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1. WO2010100479 - ORAL DELIVERY OF HYDROPHILIC DRUGS TO THE BRAIN

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Publication Number WO/2010/100479
Publication Date 10.09.2010
International Application No. PCT/GB2010/050355
International Filing Date 01.03.2010
IPC
A61K 47/18 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
16containing nitrogen
18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
A61K 47/36 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
A61K 47/48 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
CPC
A61K 47/36
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
A61K 47/543
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
51the non-active ingredient being a modifying agent
54the modifying agent being an organic compound
543Lipids, e.g. triglycerides; Polyamines, e.g. spermine or spermidine
A61K 47/6921
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
6921the form being a particulate, a powder, an adsorbate, a bead or a sphere
A61K 47/6935
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
47Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
50the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
69the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
6921the form being a particulate, a powder, an adsorbate, a bead or a sphere
6927the form being a solid microparticle having no hollow or gas-filled cores
6929the form being a nanoparticle, e.g. an immuno-nanoparticle
6931the material constituting the nanoparticle being a polymer
6935the polymer being obtained otherwise than by reactions involving carbon to carbon unsaturated bonds, e.g. polyesters, polyamides or polyglycerol
A61K 9/0019
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
A61K 9/0053
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
0012Galenical forms characterised by the site of application
0053Mouth and digestive tract, i.e. intraoral and peroral administration
Applicants
  • SCHOOL OF PHARMACY, UNIVERSITY OF LONDON [GB]/[GB](AllExceptUS)
  • UCHEGBU, Ijeoma [GB]/[GB](UsOnly)
  • SCHATZLEIN, Andreas [DE]/[GB](UsOnly)
  • LALATSA, Aikaterini [GR]/[GB](UsOnly)
Inventors
  • UCHEGBU, Ijeoma
  • SCHATZLEIN, Andreas
  • LALATSA, Aikaterini
Agents
  • GILL JENNINGS & EVERY LLP
Priority Data
0903559.302.03.2009GB
12/420,89609.04.2009US
Publication Language English (en)
Filing Language English (en)
Designated States
Title
(EN) ORAL DELIVERY OF HYDROPHILIC DRUGS TO THE BRAIN
(FR) ADMINISTRATION PAR VOIE ORALE DE MÉDICAMENTS HYDROPHILES POUR LE CERVEAU
Abstract
(EN) A composition comprising a lipophilic derivative of a hydrophilic drug and an amphiphile compound for use in therapy wherein the composition is orally administered to the human or animal body. The invention includes derivatives such as palmitoylated Leucine[5]-Enkephalin and is useful in the treatment of schizophrenia, obsesity, pain and sleep disorders, psychiatric diseases, neurodegenerative conditions, brain cancers and infective diseases.
(FR) La présente invention concerne une composition comprenant un dérivé lipophile d'un médicament hydrophile et un composé amphiphile destiné à être utilisé en thérapie, la composition étant administrée par voie orale au corps humain ou animal. L'invention concerne des dérivés tels que la leucine[5]-encéphaline palmitoylée et est utile dans le traitement de la schizophrénie, de l'obésité, de la douleur et des troubles du sommeil, de maladies psychiatriques, de troubles neurodégénératifs, de cancers du cerveau et de maladies infectieuses.
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