CN104736142B - 阿哌沙班液体制剂 - Google Patents

阿哌沙班液体制剂 Download PDF

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Publication number
CN104736142B
CN104736142B CN201380049617.6A CN201380049617A CN104736142B CN 104736142 B CN104736142 B CN 104736142B CN 201380049617 A CN201380049617 A CN 201380049617A CN 104736142 B CN104736142 B CN 104736142B
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CN
China
Prior art keywords
vehicle
apixaban
liquid formulation
content
dose
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.)
Expired - Fee Related
Application number
CN201380049617.6A
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English (en)
Chinese (zh)
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CN104736142A (zh
Inventor
S·I·F·巴达维
S·卢姆
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Pfizer Inc
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Bristol Myers Squibb Co
Pfizer Inc
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Publication of CN104736142A publication Critical patent/CN104736142A/zh
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Publication of CN104736142B publication Critical patent/CN104736142B/zh
Expired - Fee Related legal-status Critical Current
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12—Carboxylic acids; Salts or anhydrides thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/20—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61P7/02—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
    • 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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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Hematology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
CN201380049617.6A 2012-09-26 2013-09-26 阿哌沙班液体制剂 Expired - Fee Related CN104736142B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261705943P 2012-09-26 2012-09-26
US61/705,943 2012-09-26
US201361773032P 2013-03-05 2013-03-05
US61/773,032 2013-03-05
PCT/US2013/062051 WO2014052678A1 (en) 2012-09-26 2013-09-26 Apixaban liquid formulations

Publications (2)

Publication Number Publication Date
CN104736142A CN104736142A (zh) 2015-06-24
CN104736142B true CN104736142B (zh) 2020-03-03

Family

ID=49447800

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201380049617.6A Expired - Fee Related CN104736142B (zh) 2012-09-26 2013-09-26 阿哌沙班液体制剂

Country Status (18)

Country Link
US (2) US9452134B2 (enExample)
EP (1) EP2900217A1 (enExample)
JP (1) JP6248112B2 (enExample)
KR (1) KR102035373B1 (enExample)
CN (1) CN104736142B (enExample)
AU (1) AU2013323435C1 (enExample)
BR (1) BR112015005995A2 (enExample)
CA (1) CA2885899A1 (enExample)
HK (1) HK1212900A1 (enExample)
IL (1) IL237804A0 (enExample)
IN (1) IN2015DN01902A (enExample)
MX (1) MX358097B (enExample)
MY (1) MY179191A (enExample)
NZ (1) NZ630763A (enExample)
PH (1) PH12015500590B1 (enExample)
RU (1) RU2660358C2 (enExample)
SG (2) SG11201501743UA (enExample)
WO (1) WO2014052678A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2907507A1 (en) * 2014-02-17 2015-08-19 Sandoz Ag Pharmaceutical composition comprising apixaban
WO2017221209A1 (en) 2016-06-23 2017-12-28 Lupin Limited Pharmaceutical formulations of apixaban
MX2020010673A (es) * 2018-04-16 2020-10-28 Bristol Myers Squibb Co Formulaciones de apixaban.
WO2020034989A1 (zh) 2018-08-14 2020-02-20 江苏恒瑞医药股份有限公司 一种可注射的药物组合物及其制备方法
KR20220101103A (ko) 2019-11-13 2022-07-19 유니슨 파마슈티컬스 피브이티. 엘티디. 아픽사반의 구강 붕해성 약학적 조성물
CA3202161A1 (en) 2020-12-13 2022-06-16 Matthaios VIDALIS Liquid apixaban formulation in small dose volume
CN113384526A (zh) * 2021-08-03 2021-09-14 合肥医工医药股份有限公司 一种稳定的阿哌沙班口服溶液制剂及其制备方法
NL2029536B1 (en) 2021-10-27 2023-05-26 Pharma Data S A Apixaban suspension and preparation method
AU2022374714B2 (en) 2021-10-27 2024-05-23 Pharma-Data Research And Development Single Member S.A. Apixaban suspension and preparation method
US12194028B2 (en) * 2022-03-09 2025-01-14 Slayback Pharma Llc Stable pharmaceutical compositions of apixaban
WO2023218482A1 (en) * 2022-05-09 2023-11-16 Syri Research Private Limited Liquid oral formulation of apixaban or pharmaceutically acceptable salt thereof
US12213972B2 (en) * 2022-07-27 2025-02-04 Slayback Pharma Llc Stable pharmaceutical compositions of apixaban
US11833138B1 (en) 2023-01-30 2023-12-05 Tap Pharmaceuticals Ag Liquid pharmaceutical formulations of apixaban
EP4658238A1 (en) 2023-01-30 2025-12-10 TAP Pharmaceuticals AG Liquid pharmaceutical formulations of apixaban
US20250319077A1 (en) 2023-04-14 2025-10-16 Novick BioSciences Private Limited Apixaban compositions

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007022165A2 (en) * 2005-08-17 2007-02-22 Bristol-Myers Squibb Company Factor xa inhibitor inclusion complex with cyclodextrin
WO2010147978A1 (en) * 2009-06-16 2010-12-23 Pfizer Inc. Dosage forms of apixaban
WO2011106478A2 (en) * 2010-02-25 2011-09-01 Bristol-Myers Squibb Company Apixaban formulations

