HRP20201140T1 - Oralna farmaceutska kompozicija - Google Patents

Oralna farmaceutska kompozicija Download PDF

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Publication number
HRP20201140T1
HRP20201140T1 HRP20201140TT HRP20201140T HRP20201140T1 HR P20201140 T1 HRP20201140 T1 HR P20201140T1 HR P20201140T T HRP20201140T T HR P20201140TT HR P20201140 T HRP20201140 T HR P20201140T HR P20201140 T1 HRP20201140 T1 HR P20201140T1
Authority
HR
Croatia
Prior art keywords
uncoated tablet
tablet according
trifluorothymidine
salt
iminopyrrolidin
Prior art date
Application number
HRP20201140TT
Other languages
English (en)
Inventor
Yoshito Ohnishi
Tetsuo Ogata
Original Assignee
Taiho Pharmaceutical Co., Ltd.
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=48984244&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20201140(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Taiho Pharmaceutical Co., Ltd. filed Critical Taiho Pharmaceutical Co., Ltd.
Publication of HRP20201140T1 publication Critical patent/HRP20201140T1/hr

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • 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
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • 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
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • 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
    • A61K9/20Pills, 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
    • 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
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (13)

1. Neobložena tableta koja sadrži α,α,α-trifluorotimidin i 5-kloro-6-(2-iminopirolidin-1-il)metil-2,4(1H,3H)-pirimidin dion hidroklorid kao aktivni sastojak; koja sadrži šećerni alkohol ili disaharid kao ekscipijens, jedan ili više odabranih iz grupe koja se sastoji od hidrogeniziranih ulja i stearinske kiseline kao lubrikanta, i koja je bez aditiva koji sadrži sol metala.
2. Neobložena tableta prema patentnom zahtjevu 1, gdje je sol metala odabrana od soli alkalnih metala ili soli zemnoalkalnih metala.
3. Neobložena tableta prema patentnom zahtjevu 1 ili 2, gdje je sol metala odabrana od soli natrija, soli kalija, soli kalcija, i soli magnezija.
4. Neobložena tableta prema patentnom zahtjevu 1, gdje šećerni alkohol ili disaharid sadržan kao ekscipijens je jedan ili više odabranih od laktoze, saharoze, eritritola, i manitola.
5. Neobložena tableta prema patentnom zahtjevu 4, gdje je sadržaj šećernog alkohola ili disaharida 3.6 dijelova po masi ili više bazirano na 1 dijelu po masi α,α,α-trifluorotimidina.
6. Neobložena tableta prema bilo kom od patentnih zahtjeva 1 do 5, koja dalje sadrži jedan ili više odabranih od nisko-supstituirane hidroksipropil celuloze, kukuruznog škroba, djelomično preželatiniziranog škroba, karmeloze, i krospovidona kao agens za raspadanje.
7. Neobložena tableta prema patentnom zahtjevu 6, gdje je sadržaj agensa za raspadanje od 2 do 16% po masi u ukupnoj količini kompozicije.
8. Neobložena tableta prema patentnom zahtjevu 1, gdje je sadržaj lubrikanta od 0.001 do 3% po masi u ukupnoj kompoziciji.
9. Neobložena tableta prema bilo kom od patentnih zahtjeva 1 do 8, koja sadrži α,α,α-trifluorotimidin i 5-kloro-6-(2-iminopirolidin-1-il)metil-2,4(1H,3H)-pirimidin dion hidroklorid u molarnom odnosu od 1:0.5.
10. Neobložena tableta prema bilo kom od patentnih zahtjeva 1 do 9, gdje neobložena tableta sadrži α,α,α-trifluorotimidin i 5-kloro-6-(2-iminopirolidin-1-il)metil-2,4(1H,3H)-pirimidin dion hidroklorid kao aktivne sastojke u molarnom odnosu od 1:0.5; sadrži jedan ili više odabranih od laktoze, saharoze, ili manitola kao ekscipijens; i jedan ili više odabranih od nisko-supstituirane hidroksipropil celuloze, kukuruznog škroba, djelomično preželatiniziranog škroba, i karmeloza kao agens za raspadanje.
11. Oralna farmaceutska formulacija koja sadrži neobloženu tabletu prema bilo kojem od patentnih zahtjeva 1 do 10, gdje je tableta obložena.
12. Obložena tableta prema patentnom zahtjevu 11, gdje tableta sadrži magnezij stearat na površini.
13. Metoda za stabilizaciju neobložene tablete koja sadrži α,α,α-trifluorotimidin i 5-kloro-6-(2-iminopirolidin-1-il)metil-2,4(1H,3H)-pirimidin dion hidroklorid kao aktivni sastojak; koja sadrži šećerni alkohol ili disaharid kao ekscipijens, i jedan ili više odabranih iz grupe koja se sastoji od hidrogeniziranih ulja i stearinske kiseline kao lubrikant, naznačena time da se ne dodaje aditiv koji sadrži sol metala.
HRP20201140TT 2012-02-15 2020-07-21 Oralna farmaceutska kompozicija HRP20201140T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
JP2012031144 2012-02-15
EP13749905.9A EP2815752B1 (en) 2012-02-15 2013-02-14 Oral pharmaceutical composition
PCT/JP2013/053514 WO2013122135A1 (ja) 2012-02-15 2013-02-14 経口用医薬組成物

