HRP20151382T1 - Formulacija koja sadrži derivat fenilaminopirimidina kao djelatnu tvar - Google Patents

Formulacija koja sadrži derivat fenilaminopirimidina kao djelatnu tvar Download PDF

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HRP20151382T1
HRP20151382T1 HRP20151382TT HRP20151382T HRP20151382T1 HR P20151382 T1 HRP20151382 T1 HR P20151382T1 HR P20151382T T HRP20151382T T HR P20151382TT HR P20151382 T HRP20151382 T HR P20151382T HR P20151382 T1 HRP20151382 T1 HR P20151382T1
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Durga Maheswari Parvataneni
Siddhartha YEDLURI
Venkata Satyanarayana APPADWEDULA
Kali Satya Bhujanga Rao Adibhatla
Venkaiah Chowdary Nannapaneni
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Natco Pharma Limited
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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
    • A61K9/10Dispersions; Emulsions
    • 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
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • 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
    • 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
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/10Dispersions; Emulsions
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • 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
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • A61K9/4858Organic compounds
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Oil, Petroleum & Natural Gas (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dispersion Chemistry (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Inorganic Chemistry (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Plural Heterocyclic Compounds (AREA)

Claims (15)

1. Farmaceutski pripravak za oralnu primjenu koji sadrži: a) terapijski djelotvornu količinu (3,5-bis trifluorometil)-N-[4-metil-3-(4-piridin-3il-pirimidin-2il amino) fenil] benzamida (NRC-AN-019) ili njegove farmaceutske prihvatljive soli; b) lipofilnu fazu; c) najmanje jedan farmaceutski prihvatljiv surfaktant; i d) farmaceutski prihvatljivo otapalo koje je mješljivo s vodom.
2. Farmaceutski pripravak prema zahtjevu 1, naznačen time, što - sastojak (a) je prisutan u količini od 0,1 do 20 % težine relativne ukupnoj težini pripravka, poželjno od 0,25 do 10 % težine relativne ukupnoj težini pripravka; - sastojak (b) je prisutan u količini od 10 do 75 % težine relativne ukupnoj težini pripravka, poželjno od 12,5 do 65 % težine relativne ukupnoj težini pripravka; - sastojak (c) je prisutan u količini od 4 do 70 % težine relativne ukupnoj težini pripravka, poželjno od 8 do 60 % težine relativne ukupnoj težini pripravka; i - sastojak (d) je prisutan u količini od 5 do 30 % težine relativne ukupnoj težini pripravka, poželjno od 5,5 do 25 % težine relativne ukupnoj težini pripravka.
3. Farmaceutski pripravak prema zahtjevu 1 ili 2 koji se sastoji od oblika I, oblika II ili oblika III polimorfa izuma NRC-AN-019.
4. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time, što se lipofilna faza sastoji od triglicerida, diglicerida, monoglicerida, masne kiseline, derivata masne kiseline ili njihove smjese, pri čemu je masna kiselina poželjno dugolančana masna kiselina, poželjnije od C12 do C22 masna kiselina, još poželjnije mononezasićena C12-20 masna kiselina koja je u tečnom stanju na sobnoj temperaturi, najpoželjnije (Z)-9-oktadekaenska kiselina.
5. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time, što su ostaci C18 nezasićene masne kiseline prisutni u lipofilnoj fazi u količini od najmanje 20 % težine, poželjno najmanje 40 % težine relativne ukupnoj težini lipofilne faze, i/ili su ostaci zasićene masne kiseline prisutni u lipofilnoj fazi u količini od 50 % težine ili manje na osnovi ukupne težine lipofilne faze.
6. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time, što se najmanje jedan surfaktant sastoji od glavnog surfaktanta i jednog ili više pomoćnih surfaktanata, pri čemu je pomoćni surfaktant tipično prisutan u količino od 2 do 60 % težine relativne ukupnoj težini pripravka, poželjno od 5 do 45 % težine relativne ukupnoj težini pripravka, a pri čemu pomoćni surfaktant poželjno sadrži polioksil glicerid, poželjnije kaprilokaproil polioksiglicerid.
7. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time, što najmanje jedan surfaktant sadrži polioksietilen glikolizirano biljno ulje, poželjno polioksietilen glikolizirano ricinusovo ulje, najpoželjnije polioksil 35 ricinusovo ulje.
8. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time, što otapalo koje je mješljivo s vodom djeluje kao prijenosni medij za NRC-AN-019.
9. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time, što otapalo koje je mješljivo u vodi jeste α-hidroksi-ω-hidroksi poli(oksi-1, 2-ehanediil) derivat, poželjno polietilen glikol 600.
10. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, koji dalje sadrži antioksidans koji je poželjno odabran iz butil hidroksianizola, butil hidroksitoluena i njihove smjese, poželjnije smjese butil hidroksianizola i butil hidroksitoluena u omjeru od 6:4 do 9:1, najpoželjnije smjese butil hidroksianizola i butil hidroksitoluena u omjeru od 7:3 do 8:2.
11. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, koji dalje sadrži sredstvo za zaslađivanje i/ili sredstvo za poboljšanje okusa, pri čemu je sredstvo za zaslađivanje poželjno saharin, poželjnije saharin u količini od 0,1 težine do 10 % težine relativne ukupnoj težini u pripravku, najpoželjnije saharin u količini od 0,25 % težine do oko 5 % težine relativne ukupnoj težini pripravka, dok je sredstvo za poboljšanje okusa poželjno odabrano iz aroma na bazi ulja, bilo zasebnih ili u kombinaciji, pri čemu je sredstvo za poboljšanje okusa poželjno prisutno u količini od 0,1 težinskih postotaka do oko 10 težinskih postotaka relativnih ukupnoj težini pripravka, poželjnije od 0,25 težinskih postotaka do 1 težinski postotak relativan ukupnoj težini pripravka.
12. Farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva koji se nalazi u obliku otopine, mekog gela ili formulacije u tvrdoj kapsuli.
13. Farmaceutski pripravak kao što je definirano u bilo kojem od prethodnih zahtjeva za primjenu u terapijskom liječenju tijela čovjeka ili životinje.
14. Farmaceutski pripravak kao što je definiranu u bilo kojem od zahtjeva 1 do 12 za primjenu u liječenju raka.
15. Postupak za dobivanje farmaceutskog pripravka kao što je definirano u bilo kojem od zahtjeva 1 do 12, koji se sastoji od - primiješanja NRC-AN-019 s otapalom koje je mješljivo s vodom, - dodavanja lipofilne faze, - dodavanja surfaktanta i opcionalno dodatnog surfaktanta, i - miješanja uz primjenu topline.
HRP20151382TT 2011-03-07 2015-12-16 Formulacija koja sadrži derivat fenilaminopirimidina kao djelatnu tvar HRP20151382T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GB1103860.1A GB2488788B (en) 2011-03-07 2011-03-07 Oral formulation of phenylaminopyrymidine compound with enhanced bioavailability and pharmacological response
PCT/IB2011/001842 WO2012120328A1 (en) 2011-03-07 2011-08-10 Formulation comprising phenylaminopyrimidine derivative as active agent
EP11764851.9A EP2683381B1 (en) 2011-03-07 2011-08-10 Formulation comprising phenylaminopyrimidine derivative as active agent

