ME01980B - Terapeutske kompozicije koje sadrže rilpivirin hcl i tenofovir dizoproksil fumarat - Google Patents

Terapeutske kompozicije koje sadrže rilpivirin hcl i tenofovir dizoproksil fumarat

Info

Publication number
ME01980B
ME01980B MEP-2014-150A MEP15014A ME01980B ME 01980 B ME01980 B ME 01980B ME P15014 A MEP15014 A ME P15014A ME 01980 B ME01980 B ME 01980B
Authority
ME
Montenegro
Prior art keywords
tablet
layer
microcrystalline cellulose
sodium
rilpivirine
Prior art date
Application number
MEP-2014-150A
Other languages
English (en)
French (fr)
Inventor
Reza Oliyai
Lauren Wiser
Mark Menning
Original Assignee
Gilead Sciences Inc
Janssen Sciences Ireland Uc
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=45094284&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ME01980(B) "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 Sciences Ireland Uc filed Critical Gilead Sciences Inc
Publication of ME01980B publication Critical patent/ME01980B/me

Links

Classifications

    • 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

Landscapes

  • 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 procenta prvog sloja je rilpivirin HCl; b) drugi sloj sadrži tenofovir dizoproksil fumarat, i i suštinski je bez rilpivirin HCl-a; i c) tableta dalje sadrži emtricitabin.
2.Tableta zahteva 1 gde prvi sloj ne sadrži emtricitabin.
3.Tableta zahteva 1 ili 2 koja sadrži 27.5 ± 1.4 rng rilpivirin HCl-a.
4.Tableta bilo kog od zahteva 1-3 koja sadrži 200 ± 10.0 mgemtricitabina.
5.Tableta bilo kog od zahteva 1-4 koja sadrži 300 ± 15.0 mgtenofovir dizoproksil fumarata.
6.Tableta bilo kog od zahteva 1-5 gde prvi sloj dalje sadrži jedan ili više rastvarača, sredstva za raspadanje, sredstva za vezivanje, ili lubrikante.
7.Tableta zahteva 6 gde je totalna masa prvog sloja 275 ± 75 mg, pre svega veća od225 mg a posebno je 275 ± 50 mg.
8.Tableta bilo kog od zahteva 1-7 gde prvi sloj sadrži sredstvo za povećanje baznosti koje je prvenstveno izabrano od natrijum kroskarmeloze, kalcijum karbonata, natrijum hidroksida, aluminijum oksida, hidroksida alkalnih metala, hidroksida zemnoalkalnih metala, aluminijum hidroksida, dihidroaluminijuma, natrijum karbonata, amonijum hidroksida, magnezijum karbonata, magnezijum stearata, piperazina, natrijum acetata, natrijum citrata, natrijum tartarata, natrijum maleata, i natrijum sukcinata i njihovih mikstura.
9.Tableta bilo kog od zahteva 1-8 gde prvi sloj sadrži natrijum kroskarmelozu, i polisorbat 20 i posebno sadrži laktozu monohidrat, povidon, natrijum kroskarmelozu, polisorbat 20, mikrokristalnu celulozu, i megnezijum stearat.
10.Tableta bilo kog od zahteva 1-9 gde drugi sloj sadrži mikrokristalnu celulozu i natrijum kroskarmelozu a posebno sadrži laktozu monohidrat, preželatinizirani skrob, mikrokristalnu celulozu, natrijum kroskarmelozu, i magnezijum stearat.
11.Tableta bilo kog od zahteva 1-10 gde je prvi sloj u kontaktu sa drugim slojem.
12.Tableta bilo kog od zahteva 1-10 koja dalje sadrži treći sloj koje je između i koji razdvaja prvi sloj i drugi sloj.
13.Tableta zahteva 12 gde treći sloj sadrži laktozu monohidrat i/ili mikrokristalnu celulozu.
14.Supstanca Jedinica formule za tablete (mg/tableta) Rilpivirin HCl 27.5 Mikrokristalna celuloza 60.0 Laktoza monohidrat 189.8 Povidon 3.3 Polisorbat 20 0.4 Tableta bilo kog od zahteva 1-5 gde je prvi sloj omotač od polimernog filma koji je u kontaktu sa drugim slojem i poželjno potpuno prekriva drugi sloj.
