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RU2008142261A - Фармацевтическая композиция с модифицированным высвобождением и ее применение - Google Patents

Фармацевтическая композиция с модифицированным высвобождением и ее применение Download PDF

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RU2008142261A
RU2008142261A RU2008142261/15A RU2008142261A RU2008142261A RU 2008142261 A RU2008142261 A RU 2008142261A RU 2008142261/15 A RU2008142261/15 A RU 2008142261/15A RU 2008142261 A RU2008142261 A RU 2008142261A RU 2008142261 A RU2008142261 A RU 2008142261A
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Андерс МАГНУССОН (SE)
Андерс МАГНУССОН
Микаэль ТУНЕ (SE)
Микаэль ТУНЕ
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Астразенека Аб (Se)
Астразенека Аб
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    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10—Antioedematous agents; Diuretics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

1. Фармацевтическая композиция с модифицированным высвобождением, содержащая в качестве активного ингредиента соединение формулы (I) ! ! где R1 представляет собой С1-2алкил, замещенный одним или более чем одним заместителем, представляющим собой фтор; ! R2 представляет собой водород, гидрокси, метокси или этокси; и ! n представляет собой 0, 1 или 2; ! и фармацевтически приемлемый разбавитель или носитель; при условии, что эта композиция не содержит йота-каррагинан и нейтральный гелеобразующий полимер. ! 2. Композиция по п.1, где активный ингредиент представляет собой: ! Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-(S)Aze-Pab(OMe); ! Рh(3-Сl)(5-ОСНF2)-(R)СН(ОН)С(O)-(S)Аzе-Раb(2,6-диF)(ОМе) или ! Ph(3-Cl)(5-OCH2CH2F)-(R)CH(OH)C(O)-(S)Aze-Pab(OMe). ! 3. Композиция по п.1 или 2, содержащая гелеобразующую матрицу. !4. Композиция по п.3, где эта матрица содержит ГПМЦ (гидроксипропилметилцеллюлозу). ! 5. Композиция по п.3, где эта матрица содержит содержит ДСН (додецилсульфат натрия). ! 6. Применение композиции по п.1 в изготовлении лекарства для лечения сердечно-сосудистого расстройства.

Claims (6)

1. Фармацевтическая композиция с модифицированным высвобождением, содержащая в качестве активного ингредиента соединение формулы (I)
Figure 00000001
где R1 представляет собой С1-2алкил, замещенный одним или более чем одним заместителем, представляющим собой фтор;
R2 представляет собой водород, гидрокси, метокси или этокси; и
n представляет собой 0, 1 или 2;
и фармацевтически приемлемый разбавитель или носитель; при условии, что эта композиция не содержит йота-каррагинан и нейтральный гелеобразующий полимер.
2. Композиция по п.1, где активный ингредиент представляет собой:
Ph(3-Cl)(5-OCHF2)-(R)CH(OH)C(O)-(S)Aze-Pab(OMe);
Рh(3-Сl)(5-ОСНF2)-(R)СН(ОН)С(O)-(S)Аzе-Раb(2,6-диF)(ОМе) или
Ph(3-Cl)(5-OCH2CH2F)-(R)CH(OH)C(O)-(S)Aze-Pab(OMe).
3. Композиция по п.1 или 2, содержащая гелеобразующую матрицу.
4. Композиция по п.3, где эта матрица содержит ГПМЦ (гидроксипропилметилцеллюлозу).
5. Композиция по п.3, где эта матрица содержит содержит ДСН (додецилсульфат натрия).
6. Применение композиции по п.1 в изготовлении лекарства для лечения сердечно-сосудистого расстройства.
RU2008142261/15A 2002-05-31 2003-05-27 Фармацевтическая композиция с модифицированным высвобождением и ее применение RU2474416C2 (ru)

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SE9802973D0 (sv) * 1998-09-03 1998-09-03 Astra Ab Immediate release tablet
SE9802974D0 (sv) * 1998-09-03 1998-09-03 Astra Ab New crystalline forms
WO2000013710A2 (en) 1998-09-04 2000-03-16 Scios Inc. Hydrogel compositions for the controlled release administration of growth factors
SE9804313D0 (sv) 1998-12-14 1998-12-14 Astra Ab New compounds
CZ20012529A3 (cs) * 1999-01-13 2001-11-14 Astrazeneca Ab Nový amidinobenzylamidový derivát a jeho pouľití jako inhibitoru thrombinu
SE9902550D0 (sv) 1999-07-02 1999-07-02 Astra Ab New crystalline forms
SE0001803D0 (sv) 2000-05-16 2000-05-16 Astrazeneca Ab New compounds i
IL154077A0 (en) 2000-08-16 2003-07-31 Astrazeneca Ab New amidino derivatives and their use as thrombin inhibitors
SE0003125D0 (sv) * 2000-09-05 2000-09-05 Astrazeneca Ab Modified polymers
US7129233B2 (en) * 2000-12-01 2006-10-31 Astrazeneca Ab Mandelic acid derivatives and their use as thrombin inhibitors
AR035216A1 (es) * 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
SE0102921D0 (sv) * 2001-08-30 2001-08-30 Astrazeneca Ab Pharmaceutically useful compounds
AR034517A1 (es) 2001-06-21 2004-02-25 Astrazeneca Ab Formulacion farmaceutica
UA78195C2 (ru) 2001-08-30 2007-03-15 Astrazeneca Ab Производные миндальной кислоты и их применения в качестве ингибиторов тромбина, фармацевтическая композиция на их основе
SE0201658D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab Immediate release pharmaceutical formulation
SE0201661D0 (sv) 2002-05-31 2002-05-31 Astrazeneca Ab New salts

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JP4603353B2 (ja) 2010-12-22
ZA200409234B (en) 2005-07-12
RU2352323C2 (ru) 2009-04-20
CN101264051A (zh) 2008-09-17
TW200403992A (en) 2004-03-16
TWI319317B (en) 2010-01-11
CA2485535C (en) 2011-05-10
KR20050010013A (ko) 2005-01-26
IL165029A0 (en) 2005-12-18
EG24479A (en) 2009-08-03
NZ536621A (en) 2006-10-27
AR039936A1 (es) 2005-03-09
CN100402025C (zh) 2008-07-16
WO2003101424A1 (en) 2003-12-11
CA2485535A1 (en) 2003-12-11
PL374299A1 (en) 2005-10-03
RU2004132856A (ru) 2005-08-10
MXPA04011914A (es) 2005-03-31
US7202236B2 (en) 2007-04-10
JP2005536472A (ja) 2005-12-02
JP2009298795A (ja) 2009-12-24
AU2003232870A1 (en) 2003-12-19
SA03240402B1 (ar) 2008-03-23
TW200913989A (en) 2009-04-01
CN1655761A (zh) 2005-08-17
TWI319318B (en) 2010-01-11
SG165162A1 (en) 2010-10-28
US20050171083A1 (en) 2005-08-04
BR0311460A (pt) 2005-03-29
KR101166921B1 (ko) 2012-07-23
CN101264051B (zh) 2010-12-22
NO20044767L (no) 2005-02-25
EP1513495A1 (en) 2005-03-16
AU2009243524A1 (en) 2009-12-24
RU2474416C2 (ru) 2013-02-10
SE0201659D0 (sv) 2002-05-31
AU2003232870B2 (en) 2009-09-10

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