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1. WO2005097197 - POLYMER PARTICLES CONTAINING ACTIVE AGENTS

Publication Number WO/2005/097197
Publication Date 20.10.2005
International Application No. PCT/EP2005/003493
International Filing Date 02.04.2005
IPC
A61K 47/32 2006.01
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
A61K 47/48 2006.01
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
48the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
C08F 220/12 2006.01
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
220Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride, ester, amide, imide, or nitrile thereof
02Monocarboxylic acids having less than ten carbon atoms; Derivatives thereof
10Esters
12of monohydric alcohols or phenols
CPC
A61K 9/1635
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
16Agglomerates; Granulates; Microbeadlets ; ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
1605Excipients; Inactive ingredients
1629Organic macromolecular compounds
1635obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
A61K 9/5138
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;
5107Excipients; Inactive ingredients
513Organic macromolecular compounds; Dendrimers
5138obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
C08F 220/06
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
220Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride ester, amide, imide or nitrile thereof
02Monocarboxylic acids having less than ten carbon atoms; Derivatives thereof
04Acids; Metal salts or ammonium salts thereof
06Acrylic acid; Methacrylic acid; Metal salts or ammonium salts thereof
C08F 220/14
CCHEMISTRY; METALLURGY
08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
FMACROMOLECULAR COMPOUNDS OBTAINED BY REACTIONS ONLY INVOLVING CARBON-TO-CARBON UNSATURATED BONDS
220Copolymers of compounds having one or more unsaturated aliphatic radicals, each having only one carbon-to-carbon double bond, and only one being terminated by only one carboxyl radical or a salt, anhydride ester, amide, imide or nitrile thereof
02Monocarboxylic acids having less than ten carbon atoms; Derivatives thereof
10Esters
12of monohydric alcohols or phenols
14Methyl esters ; , e.g. methyl (meth)acrylate
Applicants
  • BASF AKTIENGESELLSCHAFT [DE]/[DE] (AllExceptUS)
  • SIOL, Werner [DE]/[DE] (UsOnly)
Inventors
  • SIOL, Werner
Common Representative
  • BASF AKTIENGESELLSCHAFT
Priority Data
10 2004 016 685.405.04.2004DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) WIRKSTOFFHALTIGE POLYMERTEILCHEN
(EN) POLYMER PARTICLES CONTAINING ACTIVE AGENTS
(FR) PARTICULES POLYMERES CONTENANT DES AGENTS ACTIFS
Abstract
(DE)
Die Erfindung betrifft wirkstoffhaltige Polymerteilchen, enthaltend ein Vinylpolymerisat aus 10- 80 Gew% Amino- und/oder Carboxylgruppen enthaltenden Monomeren, das in einem Teil des pH- Bereichs von 0- 10 unlöslich ist und in einem anderen Teilbereich löslich ist, dadurch gekennzeichnet, dass diese wirkstoffhaltigen Polymerteilchen pro Teil Vinylpolymerisat 3- 1000 Teile Wirkstoff enthalten, eine Teilchengröße im Bereich 20nm - 8µm aufweisen und das Vinylpolymerisat zu > 50 Gew% aus Polymeren mit einem Molekulargewicht < 100.000 Daltons aufgebaut ist.
(EN)
The invention relates to polymer particles containing active agents, comprising a vinyl polymer of 10- 80 wt. % of monomers comprising amino and/or carboxyl groups, insoluble in a part of the pH range from 0- 10 and soluble in another part range, characterised in that said polymer particles, containing active agents, comprise 3- 1000 parts of active agent per part of vinyl polymer, with a particle size in the range 20nm - 8µm and the vinyl polymer is made up of > 50 wt. % of polymers with a molecular weight of < 100,000 Daltons.
(FR)
L'invention concerne des particules polymères contenant des agents actifs, lesquelles particules comprennent un polymère vinylique constitué de 10 à 80 % en poids de monomères à groupes amino et/ou carboxyle, lequel polymère est insoluble dans une partie de la plage de pH de 0 à 10 et soluble dans une autre plage partielle. L'invention se caractérise en ce que ces particules polymères contenant des agents actifs comprennent 3 à 1 000 parties d'agent actif par partie de polymère vinylique, présentent une dimension de particules dans la plage de 20 nm à 8 µm et le polymère vinylique est constitué à > 50 % en poids de polymères de poids moléculaire < 100 000 daltons.
Also published as
US2007224274
ZA200609155
RU2006139003
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