WO2014142521A1 - 발사르탄 및 로수바스타틴 칼슘을 포함하는 복합 제제 및 이의 제조방법 - Google Patents
발사르탄 및 로수바스타틴 칼슘을 포함하는 복합 제제 및 이의 제조방법 Download PDFInfo
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- WO2014142521A1 WO2014142521A1 PCT/KR2014/002008 KR2014002008W WO2014142521A1 WO 2014142521 A1 WO2014142521 A1 WO 2014142521A1 KR 2014002008 W KR2014002008 W KR 2014002008W WO 2014142521 A1 WO2014142521 A1 WO 2014142521A1
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- WIPO (PCT)
- Prior art keywords
- valsartan
- rosuvastatin
- pharmaceutical composition
- rosuvastatin calcium
- calcium
- Prior art date
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Abstract
Description
Claims (16)
- 발사르탄(valsartan)과 로수바스타틴 칼슘(rosuvastatin calcium)을 활성 성분으로 포함하는 것을 특징으로 하는 심혈관계 질환 및 고지혈증 질환의 예방 또는 치료용 약제학적 조성물.
- 제 1 항에 있어서, 발사르탄과 로수바스타틴 칼슘이 분리된 상태로 존재하는 것을 특징으로 하는 약제학적 조성물.
- 제 2 항에 있어서, 발사르탄 과립에 로수바스타틴 칼슘이 혼합된 상태인 것을 특징으로 하는 약제학적 조성물.
- 제 3 항에 있어서, 발사르탄 과립 및 로수바스타틴 칼슘에 약제학적으로 허용 가능한 첨가제를 추가로 포함하는 것을 특징으로 하는 약제학적 조성물.
- 제 2 항에 있어서, 발사르탄과 로수바스타틴 칼슘이 각각 별개의 층에 존재하는 이층정 형태인 것을 특징으로 하는 약제학적 조성물.
- 제 1 항에 있어서, 로수바스타틴과 발사르탄을 1:2 내지 1:32의 중량비로 포함하는 것을 특징으로 하는 약제학적 조성물.
- 제 6 항에 있어서, 로수바스타틴과 발사르탄을 1:4, 1:8, 1:16 또는 1:32의 중량비로 포함하는 것을 특징으로 하는 약제학적 조성물.
- 제 7 항에 있어서, 약제학적 조성물이 정제이고, 1 정당 로수바스타틴 5 ㎎ + 발사르탄 80 ㎎, 로수바스타틴 5 ㎎ + 발사르탄 160 ㎎, 로수바스타틴 10 ㎎ + 발사르탄 80 ㎎, 로수바스타틴 10 ㎎ + 발사르탄 160 ㎎, 로수바스타틴 20 ㎎ + 발사르탄 80 ㎎, 또는 로수바스타틴 20 ㎎ + 발사르탄 160 ㎎을 포함하는 것을 특징으로 하는 약제학적 조성물.
- 제 1 항에 있어서, 협심증, 고혈압, 고지혈증, 동맥연축, 심부정맥, 심비대, 뇌경색, 울혈심부전 및 심근경색 중에서 선택된 하나 이상의 질환을 예방 또는 치료하기 위한 약제학적 조성물.
- (a) 발사르탄과 약제학적으로 허용 가능한 첨가제의 혼합물을 과립화하는 단계;(b) 로수바스타틴 칼슘과 약제학적으로 허용 가능한 첨가제를 단계 (a)의 발사르탄 과립에 혼합하는 단계를 포함하는, 심혈관계 질환 및 고지혈증 질환의 예방 또는 치료용 약제학적 조성물의 제조방법.
- 제 10 항에 있어서, (a) 단계에서 발사르탄 1 중량부당 약제학적으로 허용 가능한 첨가제 1 내지 3 중량부의 혼합물을 과립화하는 것을 특징으로 하는 제조방법.
- 제 10 항에 있어서, (b) 단계에서 로수바스타틴 칼슘 1 중량부당 약제학적으로 허용 가능한 첨가제 1 내지 10 중량부를 혼합하는 것을 특징으로 하는 제조방법.
- 발사르탄(valsartan)과 로수바스타틴 칼슘(rosuvastatin calcium)을 활성 성분으로 포함하는 것을 특징으로 하는 상승적 효과를 갖는 고혈압 치료용 약제학적 조성물.
- 제 13 항에 있어서, 조성물이 정제이고, 1 정당 발사르탄 160 ㎎ 및 로수바스타틴 20 ㎎을 포함하는 것을 특징으로 하는 조성물.
- 발사르탄(valsartan)과 로수바스타틴 칼슘(rosuvastatin calcium)을 활성 성분으로 포함하는 약제학적 조성물의, 심혈관계 질환 및 고지혈증 질환의 예방 또는 치료를 위한 용도.
