HRP20211590T1 - Farmaceutske kompozicije koje sadrže derivat fenilaminopirimidina - Google Patents

Farmaceutske kompozicije koje sadrže derivat fenilaminopirimidina Download PDF

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Publication number
HRP20211590T1
HRP20211590T1 HRP20211590TT HRP20211590T HRP20211590T1 HR P20211590 T1 HRP20211590 T1 HR P20211590T1 HR P20211590T T HRP20211590T T HR P20211590TT HR P20211590 T HRP20211590 T HR P20211590T HR P20211590 T1 HRP20211590 T1 HR P20211590T1
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Croatia
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nrc
parts
eudragit
methacrylic acid
formulation
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HRP20211590TT
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English (en)
Inventor
Durga Maheswari Parvataneni
Mitrabhanu MOHANTY
Venkata Satyanarayana APPADWEDULA
Kali Satya Bhujanga Rao Adibhatla
Venkaiah Chowdary Nannapaneni
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Natco Pharma Ltd
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Publication of HRP20211590T1 publication Critical patent/HRP20211590T1/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
    • A61K9/08Solutions
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K9/0087Galenical forms not covered by A61K9/02 - A61K9/7023
    • A61K9/0095Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
    • 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
    • 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
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • A61K9/1635Organic 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
    • A61K9/14Particulate 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
    • A61K9/1641Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • 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
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • 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
    • A61K9/2027Organic 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
    • A61K9/20Pills, 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
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia

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

Claims (15)

