CN111249228B - 包含释放一氧化氮的前列酰胺的眼用组合物 - Google Patents

包含释放一氧化氮的前列酰胺的眼用组合物 Download PDF

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Publication number
CN111249228B
CN111249228B CN202010145208.8A CN202010145208A CN111249228B CN 111249228 B CN111249228 B CN 111249228B CN 202010145208 A CN202010145208 A CN 202010145208A CN 111249228 B CN111249228 B CN 111249228B
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Prior art keywords
ophthalmic
solution
polyethylene glycol
ester
propen
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Chinese (zh)
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CN111249228A (zh
Inventor
F·皮洛塔茨
A·L·韦纳
M·多
J·萨尔多
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Nicox SA
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Nicox SA
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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
    • A61K31/557Eicosanoids, e.g. leukotrienes or prostaglandins
    • A61K31/5575Eicosanoids, e.g. leukotrienes or prostaglandins having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/216Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acids having aromatic rings, e.g. benactizyne, clofibrate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/21Esters, e.g. nitroglycerine, selenocyanates
    • A61K31/215Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
    • A61K31/22Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin
    • A61K31/222Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids of acyclic acids, e.g. pravastatin with compounds having aromatic groups, e.g. dipivefrine, ibopamine
    • 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
    • A61K47/08Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/12Carboxylic acids; Salts or anhydrides thereof
    • 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
    • A61K47/14Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • 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
    • 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
    • A61K47/24Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
    • 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
    • A61K9/08Solutions
    • 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
    • A61P27/06Antiglaucoma agents or miotics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Ophthalmology & Optometry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Inorganic Chemistry (AREA)
  • Emergency Medicine (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN202010145208.8A 2018-07-12 2019-07-10 包含释放一氧化氮的前列酰胺的眼用组合物 Active CN111249228B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP18290082.9 2018-07-12
EP18290082 2018-07-12
CN201910622356.1A CN110237031B (zh) 2018-07-12 2019-07-10 包含释放一氧化氮的前列酰胺的眼用组合物

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CN111249228A CN111249228A (zh) 2020-06-09
CN111249228B true CN111249228B (zh) 2022-05-03

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CN201910622356.1A Active CN110237031B (zh) 2018-07-12 2019-07-10 包含释放一氧化氮的前列酰胺的眼用组合物

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US (5) US10688073B2 (https=)
EP (2) EP3718535B1 (https=)
JP (4) JP6672512B2 (https=)
KR (1) KR102861273B1 (https=)
CN (2) CN111249228B (https=)
AR (1) AR115734A1 (https=)
AU (2) AU2019300203B2 (https=)
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CA (1) CA3105989A1 (https=)
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Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2019300203B2 (en) * 2018-07-12 2025-01-30 Nicox S.A. Ophthalmic compositions containing a nitric oxide releasing prostamide
EP4404936A1 (en) * 2021-09-20 2024-07-31 Nicox SA Nitric oxide releasing prostamide as neuroprotective agent
JP7665073B1 (ja) 2024-04-05 2025-04-18 ロート製薬株式会社 容器に収容してなる眼科用組成物
US20260053768A1 (en) * 2024-05-07 2026-02-26 Maher Hadaya Sustained Nitric Oxide Releasing Drug Delivery Systems

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WO2009013435A2 (fr) * 2007-07-20 2009-01-29 Laboratoires Thea Solution ophtalmique à base de prostaglandines sans conservateur
CN101835473A (zh) * 2007-10-16 2010-09-15 太阳医药高级研发有限公司 新型眼药组合物
CN102099330A (zh) * 2008-05-09 2011-06-15 尼科克斯公司 供给氧化氮的前列酰胺
CN103764120A (zh) * 2011-06-29 2014-04-30 阿勒根公司 聚乙二醇15羟基硬脂酸酯制剂
CN105012231A (zh) * 2014-04-30 2015-11-04 四川科伦药物研究院有限公司 一种包含PGF2α衍生物的稳定性良好的眼用制剂及其制备方法
CN105380901A (zh) * 2015-11-18 2016-03-09 侯宇华 一种他氟前列素滴眼剂及其制备方法

