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AR101116A1 - Formas de dosificación farmacéuticas para administración oral - Google Patents

Formas de dosificación farmacéuticas para administración oral

Info

Publication number
AR101116A1
AR101116A1 ARP150102160A ARP150102160A AR101116A1 AR 101116 A1 AR101116 A1 AR 101116A1 AR P150102160 A ARP150102160 A AR P150102160A AR P150102160 A ARP150102160 A AR P150102160A AR 101116 A1 AR101116 A1 AR 101116A1
Authority
AR
Argentina
Prior art keywords
weight
pharmaceutical dosage
dosage form
drug
microcrystalline cellulose
Prior art date
Application number
ARP150102160A
Other languages
English (en)
Original Assignee
Novartis Ag
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
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR101116A1 publication Critical patent/AR101116A1/es

Links

Classifications

    • 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
    • A61K9/20Pills, tablets, discs, rods
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41881,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • 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
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/45Non condensed piperidines, e.g. piperocaine having oxo groups directly attached to the heterocyclic ring, e.g. cycloheximide
    • 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
    • A61K9/2009Inorganic compounds
    • 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
    • A61K9/2031Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
    • A61K9/2036Silicones; Polysiloxanes
    • 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
    • A61K9/2095Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2813Inorganic compounds
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/282Organic compounds, e.g. fats
    • A61K9/2826Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
    • 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
    • A61K9/28Dragees; Coated pills or tablets, e.g. with film or compression coating
    • A61K9/2806Coating materials
    • A61K9/2833Organic macromolecular compounds
    • A61K9/286Polysaccharides, e.g. gums; Cyclodextrin
    • A61K9/2866Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/46Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of glucocorticosteroids

Landscapes

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

Abstract

Reivindicación 1: Una forma de dosificación farmacéutica para administración oral que comprende (a) el fármaco 4-[(5R)-6,7-dihidro-5H-pirrolo[1,2-c]imidazol-5-il]-3-fluorobenzonitrilo como se define por la fórmula [1] o cualquier sal farmacéuticamente aceptable del mismo, y (b) al menos 30% por peso de celulosa microcristalina con base en el peso total de dicha forma de dosificación farmacéutica. Reivindicación 3: La forma de dosificación farmacéutica según cualquiera de las reivindicaciones anteriores, en donde dicho fármaco está presente como sal de fosfato, preferiblemente como sal de mono-fosfato. Reivindicación 11: La forma de dosificación farmacéutica según cualquiera de las reivindicaciones anteriores que comprende: (a) 4 ± 1%, calculado con base a su base libre, por peso del fármaco 4-[(5R)-6,7-dihidro-5H-pirrolo[1,2-c]imidazol-5-il]-3-fluorobenzonitrilo presente como sal de monofosfato, (b) 77 ± 7% por peso de la celulosa microcristalina, (c) 0.6 ± 0.2% por peso de dióxido de silicio coloidal, (b) 10 ± 2% por peso de manitol, y opcionalmente que comprende además: (e) 2 ± 0.5% por peso de un agente disgregante, preferiblemente croscarmelosa de sodio, y (f) 1.5 ± 0.5%, por peso de un lubricante, preferiblemente estearato de magnesio con base en el peso total de dicha forma de dosificación farmacéutica. Reivindicación 15: El proceso según las reivindicaciones 12 a 14 caracterizado además por los siguientes pasos del proceso: (1) mezclar el fármaco junto con la celulosa microcristalina y opcionalmente ingredientes adicionales tales como un agente deslizante, un agente disgregante. y un agente lubricante, para obtener una mezcla compactable por máquina, (2) compactar la mezcla compactable por máquina mediante granulación en seco, preferiblemente mediante compactación con rodillo, para obtener un material compactado, (3) mezclar el material compactado con dióxido de silicio coloidal, y opcionalmente con ingredientes adicionales tales como celulosa microcristalina, manitol, un agente disgregante, y un lubricante, para obtener una mezcla comprensible por máquina, (4) comprimir la mezcla comprensible por máquina mediante el uso de una máquina de formación de comprimidos para obtener los comprimidos. Reivindicación 17: El uso de celulosa microcristalina para transformar el fármaco 4-[(5R)-6,7-dihidro-5H-pirrolo[1,2-c]imidazol-5 il]-3-fluorobenzonitrilo en un material farmacéuticamente procesable. Reivindicación 18: Una forma de dosificación farmacéutica según cualquiera de las reivindicaciones 1 - 11 o la reivindicación 16 para uso en el tratamiento de la enfermedad de Cushing o síndrome de Cushing.
ARP150102160A 2014-07-07 2015-07-06 Formas de dosificación farmacéuticas para administración oral AR101116A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462021271P 2014-07-07 2014-07-07

Publications (1)

Publication Number Publication Date
AR101116A1 true AR101116A1 (es) 2016-11-23

Family

ID=53610933

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150102160A AR101116A1 (es) 2014-07-07 2015-07-06 Formas de dosificación farmacéuticas para administración oral

Country Status (29)