1. Formulacija koja je pogodna za oralno davanje koja sadrži terapeutski efikasnu količinu (3,5-Bis trifluorometil)-N-[4-metil-3-(4-piridin-3il-pirimidin-2-il-amino)fenil]benzamida (NRC-AN-019) ili njegove soli, i bar jedno polimerno matrično sredstvo, gdje: formulacija je u obliku čvrste disperzije; i polimerno matrično sredstvo je ionski polimer ili ne-ionski polimer ili njihova kombinacija, pri čemu je ionski polimer celulozni polimer ili kopolimer metakrilne kiseline ili njihova kombinacija, i gdje je ne-ionski polimer celulozni polimer.
2. Formulacija prema zahtjevu 1, gdje NRC-AN-019 je u kristalnom ili amorfnom obliku ili njihovoj kombinaciji, poželjno gdje je NRC-AN-019 u kristalnom Obliku I, Obliku II, Obliku III ili njihovoj kombinaciji.
3. Formulacija prema bilo kojem od prethodnih zahtjeva, gdje je odnos NRC-AN-019 prema polimernom matričnom sredstvu od 1:1 do 1:8 u ukupnoj masi sastava.
4. Formulacija prema bilo kojem od prethodnih zahtjeva, gdje je ionski polimer kombinacija ionskog polimera i kopolimera metakrilne kiseline.
5. Formulacija prema bilo kojem od prethodnih zahtjeva, gdje je kopolimer metakrilne kiseline izabran od poli(metakrilne kiseline, metil metakrilata), poli(metakrilne kiseline, etil akrilata) i njihove kombinacije.
6. Formulacija prema bilo kojem od prethodnih zahtjeva, gdje je kopolimer metakrilne kiseline poli(metakrilna kiselina, metil metakrilat) i poli(metakrilna kiselina, etil akrilat).
7. Formulacija prema bilo kojem od prethodnih zahtjeva, gdje čvrsta disperzija dalje sadrži dodatnu farmaceutski prihvatljivu pomoćnu tvar izabranu od nosača, punjenja, površinski aktivnih sredstava, inhibitora kristalizacije, sredstava za zgušnjavanje, dezintegranata, plastifikatora, sredstava za uklanjanje pjene, antioksidansa, stabilizatora, glidanata i lubrikanata.
8. Formulacija prema zahtjevu 1, pri čemu se formulacija sastoji iz: (a) 1 dijela NRC-AN-019, 2.5 dela Eudragit L 100 55, 4.5 dijela HPMCAS (hipromeloza acetat sukcinat) i 0.05 dijelova Carbopol 974; (b) 1 dijela NRC-AN-019, 2 dijela Eudragit L 100 55, 1 dijela Eudragit S 100 i 0.05 dijelova Carbopol 974; (c) 1 dijela NRC-AN-019, 2 dijela Eudragit L 100 55, 1 dijela Eudragit S 100 and 0.1 dijela Carbopol 974; (d) 1 dijela NRC-AN-019, 4 dijela Eudragit L 100 55, 2 dijela Eudragit S 100 i 0.08 dijelova Carbopol 974; (e) 1 dijela NRC-AN-019, 5 dijela Eudragit L 100 55 i 1 dijela HPMCP HP-55 (hipromeloza ftalat); (f) 1 dijela NRC-AN-019, 5 dijela Eudragit L 100 55, 1 dijela Eudragit S 100, 1 dijela HPMCAS (hipromeloza acetat sukcinat) i 0.5 dijelova etil celuloze; (g) 1 dijela NRC-AN-019, 5 dijela Eudragit L 100 55, 1 dijela Eudragit S 100 i 1 dijela HPMCP HP-55 (hipromeloza ftalata); ili (h) 1 dijela NRC-AN-019, 5 dijela Eudragit L 100 55, 1 dijela Eudragit S 100, 1 dijela HPMCP HP-55 (hipromeloza ftalat) i 0.5 dijelova etil celuloze.
9. Formulacija prema bilo kojem od zahtjeva 1 do 7, pri čemu se čvrsta disperzija može dobiti taloženjem kontroliranim rastvaračem, isparavanjem rastvarača, liofilizacijom, pH kontroliranim taloženjem, ekstruzijom vrelim topljenjem i tehnologijom superkritičnog fluida.
10. Postupak za dobivanje čvrste disperzije prema zahtjevu 9, pri čemu postupak obuhvaća miješanje NRC-AN-019 i polimernog matričnog sredstva kao što je definirano u bilo kojem od zahtjeva 1 i 4 do 6 da bi se formirala homogena, molekularno disperzirana smjesa.
11. Postupak prema zahtjevu 10, pri čemu je miješanje izvedeno rastvaranjem NRC-AN-019 i polimernog matričnog sredstva u organskom rastvaraču, praćeno raspršivanjem u anti-rastvaraču i dobivanjem mješovitog taloga NRC-AN-019 i polimernog matričnog sredstva.
12. Postupak prema zahtjevu 11, gdje: rastvarač je dimetilformamid, dimetilacetamid, dimetilsulfoksid i N-Metil-2-pirolidon ili njihove smjese; ili gdje anti-rastvarač je voda, klorovodonična kiselina, etil acetat, toluen, metilen hlorid, acetonitril ili njihove smjese.
13. Formulacija kao što je definirano u bilo kojem od zahtjeva 1 do 9 za upotrebu u terapiji.
14. Formulacija kao što je definirano u bilo kojem od zahtjeva 1 do 9 za upotrebu u postupku liječenja karcinoma.
15. Formulacija prema zahtjevu 14 pri čemu je karcinom kronična mijeloidna leukemija, karcinom glave, karcinom vrata ili karcinom prostate.
HRP20211590TT 2015-12-18 2016-01-30 Farmaceutske kompozicije koje sadrže derivat fenilaminopirimidina HRP20211590T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IN6951CH2015 2015-12-18
PCT/IN2016/050035 WO2017103941A1 (en) 2015-12-18 2016-01-30 Pharmaceutical compositions comprising phenylaminopyrimidine derivative
EP16875074.3A EP3389633B1 (en) 2015-12-18 2016-01-30 Pharmaceutical compositions comprising phenylaminopyrimidine derivative

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HRP20211590T1 true HRP20211590T1 (hr) 2022-01-07

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US (1) US10383872B2 (hr)
EP (1) EP3389633B1 (hr)
JP (2) JP6896738B2 (hr)
KR (1) KR20180102584A (hr)
CN (1) CN108495620B (hr)
AU (1) AU2016373574B2 (hr)
BR (1) BR112018012458A2 (hr)
CA (1) CA3008634A1 (hr)
CL (1) CL2018001590A1 (hr)
CO (1) CO2018007112A2 (hr)
CY (1) CY1124580T1 (hr)
DK (1) DK3389633T3 (hr)
EA (1) EA036513B1 (hr)
ES (1) ES2881883T3 (hr)
GB (1) GB2564262A (hr)
GE (1) GEP20207176B (hr)
HK (1) HK1254573A1 (hr)
HR (1) HRP20211590T1 (hr)
HU (1) HUE056269T2 (hr)
IL (1) IL260085B (hr)
LT (1) LT3389633T (hr)
MA (1) MA44079B1 (hr)
MX (1) MX2018007281A (hr)
PH (1) PH12018501292A1 (hr)
PL (1) PL3389633T3 (hr)
PT (1) PT3389633T (hr)
RS (1) RS62422B1 (hr)
SG (1) SG11201805142RA (hr)
SI (1) SI3389633T1 (hr)
UA (1) UA122592C2 (hr)
WO (1) WO2017103941A1 (hr)
ZA (1) ZA201804203B (hr)