Family Cites Families (12)

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Publication number Priority date Publication date Assignee Title
US5763449A (en) * 1996-08-07 1998-06-09 Ascent Pediatrics, Inc. Pleasant-tasting aqueous liquid composition of a bitter-tasting drug
YU43702A (sh) 1999-12-23 2004-11-25 Pfizer Products Inc. Farmaceutske kompozicije koje obezbeđuju povećanje koncentracije leka
MY129350A (en) * 2001-04-25 2007-03-30 Bristol Myers Squibb Co Aripiprazole oral solution
EP1269994A3 (en) 2001-06-22 2003-02-12 Pfizer Products Inc. Pharmaceutical compositions comprising drug and concentration-enhancing polymers
TWI320039B (en) 2001-09-21 2010-02-01 Lactam-containing compounds and derivatives thereof as factor xa inhibitors
AU2002341693B2 (en) * 2001-09-21 2008-05-29 Bristol-Myers Squibb Holdings Ireland Unlimited Company Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
US7101572B2 (en) * 2001-12-07 2006-09-05 Unilab Pharmatech, Ltd. Taste masked aqueous liquid pharmaceutical composition
MX2007010163A (es) * 2005-02-25 2008-02-22 Biomarin Pharm Inc Composicion farmaceutica liquida acuosa estable a temperatura ambiente.
AU2009205314A1 (en) * 2008-01-14 2009-07-23 Foamix Ltd. Poloxamer foamable pharmaceutical compositions with active agents and/or therapeutic cells and uses
PL3100728T3 (pl) * 2009-05-13 2020-05-18 Cydex Pharmaceuticals, Inc. Kompozycje farmaceutyczne zawierające prasugrel i pochodne cyklodekstryny oraz sposoby ich wytwarzania i zastosowania
EP2484775A1 (de) 2011-02-07 2012-08-08 Siemens Healthcare Diagnostics Products GmbH Heparin-insensitives Verfahren zur Bestimmung von direkten Gerinnungsfaktorinhibitoren
RU2638155C1 (ru) * 2016-02-29 2017-12-12 Общество С Ограниченной Ответственностью "Сай Фарма" Производные бензо[d]изоксазола и их применение

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007022165A2 (en) * 2005-08-17 2007-02-22 Bristol-Myers Squibb Company Factor xa inhibitor inclusion complex with cyclodextrin
WO2010147978A1 (en) * 2009-06-16 2010-12-23 Pfizer Inc. Dosage forms of apixaban
WO2011106478A2 (en) * 2010-02-25 2011-09-01 Bristol-Myers Squibb Company Apixaban formulations

Also Published As

Publication number Publication date
CA2885899A1 (en) 2014-04-03
CN104736142A (zh) 2015-06-24
US20160263097A1 (en) 2016-09-15
US20150224053A1 (en) 2015-08-13
SG11201501743UA (en) 2015-04-29
JP6248112B2 (ja) 2017-12-13
MY179191A (en) 2020-10-30
RU2015115127A (ru) 2016-11-20
WO2014052678A1 (en) 2014-04-03
JP2015531377A (ja) 2015-11-02
IN2015DN01902A (enExample) 2015-08-07
BR112015005995A2 (pt) 2017-07-04
AU2013323435B2 (en) 2017-10-19
PH12015500590B1 (en) 2019-08-23
KR102035373B1 (ko) 2019-10-22
AU2013323435A8 (en) 2015-04-23
EP2900217A1 (en) 2015-08-05
KR20150058243A (ko) 2015-05-28
MX358097B (es) 2018-08-06
SG10201702048VA (en) 2017-04-27
HK1212900A1 (zh) 2016-06-24
NZ630763A (en) 2017-01-27
IL237804A0 (en) 2015-05-31
US10016362B2 (en) 2018-07-10
RU2660358C2 (ru) 2018-07-05
AU2013323435C1 (en) 2018-04-12
US9452134B2 (en) 2016-09-27
MX2015003393A (es) 2015-09-25
PH12015500590A1 (en) 2015-05-25
AU2013323435A1 (en) 2014-04-03

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Effective date of registration: 20160720

Address after: Swiss Stein Schoenberg

Applicant after: Bristol-Myers Squibb Co.

Applicant after: PFIZER Inc.

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Applicant before: Pfizer Inc.

CB02 Change of applicant information
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Address after: Swiss Stein Schoenberg

Applicant after: Bristol Myers Squibb Ireland Holdings Ltd.

Applicant after: PFIZER Inc.

Address before: Swiss Stein Schoenberg

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Applicant before: Pfizer Inc.

CB02 Change of applicant information
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Address after: Swiss Stein Schoenberg

Applicant after: Bristol-Squibb Ireland Holdings Ltd.

Applicant after: PFIZER Inc.

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Applicant before: Pfizer Inc.

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Applicant after: Bristol-Squibb Holdings Ireland Infinite

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Granted publication date: 20200303