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AR072557A1 - Proceso para preparar composiciones de medicamentos que contienen dabigatran - Google Patents

Proceso para preparar composiciones de medicamentos que contienen dabigatran

Info

Publication number
AR072557A1
AR072557A1 ARP090102638A AR072557A1 AR 072557 A1 AR072557 A1 AR 072557A1 AR P090102638 A ARP090102638 A AR P090102638A AR 072557 A1 AR072557 A1 AR 072557A1
Authority
AR
Argentina
Prior art keywords
dabigatran
suspension
preparing
polymorphic form
talc
Prior art date
Application number
Other languages
English (en)
Inventor
Guido Benhard Edmund Radtke
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40030321&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR072557(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of AR072557A1 publication Critical patent/AR072557A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816Wall or shell material
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/485Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5073Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings
    • A61K9/5078Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals having two or more different coatings optionally including drug-containing subcoatings with drug-free core
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Reivindicacion 1: Un proceso para preparar una suspension 4 de la forma polimorfica 1 de la sal del ácido metanosulfonico del etexilato de dabigatrán de formula 1 caracterizado porque la forma polimorfica 1 de metanosulfonato de etexilato de dabigatrán que se caracteriza por un punto de fusion de Tpf = 180 +- 3°C (determinado por DSC; velocidad de calentamiento: 10°C/min) se suspende junto con talco en una disolucion de hidroxipropilcelulosa en alcohol isopropílico, llevándose a cabo la preparacion de la suspension a una temperatura que no excede 30°C por el proceso de dispersion circulatoria. Reivindicacion 2: El proceso segun la reivindicacion 1 caracterizado porque en primer lugar se disuelve hidroxipropilcelulosa en alcohol isopropílico y después la forma polimorfica 1 de metanosulfonato de etexilato de dabigatrán y talco se suspenden en esta disolucion. Reivindicacion 9: El uso de una suspension 4 segun una de las reivindicaciones 6 a 8 caracterizado porque es como material de partida para preparar bolitas 5 de metanosulfonato de etexilato de dabigatrán.
ARP090102638 2008-07-14 2009-07-13 Proceso para preparar composiciones de medicamentos que contienen dabigatran AR072557A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08160335 2008-07-14

Publications (1)

Publication Number Publication Date
AR072557A1 true AR072557A1 (es) 2010-09-08

Family

ID=40030321

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090102638 AR072557A1 (es) 2008-07-14 2009-07-13 Proceso para preparar composiciones de medicamentos que contienen dabigatran

Country Status (16)

Country Link
US (2) US20110123635A1 (es)
EP (2) EP2296631A1 (es)
JP (1) JP2011527318A (es)
KR (1) KR20110039261A (es)
CN (1) CN102099012A (es)
AR (1) AR072557A1 (es)
AU (1) AU2009272796A1 (es)
BR (1) BRPI0915942A2 (es)
CA (1) CA2730218A1 (es)
CL (1) CL2010001588A1 (es)
IL (1) IL209346A0 (es)
MX (1) MX2011000480A (es)
NZ (1) NZ589746A (es)
RU (1) RU2529798C2 (es)
TW (1) TWI436994B (es)
WO (1) WO2010007016A1 (es)

