CA2942236C - Dosage form of siponimod - Google Patents

Dosage form of siponimod Download PDF

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Publication number
CA2942236C
CA2942236C CA2942236A CA2942236A CA2942236C CA 2942236 C CA2942236 C CA 2942236C CA 2942236 A CA2942236 A CA 2942236A CA 2942236 A CA2942236 A CA 2942236A CA 2942236 C CA2942236 C CA 2942236C
Authority
CA
Canada
Prior art keywords
siponimod
dosage form
amount
protective agent
moisture
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.)
Active
Application number
CA2942236A
Other languages
English (en)
French (fr)
Other versions
CA2942236A1 (en
Inventor
Philippe Michel Rene BOUILLOT
Emeric Reynaud
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.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of CA2942236A1 publication Critical patent/CA2942236A1/en
Application granted granted Critical
Publication of CA2942236C publication Critical patent/CA2942236C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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Classifications

    • 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
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • 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
    • 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
    • A61K31/397Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K9/16Agglomerates; 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
    • A61K9/20Pills, 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2077Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • 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
    • A61K9/2072Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
    • 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
    • A61K9/2806Coating materials
    • 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
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/2886Dragees; Coated pills or tablets, e.g. with film or compression coating having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5005Wall or coating material
    • A61K9/5021Organic macromolecular compounds
    • A61K9/5026Organic 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
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/5089Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04Antibacterial agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Transplantation (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CA2942236A 2014-04-10 2015-04-08 Dosage form of siponimod Active CA2942236C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201461977806P 2014-04-10 2014-04-10
US61/977,806 2014-04-10
PCT/IB2015/052552 WO2015155711A1 (en) 2014-04-10 2015-04-08 Immunosuppressant formulation

Publications (2)

Publication Number Publication Date
CA2942236A1 CA2942236A1 (en) 2015-10-15
CA2942236C true CA2942236C (en) 2023-08-29

Family

ID=53525213

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2942236A Active CA2942236C (en) 2014-04-10 2015-04-08 Dosage form of siponimod

Country Status (23)

Country Link
US (5) US20170027906A1 (cg-RX-API-DMAC7.html)
EP (1) EP3129006B1 (cg-RX-API-DMAC7.html)
JP (2) JP6679495B2 (cg-RX-API-DMAC7.html)
KR (1) KR102466348B1 (cg-RX-API-DMAC7.html)
CN (1) CN106163502B (cg-RX-API-DMAC7.html)
AR (1) AR100002A1 (cg-RX-API-DMAC7.html)
AU (1) AU2015246038C1 (cg-RX-API-DMAC7.html)
CA (1) CA2942236C (cg-RX-API-DMAC7.html)
CL (1) CL2016002560A1 (cg-RX-API-DMAC7.html)
DK (1) DK3129006T3 (cg-RX-API-DMAC7.html)
EA (1) EA201692043A1 (cg-RX-API-DMAC7.html)
ES (1) ES2865451T3 (cg-RX-API-DMAC7.html)
HU (1) HUE054245T2 (cg-RX-API-DMAC7.html)
IL (1) IL247599B (cg-RX-API-DMAC7.html)
MX (1) MX2016013236A (cg-RX-API-DMAC7.html)
PE (1) PE20161385A1 (cg-RX-API-DMAC7.html)
PH (1) PH12016501841A1 (cg-RX-API-DMAC7.html)
PL (1) PL3129006T3 (cg-RX-API-DMAC7.html)
PT (1) PT3129006T (cg-RX-API-DMAC7.html)
SG (1) SG11201607354PA (cg-RX-API-DMAC7.html)
SI (1) SI3129006T1 (cg-RX-API-DMAC7.html)
TW (1) TW201622707A (cg-RX-API-DMAC7.html)
WO (1) WO2015155711A1 (cg-RX-API-DMAC7.html)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101951966B1 (ko) 2011-01-07 2019-02-25 노파르티스 아게 면역억제제 제제
JP6679495B2 (ja) * 2014-04-10 2020-04-15 ノバルティス アーゲー 免疫抑制製剤
US11434200B2 (en) 2017-03-09 2022-09-06 Novartis Ag Solid forms comprising an oxime ether compound and a coformer, compositions and methods of use thereof
US11629124B2 (en) 2017-03-09 2023-04-18 Novartis Ag Solid forms comprising an oxime ether compound, compositions and methods of use thereof
WO2019064185A1 (en) 2017-09-27 2019-04-04 Novartis Ag PARENTERAL FORMULATION COMPRISING SITOMOD
CA3074416A1 (en) 2017-09-29 2019-04-04 Novartis Ag Dosing regimen of siponimod
WO2019064212A1 (en) 2017-09-29 2019-04-04 Novartis Ag DOSAGE DIAGRAM OF SIPONIMOD
WO2019144094A1 (en) * 2018-01-22 2019-07-25 Teva Pharmaceuticals International Gmbh Crystalline siponimod fumaric acid and polymorphs thereof
CN109908095A (zh) * 2019-04-08 2019-06-21 肇庆学院 一种西尼莫德片剂及制备方法
WO2021214717A1 (en) 2020-04-23 2021-10-28 Novartis Ag Dosing regimen for the use of siponimod for the treatment of acute respiratory distress syndrome
CN113633632A (zh) * 2021-09-09 2021-11-12 暨南大学附属第一医院(广州华侨医院) siponimod在制备抗肿瘤转移药物中的应用
WO2024126409A1 (en) 2022-12-12 2024-06-20 Synthon B.V. Pharmaceutical composition of siponimod

