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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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
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    • 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
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    • A—HUMAN NECESSITIES
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    • 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
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    • 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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    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
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    • 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]
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
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    • 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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  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Neurosurgery (AREA)
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AU2013294917A 2012-07-27 2013-07-29 Enhanced brain bioavailability of galantamine by selected formulations and transmucosal administration of lipophilic prodrugs Active AU2013294917B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261676348P 2012-07-27 2012-07-27
EP12178187 2012-07-27
US61/676,348 2012-07-27
EP12178187.6 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

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

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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) DK2877165T3 (enExample)
ES (1) ES2700473T3 (enExample)
HK (1) HK1206242A1 (enExample)
IN (1) IN2015DN00229A (enExample)
PL (2) PL3417862T3 (enExample)
WO (1) WO2014016430A1 (enExample)

Families Citing this family (11)

* 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
PT3417862T (pt) * 2012-07-27 2021-08-06 Neurodyn Life Sciences Inc Biodisponibilidade cerebral da galantamina melhorada através de formulações selecionadas e administração transmucosal de pró-fármacos lipofílicos
US11219627B2 (en) 2014-05-16 2022-01-11 Synaptec Development Llc Clearance of amyloid beta
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
CN114828848A (zh) * 2019-06-28 2022-07-29 宾夕法尼亚大学理事会 用于治疗阿尔茨海默氏病的鼻内丹曲林施用
EP4029867A1 (en) * 2021-01-13 2022-07-20 Alpha Cognition Inc. Solid forms of galantamine benzoate gluconate
AU2021445637A1 (en) * 2021-05-14 2023-11-23 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
EP4436575A4 (en) * 2021-11-26 2025-11-19 Alpha Cognition Inc ALPHA-1062 INTENDED FOR THE TREATMENT OF TRAUMATIC BRAIN INJURY
WO2024239120A1 (en) * 2023-05-25 2024-11-28 Alpha Cognition Inc. Benzgalantamine for treating persistent post-concussion symptoms
US12208167B1 (en) * 2024-02-06 2025-01-28 Alpha Cognition Inc. Coated tablets for pH-dependent release of 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
SK1912004A3 (en) * 2001-10-31 2004-09-08 Pfizer Prod Inc Nicotinic acetylcholine receptor agonists in the treatment of restless legs syndrome
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
JP2009508903A (ja) * 2005-09-22 2009-03-05 ガラントス ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング 認知障害を伴う疾患の治療に用いるための脳血液関門透過性が改善されたコリン作用増強剤
US9808509B2 (en) * 2007-06-08 2017-11-07 Healthpartners Research Foundation Pharmaceutical compositions and methods for enhancing 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)

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

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