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TW202246215A (zh) 2015-12-18 2022-12-01 美商亞德利克斯公司 作為非全身tgr5促效劑之經取代之4-苯基吡啶化合物
CZ2017821A3 (cs) * 2017-12-20 2019-07-03 Zentiva, K.S. Léková forma obsahující krystalický nilotinib
US20210369620A1 (en) * 2018-05-14 2021-12-02 Capsugel Belgium Nv Solid dosage forms with high active agent loading
JP7368548B2 (ja) * 2021-07-02 2023-10-24 昊運股▲フン▼有限公司 薬学的組成物及びその使用
CN115583634B (zh) * 2022-09-21 2023-06-06 广东工业大学 一种碳氮聚合物材料的制备方法及应用

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JP2002241268A (ja) * 2000-12-11 2002-08-28 Takeda Chem Ind Ltd 水溶解性が改善された医薬組成物
CA2591321C (en) 2004-09-09 2013-09-24 Natco Pharma Limited Phenylaminopyrimidine derivatives as inhibitors of bcr-abl kinase
US8067422B2 (en) 2008-03-04 2011-11-29 Natco Pharma Limited Crystal form of phenylamino pyrimidine derivatives
WO2012002547A1 (ja) * 2010-07-02 2012-01-05 富士化学工業株式会社 ボセンタン固体分散体
GB2488788B (en) 2011-03-07 2013-07-10 Natco Pharma Ltd Oral formulation of phenylaminopyrymidine compound with enhanced bioavailability and pharmacological response
CN102836159B (zh) * 2011-06-24 2014-12-10 南京圣和药业股份有限公司 达沙替尼分散体及其制备方法和其在片剂中的应用
JP2017500343A (ja) * 2013-12-20 2017-01-05 フォスフォレックス,インコーポレーテッド インジルビン固体分散体組成物

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GB201811142D0 (en) 2018-08-22
SI3389633T1 (sl) 2021-11-30
HK1254573A1 (zh) 2019-07-19
PT3389633T (pt) 2021-08-05
PH12018501292A1 (en) 2019-02-04
PL3389633T3 (pl) 2021-12-13
GEAP201614833A (hr) 2020-06-25
GEP20207176B (en) 2020-11-10
WO2017103941A1 (en) 2017-06-22
EA201891443A1 (ru) 2019-01-31
KR20180102584A (ko) 2018-09-17
CL2018001590A1 (es) 2018-11-30
CN108495620A (zh) 2018-09-04
UA122592C2 (uk) 2020-12-10
IL260085B (en) 2021-09-30
CN108495620B (zh) 2021-09-03
EA036513B1 (ru) 2020-11-18
EP3389633B1 (en) 2021-07-14
AU2016373574B2 (en) 2021-10-14
EP3389633A4 (en) 2019-08-07
SG11201805142RA (en) 2018-07-30
BR112018012458A2 (pt) 2018-12-18
LT3389633T (lt) 2021-09-10
US10383872B2 (en) 2019-08-20
RS62422B1 (sr) 2021-10-29
CA3008634A1 (en) 2017-06-22
GB2564262A (en) 2019-01-09
HUE056269T2 (hu) 2022-02-28
MX2018007281A (es) 2018-11-29
DK3389633T3 (da) 2021-08-30
JP2021059551A (ja) 2021-04-15
JP2018538325A (ja) 2018-12-27
ZA201804203B (en) 2020-08-26
IL260085A (en) 2018-07-31
EP3389633A1 (en) 2018-10-24
US20190015412A1 (en) 2019-01-17
ES2881883T3 (es) 2021-11-30
MA44079A (fr) 2021-04-21
MA44079B1 (fr) 2021-10-29
CY1124580T1 (el) 2022-07-22
AU2016373574A1 (en) 2018-07-12
JP6896738B2 (ja) 2021-06-30
CO2018007112A2 (es) 2018-07-19

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