atpアーゼ阻害剤を含む微粒子の製造方法 |
JP2004521955A (ja) * | 2001-07-09 | 2004-07-22 | キュレーターズ・オブ・ザ・ユニバーシティ・オブ・ミズーリ | 新規置換ベンズイミダゾール製剤およびその使用方法 |
Cited By (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
KR20190091879A (ko) * | 2018-01-29 | 2019-08-07 | 주식회사 종근당 | 에스오메프라졸 및 탄산수소나트륨을 포함하는 안정한 약제학적 조성물 |
KR102080023B1 (ko) | 2018-01-29 | 2020-02-21 | 주식회사 종근당 | 에스오메프라졸 및 탄산수소나트륨을 포함하는 안정한 약제학적 조성물 |
JP2021512081A (ja) * | 2018-01-29 | 2021-05-13 | チョン クン ダン ファーマシューティカル コーポレイション | エソメプラゾール及び炭酸水素ナトリウムを含む安定な薬剤学的組成物 |
JP7003279B2 (ja) | 2018-01-29 | 2022-01-20 | チョン クン ダン ファーマシューティカル コーポレイション | エソメプラゾール及び炭酸水素ナトリウムを含む安定な薬剤学的組成物 |
US11759428B2 (en) | 2018-01-29 | 2023-09-19 | Chong Kun Dang Pharmaceutical Corp. | Pharmaceutical formulation comprising esomeprazole and sodium bicarbonate |
US11813285B2 (en) | 2018-01-29 | 2023-11-14 | Chong Kun Dang Pharmaceutical Corp. | Stable pharmaceutical composition comprising esomeprazole and sodium bicarbonate |
Also Published As
Publication number | Publication date |
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CA2648538A1 (en) | 2007-11-01 |
EP2012754A1 (en) | 2009-01-14 |
CA2648538C (en) | 2014-12-09 |
WO2007122212A1 (en) | 2007-11-01 |
JP5211040B2 (ja) | 2013-06-12 |
CH698658B1 (de) | 2009-09-30 |
US20090068261A1 (en) | 2009-03-12 |
PT2012754E (pt) | 2013-09-05 |
EP2012754B1 (en) | 2013-06-05 |
ES2424865T3 (es) | 2013-10-09 |
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