- 발사르탄(valsartan)과 로수바스타틴 칼슘(rosuvastatin calcium)을 활성 성분으로 포함하는 약제학적 조성물을 필요로 하는 대상에 투여하는 단계를 포함하는, 심혈관계 질환 및 고지혈증 질환의 예방 또는 치료 방법.
Priority Applications (9)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
MX2015012666A MX2015012666A (es) | 2013-03-12 | 2014-03-11 | Preparacion de complejo que incluye valsartan y rosuvastatina calcica y metodo de fabricacion para el mismo. |
RU2015143218A RU2663460C2 (ru) | 2013-03-12 | 2014-03-11 | Комбинированный препарат, содержащий валсартан и розувастатин кальция и способ его изготовления |
AU2014230304A AU2014230304B2 (en) | 2013-03-12 | 2014-03-11 | Complex preparation including valsartan and rosuvastatin calcium and manufacturing method therefor |
US14/775,422 US20160045497A1 (en) | 2013-03-12 | 2014-03-11 | Complex preparation including valsartan and rosuvastatin calcium and manufacturing method therefor |
JP2015562916A JP2016514125A (ja) | 2013-03-12 | 2014-03-11 | バルサルタン及びロスバスタチンカルシウムを含む複合製剤及びその製造方法 |
BR112015022103A BR112015022103A2 (pt) | 2013-03-12 | 2014-03-11 | composição farmacêutica, método para preparar uma composição farmacêutica, uso de uma composição farmacêutica, e, método para prevenir ou tratar uma doença |
CN201480022809.2A CN105163734A (zh) | 2013-03-12 | 2014-03-11 | 包含缬沙坦及罗舒伐他汀钙的复合制剂及其制造方法 |
CA2903961A CA2903961A1 (en) | 2013-03-12 | 2014-03-11 | Complex preparation including valsartan and rosuvastatin calcium and manufacturing method therefor |
EP14764870.3A EP2977048A4 (en) | 2013-03-12 | 2014-03-11 | Complex preparation including valsartan and rosuvastatin calcium and manufacturing method therefor |
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KR20130026146 | 2013-03-12 | ||
KR10-2013-0026146 | 2013-03-12 |
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US (1) | US20160045497A1 (ko) |
EP (1) | EP2977048A4 (ko) |
JP (1) | JP2016514125A (ko) |
KR (2) | KR20140111982A (ko) |
CN (1) | CN105163734A (ko) |
AU (1) | AU2014230304B2 (ko) |
BR (1) | BR112015022103A2 (ko) |
CA (1) | CA2903961A1 (ko) |
MX (1) | MX2015012666A (ko) |
RU (1) | RU2663460C2 (ko) |
WO (1) | WO2014142521A1 (ko) |
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KR20160095826A (ko) * | 2015-02-04 | 2016-08-12 | 제이더블유중외제약 주식회사 | 피타바스타틴 또는 이의 약학적으로 허용 가능한 염 및 발사르탄 또는 이의 약학적으로 허용 가능한 염을 포함하는 약제학적 조성물 |
EP3320903B1 (en) * | 2015-07-08 | 2021-05-19 | HK inno.N Corporation | Pharmaceutical composition containing amlodipine, valsartan, and rosuvastatin |
Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5399578A (en) | 1990-02-19 | 1995-03-21 | Ciba-Geigy Corp | Acyl compounds |
USRE37314E1 (en) | 1991-07-01 | 2001-08-07 | Shionogi Seiyaku Kabushiki Kaisha | Pyrimidine derivatives |
US6316460B1 (en) | 2000-01-26 | 2001-11-13 | Astrazeneca Ab | Pharmaceutical compositions |
US20040087484A1 (en) * | 2000-12-01 | 2004-05-06 | Sahota Pritam Singh | Combination of organic compounds |
KR20040106591A (ko) * | 1997-08-29 | 2004-12-17 | 화이자 인코포레이티드 | 아토르바스타틴 및 고혈압치료제를 포함하는 복합 처방 |
KR100582347B1 (ko) * | 2004-12-30 | 2006-05-22 | 한미약품 주식회사 | 3-하이드록시-3-메틸글루타릴 조효소 a 환원효소 억제제및 고혈압 치료제의 복합제제 및 그의 제조방법 |
KR20100045344A (ko) * | 2008-10-23 | 2010-05-03 | 한올바이오파마주식회사 | 방출성이 제어된 베타 아드레날린 차단제와 HMG-CoA 환원 효소 억제제의 신규 복합 조성물 |
KR100985254B1 (ko) * | 2006-10-30 | 2010-10-04 | 한올바이오파마주식회사 | 방출성이 제어된 안지오텐신―Ⅱ―수용체 차단제와HMG―CoA 환원 효소 억제제의 복합 조성물 |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US6465502B1 (en) * | 1998-12-23 | 2002-10-15 | Novartis Ag | Additional therapeutic use |