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DE102005061623A1 (de) 2005-12-21 2007-06-28 Boehringer Ingelheim Pharma Gmbh & Co. Kg Verbessertes Verfahren zur Herstellung von 4-(Benzimidazolylmethylamino)-Benzamidinen und deren Salzen
AU2009228795B2 (en) * 2008-03-28 2014-02-13 Boehringer Ingelheim International Gmbh Process for preparing orally administered dabigatran formulations
NZ588488A (en) 2008-06-16 2012-08-31 Boehringer Ingelheim Int Method for producing an intermediate product of dabigatran etexilate
MX2011004614A (es) 2008-11-11 2011-05-31 Boehringer Ingelheim Int Metodo para tratar o prevenir la trombosis usando etexilato de dabigatran o una sal del mismo con un perfil de seguridad mejorado sobre la terapia con warfarina convencional.
US8399678B2 (en) 2009-11-18 2013-03-19 Boehringer Ingelheim International Gmbh Process for the manufacture of dabigatran etexilate
SI2542224T1 (sl) * 2010-03-01 2014-10-30 Ratiopharm Gmbh Oralni farmacevtski sestavek, ki vsebuje dabigatran eteksilat
EA022969B1 (ru) 2010-07-01 2016-03-31 Крка, Товарна Здравил, Д.Д., Ново Место Пероральные фармацевтические лекарственные формы, содержащие дабигатрана этексилат и его фармацевтически приемлемые соли
EA201400737A1 (ru) * 2011-12-22 2014-12-30 Бёрингер Ингельхайм Интернациональ Гмбх Система доставки на основе множества пеллет с немедленным высвобождением активного вещества
CN104114158A (zh) * 2012-02-21 2014-10-22 埃斯特韦实验室有限公司 达比加群酯的口服药物组合物
WO2014001220A1 (en) 2012-06-25 2014-01-03 Boehringer Ingelheim International Gmbh Method for prevention of stroke
CN103127109B (zh) * 2013-02-05 2014-08-13 南京华威医药科技开发有限公司 含达比加群酯或其盐和水合物的药用组合
CN104224754A (zh) * 2013-06-21 2014-12-24 四川海思科制药有限公司 一种达比加群酯药物组合物及其制备方法
CN105640909B (zh) * 2014-11-14 2019-09-20 正大天晴药业集团股份有限公司 一种含有达比加群酯的药用组合物
CN109125274A (zh) * 2017-06-28 2019-01-04 上海美悦生物科技发展有限公司 注射用苯并咪唑类药用酸组合物及其制备方法和用途
CN110339193B (zh) * 2018-04-04 2022-04-29 上海汉都医药科技有限公司 含达比加群酯的药物组合物及其制备方法
CN111840245B (zh) * 2019-04-28 2023-07-18 成都倍特药业股份有限公司 一种达比加群酯药物组合物及其制备方法
EP3771465A1 (en) 2019-08-01 2021-02-03 Zaklady Farmaceutyczne Polpharma SA Pharmaceutical composition comprising dabigatran etexilate
CN111150714A (zh) * 2020-03-17 2020-05-15 南京嘉晨医药科技有限公司 一种甲磺酸达比加群酯固体药物制剂及其制备方法
WO2023139243A1 (en) 2022-01-21 2023-07-27 Adamed Pharma S.A A process for preparation of tartaric acid cores for dabigatran pellets and the pellets containing dabigatran
GR1010399B (el) * 2022-04-05 2023-02-03 Φαρματεν Α.Β.Ε.Ε., Φαρμακευτικο σκευασμα που περιλαμβανει εναν αντιπηκτικο παραγοντα και μεθοδος παραγωγης αυτου
WO2024217830A1 (en) 2023-03-30 2024-10-24 Adamed Pharma S.A A process for preparation of hard capsules filled with dabigatran pellets

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JP2010505906A (ja) * 2006-10-10 2010-02-25 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 3−[(2−{[4−(ヘキシルオキシカルボニルアミノ−イミノ−メチル)−フェニルアミノ]−メチル}−1−メチル−1h−ベンゾイミダゾール−5−カルボニル)−ピリジン−2−イル−アミノ]−プロピオン酸エチルエステルの生理学的に許容される塩
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CA2716642C (en) 2008-03-28 2017-02-28 Boehringer Ingelheim International Gmbh Method for manufacturing acid pellets
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NZ588488A (en) * 2008-06-16 2012-08-31 Boehringer Ingelheim Int Method for producing an intermediate product of dabigatran etexilate
JP5642670B2 (ja) * 2008-06-16 2014-12-17 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング ダビガトランの合成の中間体の製造方法
EA020194B1 (ru) * 2009-02-02 2014-09-30 Бёрингер Ингельхайм Интернациональ Гмбх Лиофилизированный дабигатран
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Also Published As

Publication number Publication date
WO2010007016A1 (en) 2010-01-21
US20110123635A1 (en) 2011-05-26
CN102099012A (zh) 2011-06-15
AU2009272796A1 (en) 2010-01-21
RU2529798C2 (ru) 2014-09-27
RU2011105056A (ru) 2012-08-20
JP2011527318A (ja) 2011-10-27
CL2010001588A1 (es) 2011-06-17
KR20110039261A (ko) 2011-04-15
US20130251811A1 (en) 2013-09-26
NZ589746A (en) 2012-10-26
TW201006818A (en) 2010-02-16
TWI436994B (zh) 2014-05-11
IL209346A0 (en) 2011-01-31
MX2011000480A (es) 2011-05-02
EP2638897A1 (en) 2013-09-18
EP2296631A1 (en) 2011-03-23
CA2730218A1 (en) 2010-01-21
BRPI0915942A2 (pt) 2019-04-09
US9089488B2 (en) 2015-07-28

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