HRP20230613T1 - Tableta koja sadrži derivat metoksiureje i čestice manitola - Google Patents

Tableta koja sadrži derivat metoksiureje i čestice manitola Download PDF

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Publication number
HRP20230613T1
HRP20230613T1 HRP20230613TT HRP20230613T HRP20230613T1 HR P20230613 T1 HRP20230613 T1 HR P20230613T1 HR P20230613T T HRP20230613T T HR P20230613TT HR P20230613 T HRP20230613 T HR P20230613T HR P20230613 T1 HRP20230613 T1 HR P20230613T1
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HR
Croatia
Prior art keywords
methoxyurea
tablet
film envelope
tetrahydrothieno
difluorobenzyl
Prior art date
Application number
HRP20230613TT
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English (en)
Inventor
Ikuro YAMANE
Yukihiro Nomura
Yutaka Nishimoto
Wataru Hoshina
Original Assignee
Takeda Pharmaceutical Company Limited
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Application filed by Takeda Pharmaceutical Company Limited filed Critical Takeda Pharmaceutical Company Limited
Publication of HRP20230613T1 publication Critical patent/HRP20230613T1/hr

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    • 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
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • 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
    • 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
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with 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
    • A61K47/06Organic 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
    • A61K47/10Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • 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
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • A61K47/34Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
    • 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
    • A61K9/28Dragees; 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (10)

1. Tableta koja sadrži: N-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metoksi-3-piridazinil)-2,4-diokso-1,2,3,4-tetrahidrotieno[2,3-d]pirimidin-6-il)fenil)-N'-metoksiureju ili njezinu sol u količini od 40 mg mjereno na temelju slobodnog oblika N-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metoksi-3-piridazinil)-2,4-diokso-1,2,3,4-tetrahidrotieno[2,3-d]pirimidin-6-il)fenil)-N'-metoksiureje, 51 mg čestica D-manitola koje imaju prosječnu veličinu čestica od 70 - 200 µm, 5 mg natrijevog škrobnog glikolata, 3 mg hidroksipropilceluloze, i 1 mg magnezijevog stearata.
2. Tableta prema zahtjevu 1, naznačena time što dodatno sadrži filmsku ovojnicu, pri čemu filmska ovojnica sadrži hidroksipropilmetilcelulozu, titanijev oksid i crveni željezov oksid.
3. Tableta prema zahtjevu 1, naznačena time što dodatno sadrži filmsku ovojnicu, pri čemu filmska ovojnica sadrži 3,56 mg hidroksipropilmetilceluloze, 0,40 mg titanijevog oksida i 0,04 mg crvenog željezovog oksida.
4. Tableta koja sadrži: N-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metoksi-3-piridazinil)-2,4-diokso-1,2,3,4-tetrahidrotieno[2,3-d]pirimidin-6-il)fenil)-N'-metoksiureju ili njezinu sol u količini od 120 mg mjereno na temelju slobodnog oblika N-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metoksi-3-piridazinil)-2,4-diokso-1,2,3,4-tetrahidrotieno[2,3-d]pirimidin-6-il)fenil)-N'-metoksiureje, 153 mg čestica D-manitola koje imaju prosječnu veličinu čestica od 70 - 200 µm, 15 mg natrijevog škrobnog glikolata, 9 mg hidroksipropilceluloze, i 3 mg magnezijevog stearata.
5. Tableta prema zahtjevu 4, naznačena time što dodatno sadrži filmsku ovojnicu, pri čemu filmska ovojnica sadrži hidroksipropilmetilcelulozu, titanijev oksid i crveni željezov oksid.
6. Tableta koja sadrži: N-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metoksi-3-piridazinil)-2,4-diokso-1,2,3,4-tetrahidrotieno[2,3-d]pirimidin-6-il)fenil)-N'-metoksiureju ili njezinu sol u količini od 80 mg mjereno na temelju slobodnog oblika N-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metoksi-3-piridazinil)-2,4-diokso-1,2,3,4-tetrahidrotieno[2,3-d]pirimidin-6-il)fenil)-N'-metoksiureje, 102 mg čestica D-manitola koje imaju prosječnu veličinu čestica od 70 - 200 µm, 10 mg natrijevog škrobnog glikolata, 6 mg hidroksipropilceluloze, i 2 mg magnezijevog stearata.
7. Tableta prema zahtjevu 6, naznačena time što dodatno sadrži filmsku ovojnicu, pri čemu filmska ovojnica sadrži hidroksipropilmetilcelulozu, titanijev oksid i crveni željezov oksid.
8. Tableta prema zahtjevu 6, naznačena time što dodatno sadrži filmsku ovojnicu, pri čemu filmska ovojnica sadrži 7,12 mg hidroksipropilmetilceluloze, 0,80 mg titanijevog oksida i 0,08 mg crvenog željezovog oksida.
9. Tableta prema bilo kojem od zahtjeva 1-8, naznačena time što čestice D-manitola imaju prosječnu veličinu čestica od 75 - 150 µm.
10. Postupak za izradu tablete prema bilo kojem od zahtjeva 1, 4 ili 6, naznačen time što navedeni postupak obuhvaća: 1) miješanje N-(4-(1-(2,6-difluorobenzil)-5-((dimetilamino)metil)-3-(6-metoksi-3-piridazinil)-2,4-diokso-1,2,3,4-tetrahidrotieno[2,3-d]pirimidin-6-il)fenil)-N'-metoksiureje ili njezine soli s česticama D-manitola koje imaju prosječnu veličinu čestica od 70 - 200 µm i natrijevog škrobnog glikolata; 2) raspršivanje u smjesu iz koraka 1) otopine hidroksipropilceluloze u otapalu ili mediju za raspršivanje; 3) sušenje ili prosijavanje smjese iz koraka 2) da se dobije granulirani prah ili prosijani prah; 4) dodavanje magnezijevog stearata u granulirani prah ili prosijani prah iz koraka 3) i miješanje da se dobiju granule za tabletiranje; 5) tabletiranje granula iz koraka 4) da se dobije jezgra tablete; i, izborno, 6) raspršivanje otopine za oblaganje filmom na jezgru tablete iz koraka 5) kako bi se dobila tableta obložena filmom.
HRP20230613TT 2015-02-26 2016-02-25 Tableta koja sadrži derivat metoksiureje i čestice manitola HRP20230613T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2015037462 2015-02-26
PCT/JP2016/055540 WO2016136849A1 (ja) 2015-02-26 2016-02-25 固形製剤
EP16755593.7A EP3263110B1 (en) 2015-02-26 2016-02-25 A tablet comprising a methoxyurea derivative and mannitol particles

