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WO2014128079A1 - Formulation multidose d'acétate de glatiramère - Google Patents

Formulation multidose d'acétate de glatiramère Download PDF

Info

Publication number
WO2014128079A1
WO2014128079A1 PCT/EP2014/053019 EP2014053019W WO2014128079A1 WO 2014128079 A1 WO2014128079 A1 WO 2014128079A1 EP 2014053019 W EP2014053019 W EP 2014053019W WO 2014128079 A1 WO2014128079 A1 WO 2014128079A1
Authority
WO
WIPO (PCT)
Prior art keywords
glatiramer acetate
formulation
benzyl alcohol
formulation according
preservative
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.)
Ceased
Application number
PCT/EP2014/053019
Other languages
English (en)
Inventor
Lisa BAKKER-HOLMDAHL
Frans Henri Nicolaas HAAN DE
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.)
Synthon BV
Original Assignee
Synthon 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 Synthon BV filed Critical Synthon BV
Publication of WO2014128079A1 publication Critical patent/WO2014128079A1/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/02—Peptides of undefined number of amino acids; Derivatives thereof
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin

Definitions

  • the present invention relates to a formulation comprising multiple doses of glatiramer acetate and one or more preservatives selected from the group consisting of benzyl alcohol, m-cresol, phenol, methylparaben, and propylparaben.
  • Glatiramer acetate is the Active Pharmaceutical Ingredient (API) in the drug product COPAXONE® (20 mg/ml, subcutaneous (sc) injection), which is authorized by a number of regulatory authorities, e.g. since 2002 by the FDA for marketing and sale in the US, for the treatment of various forms of multiple sclerosis (MS), including relapsing-remitting MS.
  • the product is currently available as a pre-filled syringe for daily administration. Each syringe is discarded after single use.
  • a three-times weekly dosing regimen of a 40 mg/ml formulation for subcutaneous injection is in clinical development.
  • no multidose formulation of glatiramer acetate exists or has been disclosed in publicly available documents.
  • the present invention relates to a formulation comprising multiple doses of glatiramer acetate and one or more preservatives selected from the group consisting of benzyl alcohol, m-cresol, phenol, methylparaben, and propylparaben.
  • Glatiramer acetate is a well-known active pharmaceutical ingredient and the drug substance may either be obtained from a commercial source or it may be prepared in accordance with prior art publications using methods and equipment described therein. See e.g. WO 95/31990.
  • the formulation of the present invention comprises one or more preservatives selected from the group consisting of benzyl alcohol, m-cresol, phenol, methylparaben, and propylparaben.
  • the preservative is benzyl alcohol or m-cresol. Most preferably, benzyl alcohol is used.
  • the formulation according to the present invention further comprises one or more pharmaceutically acceptable excipients, such as mannitol which is present in the commercial product.
  • the one or more pharmaceutically acceptable excipients are selected from mannitol, sorbitol, trehalose, histidine, and polyoxyethylene sorbitan fatty acid esters (e.g. polysorbates), preferably selected from mannitol and a polysorbate. These excipients act as tonicity agents and/or stabilizers.
  • the formulation according to the present invention comprises from 0.005 wt to 3 wt of the preservative.
  • the formulation comprises from 0.01 wt to 2 wt of a preservative, more preferably from 0.1 wt to 2 wt , most preferably from 0.1 wt% to 0.5 wt%.
  • the formulation according to the present invention typically comprises from 40 mg to 560 mg of glatiramer acetate.
  • the formulation comprises from 120 mg to 560 mg, more preferably from 120 mg to 240 mg of glatiramer acetate.
  • the present invention also relates to a multiple dose device (or multiple dose medication dispensing device) comprising a formulation according to any one of the embodiments described hereinabove.
  • a multiple dose device or multiple dose medication dispensing device
  • suitable devices are well-known to the person skilled in this art.
  • the device according to the present invention is in the form of a multiple dose injection pen.
  • MFI Micro flow Imaging

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Medicinal Preparation (AREA)