15. Tableta zahteva 2 gde prvi sloj sadrži: Supstanca Jedinica formule za tablete (mg/tableta) Rilpivirin HCl 27.5 ± 1.4 Mikrokristalna celuloza 60.0 ±3 Polisorbat 20 0.4 ± 0.02 Natrijum kroskarmeloza
16.1 ±0.8 a drugi sloj sadrži: Supstanca Jedinica formule za tablete (mg/tableta) Emtricitabin 200 ± 10 Tenofovir dizoproksil fumarat 300 ± 15 Mikrokristalna celuloza 150 ± 7.5 Natrijum kroskarmeloza 60 ±3. ili gde se prvi sloj sastoji od: Supstanca Jedinica formule za tablete (mg/tableta) Natrijum kroskarmeloza 16.1 Magnezijum Stearat 3.0 a drugi sloj se sastoji od: Supstanca Jedinica formule za tablete (mg/tableta) Emtricitabin 200.0 Tenofovir dizoproksil fumarat 300.0 Mikrokristalna celuloza 150.0 Laktoza monohidrat 80.0 Preželatinizirani skrob 50.0 Natrijum kroskarmeloza 60.0 Magnezijum Stearat 10.0. 16. Tableta zahteva 12 gde se prvi sloj sastoji od: Supstanca Jedinica formule za tablete (mg/tableta) Rilpivirin HCl 27.5 Mikrokristalna celuloza 60.0 Laktoza monohidrat 189.8 Povidon 3.3 Polisorbat 20 0.4 Natrijum kroskarmeloza 16.1 Magnezijum Stearat 3.0 drugi sloj se sastoji od: Supstanca Jedinica formule za tablete (mg/tableta) Emtricitabin 200.0 Tenofovir dizoproksil fumarat 300.0 Mikrokristalna celuloza 150.0 Laktoza monohidrat 80.0 Preželatinizirani skrob 50.0 Natrijum kroskarmeloza 60.0 Magnezijum Stearat 10.0 a treći sloj sadrži 150 ± 8.0 mg mikrokristalne celuloze ili laktoza monohidrata, ili njihove miksture.
17.Tableta bilo kog od zahteva 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 satoji od: Supstanca mg Rilpivirin HCl 27.5 Mikrokristalna celuloza 60.0 Laktoza monohidrat 189.8 Povidon 3.3 Polisorbat 20 0.4 Natrijum kroskarmeloza 16.1 Magnezijum Stearat 3.0 Ukupna masa sloja 300.0 adrugi sloj se sastoji od: Supstanca mg Supstanca mg Emtricitabin 200.0 Tenofovir DF 300.0b Mikrokristalna celuloza 150.0 Laktoza monohidrat 80.0 Preželatinizirani skrob 50.0 Natrijum kroskarmeloza 60.0 Magnezijum Stearat 10.0 Ukupna masa sloja 850.0 a omotač se sastoji od: Supstanca mg Opadry II Purple 33G100000 34.5 Ukupna masa tablete 1184.5.
19.Tableta bilo kog od zahteva 1-13 gde najmanje oko 5.4 masenog procenta prvog sloja je natrijum kroskarmeloza i najmanje oko 63.3 masenog procenta prvog sloja je laktoza monohidrat.
20.Tableta bilo kog od zahteva 1-14 gde manje od oko 12 masenog procenta prvog sloja je rilpivirin hidrohloriđ.
21.Tableta zahteva 1 gde prvi sloj sadrži 27.5 ± 1.4 mg rilpivirin hidrohlorida i gde je totalna masa prvog sloja najmanje oko 230 mg.
22.Tableta kao što je opisano u bilo kom od zahteva 1-21 za primenu u profilaktičkom ili terapeutskom tretmanu HIV infekcije, gde rilpivirin AUC (area under the curve-površina ispod krive) koji je postignut primenom kod čoveka uz ishranu nije više od oko 25% veći od rilpivirin AUCkoji je postignut primenom kod čoveka na dijeti ili gde rilpivirin Cmaxkoji je postignut primenom kod čoveka uz ishranu nije više od oko 25% veći od rilpivirin Cmax koji je postignut primenom kod čoveka na dijeti.
23. Tableta kao što je opisano u bilo kom od zahteva 1-21 za primenu profilaktičkom ili terapeutskom tretmanu HIV infekcije.
MEP-2014-150A 2010-11-19 2011-11-18 Terapeutske kompozicije koje sadrže rilpivirin hcl i tenofovir dizoproksil fumarat ME01980B (me)