Country Link
US (2) US10143680B2 (es)
EP (2) EP3166596B1 (es)
JP (2) JP6731136B2 (es)
KR (1) KR102468610B1 (es)
CN (1) CN106470704B (es)
AR (1) AR101116A1 (es)
AU (1) AU2015287336B2 (es)
BR (1) BR112016030243B1 (es)
CA (1) CA2954393C (es)
CL (1) CL2017000026A1 (es)
CY (1) CY1120749T1 (es)
DK (1) DK3166596T3 (es)
EA (2) EA033685B1 (es)
EC (1) ECSP17008187A (es)
ES (1) ES2686704T3 (es)
HR (1) HRP20181406T1 (es)
HU (1) HUE039037T2 (es)
IL (1) IL249374B (es)
LT (1) LT3166596T (es)
MX (1) MX2016017315A (es)
PE (1) PE20170201A1 (es)
PH (1) PH12016502540B1 (es)
PL (1) PL3166596T3 (es)
PT (1) PT3166596T (es)
SG (1) SG11201610227TA (es)
SI (1) SI3166596T1 (es)
TN (1) TN2016000557A1 (es)
TW (1) TWI707682B (es)
WO (1) WO2016005880A1 (es)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL301471B2 (en) 2016-10-27 2025-02-01 Damian Pharma Ag Aldosterone synthase inhibitor
SG11202010906XA (en) 2018-05-03 2020-12-30 Damian Pharma Ag R-fadrozole for use in the treatment of aldostonerism

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070191487A1 (en) 2004-03-17 2007-08-16 Rigassi-Dietrich Petra G Galenic formulations of organic compounds
GT200600381A (es) * 2005-08-25 2007-03-28 Compuestos organicos
CA2680684A1 (en) * 2007-03-13 2008-09-25 Takeda Pharmaceutical Company Limited Solid preparation comprising 2-[[6-[(3r)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1 (2h)-pyrimidinyl]methyl]-4-fluorobenzonitrile
LT2523731T (lt) * 2010-01-14 2019-02-11 Novartis Ag Antinksčių hormoną modifikuojančio agento panaudojimas
US20120064157A1 (en) * 2010-08-27 2012-03-15 Vertex Pharmaceuticals Incorporated Pharmaceutical composition and administrations thereof
DK2753312T3 (da) * 2011-09-08 2017-02-13 Mereo Biopharma 2 Ltd Anvendelse af en aromatase-inhibitor i behandlingen af hypogonadisme og relaterede sygdomme
PE20142358A1 (es) * 2012-01-17 2015-01-30 Novartis Ag Nuevas formas y sales de un dihidropirrolo[1,2-c]imidazolilo, inhibidor de la aldosterona sintasa o aromatasa
WO2013126326A1 (en) 2012-02-21 2013-08-29 Celgene Corporation Solid forms of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione, compositions and methods of use thereof
AU2013246908B2 (en) * 2012-04-12 2016-06-30 Novartis Ag Combination of somatostatin-analogs with 11beta-hydroxylase inhibitors
EP2815749A1 (en) 2013-06-20 2014-12-24 IP Gesellschaft für Management mbH Solid form of 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione having specified X-ray diffraction pattern

Also Published As

Publication number Publication date
KR20170029491A (ko) 2017-03-15
EP3166596B1 (en) 2018-06-06
BR112016030243A2 (pt) 2017-08-22
IL249374A0 (en) 2017-02-28
KR102468610B1 (ko) 2022-11-21
TW201613586A (en) 2016-04-16
DK3166596T3 (en) 2018-09-10
AU2015287336A1 (en) 2017-01-12
CA2954393C (en) 2022-07-19
SG11201610227TA (en) 2017-01-27
EA033685B1 (ru) 2019-11-15
IL249374B (en) 2021-09-30
US10709691B2 (en) 2020-07-14
EA201991359A1 (ru) 2020-03-13
HRP20181406T1 (hr) 2018-10-19
CL2017000026A1 (es) 2017-07-28
CN106470704A (zh) 2017-03-01
JP6731136B2 (ja) 2020-07-29
PH12016502540B1 (en) 2022-07-20
BR112016030243B1 (pt) 2023-04-11
JP2019194221A (ja) 2019-11-07
US20190060283A1 (en) 2019-02-28
ES2686704T3 (es) 2018-10-19
HUE039037T2 (hu) 2018-12-28
EP3412278A1 (en) 2018-12-12
CN106470704B (zh) 2020-07-31
CY1120749T1 (el) 2019-12-11
TN2016000557A1 (en) 2018-04-04
JP2017520590A (ja) 2017-07-27
AU2015287336B2 (en) 2018-06-14
PH12016502540A1 (en) 2017-04-10
EP3166596A1 (en) 2017-05-17
TWI707682B (zh) 2020-10-21
US10143680B2 (en) 2018-12-04
PT3166596T (pt) 2018-10-19
US20170202808A1 (en) 2017-07-20
ECSP17008187A (es) 2018-03-31
EA201790140A1 (ru) 2017-05-31
WO2016005880A1 (en) 2016-01-14
LT3166596T (lt) 2018-09-25
PE20170201A1 (es) 2017-04-08
SI3166596T1 (sl) 2018-10-30
MX2016017315A (es) 2017-04-27
CA2954393A1 (en) 2016-01-14
PL3166596T3 (pl) 2018-11-30

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