HRP20140946T1 - Terapeutske kompozicije koje sadrže rilpivirin hcl i tenovofir dizoproksil fumarat - Google Patents

Terapeutske kompozicije koje sadrže rilpivirin hcl i tenovofir dizoproksil fumarat Download PDF

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Publication number
HRP20140946T1
HRP20140946T1 HRP20140946AT HRP20140946T HRP20140946T1 HR P20140946 T1 HRP20140946 T1 HR P20140946T1 HR P20140946A T HRP20140946A T HR P20140946AT HR P20140946 T HRP20140946 T HR P20140946T HR P20140946 T1 HRP20140946 T1 HR P20140946T1
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HR
Croatia
Prior art keywords
layer
tablet
rilpivirine
image
sodium
Prior art date
Application number
HRP20140946AT
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English (en)
Inventor
Reza Oliyai
Lauren Wiser
Mark Menning
Original Assignee
Gilead Sciences, Inc.
Janssen R&D Ireland
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45094284&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20140946(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Sciences, Inc., Janssen R&D Ireland filed Critical Gilead Sciences, Inc.
Publication of HRP20140946T1 publication Critical patent/HRP20140946T1/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
    • A61K31/33Heterocyclic 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
    • 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
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • 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
    • A61K9/2072Pills, 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
    • A61K9/2086Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
    • A61K9/209Layered 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV

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

Claims (23)

