CL2016002560A1 - Forma de dosificación farmacéutica sólida oral que comprende siponimod, un agente protector de la humedad y opcionalmente un excipiente farmacéutico; procedimiento de preparación. - Google Patents

Forma de dosificación farmacéutica sólida oral que comprende siponimod, un agente protector de la humedad y opcionalmente un excipiente farmacéutico; procedimiento de preparación.

Info

Publication number
CL2016002560A1
CL2016002560A1 CL2016002560A CL2016002560A CL2016002560A1 CL 2016002560 A1 CL2016002560 A1 CL 2016002560A1 CL 2016002560 A CL2016002560 A CL 2016002560A CL 2016002560 A CL2016002560 A CL 2016002560A CL 2016002560 A1 CL2016002560 A1 CL 2016002560A1
Authority
CL
Chile
Prior art keywords
dosage form
optionally
siponimod
protective agent
pharmaceutical excipient
Prior art date
Application number
CL2016002560A
Other languages
English (en)
Inventor
Philippe Michel Rene Bouillot
Emeric Reynaud
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 CL2016002560A1 publication Critical patent/CL2016002560A1/es

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1617—Organic compounds, e.g. phospholipids, fats
    • A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
    • 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
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2013—Organic compounds, e.g. phospholipids, fats
    • A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, 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
    • A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
    • A61K9/2081—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets with microcapsules or coated microparticles according to A61K9/50
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, 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
    • A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209—Layered 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
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806—Coating materials
    • A61K9/2833—Organic macromolecular compounds
    • A61K9/286—Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2886—Dragees; 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
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules 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
    • A61K9/5005—Wall or coating material
    • A61K9/5021—Organic macromolecular compounds
    • A61K9/5026—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • 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
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50—Microcapsules 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
    • A61K9/5089—Processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection

Abstract

En la presente solicitud se describe a una forma de dosificación sólida oral que contiene entre 0,2 a 12% (p/p) de siponimod, entre 1 y 8% (p/p) de un agente protector de humedad, y entre 80 y 98,8% de excipiente (s) farmacéutico (s); y el procedimiento de preparación de la forma de dosificación que comprende las etapas de: (i) proporcionar siponimod, (ii) pre-mezclar los compuestos de la etapa i) con un agente protector de humedad y opcionalmente un excipiente farmacéutico, (iii) combinar la mezcla de la etapa ii) con el o los excipiente (s) farmacéutico (s), (iv) comprimir la mezcla de la etapa iii) a una forma de dosificación, opcionalmente, el recubrimiento de película de la forma de dosificación.
CL2016002560A 2014-04-10 2016-10-07 Forma de dosificación farmacéutica sólida oral que comprende siponimod, un agente protector de la humedad y opcionalmente un excipiente farmacéutico; procedimiento de preparación. CL2016002560A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201461977806P 2014-04-10 2014-04-10

Publications (1)

Publication Number Publication Date
CL2016002560A1 true CL2016002560A1 (es) 2017-04-07

Family

ID=53525213

Family Applications (1)

Application Number Title Priority Date Filing Date
CL2016002560A CL2016002560A1 (es) 2014-04-10 2016-10-07 Forma de dosificación farmacéutica sólida oral que comprende siponimod, un agente protector de la humedad y opcionalmente un excipiente farmacéutico; procedimiento de preparación.

Country Status (23)

