ES2905793T3 - Procedimiento para la preparación de suspensiones acuosas estériles oftálmicas de nanocristales de propionato de fluticasona de Forma A - Google Patents

Procedimiento para la preparación de suspensiones acuosas estériles oftálmicas de nanocristales de propionato de fluticasona de Forma A Download PDF

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Publication number
ES2905793T3
ES2905793T3 ES20186965T ES20186965T ES2905793T3 ES 2905793 T3 ES2905793 T3 ES 2905793T3 ES 20186965 T ES20186965 T ES 20186965T ES 20186965 T ES20186965 T ES 20186965T ES 2905793 T3 ES2905793 T3 ES 2905793T3
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Prior art keywords
fluticasone propionate
nanocrystals
aqueous
nanosuspension
concentration
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Application number
ES20186965T
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English (en)
Spanish (es)
Inventor
Jean-Michel Bukowski
Akshay Nadkarni
José L Boyer
Brigitte Duquesroix-Chakroun
Tomas Navratil
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nicox Ophthalmics Inc
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Nicox Ophthalmics Inc
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Publication of ES2905793T3 publication Critical patent/ES2905793T3/es
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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
    • A61K9/08Solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/567Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in position 17 alpha, e.g. mestranol, norethandrolone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/565Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol
    • A61K31/568Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone
    • A61K31/569Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. estrane, estradiol substituted in positions 10 and 13 by a chain having at least one carbon atom, e.g. androstanes, e.g. testosterone substituted in position 17 alpha, e.g. ethisterone
    • 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
    • A61K47/02Inorganic compounds
    • 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
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/183Amino acids, e.g. glycine, EDTA or aspartame
    • 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
    • A61K47/16Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
    • A61K47/18Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
    • A61K47/186Quaternary ammonium compounds, e.g. benzalkonium chloride or cetrimide
    • 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
    • A61K47/26Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
    • 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
    • A61K47/36Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
    • A61K47/38Cellulose; Derivatives thereof
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0048Eye, e.g. artificial tears
    • 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
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • A61P27/04Artificial tears; Irrigation solutions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B82NANOTECHNOLOGY
    • B82YSPECIFIC USES OR APPLICATIONS OF NANOSTRUCTURES; MEASUREMENT OR ANALYSIS OF NANOSTRUCTURES; MANUFACTURE OR TREATMENT OF NANOSTRUCTURES
    • B82Y5/00Nanobiotechnology or nanomedicine, e.g. protein engineering or drug delivery
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J31/00Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
    • C07J31/006Normal steroids containing one or more sulfur atoms not belonging to a hetero ring not covered by C07J31/003

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Ophthalmology & Optometry (AREA)
  • Inorganic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dispersion Chemistry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Nanotechnology (AREA)
  • Rheumatology (AREA)
  • Biophysics (AREA)
  • Biotechnology (AREA)
  • General Engineering & Computer Science (AREA)
  • Medical Informatics (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Pain & Pain Management (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
ES20186965T 2019-07-23 2020-07-21 Procedimiento para la preparación de suspensiones acuosas estériles oftálmicas de nanocristales de propionato de fluticasona de Forma A Active ES2905793T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201962877599P 2019-07-23 2019-07-23
US201962942551P 2019-12-02 2019-12-02

Publications (1)

Publication Number Publication Date
ES2905793T3 true ES2905793T3 (es) 2022-04-12

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ES20186965T Active ES2905793T3 (es) 2019-07-23 2020-07-21 Procedimiento para la preparación de suspensiones acuosas estériles oftálmicas de nanocristales de propionato de fluticasona de Forma A

Country Status (23)

