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AR123619A2 - Método para producir y para controlar la viscosidad de una composición farmacéutica liofilizada de degarelix - Google Patents

Método para producir y para controlar la viscosidad de una composición farmacéutica liofilizada de degarelix

Info

Publication number
AR123619A2
AR123619A2 ARP210102681A ARP210102681A AR123619A2 AR 123619 A2 AR123619 A2 AR 123619A2 AR P210102681 A ARP210102681 A AR P210102681A AR P210102681 A ARP210102681 A AR P210102681A AR 123619 A2 AR123619 A2 AR 123619A2
Authority
AR
Argentina
Prior art keywords
degarelix
lyophilized
pharmaceutical composition
water
viscosity
Prior art date
Application number
ARP210102681A
Other languages
English (en)
Inventor
Grgoire Schwach
Anders Nilsson
Bving Tine Elisabeth Gottschalk
Jon Holbech Rasmussen
Birgitta Mrnstam
Anders Tsirk
Ulf Annby
Jens Fomsgaard
Original Assignee
Ferring 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=48539181&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR123619(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ferring Bv filed Critical Ferring Bv
Publication of AR123619A2 publication Critical patent/AR123619A2/es

Links

Classifications

    • 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
    • A61K38/08Peptides having 5 to 11 amino acids
    • A61K38/09Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • A61K38/16Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof
    • A61K38/17Peptides having more than 20 amino acids; Gastrins; Somatostatins; Melanotropins; Derivatives thereof from animals; from humans
    • A61K38/22Hormones
    • A61K38/25Growth hormone-releasing factor [GH-RF], i.e. somatoliberin
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K47/06Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K9/0024Solid, 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
    • 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
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • A61K9/1623Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/06Linear peptides containing only normal peptide links having 5 to 11 amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/04Linear peptides containing only normal peptide links
    • C07K7/23Luteinising hormone-releasing hormone [LHRH]; Related peptides

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Endocrinology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Zoology (AREA)
  • Genetics & Genomics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)

Abstract

Un método para producir una composición farmacéutica liofilizada de degarelix y método para controlar su viscosidad y producto de degarelix, en donde el producto de degarelix liofilizado, al estar reconstituido con agua para inyección en una cantidad de 20 mg/ml, presenta una viscosidad de hasta 15 mPas, y también proporciona una sustancia de droga degarelix liofilizada que muestra, ante la disolución en agua en una cantidad de 20 mg/ml, una viscosidad de hasta 3.2 mPas, y procesos para proveer esta sustancia de droga degarelix liofilizado. Reivindicación 1: Un método para producir una composición farmacéutica liofilizada de degarelix, caracterizado porque comprende las etapas de: a. Purificar el degarelix en la forma obtenida mediante síntesis péptida de fase líquida o sólida para obtener una solución de degarelix con una pureza de por lo menos 95%; b. Evaporar el solvente a una temperatura máxima de 40ºC para concentrar la solución de degarelix para obtener degarelix aglomerado, en donde la concentración de degarelix (base libre) está en el rango de 10 a 35 g/l; c. Desaglomerar el degarelix aglomerado con ácido acético, en donde la concentración final del ácido acético está en el rango de 15% a 35% v/v; y d. Liofilizar el degarelix desaglomerado de manera de proveer la composición farmacéutica liofilizada de degarelix, en donde la composición farmacéutica liofilizada de degarelix consiste de degarelix, 4.5 a 10.0% (p/p) de ácido acético, una cantidad residual de agua, e impurezas, si las hay, resultantes del proceso de producción, y que muestra, ante la disolución en agua en una cantidad de 20 mg de degarelix base libre/ml de agua conteniendo 2.5% en peso de manitol, una viscosidad de hasta 3.2 mPas. Reivindicación 11: Un método para controlar la viscosidad de un producto de droga liofilizado que comprende una composición farmacéutica liofilizada de degarelix, para obtener un valor no mayor de 15 mPas, preferentemente dentro de una escala de 2 a 12 mPas, determinado ante la reconstitución con agua para inyección en una cantidad de 20 mg de base libre de degarelix/ml, caracterizado porque comprende las etapas de: a. Proveer la composición farmacéutica liofilizada de degarelix; b. Disolver la composición farmacéutica liofilizada de degarelix en agua conteniendo manitol para proveer una mezcla de degarelix-manitol acuosa; y c. Liofilizar la mezcla de degarelix-manitol acuosa para proveer el producto de droga, en donde la composición farmacéutica liofilizada de degarelix consiste de degarelix, 4.5 a 10.0% (p/p) de ácido acético, una cantidad residual de agua, e impurezas, si las hay, resultantes del proceso de producción, y que muestra, ante la disolución en agua en una cantidad de 20 mg de degarelix base libre/ml de agua conteniendo 2.5% en peso de manitol, una viscosidad de hasta 3.2 mPas.
ARP210102681A 2012-06-01 2021-09-27 Método para producir y para controlar la viscosidad de una composición farmacéutica liofilizada de degarelix AR123619A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12170454 2012-06-01