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HRP20151382T1 true HRP20151382T1 (hr) 2016-02-12

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US (1) US9895367B2 (hr)
EP (1) EP2683381B1 (hr)
JP (1) JP5788534B2 (hr)
KR (1) KR101767296B1 (hr)
CN (1) CN103561742B (hr)
AP (1) AP4076A (hr)
AU (1) AU2011361921B2 (hr)
BR (1) BR112013022930A2 (hr)
CA (1) CA2829015C (hr)
CO (1) CO6811851A2 (hr)
CY (1) CY1116968T1 (hr)
DK (1) DK2683381T3 (hr)
EA (1) EA024610B1 (hr)
ES (1) ES2554927T3 (hr)
GB (1) GB2488788B (hr)
GE (1) GEP20156410B (hr)
HR (1) HRP20151382T1 (hr)
HU (1) HUE025562T2 (hr)
IL (1) IL228218A (hr)
MA (1) MA35088B1 (hr)
MX (1) MX339130B (hr)
MY (1) MY158693A (hr)
NZ (1) NZ614903A (hr)
PL (1) PL2683381T3 (hr)
PT (1) PT2683381E (hr)
RS (1) RS54420B1 (hr)
SG (1) SG193349A1 (hr)
SI (1) SI2683381T1 (hr)
SM (1) SMT201500235B (hr)
UA (1) UA111074C2 (hr)
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WO2017115316A1 (en) * 2015-12-29 2017-07-06 Noivita S.R.L.S. Lipophilic formulations
CN107184549B (zh) * 2017-04-11 2020-11-20 江苏大学 一种尼达尼布自微乳制剂和其制成的软胶囊及制备方法
CN107564610A (zh) * 2017-10-20 2018-01-09 浙江中大元通特种电缆有限公司 一种陶瓷化硅橡胶绝缘护套不锈钢连锁铠装防火电缆
PT3765024T (pt) 2018-03-14 2024-02-19 Kandy Therapeutics Ltd Formulação farmacêutica inovadora que compreende antagonistas duplos dos recetores nk-1/nk-3
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GB2488788B (en) 2013-07-10
MA35088B1 (fr) 2014-05-02
PL2683381T3 (pl) 2016-06-30
MY158693A (en) 2016-11-15
AP2013007128A0 (en) 2013-09-30
EP2683381B1 (en) 2015-09-16
CY1116968T1 (el) 2017-04-05
GEP20156410B (en) 2015-12-10
EA024610B1 (ru) 2016-10-31
DK2683381T3 (en) 2015-12-21
NZ614903A (en) 2014-08-29
RS54420B1 (en) 2016-04-28
MX2013010160A (es) 2013-12-06
GB2488788A (en) 2012-09-12
CA2829015C (en) 2018-01-02
BR112013022930A2 (pt) 2016-12-06
US20130338180A1 (en) 2013-12-19
CN103561742B (zh) 2016-04-27
CA2829015A1 (en) 2012-09-13
CN103561742A (zh) 2014-02-05
CO6811851A2 (es) 2013-12-16
GB201103860D0 (en) 2011-04-20
EP2683381A1 (en) 2014-01-15
WO2012120328A1 (en) 2012-09-13
KR101767296B1 (ko) 2017-08-10
AU2011361921B2 (en) 2016-06-09
SI2683381T1 (sl) 2016-01-29
HUE025562T2 (en) 2016-03-29
MX339130B (es) 2016-05-13
ES2554927T3 (es) 2015-12-28
AU2011361921A2 (en) 2014-10-30
JP2014507463A (ja) 2014-03-27
SG193349A1 (en) 2013-10-30
JP5788534B2 (ja) 2015-09-30
AU2011361921A1 (en) 2013-09-26
KR20140016926A (ko) 2014-02-10
PT2683381E (pt) 2015-11-02
ZA201306643B (en) 2014-11-26
AP4076A (en) 2017-03-23
SMT201500235B (it) 2015-10-30
EA201391280A1 (ru) 2014-02-28
US9895367B2 (en) 2018-02-20
IL228218A (en) 2016-06-30
UA111074C2 (uk) 2016-03-25

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