Country Link
US (3) US11406596B2 (enExample)
EP (1) EP3769753B1 (enExample)
JP (2) JP7021301B2 (enExample)
KR (1) KR20220038443A (enExample)
CN (2) CN115120557B (enExample)
AU (1) AU2020317084A1 (enExample)
CA (1) CA3145055A1 (enExample)
CY (1) CY1124930T1 (enExample)
DK (1) DK3769753T3 (enExample)
ES (1) ES2905793T3 (enExample)
HR (1) HRP20220165T1 (enExample)
HU (1) HUE057416T2 (enExample)
LT (1) LT3769753T (enExample)
MD (1) MD3769753T2 (enExample)
MX (1) MX420447B (enExample)
PH (1) PH12022550003A1 (enExample)
PL (1) PL3769753T3 (enExample)
PT (1) PT3769753T (enExample)
RS (1) RS62932B1 (enExample)
SI (1) SI3769753T1 (enExample)
SM (1) SMT202200082T1 (enExample)
TW (1) TWI864053B (enExample)
WO (1) WO2021014348A1 (enExample)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2020317084A1 (en) * 2019-07-23 2022-03-03 Nicox Ophthalmics, Inc. Process for the preparation of sterile ophthalmic aqueous fluticasone propionate form a nanocrystals suspensions
CN115887372A (zh) * 2022-10-25 2023-04-04 苏州欧康维视生物科技有限公司 丙酸氟替卡松混悬液及其制备方法
CN115554238A (zh) * 2022-10-25 2023-01-03 苏州欧康维视生物科技有限公司 眼用混悬液及其制备方法

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK0639070T4 (da) 1992-05-06 2010-12-13 Alcon Lab Inc Anvendelse af borat-polyolkomplekser til ophtalmiske præparater
JP3450805B2 (ja) * 2000-08-08 2003-09-29 わかもと製薬株式会社 水性医薬組成物
US6900184B2 (en) * 2003-04-14 2005-05-31 Wyeth Holdings Corporation Compositions containing pipercillin and tazobactam useful for injection
US20060229219A1 (en) 2005-04-11 2006-10-12 Advanced Medical Optics, Inc. Borate-polyol mixtures as a buffering system
US8010032B2 (en) * 2005-05-23 2011-08-30 Xerox Corporation Fuser member comprising deflocculated material
WO2010141834A1 (en) 2009-06-05 2010-12-09 Aciex Therapeutics, Inc. Ophthalmic formulations of fluticasone and methods of use
TWI489997B (zh) 2009-06-19 2015-07-01 Alcon Res Ltd 含有硼酸-多元醇錯合物之水性藥學組成物
US20130065888A1 (en) 2011-08-15 2013-03-14 Biserka Cetina-Cizmek Ophthalmic formulations and processes for their preparation
DK3517541T3 (da) 2012-05-08 2020-09-07 Nicox Ophthalmics Inc Polymorf form af fluticasonpropionat
CA2893654A1 (en) * 2012-12-17 2014-06-26 Glaxo Group Limited Combination of levocabastine and fluticasone furoate for the treatment of inflammatory and/or allergic conditions
TWI773641B (zh) 2015-05-08 2022-08-11 日商活效製藥股份有限公司 含有糖皮質類固醇(glucocorticoids)之奈米微粒子之水性懸浮液劑
AU2020317084A1 (en) * 2019-07-23 2022-03-03 Nicox Ophthalmics, Inc. Process for the preparation of sterile ophthalmic aqueous fluticasone propionate form a nanocrystals suspensions

Also Published As

Publication number Publication date
RS62932B1 (sr) 2022-03-31
PT3769753T (pt) 2022-02-15
AU2020317084A1 (en) 2022-03-03
WO2021014348A1 (en) 2021-01-28
TW202116326A (zh) 2021-05-01
US11406596B2 (en) 2022-08-09
EP3769753A1 (en) 2021-01-27
SI3769753T1 (sl) 2022-04-29
MD3769753T2 (ro) 2022-04-30
SMT202200082T1 (it) 2022-03-21
MX420447B (es) 2025-02-10
JP7494230B2 (ja) 2024-06-03
CN111821261B (zh) 2022-07-26
DK3769753T3 (da) 2022-01-31
HUE057416T2 (hu) 2022-05-28
US20210023001A1 (en) 2021-01-28
CN115120557A (zh) 2022-09-30
EP3769753B1 (en) 2021-11-17
JP2022062172A (ja) 2022-04-19
HRP20220165T1 (hr) 2022-04-29
JP7021301B2 (ja) 2022-02-16
CN115120557B (zh) 2024-05-07
MX2022000928A (es) 2022-02-22
KR20220038443A (ko) 2022-03-28
PH12022550003A1 (en) 2022-11-14
JP2021017449A (ja) 2021-02-15
CN111821261A (zh) 2020-10-27
US20220241296A1 (en) 2022-08-04
US20220323352A1 (en) 2022-10-13
CY1124930T1 (el) 2023-01-05
TWI864053B (zh) 2024-12-01
CA3145055A1 (en) 2021-01-28
PL3769753T3 (pl) 2022-04-04
LT3769753T (lt) 2022-05-10

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