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HUE027696T2 (en) * 2007-10-12 2016-10-28 Novartis Ag Preparations containing sphingosine-1-phosphate (S1P) receptor modulators
GB2473399B (en) 2008-07-16 2012-06-27 Nec Corp Method for reporting information about result of Iu-UP protocol negotiation protocol conversion method,communication network system
US20120115840A1 (en) 2008-12-18 2012-05-10 Lech Ciszewski Hemifumarate salt of 1-[4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl]-azetidine-3-carboxylic acid
BRPI0922457A2 (pt) 2008-12-18 2015-12-15 Novartis Ag forma polimórfica de ácido 1-(4-{1-[(e)-4-ciclo-hexil-3-trifluormetil-benziloxi-imino]-etil)-2-etil-benzil)-azetidino-3-carboxílico"
CA2981830A1 (en) * 2008-12-22 2010-07-01 Novartis Ag Dosage regimen of an s1p receptor agonist
CN101480374A (zh) * 2009-01-20 2009-07-15 苏州中化药品工业有限公司 一种稳定的固体药物组合物
KR101951966B1 (ko) * 2011-01-07 2019-02-25 노파르티스 아게 면역억제제 제제
WO2012095853A1 (en) * 2011-01-10 2012-07-19 Novartis Pharma Ag Modified release formulations comprising sip receptor modulators
JP6679495B2 (ja) * 2014-04-10 2020-04-15 ノバルティス アーゲー 免疫抑制製剤

Also Published As

Publication number Publication date
DK3129006T3 (da) 2021-04-19
JP2020097591A (ja) 2020-06-25
AU2015246038C1 (en) 2018-05-31
KR102466348B1 (ko) 2022-11-10
AU2015246038A1 (en) 2016-09-22
SG11201607354PA (en) 2016-10-28
US20210161860A1 (en) 2021-06-03
IL247599A0 (en) 2016-11-30
AU2015246038B2 (en) 2017-11-30
IL247599B (en) 2020-08-31
PE20161385A1 (es) 2017-01-05
EA201692043A1 (ru) 2017-02-28
MX2016013236A (es) 2017-01-16
CA2942236A1 (en) 2015-10-15
EP3129006A1 (en) 2017-02-15
EP3129006B1 (en) 2021-01-27
US20250073203A1 (en) 2025-03-06
HUE054245T2 (hu) 2021-08-30
CL2016002560A1 (es) 2017-04-07
TW201622707A (zh) 2016-07-01
US20180207128A1 (en) 2018-07-26
PH12016501841A1 (en) 2017-01-09
US20190328705A1 (en) 2019-10-31
WO2015155711A4 (en) 2015-12-10
ES2865451T3 (es) 2021-10-15
CN106163502A (zh) 2016-11-23
JP2017510602A (ja) 2017-04-13
PT3129006T (pt) 2021-04-09
AR100002A1 (es) 2016-08-31
KR20160144366A (ko) 2016-12-16
CN106163502B (zh) 2020-12-01
JP6679495B2 (ja) 2020-04-15
PL3129006T3 (pl) 2021-07-05
SI3129006T1 (sl) 2021-08-31
US20170027906A1 (en) 2017-02-02
WO2015155711A1 (en) 2015-10-15

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