Abstract

La présente invention concerne une formulation comprenant de multiples doses d'acétate de glatiramère et un ou plusieurs conservateurs sélectionnés dans le groupe constitué d'alcool benzylique, de m-crésol, de phénol, de méthylparabène et de propylparabène. De préférence, le conservateur est de l'alcool benzylique ou du m-crésol, mieux encore de l'alcool benzylique.
PCT/EP2014/053019 2013-02-19 2014-02-17 Formulation multidose d'acétate de glatiramère Ceased WO2014128079A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2013053289 2013-02-19
EPPCT/EP2013/053289 2013-02-19

Publications (1)

Publication Number Publication Date
WO2014128079A1 true WO2014128079A1 (fr) 2014-08-28

Family

ID=50150694

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2014/053019 Ceased WO2014128079A1 (fr) 2013-02-19 2014-02-17 Formulation multidose d'acétate de glatiramère

Country Status (1)

Country Link
WO (1) WO2014128079A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9155775B1 (en) 2015-01-28 2015-10-13 Teva Pharmaceutical Industries, Ltd. Process for manufacturing glatiramer acetate product

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995031990A1 (fr) 1994-05-24 1995-11-30 Yeda Research And Development Co., Ltd. Ameliorations apportees a des compositions de copolymeres contenant du copolymere-1
US20070161566A1 (en) * 2006-01-11 2007-07-12 Teva Pharmaceutical Industries, Ltd. Method of treating multiple sclerosis
EP2275086A1 (fr) * 2009-07-15 2011-01-19 Teva Pharmaceutical Industries, Ltd. Formulation de volume réduit d'acétate de glatiramère et procédés d'administration
WO2011080733A1 (fr) * 2010-01-04 2011-07-07 Mapi Pharma Limited Systèmes de dépôt comprenant du glatiramer ou un sel pharmacologiquement acceptable de celui-ci
WO2011086470A1 (fr) * 2010-01-13 2011-07-21 Ramot At Tel-Aviv University Ltd Traitement de la sclérose en plaques

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995031990A1 (fr) 1994-05-24 1995-11-30 Yeda Research And Development Co., Ltd. Ameliorations apportees a des compositions de copolymeres contenant du copolymere-1
US20070161566A1 (en) * 2006-01-11 2007-07-12 Teva Pharmaceutical Industries, Ltd. Method of treating multiple sclerosis
EP2275086A1 (fr) * 2009-07-15 2011-01-19 Teva Pharmaceutical Industries, Ltd. Formulation de volume réduit d'acétate de glatiramère et procédés d'administration
WO2011080733A1 (fr) * 2010-01-04 2011-07-07 Mapi Pharma Limited Systèmes de dépôt comprenant du glatiramer ou un sel pharmacologiquement acceptable de celui-ci
WO2011086470A1 (fr) * 2010-01-13 2011-07-21 Ramot At Tel-Aviv University Ltd Traitement de la sclérose en plaques

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9155775B1 (en) 2015-01-28 2015-10-13 Teva Pharmaceutical Industries, Ltd. Process for manufacturing glatiramer acetate product
EP3050556B1 (fr) 2015-01-28 2017-03-22 Teva Pharmaceutical Industries, Ltd. Procédé de fabrication d'un produit pharmaceutique à base d'acétate de glatiramer
KR101737295B1 (ko) 2015-01-28 2017-05-29 테바 파마슈티컬 인더스트리즈 리미티드 글라티라머 아세테이트 제품의 제조 방법
US9763993B2 (en) 2015-01-28 2017-09-19 Teva Pharmaceutical Industries Ltd. Process for manufacturing glatiramer acetate product
EA028811B1 (ru) * 2015-01-28 2018-01-31 Тева Фармасьютикал Индастриз Лтд. Способ изготовления фармацевтического препарата, содержащего ацетат глатирамера и маннит
RU2669769C2 (ru) * 2015-01-28 2018-10-16 Тева Фармасьютикал Индастриз Лтд. Способ получения продукта глатирамера ацетата

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