AR113096A1 - Mezclas de composiciones biodegradables que modulan la cinética de liberación de al menos un ingrediente activo en la administración de fármacos - Google Patents

Mezclas de composiciones biodegradables que modulan la cinética de liberación de al menos un ingrediente activo en la administración de fármacos

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Publication number
AR113096A1
AR113096A1 ARP180101987A ARP180101987A AR113096A1 AR 113096 A1 AR113096 A1 AR 113096A1 AR P180101987 A ARP180101987 A AR P180101987A AR P180101987 A ARP180101987 A AR P180101987A AR 113096 A1 AR113096 A1 AR 113096A1
Authority
AR
Argentina
Prior art keywords
biodegradable
range
administration
repeating units
composition
Prior art date
Application number
ARP180101987A
Other languages
English (en)
Inventor
Jean Cros
- Rech Anthony Manuel
Christophe Roberge
Juliette Serindoux
Audrey Petit
Lea Pebrel
Adolfo Lpez-Noriega
Myriam Abbassi
Original Assignee
Medincell
Christophe Roberge
Rech Anthony
Cros Jean Manuel
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 Medincell, Christophe Roberge, Rech Anthony, Cros Jean Manuel filed Critical Medincell
Publication of AR113096A1 publication Critical patent/AR113096A1/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0024Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/5415Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7048Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08Peptides having 5 to 11 amino acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/04Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/30Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
    • A61K47/34Macromolecular 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A61K9/0029Parenteral nutrition; Parenteral nutrition compositions as drug carriers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/06Ointments; Bases therefor; Other semi-solid forms, e.g. creams, sticks, gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A61K9/204Polyesters, e.g. poly(lactide-co-glycolide)
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08GMACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
    • C08G63/00Macromolecular compounds obtained by reactions forming a carboxylic ester link in the main chain of the macromolecule
    • C08G63/66Polyesters containing oxygen in the form of ether groups
    • C08G63/664Polyesters containing oxygen in the form of ether groups derived from hydroxy carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L67/00Compositions of polyesters obtained by reactions forming a carboxylic ester link in the main chain; Compositions of derivatives of such polymers
    • C08L67/04Polyesters derived from hydroxycarboxylic acids, e.g. lactones
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L71/00Compositions of polyethers obtained by reactions forming an ether link in the main chain; Compositions of derivatives of such polymers
    • C08L71/02Polyalkylene oxides
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2203/00Applications
    • C08L2203/02Applications for biomedical use
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2205/00Polymer mixtures characterised by other features
    • C08L2205/02Polymer mixtures characterised by other features containing two or more polymers of the same C08L -group
    • C08L2205/025Polymer mixtures characterised by other features containing two or more polymers of the same C08L -group containing two or more polymers of the same hierarchy C08L, and differing only in parameters such as density, comonomer content, molecular weight, structure
    • CCHEMISTRY; METALLURGY
    • C08ORGANIC MACROMOLECULAR COMPOUNDS; THEIR PREPARATION OR CHEMICAL WORKING-UP; COMPOSITIONS BASED THEREON
    • C08LCOMPOSITIONS OF MACROMOLECULAR COMPOUNDS
    • C08L2205/00Polymer mixtures characterised by other features
    • C08L2205/03Polymer mixtures characterised by other features containing three or more polymers in a blend

