EP2408431A1 - Rétigabine solide sous forme non cristalline - Google Patents

Rétigabine solide sous forme non cristalline

Info

Publication number
EP2408431A1
EP2408431A1 EP10709698A EP10709698A EP2408431A1 EP 2408431 A1 EP2408431 A1 EP 2408431A1 EP 10709698 A EP10709698 A EP 10709698A EP 10709698 A EP10709698 A EP 10709698A EP 2408431 A1 EP2408431 A1 EP 2408431A1
Authority
EP
European Patent Office
Prior art keywords
retigabine
surface stabilizer
crystalline
solid
intermediate according
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.)
Withdrawn
Application number
EP10709698A
Other languages
German (de)
English (en)
Inventor
Katrin Rimkus
Jana Pätz
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.)
Ratiopharm GmbH
Original Assignee
Ratiopharm GmbH
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
Application filed by Ratiopharm GmbH filed Critical Ratiopharm GmbH
Publication of EP2408431A1 publication Critical patent/EP2408431A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • 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
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • 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
    • A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/167—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface
    • A61K9/1676—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction with an outer layer or coating comprising drug; with chemically bound drugs or non-active substances on their surface having a drug-free core with discrete complete coating layer containing drug
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • A61K9/20—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
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets

Landscapes

  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pain & Pain Management (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Saccharide Compounds (AREA)

Abstract

L'invention porte sur la rétigabine solide sous une forme non-cristalline associée à un stabilisant superficiel, sous la forme d'un intermédiaire stable. Dans l'intermédiaire selon l'invention, la rétigabine se présente de préférence sous forme amorphe ou sous forme d'une solution solide. L'invention concerne en outre un procédé de préparation de rétigabine sous une forme solide non cristalline, et des formulations pharmaceutiques contenant de la rétigabine solide non cristalline.
EP10709698A 2009-03-17 2010-03-17 Rétigabine solide sous forme non cristalline Withdrawn EP2408431A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102009013611A DE102009013611A1 (de) 2009-03-17 2009-03-17 Festes Retigabin in nicht-kristalliner Form
PCT/EP2010/001691 WO2010105823A1 (fr) 2009-03-17 2010-03-17 Rétigabine solide sous forme non cristalline

Publications (1)

Publication Number Publication Date
EP2408431A1 true EP2408431A1 (fr) 2012-01-25

Family

ID=42115481

Family Applications (1)

Application Number Title Priority Date Filing Date
EP10709698A Withdrawn EP2408431A1 (fr) 2009-03-17 2010-03-17 Rétigabine solide sous forme non cristalline

Country Status (6)

Country Link
US (1) US20120053238A1 (fr)
EP (1) EP2408431A1 (fr)
CA (1) CA2760043A1 (fr)
DE (1) DE102009013611A1 (fr)
EA (1) EA201171141A1 (fr)
WO (1) WO2010105823A1 (fr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE102009013613A1 (de) * 2009-03-17 2010-09-23 Ratiopharm Gmbh Trockenverarbeitung von Retigabin
WO2011039369A2 (fr) * 2009-10-02 2011-04-07 Medichem S.A. Formes amorphes d'un dérivé de 2-amino-4-(4-fluorobenzylamino)phénylcarbamate
WO2011101456A2 (fr) * 2010-02-19 2011-08-25 Medichem S.A. Dérivé de phénylcarbamate stabilisé à l'état solide
WO2013008250A2 (fr) * 2011-07-01 2013-01-17 Dr.Reddys Laboratories Limited. Forme cristalline de la rétigabine et procédés de mélange de variétés cristallines de la rétigabine
US20130267590A1 (en) * 2011-09-13 2013-10-10 Dr. Reddy's Laboratories Limited Retigabine compositions
WO2013114379A1 (fr) * 2012-01-30 2013-08-08 Symed Labs Limited Nouveaux polymorphes d'ester éthylique de l'acide carbamique n-[2-amino-4-(4-fluorobenzylamino)-phényl] et procédés associés
WO2014023270A1 (fr) 2012-08-09 2014-02-13 Zentiva, K.S. Sels ou co-cristaux de n-[2-amino-4-[(4-fluorophényl)méthylamino]-phényl]carbamate d'éthyle
CN104188936A (zh) * 2014-08-14 2014-12-10 中美华世通生物医药科技（武汉）有限公司 瑞替加滨微丸胶囊及其制备方法
CN108403652A (zh) * 2018-05-21 2018-08-17 威海贯标信息科技有限公司 一种瑞替加滨片剂组合物
CN111803447B (zh) * 2020-06-22 2022-08-09 三明学院 一种制备无定形药物的方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4200259A1 (de) 1992-01-08 1993-07-15 Asta Medica Ag Neue 1,2,4-triaminobenzol-derivate und verfahren zu deren herstellung
TW486370B (en) * 1996-12-25 2002-05-11 Yamanouchi Pharma Co Ltd Rapidly disintegrable pharmaceutical composition
DE19701694A1 (de) 1997-01-20 1998-07-23 Asta Medica Ag Neue Modifikationen des 2-Amino-4-(4-fluorbenzylamino)-l-ethoxycarbonyl-aminobenzen sowie Verfahren zu ihrer Herstellung
US6117900A (en) 1999-09-27 2000-09-12 Asta Medica Aktiengesellschaft Use of retigabine for the treatment of neuropathic pain
PL202935B1 (pl) 2000-03-08 2009-08-31 Awd Pharma Gmbh & Co Kg Doustny preparat farmaceutyczny o zmiennie nastawianej charakterystyce uwalniania oraz sposób wytwarzania takiego preparatu
AU2002338333A1 (en) 2001-04-04 2002-10-21 Wyeth Methods for treating hyperactive gastric motility
CL2004001884A1 (es) * 2003-08-04 2005-06-03 Pfizer Prod Inc Procedimiento de secado por pulverizacion para la formacion de dispersiones solidas amorfas de un farmaco y polimeros.
US8158152B2 (en) * 2005-11-18 2012-04-17 Scidose Llc Lyophilization process and products obtained thereby
WO2008066900A1 (fr) * 2006-11-28 2008-06-05 Valeant Pharmaceuticals International Analogues de 1,4-diamino rétigabine bicycliques en tant que modulateurs de canaux potassiques
EP2105130A1 (fr) * 2008-03-25 2009-09-30 Ratiopharm GmbH Formule pharmaceutique et son procédé de fabrication
EP2133068A1 (fr) * 2008-06-13 2009-12-16 Ratiopharm GmbH Procédé de sélection d'un consommable secondaire adapté à la fabrication de dispersions fixes pour formules pharmaceutiques
WO2011039369A2 (fr) * 2009-10-02 2011-04-07 Medichem S.A. Formes amorphes d'un dérivé de 2-amino-4-(4-fluorobenzylamino)phénylcarbamate

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO2010105823A1 *

Also Published As

Publication number Publication date
EA201171141A1 (ru) 2012-04-30
DE102009013611A1 (de) 2010-09-23
US20120053238A1 (en) 2012-03-01
WO2010105823A1 (fr) 2010-09-23
CA2760043A1 (fr) 2010-09-23

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