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MX2011002688A (es) 2008-09-12 2011-04-12 Critical Pharmaceuticals Ltd Mejoramientos en la absorcion de agentes terapeuticos a traves de las membranas mucosas o la piel.
US20130267591A1 (en) * 2010-05-07 2013-10-10 Sun Pharma Advanced Research Company Limited Novel ophthalmic compositions
FR2961694B1 (fr) * 2010-06-29 2013-01-25 Thea Lab Systeme de delivrance polymerique d'une solution non visqueuse a base de prostaglandine sans conservateur
CA2841644A1 (en) 2011-08-02 2013-02-07 Cipla Limited Pharmaceutical composition comprising ebastine and fluticasone
AU2019300203B2 (en) * 2018-07-12 2025-01-30 Nicox S.A. Ophthalmic compositions containing a nitric oxide releasing prostamide

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WO2009013435A2 (fr) * 2007-07-20 2009-01-29 Laboratoires Thea Solution ophtalmique à base de prostaglandines sans conservateur
CN101835473A (zh) * 2007-10-16 2010-09-15 太阳医药高级研发有限公司 新型眼药组合物
CN102099330A (zh) * 2008-05-09 2011-06-15 尼科克斯公司 供给氧化氮的前列酰胺
CN103764120A (zh) * 2011-06-29 2014-04-30 阿勒根公司 聚乙二醇15羟基硬脂酸酯制剂
CN105012231A (zh) * 2014-04-30 2015-11-04 四川科伦药物研究院有限公司 一种包含PGF2α衍生物的稳定性良好的眼用制剂及其制备方法
CN105380901A (zh) * 2015-11-18 2016-03-09 侯宇华 一种他氟前列素滴眼剂及其制备方法

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US12178793B2 (en) 2024-12-31
DK3593788T3 (da) 2021-01-11
PH12020552112A1 (en) 2021-05-31
BR112021000240A2 (pt) 2021-04-06
RS61348B1 (sr) 2021-02-26
SMT202100034T1 (it) 2021-03-15
ES2847853T3 (es) 2021-08-04
JP2022116147A (ja) 2022-08-09
JP2020011955A (ja) 2020-01-23
SI3593788T1 (sl) 2021-03-31
AU2019300203B2 (en) 2025-01-30
EP3718535C0 (en) 2025-06-18
US11020368B2 (en) 2021-06-01
MX2023007091A (es) 2023-06-27
EP3593788B1 (en) 2020-10-28
AU2019300203A1 (en) 2021-03-04
US20200206176A1 (en) 2020-07-02
PL3718535T3 (pl) 2025-10-13
KR102861273B1 (ko) 2025-09-17
AR115734A1 (es) 2021-02-17
LT3593788T (lt) 2021-04-12
SG11202100064WA (en) 2021-02-25
MA48919B1 (fr) 2021-02-26
MA48919A (fr) 2020-01-15
MY205816A (en) 2024-11-14
JP2020105201A (ja) 2020-07-09
EP3593788A1 (en) 2020-01-15
MA52258B1 (fr) 2025-07-31
SMT202500425T1 (it) 2026-01-12
MX2021000411A (es) 2021-03-25
US20200016108A1 (en) 2020-01-16
MD3593788T2 (ro) 2021-03-31
CY1123706T1 (el) 2022-05-27
CN110237031B (zh) 2022-02-11
KR20210032435A (ko) 2021-03-24
MA52258A (fr) 2021-02-17
PL3593788T3 (pl) 2021-05-31
PT3593788T (pt) 2021-01-21
HUE052747T2 (hu) 2021-05-28
TW202019401A (zh) 2020-06-01
RS67054B1 (sr) 2025-08-29
EP3718535A1 (en) 2020-10-07
HRP20210138T1 (hr) 2021-03-19
EP3718535B1 (en) 2025-06-18
CN110237031A (zh) 2019-09-17
CN111249228A (zh) 2020-06-09
ES3036636T3 (en) 2025-09-23
HUE072927T2 (hu) 2025-12-28
JP7397910B2 (ja) 2023-12-13
CA3105989A1 (en) 2020-01-16
TWI839364B (zh) 2024-04-21
US20210128458A1 (en) 2021-05-06
WO2020011845A1 (en) 2020-01-16
MD3718535T2 (ro) 2025-08-31
AU2025203019A1 (en) 2025-05-15
US12186295B2 (en) 2025-01-07
JP6672512B2 (ja) 2020-03-25
JP2024023498A (ja) 2024-02-21
HRP20251098T1 (hr) 2025-11-07
US10688073B2 (en) 2020-06-23
US20250073196A1 (en) 2025-03-06
US20210220316A1 (en) 2021-07-22
JP7080268B2 (ja) 2022-06-03

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