AR124406A1 - Dispersiones sólidas amorfas - Google Patents

Dispersiones sólidas amorfas

Info

Publication number
AR124406A1
AR124406A1 ARP210103551A ARP210103551A AR124406A1 AR 124406 A1 AR124406 A1 AR 124406A1 AR P210103551 A ARP210103551 A AR P210103551A AR P210103551 A ARP210103551 A AR P210103551A AR 124406 A1 AR124406 A1 AR 124406A1
Authority
AR
Argentina
Prior art keywords
solid dispersion
weight
dispersion according
hypromellose
disease
Prior art date
Application number
ARP210103551A
Other languages
English (en)
Inventor
Faiza Laredj
Rosanna Chirico
Aymeric Ousset
Original Assignee
UCB Biopharma SRL
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 UCB Biopharma SRL filed Critical UCB Biopharma SRL
Publication of AR124406A1 publication Critical patent/AR124406A1/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/02Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61K47/32Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate 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
    • A61K9/146Intimate 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1635Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A61K9/1647Polyesters, e.g. poly(lactide-co-glycolide)
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682Processes
    • 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
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychology (AREA)
  • Inorganic Chemistry (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Compositions Of Oxide Ceramics (AREA)
  • Compositions Of Macromolecular Compounds (AREA)
  • Addition Polymer Or Copolymer, Post-Treatments, Or Chemical Modifications (AREA)

Abstract

Reivindicación 1: Una dispersión sólida caracterizada porque es de 2-(3,5-dicloro-1-metil-indazol-4-il)-1-[(1S,3R)-3-(hidroximetil)-5-(1-hidroxi-1)amorfo-metil-etil)-1-metil3,4-dihidro-1H-isoquinolin-2-il]etanona de fórmula (1) y una matriz polimérica. Reivindicación 8: Un proceso de preparación de una dispersión sólida de acuerdo a la reivindicación 1 mediante secado por pulverización caracterizado porque comprende los siguientes pasos: (i) disolver el compuesto de fórmula (1a) y acetato de hidroxipropilmetilcelulosa, copolímero N-vinil-2-pirrolidona / acetato de vinilo, polivinilpirrolidona, ftalato de hipromelosa o hipromelosa en un disolvente; (ii) transportar la solución obtenida como resultado del paso (i) a una cámara de atomización; (iii) poner en contacto las gotitas formadas como resultado de la etapa (ii) con un gas de secado en caliente; (iv) evaporar el disolvente; (v) separar la dispersión sólida obtenida del gas de secado. Reivindicación 9: Un proceso de preparación de una dispersión sólida de acuerdo a la reivindicación 1 por extrusión por fusión en caliente caracterizado porque comprende los siguientes pasos: (i) Mezclar el compuesto de fórmula (1a) y acetato de hidroxipropil metil celulosa, copolímero N-vinil-2-pirrolidona / acetato de vinilo, polivinilpirrolidona, ftalato de hipromelosa o hipromelosa; (ii) Introducir la mezcla obtenida en la etapa (i) en una extrusora por fusión en caliente en la que una sección hecha de cilindro y tornillos transporta la mezcla de forma continua a una temperatura superior a 150ºC hasta que se obtiene una masa fundida; (iii) Enfriar la masa fundida obtenida en la etapa (ii) a temperatura ambiente. Reivindicación 10: Una composición farmacéutica caracterizada porque comprende la dispersión sólida de acuerdo a la reivindicación 1 en asociación con uno o más excipientes farmacéuticamente aceptables. Reivindicación 11: Un producto farmacéutico caracterizado porque comprende una dispersión sólida de acuerdo a la reivindicación 1 que consiste en un comprimido que comprende: Entre aproximadamente 20% y aproximadamente 60% por peso de dispersión sólida amorfa; Entre aproximadamente 10% y aproximadamente 50% por peso de lactosa monohidratada; Entre aproximadamente 10% y aproximadamente 50% por peso de celulosa microcristalina; Entre aproximadamente 1% y aproximadamente 5% por peso de croscarmelosa sódica; Entre aproximadamente 0,1% y aproximadamente 2% por peso de sílice coloidal anhidra; y Entre aproximadamente 0,1% y aproximadamente 5% por peso de estearato de magnesio; En comparación con el peso total del comprimido sin recubrimiento. Reivindicación 12: Una dispersión sólida según una cualquiera de las reivindicaciones 1 - 7 o una composición farmacéutica de acuerdo a la reivindicación 10 u 11, caracterizada porque es para su uso en el tratamiento y/o prevención de síntomas cognitivos y negativos en la esquizofrenia, deterioro cognitivo relacionado con la terapia neuroléptica, deterioro cognitivo leve (MCI), impulsividad, trastorno por déficit de atención e hiperactividad (ADHD), enfermedad de Parkinson y otros trastornos del movimiento, distonía, demencia de Parkinson, enfermedad de Huntington, demencia con cuerpos de Lewy, adicción a las drogas y enfermedad de Alzheimer, trastornos del sueño, apatía, traumatismo lesión traumática de la médula espinal o dolor neuropático.
ARP210103551A 2020-12-18 2021-12-17 Dispersiones sólidas amorfas AR124406A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP20215253 2020-12-18

Publications (1)

Publication Number Publication Date
AR124406A1 true AR124406A1 (es) 2023-03-22

Family

ID=73855649

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP210103551A AR124406A1 (es) 2020-12-18 2021-12-17 Dispersiones sólidas amorfas

Country Status (15)

Country Link
US (1) US20240000769A1 (es)
EP (1) EP4262756A1 (es)
JP (1) JP2023553457A (es)
KR (1) KR20230121867A (es)
CN (1) CN116685308A (es)
AR (1) AR124406A1 (es)
AU (1) AU2021401128A1 (es)
CA (1) CA3201298A1 (es)
CL (1) CL2023001395A1 (es)
CO (1) CO2023007098A2 (es)
IL (1) IL303688A (es)
MX (1) MX2023007154A (es)
PE (1) PE20240021A1 (es)
TW (1) TW202241424A (es)
WO (1) WO2022129267A1 (es)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2978751B1 (en) * 2013-03-25 2018-12-05 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor xia inhibitors
JO3316B1 (ar) * 2013-05-30 2019-03-13 Lilly Co Eli مركبات 3، 4-داي هيدرو أيزو كوينولين -2(1h)-يل
WO2015141662A1 (ja) * 2014-03-18 2015-09-24 武田薬品工業株式会社 固体分散体
CA2963951C (en) * 2014-10-08 2023-02-28 Ucb Biopharma Sprl Tetrahydroisoquinoline derivatives
BR112018070363A2 (pt) * 2016-04-13 2019-01-29 Ucb Biopharma Sprl derivados de tetraidroisoquinolina
US20220259179A1 (en) 2019-07-01 2022-08-18 UCB Biopharma SRL A Substituted Tetrahydroisoquinoiline Derivative as a D1 Positive Allosteric Modulator

Also Published As

Publication number Publication date
EP4262756A1 (en) 2023-10-25
CL2023001395A1 (es) 2023-12-29
KR20230121867A (ko) 2023-08-21
IL303688A (en) 2023-08-01
CO2023007098A2 (es) 2023-06-09
CN116685308A (zh) 2023-09-01
TW202241424A (zh) 2022-11-01
US20240000769A1 (en) 2024-01-04
CA3201298A1 (en) 2022-06-23
AU2021401128A1 (en) 2023-07-13
WO2022129267A1 (en) 2022-06-23
MX2023007154A (es) 2023-06-28
JP2023553457A (ja) 2023-12-21
PE20240021A1 (es) 2024-01-04

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