DK3119201T3 - Sildenafilopløsninger og fremgangsmåder til fremstilling og anvendelse heraf - Google Patents

Sildenafilopløsninger og fremgangsmåder til fremstilling og anvendelse heraf Download PDF

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Publication number
DK3119201T3
DK3119201T3 DK15764710.8T DK15764710T DK3119201T3 DK 3119201 T3 DK3119201 T3 DK 3119201T3 DK 15764710 T DK15764710 T DK 15764710T DK 3119201 T3 DK3119201 T3 DK 3119201T3
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Denmark
Prior art keywords
sildenafil citrate
water
pharmaceutical composition
solution
ethanol
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DK15764710.8T
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English (en)
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Moshe Rogosnitzky
Morris Aboohi
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Vigorous Solutions Ltd
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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
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • HELECTRICITY
    • H01ELECTRIC ELEMENTS
    • H01QANTENNAS, i.e. RADIO AERIALS
    • H01Q5/00Arrangements for simultaneous operation of antennas on two or more different wavebands, e.g. dual-band or multi-band arrangements
    • H01Q5/50Feeding or matching arrangements for broad-band or multi-band operation
    • H01Q5/55Feeding or matching arrangements for broad-band or multi-band operation for horn or waveguide antennas
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • 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
    • 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
    • A61K9/0056Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A61K9/0058Chewing gums
    • 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
    • A61K9/006Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/08Vasodilators for multiple indications
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • HELECTRICITY
    • H01ELECTRIC ELEMENTS
    • H01QANTENNAS, i.e. RADIO AERIALS
    • H01Q1/00Details of, or arrangements associated with, antennas
    • H01Q1/27Adaptation for use in or on movable bodies
    • H01Q1/28Adaptation for use in or on aircraft, missiles, satellites, or balloons
    • H01Q1/288Satellite antennas
    • HELECTRICITY
    • H01ELECTRIC ELEMENTS
    • H01QANTENNAS, i.e. RADIO AERIALS
    • H01Q1/00Details of, or arrangements associated with, antennas
    • H01Q1/36Structural form of radiating elements, e.g. cone, spiral, umbrella; Particular materials used therewith

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Zoology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Physics & Mathematics (AREA)
  • Physics & Mathematics (AREA)
  • Astronomy & Astrophysics (AREA)
  • Remote Sensing (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Aviation & Aerospace Engineering (AREA)
  • Gynecology & Obstetrics (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Claims (18)

  1. SILDENAFILOPLØSNINGER OG FREMGANGSMÅDER TIL FREMSTILLING OG ANVENDELSE HERAF
    1. Farmaceutisk sammensætning, der omfatter: (a) en flydende bærer, der navnlig består af vand og mindst 20 % ethanol; og (b) sildenafilcitrat opløst i den flydende bærer ved en koncentration på mindst 7 mg/ml.
  2. 2. Farmaceutisk sammensætning ifølge krav 1, der omfatter et smagsstof og/eller et bitterhedsblokerende middel.
  3. 3. Farmaceutisk sammensætning, der omfatter (a) en flydende bærer, der navnlig består af vand, ethanol og mindre end 20 % acetone; og (b) sildenafilcitratet opløst i den flydende bærer ved en koncentration på mindst 10 mg/ml.
  4. 4. Farmaceutisk sammensætning ifølge krav 3, der omfatter mindst ét af et smagsstof eller bitterhedsblokerende middel.
  5. 5. Farmaceutisk sammensætning, der omfatter: (a) en flydende bærer, der omfatter vand, ethanol og 0,0075 % til 20 % acetone; og (b) sildenafilcitrat opløst i den flydende bærer ved en koncentration på mindst 10 mg/ml.
  6. 6. Farmaceutisk sammensætning, der omfatter: (a) en flydende bærer, der omfatter vand og mindst 60 % ethanol; og (b) sildenafilcitrat opløst i den flydende bærer ved en koncentration på mindst 7 mg/ml.
  7. 7. Sammensætning ifølge et hvilket som helst af de foregående krav 3 til 5, der omfatter et stabiliseringsmiddel.
  8. 8. Sammensætning ifølge krav 7, hvor stabiliseringsmidlet er udvalgt fra gruppen bestående af: diacetyleret monoglycerid, diethylglycolmonopalmitostearat, glycerylbehenat, glyceryldistearat, glycerylmonolinoleat, glycerylmono-oleat, glycerylmonostearat, selvemulgerende glycerylmonostearat, macrogolcetostearylethere, cetomacrogol 1000, 9 polyoxyl 20 cetostearylether, macrogol 15 hydroxystearat, macrogollaurilethere, laureth 4, lauromacrogol 400, macrogolmonomethylethere, macrogololeylethere, polyoxyl 10 oleylether, macrogolstearater, polyoxyl 40 stearater, menfegol, mono- og diglycerider, nonoxinoler, octoxinoler, poloxamere, polyoxyl castorolie, polyoxyl-hydrogenerede castorolier, polysorbater, propylenglycoldiacetat, propylenglycollaureater, propylenglycoldilaurat, propylenglycolmonolaureat, propylenglycolmonopalmitostearat, quillaia, sorbitanestere, saccharoseestere, tyloxapol, carrageenan, cellulose, ceratonia, dextrater, ethylcellulose, gastrisk mucin, hyprolose, hypromellose, hypermellosephthalat, methylcellulose, polyethylenoxid, polyvinylacetat, polyvinylalkoholer, silica, natriumstivelsesglycolat, tragacanth og xanthangummi.
  9. 9. Fremgangsmåde, der omfatter: (a) anbringelse af sildenafilcitrat i en kombination, der navnlig består af ethanol og vand, for at frembringe en blanding; og (b) opvarmning af blandingen for at frembringe en opløsning af sildenafilcitratet ved en koncentration på mindst 7 mg/ml.
  10. 10. Fremgangsmåde ifølge krav 9, der omfatter: afkøling af opløsningen og tilsætning af ethanol og/eller vand.
  11. 11. Fremgangsmåde, der omfatter: (a) tilvejebringelse af et første volumen acetone; og (b) tilsætning af et andet volumen, der navnlig består af ethanol og vand, for at frembringe et totalt opløsningsvolumen; og (c) opløsning af sildenafilcitrat ved en koncentration på mindst 7 mg/ml i forhold til det totale volumen.
  12. 12. Fremgangsmåde ifølge krav 11, der omfatter: opvarmning af opløsningen til en temperatur på ikke mindre end 5 °C under acetonens kogepunkt.
  13. 13. Fremgangsmåde ifølge krav 12, der omfatter fjernelse af mindst 25 % af acetonen.
  14. 14. Fremgangsmåde ifølge krav 12, der omfatter: afkøling af opløsningen og tilsætning af én eller flere alkoholer og/eller vand til en total alkoholkoncentration på mindst 34 %.
  15. 15. Oral doseringsform, der omfatter: en ydre belægning; og en flydende kerne, der omfatter et farmaceutisk sammensætning ifølge et af kravene 1 til 8.
  16. 16. Bukkal doseringsform, der omfatter: en bærer, der indeholder en farmaceutisk sammensætning ifølge et af kravene 1 til 8; og en indpakning, der er tilpasset til af forhindre fordampning af den flydende bærer under opbevaring.
  17. 17. Behandlingskit, der omfatter: en beholder, der indeholder en flerhed af enkeltdoser af en farmaceutisk sammensætning ifølge et af kravene 1 til 8; og en måleanordning, der er kalibreret til afmåling af en enkelt dosis fra beholderen.
  18. 18. Behandlingskit ifølge krav 17, hvor hver af de enkle doser er indeholdt i en separat beholder; og emballeringsmateriale tilpasset til at indeholde de separate beholdere.
DK15764710.8T 2014-03-19 2015-03-19 Sildenafilopløsninger og fremgangsmåder til fremstilling og anvendelse heraf DK3119201T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461955299P 2014-03-19 2014-03-19
PCT/IB2015/052014 WO2015140748A2 (en) 2014-03-19 2015-03-19 Sildenafil solutions and methods of making and using same