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Dermatology (AREA)
  • Engineering & Computer Science (AREA)
  • Organic Chemistry (AREA)
  • Polymers & Plastics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Inorganic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Nutrition Science (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se provee una composición biodegradable para la administración de fármacos que comprende: (i) una mezcla de por lo menos tres copolímeros de bloques diferentes, donde cada copolímero de bloques es: (a) un copolímero biodegradable de tribloques que tiene la fórmula: Aᵛ-Bʷ-Aˣ en donde A es un poliéster y B es polietilenglicol y v y x son entre 1 y 3.000 y w es entre 3 y 300 y v = x o v ¹ x; o (b) un copolímero biodegradable de dibloques que tiene la fórmula: Cʸ-Aᶻ en donde A es un poliéster y C es un polietilenglicol de extremos protegidos e y y z son el número de unidades repetitivas con y = 2 a 250 y z = 1 a 3.000; y en donde la mezcla comprende al menos un (a) y al menos un (b); y la proporción en peso entre (a) y (b) es entre 1:19 y 5:1; y para por lo menos uno de los copolímeros de acuerdo a (a) o (b) A es poli(ácido láctico-co-glicólico) (PLGA); y (ii) por lo menos un ingrediente farmacéuticamente activo. Reivindicación 8: Una composición biodegradable para la administración de fármacos de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizada porque la composición además comprende: (a) un copolímero biodegradable de tribloques que tiene la fórmula: PLGAᵛ-PEGʷ-PLGAˣ en donde v y x son el número de unidades repetitivas que están en el rango entre 1 y 3.000 y w es el número de unidades repetitivas que están en rango entre 3 y 300 y v = x o v ¹ x; y/o (b) un copolímero biodegradable de dibloques que tiene la fórmula: mPEGʸ-PLGAᶻ en donde y y z son el número de unidades repetitivas con y en el rango entre 2 y 250 y z en el rango entre 1 y 3.000. Reivindicación 9: Una composición biodegradable para la administración de fármacos de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizada porque la composición además comprende: y (a) un copolímero biodegradable de tribloques que tiene la fórmula: PCLAᵛ-PEGʷ-PCLAˣ en donde v y x son el número de unidades repetitivas que están en el rango entre 1 y 3.000 y w es el número de unidades repetitivas que están en rango entre 3 y 300 y v = x o v ¹ x; y/o (b) un copolímero biodegradable de dibloques que tiene la fórmula: mPEGʸ-PCLAᶻ en donde y y z son el número de unidades repetitivas con y en el rango entre 2 y 250 y z en el rango entre 1 y 3.000. Reivindicación 11: Una composición biodegradable para la administración de fármacos de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizada porque dicha composición es un líquido inyectable y es adecuada para formas un depósito cuando se inyecta en el cuerpo, o son partículas sólidas pequeñas o implantes de varilla o formulaciones espaciales. Reivindicación 15: Una composición biodegradable para la administración de fármacos de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizada porque el ingrediente farmacéuticamente activo es meloxicam, acetaminofeno o combinaciones de los mismos. Reivindicación 31: Una composición biodegradable para la administración de fármacos de acuerdo con cualquiera de las reivindicaciones precedentes, caracterizada porque es adecuada para administración parenteral.
ARP180101987A 2017-07-17 2018-07-17 Mezclas de composiciones biodegradables que modulan la cinética de liberación de al menos un ingrediente activo en la administración de fármacos AR113096A1 (es)

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ARP180101988A AR113097A1 (es) 2017-07-17 2018-07-17 Mezclas de composiciones biodegradables que modulan la cinética de liberación de al menos un ingrediente activo en la administración de fármacos
ARP180101987A AR113096A1 (es) 2017-07-17 2018-07-17 Mezclas de composiciones biodegradables que modulan la cinética de liberación de al menos un ingrediente activo en la administración de fármacos
ARP180101986A AR113248A1 (es) 2017-07-17 2018-07-17 Mezclas de composiciones biodegradables que modulan la cinética de liberación de al menos un ingrediente activo en la administración de fármacos

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US (3) US11612563B2 (es)
EP (3) EP3655037A1 (es)
JP (3) JP7187738B2 (es)
KR (1) KR20200032719A (es)
CN (1) CN111107840A (es)
AR (3) AR113097A1 (es)
AU (1) AU2018304881B2 (es)
BR (1) BR112020001031A2 (es)
CA (1) CA3069787A1 (es)
EA (1) EA202090161A1 (es)
IL (1) IL271986B2 (es)
MX (1) MX2020000618A (es)
TW (3) TWI795421B (es)
WO (3) WO2019016236A1 (es)

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