GR20120100008A - A new asymmetric method for the synthesis of rivastigmine hydrogen tartrate, crystal form type ii, its implementation for preparing oral solution for the treatment of dementia and dependences - Google Patents

A new asymmetric method for the synthesis of rivastigmine hydrogen tartrate, crystal form type ii, its implementation for preparing oral solution for the treatment of dementia and dependences

Info

Publication number
GR20120100008A
GR20120100008A GR20120100008A GR20120100008A GR20120100008A GR 20120100008 A GR20120100008 A GR 20120100008A GR 20120100008 A GR20120100008 A GR 20120100008A GR 20120100008 A GR20120100008 A GR 20120100008A GR 20120100008 A GR20120100008 A GR 20120100008A
Authority
GR
Greece
Prior art keywords
treatment
oral solution
crystal form
hydrogen tartrate
dementia
Prior art date
Application number
GR20120100008A
Other languages
Greek (el)
Inventor
Γεωργιος Σπυριδωνος Φαμπιος
Original Assignee
Farmellas Enterprises Limited,
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 Farmellas Enterprises Limited, filed Critical Farmellas Enterprises Limited,
Priority to GR20120100008A priority Critical patent/GR20120100008A/en
Publication of GR20120100008A publication Critical patent/GR20120100008A/en

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
    • A61K31/21—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
    • A61K9/08—Solutions
    • 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
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/40—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings
    • C07C271/42—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/44—Esters of carbamic acids having oxygen atoms of carbamate groups bound to carbon atoms of six-membered aromatic rings with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P13/00—Preparation of nitrogen-containing organic compounds
    • C12P13/02—Amides, e.g. chloramphenicol or polyamides; Imides or polyimides; Urethanes, i.e. compounds comprising N-C=O structural element or polyurethanes

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Microbiology (AREA)
  • Genetics & Genomics (AREA)
  • General Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Emergency Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

This invention brought a new, rapid and convenient method for industrial synthesis of (S)-3-[1-(dimethylamino)ethyl]phenyl-N-ethyl-N-methyl-carbamate hydrogen-(2R, 3R)-tartrate (Rivastigmine Hydrogen Tartrate), crystal form Type II, as well as its use for the manufacture of an oral solution with water clusters, stabilized in 40 mM citrate buffer for the treatment of dementia associated with Alzheimer's and Parkinson's disease and for severe addictions from smoking and drugs. In the present invention presented a stabilized pharmaceutical composition of the oral solution of rivastigmine hydrogen tartrate, stabilized in citric acid / sodium citrate buffer of 40mM capacity with water clusters useful for the treatment of dementia associated with Alzheimer's and Parkinson's disease and for severe addictions from smoking and drugs.
GR20120100008A 2010-12-09 2010-12-09 A new asymmetric method for the synthesis of rivastigmine hydrogen tartrate, crystal form type ii, its implementation for preparing oral solution for the treatment of dementia and dependences GR20120100008A (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
GR20120100008A GR20120100008A (en) 2010-12-09 2010-12-09 A new asymmetric method for the synthesis of rivastigmine hydrogen tartrate, crystal form type ii, its implementation for preparing oral solution for the treatment of dementia and dependences

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GR20120100008A GR20120100008A (en) 2010-12-09 2010-12-09 A new asymmetric method for the synthesis of rivastigmine hydrogen tartrate, crystal form type ii, its implementation for preparing oral solution for the treatment of dementia and dependences

Publications (1)

Publication Number Publication Date
GR20120100008A true GR20120100008A (en) 2012-07-13

Family

ID=46467343

Family Applications (1)

Application Number Title Priority Date Filing Date
GR20120100008A GR20120100008A (en) 2010-12-09 2010-12-09 A new asymmetric method for the synthesis of rivastigmine hydrogen tartrate, crystal form type ii, its implementation for preparing oral solution for the treatment of dementia and dependences

Country Status (1)

Country Link
GR (1) GR20120100008A (en)

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008081041A2 (en) * 2007-01-04 2008-07-10 Krka, Tovarna Zdravil, D.D., Novo Mesto Amorphous and crystalline forms of rivastigmine hydrogentartrate
WO2008110339A2 (en) * 2007-03-09 2008-09-18 Synthon B.V. Polymorphs of rivastigmine hydrogentartrate
WO2010065141A2 (en) * 2008-12-04 2010-06-10 D & Y Laboratories Water clusters, products with water clusters, and methods of producing

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008081041A2 (en) * 2007-01-04 2008-07-10 Krka, Tovarna Zdravil, D.D., Novo Mesto Amorphous and crystalline forms of rivastigmine hydrogentartrate
WO2008110339A2 (en) * 2007-03-09 2008-09-18 Synthon B.V. Polymorphs of rivastigmine hydrogentartrate
WO2010065141A2 (en) * 2008-12-04 2010-06-10 D & Y Laboratories Water clusters, products with water clusters, and methods of producing

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GR20120100008A (en) A new asymmetric method for the synthesis of rivastigmine hydrogen tartrate, crystal form type ii, its implementation for preparing oral solution for the treatment of dementia and dependences