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1. WO2013127490 - PROCESS FOR PRODUCING NANOPARTICLES LADEN WITH ACTIVE INGREDIENT

Publication Number WO/2013/127490
Publication Date 06.09.2013
International Application No. PCT/EP2013/000396
International Filing Date 11.02.2013
IPC
A61K 9/51 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules
51Nanocapsules
CPC
A61K 31/4375
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
4353ortho- or peri-condensed with heterocyclic ring systems
4375the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
A61K 31/573
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
573substituted in position 21, e.g. cortisone, dexamethasone, prednisone ; or aldosterone
A61K 47/32
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
32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers ; , poly(meth)acrylates, or polyvinyl pyrrolidone
A61K 47/34
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
34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
A61K 9/14
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
14Particulate form, e.g. powders, ; Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
A61K 9/51
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
9Medicinal preparations characterised by special physical form
48Preparations in capsules, e.g. of gelatin, of chocolate
50Microcapsules ; having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
51Nanocapsules; Nanoparticles;
Applicants
  • MERCK PATENT GMBH [DE]/[DE]
Inventors
  • WEIGANDT, Markus
  • VOSS, Senta
  • MILLER, Tobias
  • GOEPFERICH, Achim
Priority Data
10 2012 004 099.729.02.2012DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) VERFAHREN ZUR HERSTELLUNG WIRKSTOFFBELADENER NANOPARTIKEL
(EN) PROCESS FOR PRODUCING NANOPARTICLES LADEN WITH ACTIVE INGREDIENT
(FR) PROCÉDÉ DE FABRICATION DE NANOPARTICULES CHARGÉES D'UNE SUBSTANCE ACTIVE
Abstract
(DE)
Die vorliegende Erfindung betrifft eine neues Verfahren zur Herstellung von mit Wirkstoffen beladenen Nanopartikeln sowie deren Verwendung als Arzneimittel. Das Verfahren zur Herstellung von Nanopartikeln umfasst die Schritte (a) Lösen von mindestens einem Wirkstoff und mindestens einem Polymer in einem organischen Lösungsmittel, (b) Mischen der in Schritt (a) hergestellten Lösung mit einer wässrigen Phase, (c) Evaporieren des organischen Lösungsmittels, (d) Auf reinigen der in Schritt (c) erhaltenen, mit Wirkstoff beladenen Nanopartikel mittels Dialyse gegen den gleichen Wirkstoff enthaltende wässrige Dialyselösung
(EN)
The present invention relates to a new process for producing nanoparticles laden with active ingredients, and to the use thereof as medicaments. The process for producing nanoparticles comprises the steps (a) dissolution of at least one active ingredient and at least one polymer in an organic solvent, (b) mixing the solution prepared in step (a) with an aqueous phase, (c) evaporating the organic solvent, (d) purifying the nanoparticles laden with active ingredient obtained in step (c) by means of dialysis against aqueous dialysis solution containing the same active ingredient.
(FR)
L'invention concerne un nouveau procédé de fabrication de nanoparticules chargées d'une substance active, ainsi que l'utilisation desdites nanoparticules comme médicaments. Le procédé de fabrication de nanoparticules comporte les étapes suivantes consistant à : (a) faire dissoudre au moins une substance active et au moins un polymère dans un solvant organique; (b) mélanger la solution produite à l'étape (a) à une phase aqueuse; (c) faire évaporer le solvant organique; (d) nettoyer les nanoparticules chargées de substance active, obtenues à l'étape (c), par dialyse au moyen d'une solution de dialyse aqueuse contenant la même substance active.
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