Publications (1)

Publication Number Publication Date
HRP20201140T1 true HRP20201140T1 (hr) 2020-10-30

Family

ID=48984244

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20201140TT HRP20201140T1 (hr) 2012-02-15 2020-07-21 Oralna farmaceutska kompozicija

Country Status (24)

Country Link
US (3) US20140363512A1 (hr)
EP (1) EP2815752B1 (hr)
JP (1) JP5798642B2 (hr)
KR (1) KR101740105B1 (hr)
CN (1) CN104105490A (hr)
AU (1) AU2013219296B2 (hr)
CA (1) CA2863018C (hr)
CY (1) CY1123372T1 (hr)
DK (1) DK2815752T3 (hr)
ES (1) ES2804674T3 (hr)
HK (1) HK1199821A1 (hr)
HR (1) HRP20201140T1 (hr)
HU (1) HUE050840T2 (hr)
LT (1) LT2815752T (hr)
MX (1) MX365313B (hr)
MY (1) MY155938A (hr)
PL (1) PL2815752T3 (hr)
PT (1) PT2815752T (hr)
RS (1) RS60552B1 (hr)
RU (1) RU2639473C2 (hr)
SG (1) SG11201403875VA (hr)
SI (1) SI2815752T1 (hr)
TW (1) TWI526210B (hr)
WO (1) WO2013122135A1 (hr)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI526210B (zh) 2012-02-15 2016-03-21 Taiho Pharmaceutical Co Ltd Oral pharmaceutical composition
CN106551946B (zh) * 2015-09-24 2020-02-14 江苏奥赛康药业有限公司 一种含三氟胸苷和盐酸替比嘧啶的药物组合物及制备方法
CN106913580A (zh) * 2015-12-27 2017-07-04 南京圣和药业股份有限公司 一种含曲氟尿苷盐酸替哌拉索的药物组合物及其应用
CN106018573B (zh) * 2016-03-16 2018-09-18 江苏悦兴药业有限公司 一种tas-102中盐酸替比拉西的纯度检测方法
CN105963271A (zh) * 2016-06-01 2016-09-28 国药心制药有限公司 一种药用辅料组合物及一种曲氟尿苷、盐酸替匹嘧啶薄膜衣片
US10866219B2 (en) 2017-12-22 2020-12-15 Taiho Pharmaceutical Co., Ltd. Method for detecting trifluridine- and/or tipiracil-related substance
WO2019124544A1 (ja) 2017-12-22 2019-06-27 大鵬薬品工業株式会社 トリフルリジン及び/又はチピラシル由来の類縁物質の検出方法
WO2019135405A1 (ja) 2018-01-05 2019-07-11 大鵬薬品工業株式会社 トリフルリジン由来の類縁物質の検出方法
US10816517B2 (en) 2018-01-05 2020-10-27 Taiho Pharmaceutical Co., Ltd. Method for detecting trifluridine-related substance by high-performance liquid chromatography
US11730753B2 (en) * 2018-03-03 2023-08-22 Natco Pharma Limited Stable pharmaceutical compositions comprising trifluridine and tipiracil hydrochloride
CN114917201B (zh) * 2022-06-14 2024-05-31 国药一心制药有限公司 一种曲氟尿苷替匹嘧啶片剂及其制备方法

