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WO2026013080A1 - Composition pharmaceutique à base de polymères biodégradables comprenant de la polyoxazoline - Google Patents

Composition pharmaceutique à base de polymères biodégradables comprenant de la polyoxazoline

Info

Publication number
WO2026013080A1
WO2026013080A1 PCT/EP2025/069480 EP2025069480W WO2026013080A1 WO 2026013080 A1 WO2026013080 A1 WO 2026013080A1 EP 2025069480 W EP2025069480 W EP 2025069480W WO 2026013080 A1 WO2026013080 A1 WO 2026013080A1
Authority
WO
WIPO (PCT)
Prior art keywords
poz
biodegradable polymer
pharmaceutical composition
ranges
mol
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
PCT/EP2025/069480
Other languages
English (en)
Inventor
Ivan TERZIC
Anbu PALANISAMY
Rob Steendam
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Innocore Technologies Holding BV
Original Assignee
Innocore Technologies Holding BV
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Innocore Technologies Holding BV filed Critical Innocore Technologies Holding BV
Publication of WO2026013080A1 publication Critical patent/WO2026013080A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

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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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34—Macromolecular 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
    • 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
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • 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
    • A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G63/00—Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
    • C08G63/02—Polyesters derived from hydroxycarboxylic acids or from polycarboxylic acids and polyhydroxy compounds
    • C08G63/06—Polyesters derived from hydroxycarboxylic acids or from polycarboxylic acids and polyhydroxy compounds derived from hydroxycarboxylic acids
    • C08G63/08—Lactones or lactides
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G63/00—Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
    • C08G63/68—Polyesters containing atoms other than carbon, hydrogen and oxygen
    • C08G63/685—Polyesters containing atoms other than carbon, hydrogen and oxygen containing nitrogen
    • C08G63/6852—Polyesters containing atoms other than carbon, hydrogen and oxygen containing nitrogen derived from hydroxy carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G73/00—Macromolecular compounds obtained by reactions forming a linkage containing nitrogen with or without oxygen or carbon in the main chain of the macromolecule, not provided for in groups C08G12/00 - C08G71/00
    • C08G73/02—Polyamines
    • C08G73/0233—Polyamines derived from (poly)oxazolines, (poly)oxazines or having pendant acyl groups
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L101/00—Compositions of unspecified macromolecular compounds
    • C08L101/16—Compositions of unspecified macromolecular compounds the macromolecular compounds being biodegradable
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L67/00—Compositions of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Compositions of derivatives of such polymers
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08L—COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L87/00—Compositions of unspecified macromolecular compounds, obtained otherwise than by polymerisation reactions only involving unsaturated carbon-to-carbon bonds
    • C08L87/005—Block or graft polymers not provided for in groups C08L1/00 - C08L85/04
    • C—CHEMISTRY; METALLURGY
    • C08—ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08G—MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G2210/00—Compositions for preparing hydrogels

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Inorganic Chemistry (AREA)
  • Molecular Biology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une composition pharmaceutique comprenant : a. 20 à 75 % en poids d'un polymère biodégradable selon la formule (1) POZx,y–(B-R)z (1), dans laquelle POZx, y est une polyoxazoline, B = un fragment hydrophobe, R = H ou un groupe C1-C18-alkyle, x = le nombre d'extrémités de chaîne du groupe POZx,y et vaut 2, 3, 4, 5 ou 6, y = le nombre de points de fixation pour B-R à chaque extrémité de chaîne du groupe POZx,y et vaut 1 ou 2 et z est le nombre de groupes (B-R) par polymère biodégradable et vaut 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 ou 12; b. 20 à 79 % en poids d'un solvant organique biocompatible; et c. 1 à 40 % en poids d'un ingrédient pharmaceutique actif; les pourcentages en poids de (a), (b) et (c) étant définis par rapport à la somme de (a) + (b) + (c); la fraction en poids du groupe POZx,y étant située entre 4 et 40 % en poids par rapport au poids total du polymère biodégradable, la fraction en poids du groupe POZx,y étant déterminée par 1H-RMN. L'invention concerne également un polymère biodégradable et des compositions pharmaceutiques comprenant le polymère biodégradable et un ingrédient pharmaceutique actif, les compositions pharmaceutiques se présentant sous la forme de microparticules, de microgranules, de microsphères ou d'un implant.
PCT/EP2025/069480 2024-07-08 2025-07-08 Composition pharmaceutique à base de polymères biodégradables comprenant de la polyoxazoline Pending WO2026013080A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP24187179.7 2024-07-08
EP24187179 2024-07-08

Publications (1)

Publication Number Publication Date
WO2026013080A1 true WO2026013080A1 (fr) 2026-01-15

Family

ID=91953945

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2025/069480 Pending WO2026013080A1 (fr) 2024-07-08 2025-07-08 Composition pharmaceutique à base de polymères biodégradables comprenant de la polyoxazoline

Country Status (1)

Country Link
WO (1) WO2026013080A1 (fr)

Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5324519A (en) 1989-07-24 1994-06-28 Atrix Laboratories, Inc. Biodegradable polymer composition
WO1999051209A1 (fr) 1998-04-02 1999-10-14 Impax Pharmaceuticals, Inc. Systeme impulsionnel d'administration medicamenteuse enrobe a sec convenant pour l'administration par voie orale
WO2002026179A1 (fr) 2000-09-28 2002-04-04 Ganado Research, L.L.C. Pellet implantable pour soulager la douleur, et mode d'utilisation
US20060182710A1 (en) * 2004-12-31 2006-08-17 Industrial Technology Research Institute Amphiphilic block copolymer and pharmaceutical formulation comprising the same
WO2011002285A1 (fr) 2009-06-29 2011-01-06 Bender Analytical Holding B.V. Système d'administration de médicament comprenant de la polyoxazoline et un agent bioactif
WO2012090070A2 (fr) 2010-12-29 2012-07-05 Medincell Compositions biodégradables d'administration de médicaments
WO2014001905A1 (fr) 2012-06-27 2014-01-03 Medincell Administration de médicament biodégradable pour compositions hydrophobes
US9974866B2 (en) * 2010-04-07 2018-05-22 Board Of Regents Of The University Of Nebraska Protein-poly(2-oxazoline) conjugates for enhanced cellular delivery and transport across biological barriers
WO2020144239A1 (fr) 2019-01-08 2020-07-16 Medincell Composition pharmaceutique
WO2021048817A1 (fr) 2019-09-13 2021-03-18 Medincell S.A. Formulations d'administration de médicaments
EP3925625A1 (fr) * 2011-01-09 2021-12-22 ANP Technologies, Inc. Agrégats polymères ramifiés induits par des molécules hydrophobes et leur utilisation
WO2022229402A1 (fr) 2021-04-30 2022-11-03 Medincell Sa Nouvelle formulation

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5324519A (en) 1989-07-24 1994-06-28 Atrix Laboratories, Inc. Biodegradable polymer composition
WO1999051209A1 (fr) 1998-04-02 1999-10-14 Impax Pharmaceuticals, Inc. Systeme impulsionnel d'administration medicamenteuse enrobe a sec convenant pour l'administration par voie orale
WO2002026179A1 (fr) 2000-09-28 2002-04-04 Ganado Research, L.L.C. Pellet implantable pour soulager la douleur, et mode d'utilisation
US20060182710A1 (en) * 2004-12-31 2006-08-17 Industrial Technology Research Institute Amphiphilic block copolymer and pharmaceutical formulation comprising the same
WO2011002285A1 (fr) 2009-06-29 2011-01-06 Bender Analytical Holding B.V. Système d'administration de médicament comprenant de la polyoxazoline et un agent bioactif
US9974866B2 (en) * 2010-04-07 2018-05-22 Board Of Regents Of The University Of Nebraska Protein-poly(2-oxazoline) conjugates for enhanced cellular delivery and transport across biological barriers
WO2012090070A2 (fr) 2010-12-29 2012-07-05 Medincell Compositions biodégradables d'administration de médicaments
EP3925625A1 (fr) * 2011-01-09 2021-12-22 ANP Technologies, Inc. Agrégats polymères ramifiés induits par des molécules hydrophobes et leur utilisation
WO2014001905A1 (fr) 2012-06-27 2014-01-03 Medincell Administration de médicament biodégradable pour compositions hydrophobes
WO2020144239A1 (fr) 2019-01-08 2020-07-16 Medincell Composition pharmaceutique
WO2021048817A1 (fr) 2019-09-13 2021-03-18 Medincell S.A. Formulations d'administration de médicaments
WO2022229402A1 (fr) 2021-04-30 2022-11-03 Medincell Sa Nouvelle formulation

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BRONZERI LEONARDO BUENO ET AL: "Amphiphilic and segmented polyurethanes based on poly([epsilon]-caprolactone)diol and poly(2-ethyl-2-oxazoline)diol: Synthesis, properties, and a preliminary performance study of the 3D printing", EUROPEAN POLYMER JOURNAL, PERGAMON PRESS LTD OXFORD, GB, vol. 151, 20 April 2021 (2021-04-20), XP086558154, ISSN: 0014-3057, [retrieved on 20210420], DOI: 10.1016/J.EURPOLYMJ.2021.110449 *
CHAU-HUI WANG ET AL: "New amphiphilic poly(2-ethyl-2-oxazoline)/ poly(L-lactide) triblock copolymers", BIOMACROMOLECULES, vol. 4, no. 6, 1 January 2003 (2003-01-01), US, pages 1487 - 1490, XP055489829, ISSN: 1525-7797, DOI: 10.1021/bm034190s *
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PLET LAETITIA ET AL: "Controlled star poly(2-oxazoline)s: Synthesis, characterization", EUROPEAN POLYMER JOURNAL, PERGAMON PRESS LTD OXFORD, GB, vol. 122, 23 October 2019 (2019-10-23), XP085965172, ISSN: 0014-3057, [retrieved on 20191023], DOI: 10.1016/J.EURPOLYMJ.2019.109323 *
WILSON PAUL ET AL: "Poly(2-oxazoline)-based micro- and nanoparticles: A review", EUROPEAN POLYMER JOURNAL, PERGAMON PRESS LTD OXFORD, GB, vol. 88, 9 September 2016 (2016-09-09), pages 486 - 515, XP029942923, ISSN: 0014-3057, DOI: 10.1016/J.EURPOLYMJ.2016.09.011 *

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