Applications Claiming Priority (3)

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

Publications (1)

Publication Number Publication Date
ME01980B true ME01980B (me) 2015-05-20

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EP (2) EP2826466A1 (me)
JP (2) JP2014500261A (me)
KR (1) KR101923103B1 (me)
CN (2) CN103491948B (me)
AP (1) AP3816A (me)
AR (2) AR084500A1 (me)
AU (3) AU2011329642B2 (me)
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CL (1) CL2013001402A1 (me)
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EA (2) EA201691695A1 (me)
EC (2) ECSP13012700A (me)
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IL (1) IL226300B (me)
MA (1) MA34735B1 (me)
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MX (1) MX347512B (me)
MY (1) MY185604A (me)
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PE (3) PE20211657A1 (me)
PH (1) PH12013501002A1 (me)
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SMT201400150B (it) 2015-01-15
MA34735B1 (fr) 2013-12-03
AU2016208417A1 (en) 2016-08-18
JP2015131853A (ja) 2015-07-23
PT2640362E (pt) 2014-11-28
AU2016208417B2 (en) 2018-04-05
DK2640362T3 (en) 2014-12-01
PE20211657A1 (es) 2021-08-24
SG10201912527XA (en) 2020-02-27
ZA201304481B (en) 2022-03-30
PE20170521A1 (es) 2017-05-27
CN103491948B (zh) 2016-11-02
EA201691695A1 (ru) 2017-11-30
CL2013001402A1 (es) 2013-12-27
KR20140037799A (ko) 2014-03-27
PE20140163A1 (es) 2014-02-08
EP2640362B1 (en) 2014-09-10
IL226300B (en) 2019-05-30
NZ610729A (en) 2015-10-30
DK2640362T4 (da) 2022-03-07
ECSP19078196A (es) 2019-11-30
EA025852B1 (ru) 2017-02-28
MX347512B (es) 2017-04-28
UA114075C2 (xx) 2017-04-25
SG190333A1 (en) 2013-06-28
AU2011329642A1 (en) 2013-05-02
CA2818097C (en) 2019-07-30
CA2818097A1 (en) 2012-05-24
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CR20130293A (es) 2013-10-03
US20130243857A1 (en) 2013-09-19
CN103491948A (zh) 2014-01-01
HRP20140946T1 (hr) 2015-02-13
ES2524408T3 (es) 2014-12-09
TW201238612A (en) 2012-10-01
EA201390651A1 (ru) 2013-11-29
JP6138851B2 (ja) 2017-05-31
BR112013012245A2 (pt) 2016-08-09
EP2640362B2 (en) 2021-12-01
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US10857102B2 (en) 2020-12-08
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MX2013005669A (es) 2013-11-04
PL2640362T5 (pl) 2022-05-02
KR101923103B1 (ko) 2018-11-28
HK1206592A1 (en) 2016-01-15
AP2013006931A0 (en) 2013-06-30
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BR112013012245B1 (pt) 2022-09-27
RS53691B1 (sr) 2015-04-30
AR123409A2 (es) 2022-11-30
PH12013501002A1 (en) 2013-09-09
AP3816A (en) 2016-09-30
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ECSP13012700A (es) 2013-08-30
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