Publications (1)

Publication Number Publication Date
HRP20230613T1 true HRP20230613T1 (hr) 2023-09-29

Family

ID=56789547

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HRP20230613TT HRP20230613T1 (hr) 2015-02-26 2016-02-25 Tableta koja sadrži derivat metoksiureje i čestice manitola

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US (2) US10350170B2 (hr)
EP (2) EP4233847A1 (hr)
JP (1) JP6730978B2 (hr)
CN (1) CN107249590A (hr)
AU (1) AU2016224503B2 (hr)
BR (1) BR112017018173A2 (hr)
CA (1) CA2978223A1 (hr)
CY (1) CY1126118T1 (hr)
DK (1) DK3263110T3 (hr)
ES (1) ES2950995T3 (hr)
FI (1) FI3263110T3 (hr)
HR (1) HRP20230613T1 (hr)
HU (1) HUE062269T2 (hr)
IL (1) IL254132B (hr)
LT (1) LT3263110T (hr)
MX (1) MX2017010945A (hr)
MY (1) MY180680A (hr)
PL (1) PL3263110T3 (hr)
PT (1) PT3263110T (hr)
RS (1) RS64377B1 (hr)
SI (1) SI3263110T1 (hr)
TW (1) TWI744224B (hr)
WO (1) WO2016136849A1 (hr)

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EP2900675B1 (en) 2012-09-28 2019-03-06 Takeda Pharmaceutical Company Limited Production method of thienopyrimidine derivative
MX2019003733A (es) * 2016-09-30 2019-09-26 Myovant Sciences Gmbh Tratamiento de cancer de prostata.
HRP20220708T1 (hr) 2016-09-30 2022-07-22 Myovant Sciences Gmbh Postupci liječenja fibroida maternice i endometrioze
WO2019178304A1 (en) 2018-03-14 2019-09-19 Teva Pharmaceuticals International Gmbh Solid state forms of relugolix
CA3145993A1 (en) 2019-08-02 2021-02-11 Johnson Matthey Public Limited Company Solid-state forms of relugolix
WO2021230308A1 (ja) 2020-05-15 2021-11-18 塩野義製薬株式会社 不純物の生成を抑制した医薬組成物
KR20230028732A (ko) 2020-05-29 2023-03-02 마이오반트 사이언시즈 게엠베하 고나도트로핀 방출 호르몬 길항제의 복합 고형 경구 투여 형태
JP2023549196A (ja) 2020-11-11 2023-11-22 ミオバント サイエンシズ ゲーエムベーハー レルゴリクスの投与方法
WO2023066941A1 (en) 2021-10-18 2023-04-27 Myovant Sciences Gmbh Crystalline form of an ethanol solvate of n-(4-(1-(2,6-difluorobenzyl)-5-((dimethylamino)methyl)-3-(6-methoxy-3-pyridazinyl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl)phenyl)-n'-methoxyurea
CN115671069A (zh) * 2022-11-24 2023-02-03 北京鑫开元医药科技有限公司 一种瑞卢戈利片剂及其制备方法

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JP2015037462A (ja) 2012-06-01 2015-02-26 株式会社コナミデジタルエンタテインメント ゲーム装置、ゲーム方法、及びプログラム
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Also Published As

Publication number Publication date
CN107249590A (zh) 2017-10-13
RS64377B1 (sr) 2023-08-31
ES2950995T3 (es) 2023-10-17
MX2017010945A (es) 2018-07-06
CY1126118T1 (el) 2023-11-15
DK3263110T3 (da) 2023-07-31
AU2016224503A1 (en) 2017-09-14
LT3263110T (lt) 2023-07-10
US20180036250A1 (en) 2018-02-08
MY180680A (en) 2020-12-06
EP4233847A1 (en) 2023-08-30
PL3263110T3 (pl) 2023-11-06
PT3263110T (pt) 2023-08-01
EP3263110A4 (en) 2018-11-07
EP3263110B1 (en) 2023-05-10
WO2016136849A1 (ja) 2016-09-01
HUE062269T2 (hu) 2023-10-28
TW201639575A (zh) 2016-11-16
JPWO2016136849A1 (ja) 2017-12-07
IL254132B (en) 2020-02-27
FI3263110T3 (fi) 2023-07-25
EP3263110A1 (en) 2018-01-03
JP6730978B2 (ja) 2020-07-29
NZ735026A (en) 2021-09-24
AU2016224503B2 (en) 2021-07-08
US10350170B2 (en) 2019-07-16
BR112017018173A2 (pt) 2018-04-10
IL254132A0 (en) 2017-10-31
SI3263110T1 (sl) 2023-09-29
CA2978223A1 (en) 2016-09-01
TWI744224B (zh) 2021-11-01
US20200000730A1 (en) 2020-01-02

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