Country Link
US (4) US20170027906A1 (es)
EP (1) EP3129006B1 (es)
JP (2) JP6679495B2 (es)
KR (1) KR102466348B1 (es)
CN (1) CN106163502B (es)
AR (1) AR100002A1 (es)
AU (1) AU2015246038C1 (es)
CA (1) CA2942236C (es)
CL (1) CL2016002560A1 (es)
DK (1) DK3129006T3 (es)
EA (1) EA201692043A1 (es)
ES (1) ES2865451T3 (es)
HU (1) HUE054245T2 (es)
IL (1) IL247599B (es)
MX (1) MX2016013236A (es)
PE (1) PE20161385A1 (es)
PH (1) PH12016501841A1 (es)
PL (1) PL3129006T3 (es)
PT (1) PT3129006T (es)
SG (1) SG11201607354PA (es)
SI (1) SI3129006T1 (es)
TW (1) TW201622707A (es)
WO (1) WO2015155711A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11629124B2 (en) 2017-03-09 2023-04-18 Novartis Ag Solid forms comprising an oxime ether compound, compositions and methods of use thereof
MX2020007270A (es) 2017-09-27 2020-08-17 Novartis Ag Formulacion parenteral que comprende siponimod.
RU2020114750A (ru) 2017-09-29 2021-10-29 Новартис Аг Схема введения доз сипонимода
JP2020535139A (ja) 2017-09-29 2020-12-03 ノバルティス アーゲー シポニモドの投与レジメン
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

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2864671T3 (es) * 2007-10-12 2021-10-14 Novartis Ag Composiciones que comprenden moduladores del receptor de esfingosina 1-fosfato (s1p)
JP5190815B2 (ja) 2008-07-16 2013-04-24 日本電気株式会社 Ｉｕ−ＵＰプロトコルのネゴシエーション結果情報の通知方法、プロトコル変換方法、通信ネットワークシステム、インターワーキング装置、ＩｕＵＰネゴシエーション結果情報取得装置及びコンピュータ読み取り可能な情報記録媒体
KR20110096584A (ko) 2008-12-18 2011-08-30 노파르티스 아게 1-［4-［1-(4-시클로헥실-3-트리플루오로메틸-벤질옥시이미노)-에틸］-2-에틸-벤질］-아제티딘-3-카르복실산의 헤미푸마레이트 염
RU2011129230A (ru) 2008-12-18 2013-01-27 Новартис Аг Новая полиморфная форма 1-[4-[1-(4-циклогексил-3-трифторметилбензилоксиимино)этил]-2-этилбензил]азетидин-3-карбоновой кислоты
NZ593427A (en) * 2008-12-22 2013-11-29 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
SI2661261T1 (sl) * 2011-01-07 2019-11-29 Novartis Ag Formulacije imunosupresivov
WO2012095853A1 (en) * 2011-01-10 2012-07-19 Novartis Pharma Ag Modified release formulations comprising sip receptor modulators

Also Published As

Publication number Publication date
JP2017510602A (ja) 2017-04-13
PH12016501841A1 (en) 2017-01-09
JP2020097591A (ja) 2020-06-25
EA201692043A1 (ru) 2017-02-28
AU2015246038A1 (en) 2016-09-22
US20210161860A1 (en) 2021-06-03
HUE054245T2 (hu) 2021-08-30
JP6679495B2 (ja) 2020-04-15
AU2015246038B2 (en) 2017-11-30
US20190328705A1 (en) 2019-10-31
KR20160144366A (ko) 2016-12-16
WO2015155711A1 (en) 2015-10-15
CN106163502B (zh) 2020-12-01
IL247599A0 (en) 2016-11-30
KR102466348B1 (ko) 2022-11-10
WO2015155711A4 (en) 2015-12-10
EP3129006B1 (en) 2021-01-27
AR100002A1 (es) 2016-08-31
US20180207128A1 (en) 2018-07-26
ES2865451T3 (es) 2021-10-15
SG11201607354PA (en) 2016-10-28
IL247599B (en) 2020-08-31
SI3129006T1 (sl) 2021-08-31
MX2016013236A (es) 2017-01-16
EP3129006A1 (en) 2017-02-15
CA2942236A1 (en) 2015-10-15
PL3129006T3 (pl) 2021-07-05
US20170027906A1 (en) 2017-02-02
CA2942236C (en) 2023-08-29
TW201622707A (zh) 2016-07-01
AU2015246038C1 (en) 2018-05-31
PE20161385A1 (es) 2017-01-05
DK3129006T3 (da) 2021-04-19
CN106163502A (zh) 2016-11-23
PT3129006T (pt) 2021-04-09

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