AU2013294917B2 - Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs - Google Patents

Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs Download PDF

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Publication number
AU2013294917B2
AU2013294917B2 AU2013294917A AU2013294917A AU2013294917B2 AU 2013294917 B2 AU2013294917 B2 AU 2013294917B2 AU 2013294917 A AU2013294917 A AU 2013294917A AU 2013294917 A AU2013294917 A AU 2013294917A AU 2013294917 B2 AU2013294917 B2 AU 2013294917B2
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administration
chemical substance
brain
galantamine
salt
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AU2013294917A1 (en
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Alfred Maelicke
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Neurodyn Life Sciences Inc
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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
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/006—Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • 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
    • A61K9/10—Dispersions; Emulsions
    • A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
    • A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
    • 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
    • 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
    • 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
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • 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
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/284—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
    • A61K9/2846—Poly(meth)acrylates
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
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    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/02—Nutrients, e.g. vitamins, minerals
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Dispersion Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Physiology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pulmonology (AREA)
  • Toxicology (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Hematology (AREA)
AU2013294917A 2012-07-27 2013-07-29 Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs Ceased AU2013294917B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261676348P 2012-07-27 2012-07-27
US61/676,348 2012-07-27
EP12178187.6 2012-07-27
EP12178187 2012-07-27
PCT/EP2013/065880 WO2014016430A1 (en) 2012-07-27 2013-07-29 Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs

Publications (2)

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AU2013294917A1 AU2013294917A1 (en) 2015-01-22
AU2013294917B2 true AU2013294917B2 (en) 2016-12-15

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AU2013294917A Ceased AU2013294917B2 (en) 2012-07-27 2013-07-29 Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs

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US (1) US20150190401A1 (enExample)
EP (2) EP3417862B1 (enExample)
JP (2) JP6272857B2 (enExample)
CN (2) CN104507461A (enExample)
AU (1) AU2013294917B2 (enExample)
CA (1) CA2878135C (enExample)
DK (2) DK3417862T3 (enExample)
ES (1) ES2700473T3 (enExample)
HK (1) HK1206242A1 (enExample)
IN (1) IN2015DN00229A (enExample)
PL (2) PL2877165T3 (enExample)
WO (1) WO2014016430A1 (enExample)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090253654A1 (en) 2005-09-22 2009-10-08 Galantos Pharma Gmbh Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment
ES2880399T3 (es) * 2012-07-27 2021-11-24 Neurodyn Life Sciences Inc Biodisponibilidad cerebral mejorada de galantamina mediante formulaciones seleccionadas y administración transmucosa de profármacos lipofílicos
AU2015258814B2 (en) 2014-05-16 2018-04-05 Synaptec Development Llc Clearance of amyloid ss
JP2020033304A (ja) * 2018-08-30 2020-03-05 医療法人ふじいやさか 薬剤又はサプリメント、組成物、及び水素供給器の使用
JP2022538608A (ja) * 2019-06-28 2022-09-05 ザ トラスティーズ オヴ ザ ユニヴァーシティー オヴ ペンシルバニア アルツハイマー病の治療のための鼻腔内ダントロレン投与
EP4029867A1 (en) 2021-01-13 2022-07-20 Alpha Cognition Inc. Solid forms of galantamine benzoate gluconate
WO2022236396A1 (en) * 2021-05-14 2022-11-17 Alpha Cognition Inc. Self-preserving compositions and multi-use dispensers for administering alpha-1062
EP4186509A1 (en) 2021-11-26 2023-05-31 Alpha Cognition Inc. Alpha-1062 for treating traumatic brain injury
US12589099B2 (en) 2021-11-26 2026-03-31 Alpha Cognition Inc. Alpha-1062 for treating traumatic brain injury
CN121443298A (zh) * 2023-05-25 2026-01-30 阿尔法认知公司 用于治疗持续性脑震荡后症状的苯加兰他敏
US12208167B1 (en) * 2024-02-06 2025-01-28 Alpha Cognition Inc. Coated tablets for pH-dependent release of benzgalantamine
US12551491B1 (en) * 2025-07-23 2026-02-17 Alpha Cognition Inc. Dosage regimens for benzgalantamine

Citations (2)

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Publication number Priority date Publication date Assignee Title
US20090253654A1 (en) * 2005-09-22 2009-10-08 Galantos Pharma Gmbh Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment
WO2009127218A1 (en) * 2008-04-14 2009-10-22 Galantos Pharma Gmbh Derivatives of galantamine as pro-drugs for the treatment of human brain diseases

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IT1248059B (it) * 1991-06-14 1995-01-05 Miat Spa Insufflatore multidose per farmaci in polvere
BR0213696A (pt) * 2001-10-31 2004-10-26 Pfizer Prod Inc Agonistas do receptor de acetilcolina nicotìnicos no tratamento da sìndrome de pernas inquietas
US20040254146A1 (en) * 2002-05-21 2004-12-16 Nastech Pharmaceutical Company Inc. Carboxylate salts of galantamine and their pharmaceutical use
DE10338544B4 (de) * 2003-08-19 2017-08-31 Janssen Pharmaceutica N.V. Buccale Formulierungen des Galanthamins und deren Anwendungen
ATE473219T1 (de) * 2005-09-22 2010-07-15 Galantos Pharma Gmbh Cholinerge enhancer mit verbesserter durchgängigkeit durch die blut-hirn-schranke zur behandlung von krankheiten, die mit kognitiven störungen einhergehen
EP2152240A4 (en) * 2007-06-08 2012-05-09 Healthpartners Res Foundation PHARMACEUTICAL COMPOSITIONS AND METHOD FOR REINFORCED TARGETING OF THERAPEUTIC COMPOUNDS TO THE CENTRAL NERVOUS SYSTEM
JP2009197874A (ja) * 2008-02-20 2009-09-03 Works Bell:Kk 動力伝達装置
US20130317117A1 (en) * 2010-11-24 2013-11-28 Pharmaceutics International, Inc. Self micro-emulsifying drug delivery system with increased bioavailability

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
US20090253654A1 (en) * 2005-09-22 2009-10-08 Galantos Pharma Gmbh Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment
WO2009127218A1 (en) * 2008-04-14 2009-10-22 Galantos Pharma Gmbh Derivatives of galantamine as pro-drugs for the treatment of human brain diseases

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
Alfred Maelicke et al, "Memogain is a Galantamine Pro-drug having Dramatically Reduced Adverse Effects and Enhanced Efficacy", J Mol Neurosci, (20090811), vol. 40, doi:doi:10.1007/s12031-009-9269-5, PAGE 135 - 137 *

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DK2877165T3 (da) 2019-01-02
EP3417862B1 (en) 2021-05-05
CA2878135A1 (en) 2014-01-30
JP2018100272A (ja) 2018-06-28
EP2877165A1 (en) 2015-06-03
IN2015DN00229A (enExample) 2015-06-12
JP2015524423A (ja) 2015-08-24
ES2700473T3 (es) 2019-02-18
PL2877165T3 (pl) 2019-05-31
JP6574002B2 (ja) 2019-09-11
US20150190401A1 (en) 2015-07-09
CN104507461A (zh) 2015-04-08
AU2013294917A1 (en) 2015-01-22
CA2878135C (en) 2019-12-03
EP2877165B1 (en) 2018-09-05
PL3417862T3 (pl) 2021-11-22
HK1206242A1 (en) 2016-01-08
CN108245522A (zh) 2018-07-06
DK3417862T3 (da) 2021-07-12
EP3417862A1 (en) 2018-12-26
WO2014016430A1 (en) 2014-01-30
JP6272857B2 (ja) 2018-01-31

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