1. Tableta koja sadrži prvi sloj i drugi sloj pri čemu; a) prvi sloj sadrži rilpivirin HCl i suštinski je bez tenofovir dizoproksil fumarata, i pri čemu manje od oko 12.2 masenog postotka prvog sloja je rilpivirin HCl; b) drugi sloj sadrži tenofovir dizoproksil fumarat, i i suštinski je bez rilpivirin HCl; i c) tableta dalje sadrži emtricitabin.
2. Tableta zahtjeva 1 gdje prvi sloj ne sadrži emtricitabin.
3. Tableta zahtjeva 1 ili 2 koja sadrži 27.5 ± 1.4 mg rilpivirin HCl.
4. Tableta bilo kojeg od zahtjeva 1-3 koja sadrži 200 ± 10.0 mg emtricitabina.
5. Tableta bilo kojeg od zahtjeva 1-4 koja sadrži 300 ± 15.0 mg tenofovir dizoproksil fumarata.
6. Tableta bilo kojeg od zahtjeva 1-5 gdje prvi sloj dalje sadrži jedan ili više rastvarača, sredstva za raspadanje, sredstva za vezivanje, ili lubrikante.
7. Tableta zahtjeva 6 gdje je ukupna masa prvog sloja 275 ± 75 mg, prije svega veća od 225 mg, a posebno je 275 ± 50 mg.
8. Tableta bilo kojeg od zahtjeva 1-7 gdje prvi sloj sadrži sredstvo za povećanje baznosti koje je prvenstveno izabrano od kroskarmeloza-natrija, kalcijevog karbonata, natrijevog hidroksida, aluminijevog oksida, hidroksida alkalnih metala, hidroksida zemnoalkalnih metala, aluminijevog hidroksida, dihidroaluminija, natrijevog karbonata, amonijevog hidroksida, magnezijevog karbonata, magnezijevog stearata, piperazina, natrijevog acetata, natrijevog citrata, natrijevog tartarata, natrijevog maleata, i natrijevog sukcinata i njihovih mikstura.
9. Tableta bilo kojeg od zahtjeva 1-8 gdje prvi sloj sadrži natrijevu kroskarmelozu, i polisorbat 20 i posebno sadrži laktozu monohidrat, povidon, natrijevu kroskarmelozu, polisorbat 20, mikrokristalnu celulozu, i megnezijev stearat.
10. Tableta bilo kojeg od zahtjeva 1-9 gdje drugi sloj sadrži mikrokristalnu celulozu i natrijevu kroskarmelozu, a posebno sadrži laktozu monohidrat, pregelatinizirani škrob, mikrokristalnu celulozu, natrijevu kroskarmelozu, i magnezijev stearat.
11. Tableta bilo kojeg od zahtjeva 1-10 gdje je prvi sloj u kontaktu sa drugim slojem.
12. Tableta bilo kojeg od zahtjeva 1-10 koja dalje sadrži treći sloj koji je između i koji razdvaja prvi sloj i drugi sloj.
13. Tableta zahtjeva 12 gdje treći sloj sadrži laktozu monohidrat i/ili mikrokristalnu celulozu.
14. Tableta bilo kojeg od zahtjeva 1-5 gdje je prvi sloj omotač od polimernog filma koji je u kontaktu sa drugim slojem i poželjno potpuno prekriva drugi sloj.
15. Tableta zahtjeva 2 gdje prvi sloj sadrži: [image] a drugi sloj sadrži: [image] ili gdje se prvi sloj sastoji od: [image] a drugi sloj se sastoji od: [image]
16. Tableta zahtjeva 12 gdje se prvi sloj sastoji od: [image] drugi sloj se sastoji od: [image] a treći sloj sadrži 150 ± 8.0 mg mikrokristalne celuloze ili laktoza monohidrata, ili njihove miksture.
17. Tableta bilo kojeg od zahtjeva 1-13 i 15-16 koja dalje sadrži film omotač koji poželjno sadrži 34 ± 12 mg Opadry II Purple 33G100000.
18. Tableta koja ima prvi sloj koji se sastoji od: [image] a drugi sloj se sastoji od: [image] A omotač se sastoji od: [image]
19. Tableta bilo kojeg od zahtjeva 1-13 gdje najmanje oko 5.4 masenog postotka prvog sloja je natrijeva kroskarmeloza i najmanje oko 63.3 postotka mase prvog sloja je laktoza monohidrat.
20. Tableta bilo kojeg od zahtjeva 1-14 gdje je manje od oko 12 postotka mase prvog sloja rilpivirin hidrohlorid.
21. Tableta zahtjeva 1 gdje prvi sloj sadrži 27.5 ± 1.4 mg rilpivirin hidrohlorida i gdje je totalna masa prvog sloja najmanje oko 230 mg.
22. Tableta kao što je opisano u bilo kojem od zahtjeva 1-21 za primjenu u profilaktičkom ili terapeutskom tretmanu HIV infekcije, gdje rilpivirin AUC (area under the curve-površina ispod krivulje) koji je postignut primjenom kod čovjeka uz ishranu nije više od oko 25% veći od rilpivirin AUC koji je postignut primjenom kod čovjeka na dijeti ili gdje rilpivirin Cmaxkoji je postignut primjenom kod čovjeka uz ishranu nije više od oko 25% veći od rilpivirin Cmax koji je postignut primjenom kod čovjeka na dijeti.
23. Tableta kao što je opisano u bilo kojem od zahtjeva 1-21 za primjenu u profilaktičkom ili terapeutskom tretmanu HIV infekcije.
HRP20140946AT 2010-11-19 2014-10-01 Terapeutske kompozicije koje sadrže rilpivirin hcl i tenovofir dizoproksil fumarat HRP20140946T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41560010P 2010-11-19 2010-11-19
EP11791161.0A EP2640362B2 (en) 2010-11-19 2011-11-18 Therapeutic compositions comprising rilpivirin hcl and tenovofir disoproxil fumarate
PCT/US2011/061515 WO2012068535A1 (en) 2010-11-19 2011-11-18 Therapeutic compositions comprising rilpivirine hcl and tenofovir disoproxil fumarate

Publications (1)

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HRP20140946T1 true HRP20140946T1 (hr) 2015-02-13

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HRP20140946AT HRP20140946T1 (hr) 2010-11-19 2014-10-01 Terapeutske kompozicije koje sadrže rilpivirin hcl i tenovofir dizoproksil fumarat