Publications (1)

Publication Number Publication Date
AR123619A2 true AR123619A2 (es) 2022-12-21

Family

ID=48539181

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP130101926A AR092840A1 (es) 2012-06-01 2013-05-31 Elaboracion de degarelix
ARP210102681A AR123619A2 (es) 2012-06-01 2021-09-27 Método para producir y para controlar la viscosidad de una composición farmacéutica liofilizada de degarelix

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP130101926A AR092840A1 (es) 2012-06-01 2013-05-31 Elaboracion de degarelix

Country Status (28)

Country Link
US (5) US9592266B2 (es)
EP (4) EP2854831B1 (es)
JP (1) JP6226966B2 (es)
KR (1) KR102140982B1 (es)
CN (2) CN107569456A (es)
AR (2) AR092840A1 (es)
AU (1) AU2013269523B2 (es)
CA (2) CA2874927A1 (es)
DE (1) DE25151068T1 (es)
DK (1) DK2854831T3 (es)
ES (3) ES3037257T1 (es)
FI (3) FI2854831T3 (es)
HR (1) HRP20241284T1 (es)
HU (1) HUE068579T2 (es)
IL (1) IL235856B (es)
JO (1) JO3586B1 (es)
LT (1) LT2854831T (es)
MX (1) MX364010B (es)
MY (1) MY182320A (es)
NZ (2) NZ701978A (es)
PH (1) PH12014502682B1 (es)
PL (3) PL4512390T1 (es)
RS (1) RS66065B1 (es)
RU (1) RU2657444C2 (es)
SG (1) SG11201407679PA (es)
SI (1) SI2854831T1 (es)
TW (1) TWI580443B (es)
WO (1) WO2013178788A2 (es)

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CN112125956A (zh) * 2019-06-25 2020-12-25 深圳市健元医药科技有限公司 一种地加瑞克的制备方法
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Also Published As

Publication number Publication date
ES3037194T1 (en) 2025-09-30
TW201400143A (zh) 2014-01-01
RS66065B1 (sr) 2024-11-29
PL4512389T1 (pl) 2025-09-01
EP4512389A3 (en) 2025-06-18
JP2015518866A (ja) 2015-07-06
FI4512389T1 (fi) 2025-08-01
US20170319644A1 (en) 2017-11-09
CN107569456A (zh) 2018-01-12
AU2013269523B2 (en) 2017-09-28
WO2013178788A2 (en) 2013-12-05
RU2014146272A (ru) 2016-07-27
US11510962B2 (en) 2022-11-29
MY182320A (en) 2021-01-19
EP4512389A2 (en) 2025-02-26
ES2988481T3 (es) 2024-11-20
LT2854831T (lt) 2024-10-10
CN104334182B (zh) 2017-09-08
ES3037257T1 (en) 2025-09-30
CA3228586A1 (en) 2013-12-05
US11260102B2 (en) 2022-03-01
US10172906B2 (en) 2019-01-08
EP2854831A2 (en) 2015-04-08
FI4512390T1 (fi) 2025-08-01
US20210077564A1 (en) 2021-03-18
AU2013269523A1 (en) 2015-01-15
SI2854831T1 (sl) 2024-11-29
PL4512390T1 (pl) 2025-09-01
EP4385517A2 (en) 2024-06-19
US9592266B2 (en) 2017-03-14
EP4512390A3 (en) 2025-06-25
EP2854831B1 (en) 2024-07-10
SG11201407679PA (en) 2014-12-30
DE25151068T1 (de) 2025-10-02
FI2854831T3 (fi) 2024-10-15
AR092840A1 (es) 2015-05-06
TWI580443B (zh) 2017-05-01
JP6226966B2 (ja) 2017-11-08
JO3586B1 (ar) 2020-07-05
IL235856A0 (en) 2015-01-29
KR20150022854A (ko) 2015-03-04
US10765721B2 (en) 2020-09-08
PL2854831T3 (pl) 2024-11-25
IL235856B (en) 2018-12-31
RU2657444C2 (ru) 2018-06-13
HRP20241284T1 (hr) 2024-12-06
MX2014014662A (es) 2015-02-24
US20190224271A1 (en) 2019-07-25
KR102140982B1 (ko) 2020-08-05
HUE068579T2 (hu) 2025-01-28
PH12014502682A1 (en) 2015-01-26
NZ727679A (en) 2018-05-25
MX364010B (es) 2019-04-11
PH12014502682B1 (en) 2015-01-26
BR112014029495A2 (pt) 2017-06-27
DK2854831T3 (da) 2024-10-14
HK1209046A1 (en) 2016-03-24
WO2013178788A3 (en) 2014-02-27
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