Publications (1)

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DK3119201T3 true DK3119201T3 (da) 2018-05-28

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US (2) US9968609B2 (da)
EP (2) EP3372083A1 (da)
JP (1) JP6744821B2 (da)
KR (1) KR20160137584A (da)
CN (1) CN106132204B (da)
AU (2) AU2015233006B2 (da)
CA (1) CA2942628C (da)
CL (1) CL2016002318A1 (da)
CY (1) CY1120187T1 (da)
DK (1) DK3119201T3 (da)
EA (1) EA032819B1 (da)
ES (1) ES2668915T3 (da)
HR (1) HRP20180773T1 (da)
HU (1) HUE038431T2 (da)
IL (1) IL247840B (da)
LT (1) LT3119201T (da)
MX (1) MX371276B (da)
NO (1) NO2723977T3 (da)
PL (1) PL3119201T3 (da)
PT (1) PT3119201T (da)
RS (1) RS57206B1 (da)
SG (2) SG11201607507VA (da)
SI (1) SI3119201T1 (da)
WO (1) WO2015140748A2 (da)

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KR20160137584A (ko) 2016-11-30
RS57206B1 (sr) 2018-07-31
WO2015140748A3 (en) 2015-12-17
SI3119201T1 (en) 2018-07-31
HUE038431T2 (hu) 2018-10-29
NO2723977T3 (da) 2018-03-10
EP3119201A2 (en) 2017-01-25
US20170049776A1 (en) 2017-02-23
CN106132204A (zh) 2016-11-16
AU2018250378A1 (en) 2018-11-08
EP3119201B1 (en) 2018-03-14
PL3119201T3 (pl) 2018-08-31
AU2015233006B2 (en) 2018-07-19
CL2016002318A1 (es) 2017-03-24
AU2018250378B2 (en) 2020-05-14
MX371276B (es) 2020-01-23
CN106132204B (zh) 2019-08-20
EP3119201A4 (en) 2017-03-15
EA201691871A1 (ru) 2017-03-31
AU2015233006A1 (en) 2016-11-03
IL247840B (en) 2019-03-31
EP3372083A1 (en) 2018-09-12
MX2016012154A (es) 2016-12-15
CA2942628C (en) 2022-06-07
US9968609B2 (en) 2018-05-15
CA2942628A1 (en) 2015-09-24
SG10201808038TA (en) 2018-10-30
PT3119201T (pt) 2018-06-15
SG11201607507VA (en) 2016-10-28
US20180233823A1 (en) 2018-08-16
CY1120187T1 (el) 2018-12-12
ES2668915T3 (es) 2018-05-23
WO2015140748A2 (en) 2015-09-24
HRP20180773T1 (hr) 2018-06-15
LT3119201T (lt) 2018-05-10
EA032819B1 (ru) 2019-07-31
US10211534B2 (en) 2019-02-19
JP2017508764A (ja) 2017-03-30
JP6744821B2 (ja) 2020-08-19

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