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US (1) US10857102B2 (hr)
EP (2) EP2826466A1 (hr)
JP (2) JP2014500261A (hr)
KR (1) KR101923103B1 (hr)
CN (2) CN103491948B (hr)
AP (1) AP3816A (hr)
AR (2) AR084500A1 (hr)
AU (3) AU2011329642B2 (hr)
BR (1) BR112013012245B1 (hr)
CA (1) CA2818097C (hr)
CL (1) CL2013001402A1 (hr)
CO (1) CO6761300A2 (hr)
CR (1) CR20130293A (hr)
DK (1) DK2640362T4 (hr)
EA (2) EA201691695A1 (hr)
EC (2) ECSP13012700A (hr)
ES (1) ES2524408T5 (hr)
HK (2) HK1190064A1 (hr)
HR (1) HRP20140946T1 (hr)
IL (1) IL226300B (hr)
MA (1) MA34735B1 (hr)
ME (1) ME01980B (hr)
MX (1) MX347512B (hr)
MY (1) MY185604A (hr)
NZ (1) NZ610729A (hr)
PE (3) PE20211657A1 (hr)
PL (1) PL2640362T5 (hr)
PT (1) PT2640362E (hr)
RS (1) RS53691B1 (hr)
SG (3) SG190333A1 (hr)
SM (1) SMT201400150B (hr)
TW (1) TWI556840B (hr)
UA (1) UA114075C2 (hr)
WO (1) WO2012068535A1 (hr)
ZA (1) ZA201304481B (hr)

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SMT201400150B (it) 2015-01-15
HK1206592A1 (en) 2016-01-15
PE20211657A1 (es) 2021-08-24
TWI556840B (zh) 2016-11-11
MX347512B (es) 2017-04-28
JP2014500261A (ja) 2014-01-09
ECSP13012700A (es) 2013-08-30
RS53691B1 (en) 2015-04-30
IL226300B (en) 2019-05-30
AP2013006931A0 (en) 2013-06-30
TW201238612A (en) 2012-10-01
AU2011329642A1 (en) 2013-05-02
CN103491948B (zh) 2016-11-02
WO2012068535A1 (en) 2012-05-24
AU2011329642B2 (en) 2016-08-11
CN106511357A (zh) 2017-03-22
CO6761300A2 (es) 2013-09-30
AU2016208417B2 (en) 2018-04-05
JP2015131853A (ja) 2015-07-23
PE20140163A1 (es) 2014-02-08
CR20130293A (es) 2013-10-03
MX2013005669A (es) 2013-11-04
EA201691695A1 (ru) 2017-11-30
DK2640362T3 (en) 2014-12-01
EA201390651A1 (ru) 2013-11-29
AP3816A (en) 2016-09-30
SG10201912527XA (en) 2020-02-27
EP2640362B2 (en) 2021-12-01
MY185604A (en) 2021-05-25
EA025852B1 (ru) 2017-02-28
CA2818097A1 (en) 2012-05-24
CN103491948A (zh) 2014-01-01
AR123409A2 (es) 2022-11-30
ZA201304481B (en) 2022-03-30
SG10201509521WA (en) 2015-12-30
CL2013001402A1 (es) 2013-12-27
US20130243857A1 (en) 2013-09-19
MA34735B1 (fr) 2013-12-03
US10857102B2 (en) 2020-12-08
BR112013012245A2 (pt) 2016-08-09
EP2640362B1 (en) 2014-09-10
KR101923103B1 (ko) 2018-11-28
BR112013012245B1 (pt) 2022-09-27
PL2640362T5 (pl) 2022-05-02
ES2524408T5 (es) 2022-04-25
UA114075C2 (xx) 2017-04-25
PL2640362T3 (pl) 2015-03-31
HK1190064A1 (en) 2014-06-27
AR084500A1 (es) 2013-05-22
CA2818097C (en) 2019-07-30
SG190333A1 (en) 2013-06-28
EP2640362A1 (en) 2013-09-25
KR20140037799A (ko) 2014-03-27
PT2640362E (pt) 2014-11-28
ES2524408T3 (es) 2014-12-09
DK2640362T4 (da) 2022-03-07
ECSP19078196A (es) 2019-11-30
EP2826466A1 (en) 2015-01-21
AU2018202635A1 (en) 2018-05-10
JP6138851B2 (ja) 2017-05-31
ME01980B (me) 2015-05-20
PE20170521A1 (es) 2017-05-27
NZ610729A (en) 2015-10-30
AU2016208417A1 (en) 2016-08-18

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