WO2009084040A1 (en) * | 2007-12-28 | 2009-07-09 | Rubicon Research Private Limited | Once a day formulation of angiotensin receptor blockers |
CN101632672B (zh) * | 2008-07-24 | 2011-01-12 | 鲁南制药集团股份有限公司 | 一种用于治疗高血压的复方药物组合物 |
CN101632673B (zh) * | 2008-07-24 | 2011-08-10 | 鲁南制药集团股份有限公司 | 含有氯沙坦、吡格列酮和瑞舒伐他汀的药物组合物及其新用途 |
RU2450823C2 (ru) * | 2009-10-26 | 2012-05-20 | Общество С Ограниченной Ответственностью "Исследовательский Центр "Комкон" | Средство для лечения связанных со стрессовыми условиями заболеваний и расстройств у человека и животных, а также способ лечения и/или профилактики с использованием этого средства |
UY33772A (es) * | 2010-12-09 | 2012-07-31 | Lg Life Sciences Ltd | Composición farmacéutica que comprende clorhidrato de lercanidipina y valsartán como componentes activos y a un método para la preparacion de la misma. |
-
2014
- 2014-03-11 BR BR112015022103A patent/BR112015022103A2/pt active Search and Examination
- 2014-03-11 RU RU2015143218A patent/RU2663460C2/ru active
- 2014-03-11 MX MX2015012666A patent/MX2015012666A/es active IP Right Grant
- 2014-03-11 US US14/775,422 patent/US20160045497A1/en not_active Abandoned
- 2014-03-11 CA CA2903961A patent/CA2903961A1/en not_active Abandoned
- 2014-03-11 JP JP2015562916A patent/JP2016514125A/ja active Pending
- 2014-03-11 EP EP14764870.3A patent/EP2977048A4/en not_active Withdrawn
- 2014-03-11 AU AU2014230304A patent/AU2014230304B2/en active Active
- 2014-03-11 KR KR1020140028375A patent/KR20140111982A/ko active Search and Examination
- 2014-03-11 CN CN201480022809.2A patent/CN105163734A/zh active Pending
- 2014-03-11 WO PCT/KR2014/002008 patent/WO2014142521A1/ko active Application Filing
-
2019
- 2019-09-11 KR KR1020190112921A patent/KR102306005B1/ko active IP Right Grant
Patent Citations (8)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5399578A (en) | 1990-02-19 | 1995-03-21 | Ciba-Geigy Corp | Acyl compounds |
USRE37314E1 (en) | 1991-07-01 | 2001-08-07 | Shionogi Seiyaku Kabushiki Kaisha | Pyrimidine derivatives |
KR20040106591A (ko) * | 1997-08-29 | 2004-12-17 | 화이자 인코포레이티드 | 아토르바스타틴 및 고혈압치료제를 포함하는 복합 처방 |
US6316460B1 (en) | 2000-01-26 | 2001-11-13 | Astrazeneca Ab | Pharmaceutical compositions |
US20040087484A1 (en) * | 2000-12-01 | 2004-05-06 | Sahota Pritam Singh | Combination of organic compounds |
KR100582347B1 (ko) * | 2004-12-30 | 2006-05-22 | 한미약품 주식회사 | 3-하이드록시-3-메틸글루타릴 조효소 a 환원효소 억제제및 고혈압 치료제의 복합제제 및 그의 제조방법 |
KR100985254B1 (ko) * | 2006-10-30 | 2010-10-04 | 한올바이오파마주식회사 | 방출성이 제어된 안지오텐신―Ⅱ―수용체 차단제와HMG―CoA 환원 효소 억제제의 복합 조성물 |
KR20100045344A (ko) * | 2008-10-23 | 2010-05-03 | 한올바이오파마주식회사 | 방출성이 제어된 베타 아드레날린 차단제와 HMG-CoA 환원 효소 억제제의 신규 복합 조성물 |
Non-Patent Citations (1)
Title |
---|
See also references of EP2977048A4 |
Also Published As
Publication number | Publication date |
---|---|
AU2014230304B2 (en) | 2018-07-05 |
RU2663460C2 (ru) | 2018-08-06 |
RU2015143218A (ru) | 2017-04-17 |
CN105163734A (zh) | 2015-12-16 |
KR102306005B1 (ko) | 2021-09-28 |
EP2977048A4 (en) | 2017-04-26 |
JP2016514125A (ja) | 2016-05-19 |
US20160045497A1 (en) | 2016-02-18 |
KR20140111982A (ko) | 2014-09-22 |
CA2903961A1 (en) | 2014-09-18 |
AU2014230304A1 (en) | 2015-10-01 |
KR20190108090A (ko) | 2019-09-23 |
AU2014230304A8 (en) | 2015-10-15 |
BR112015022103A2 (pt) | 2017-07-18 |
MX2015012666A (es) | 2016-02-16 |
EP2977048A1 (en) | 2016-01-27 |
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