Family Cites Families (13)

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Publication number Priority date Publication date Assignee Title
US5232706A (en) * 1990-12-31 1993-08-03 Esteve Quimica, S.A. Oral pharmaceutical preparation containing omeprazol
JP3088757B2 (ja) * 1995-03-29 2000-09-18 大鵬薬品工業株式会社 ウラシル誘導体並びにそれを含有する抗腫瘍効果増強剤及び抗腫瘍剤
JPH11322604A (ja) * 1998-05-06 1999-11-24 Pola Chem Ind Inc ジフェニルピペラジン化合物を含有する製剤
JP4110347B2 (ja) 1999-11-05 2008-07-02 大鵬薬品工業株式会社 抗hiv剤
US6316029B1 (en) * 2000-05-18 2001-11-13 Flak Pharma International, Ltd. Rapidly disintegrating solid oral dosage form
JP4601934B2 (ja) * 2003-10-06 2010-12-22 ナガセ医薬品株式会社 ユビデカレノン錠
JP2005314413A (ja) * 2004-04-02 2005-11-10 Ono Pharmaceut Co Ltd 経口投与用医薬組成物
AU2006209547C1 (en) * 2005-01-26 2022-04-07 Taiho Pharmaceutical Co., Ltd. Anticancer drug containing alpha,alpha,alpha-trifluorothymidine and thymidine phosphorylase inhibitor
US7799783B2 (en) * 2005-01-26 2010-09-21 Taiho Pharmaceutical Co., Ltd. Method of administrating an anticancer drug containing α, α, α-trifluorothymidine and thymidine phosphorylase inhibitor
JP2007284390A (ja) * 2006-04-18 2007-11-01 Ohara Yakuhin Kogyo Kk 塩酸イミダプリル含有錠剤
RU2435587C2 (ru) * 2006-06-30 2011-12-10 Тайхо Фармасьютикал Ко., Лтд. Средство, потенцирующее радиационную терапию
RU2346684C2 (ru) * 2007-04-04 2009-02-20 Закрытое акционерное общество "Биологические исследования и системы" Фармацевтическая композиция на основе сигетина
TWI526210B (zh) 2012-02-15 2016-03-21 Taiho Pharmaceutical Co Ltd Oral pharmaceutical composition

Also Published As

Publication number Publication date
RU2639473C2 (ru) 2017-12-21
MX365313B (es) 2019-05-29
HUE050840T2 (hu) 2021-01-28
EP2815752A1 (en) 2014-12-24
TW201336499A (zh) 2013-09-16
BR112014017633A8 (pt) 2021-02-23
EP2815752A4 (en) 2015-07-29
US20200289411A1 (en) 2020-09-17
MX2014009834A (es) 2014-09-11
AU2013219296B2 (en) 2016-05-26
TWI526210B (zh) 2016-03-21
PT2815752T (pt) 2020-07-15
EP2815752B1 (en) 2020-05-20
US20140363512A1 (en) 2014-12-11
KR101740105B1 (ko) 2017-05-25
SG11201403875VA (en) 2014-10-30
CY1123372T1 (el) 2021-12-31
JP5798642B2 (ja) 2015-10-21
RU2014137158A (ru) 2016-04-10
ES2804674T3 (es) 2021-02-09
MY155938A (en) 2015-12-17
PL2815752T3 (pl) 2020-11-16
JPWO2013122135A1 (ja) 2015-05-18
SI2815752T1 (sl) 2020-08-31
CA2863018A1 (en) 2013-08-22
US20220218602A1 (en) 2022-07-14
HK1199821A1 (en) 2015-07-24
LT2815752T (lt) 2020-08-10
CN104105490A (zh) 2014-10-15
KR20150001718A (ko) 2015-01-06
DK2815752T3 (da) 2020-07-20
RS60552B1 (sr) 2020-08-31
WO2013122135A1 (ja) 2013-08-22
CA2863018C (en) 2020-01-07
AU2013219296A1 (en) 2014-07-24

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