EA201792674A1 - Способ образования наночастиц циклоспорина а/циклодекстрина - Google Patents

Способ образования наночастиц циклоспорина а/циклодекстрина

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Publication number
EA201792674A1
EA201792674A1 EA201792674A EA201792674A EA201792674A1 EA 201792674 A1 EA201792674 A1 EA 201792674A1 EA 201792674 A EA201792674 A EA 201792674A EA 201792674 A EA201792674 A EA 201792674A EA 201792674 A1 EA201792674 A1 EA 201792674A1
Authority
EA
Eurasian Patent Office
Prior art keywords
cyclodextrin
cyclosporin
formation
microparticles
nano
Prior art date
Application number
EA201792674A
Other languages
English (en)
Inventor
Торстейнн Лофтссон
Original Assignee
Окулис Эхф.
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 Окулис Эхф. filed Critical Окулис Эхф.
Publication of EA201792674A1 publication Critical patent/EA201792674A1/ru

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0048—Eye, e.g. artificial tears
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6949—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes
    • A61K47/6951—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit inclusion complexes, e.g. clathrates, cavitates or fullerenes using cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/12—Cyclic peptides, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C
    • A61K38/13—Cyclosporins
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6905—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion
    • A61K47/6907—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a colloid or an emulsion the form being a microemulsion, nanoemulsion or micelle
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/69—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit
    • A61K47/6921—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere
    • A61K47/6927—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores
    • A61K47/6929—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores the form being a nanoparticle, e.g. an immuno-nanoparticle
    • A61K47/6931—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores the form being a nanoparticle, e.g. an immuno-nanoparticle the material constituting the nanoparticle being a polymer
    • A61K47/6939—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the conjugate being characterised by physical or galenical forms, e.g. emulsion, particle, inclusion complex, stent or kit the form being a particulate, a powder, an adsorbate, a bead or a sphere the form being a solid microparticle having no hollow or gas-filled cores the form being a nanoparticle, e.g. an immuno-nanoparticle the material constituting the nanoparticle being a polymer the polymer being a polysaccharide, e.g. starch, chitosan, chitin, cellulose or pectin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605—Excipients; Inactive ingredients
    • A61K9/1629—Organic macromolecular compounds
    • A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1682—Processes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Immunology (AREA)
  • Nanotechnology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Dispersion Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Inorganic Chemistry (AREA)

Abstract

Способы образования наночастиц и микрочастиц комплексов циклоспорина/циклодекстрина и введение полученной суспензии нано- и микрочастиц в глаз человека или животного в форме водных глазных капель, подходящих для стимулирования или усиления выработки слезной жидкости и для лечения заболеваний глаз и окружающих зон. Композиция водных глазных капель содержит циклоспорин и смесь α-циклодекстрина и γ-циклодекстрина, а также один или несколько стабилизирующих полимеров, α-циклодекстрин солюбилизирует циклоспорин, а γ-циклодекстрин активизирует образование агрегатов комплексов циклоспорина/циклодекстрина. Полимеры стабилизируют водную суспензию нано- и микрочастиц.
EA201792674A 2015-05-29 2016-05-27 Способ образования наночастиц циклоспорина а/циклодекстрина EA201792674A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562168492P 2015-05-29 2015-05-29
PCT/IB2016/000816 WO2016193810A1 (en) 2015-05-29 2016-05-27 Formation of cyclosporin a/cyclodextrin nanoparticles

Publications (1)

Publication Number Publication Date
EA201792674A1 true EA201792674A1 (ru) 2018-04-30

Family

ID=56409120

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201792674A EA201792674A1 (ru) 2015-05-29 2016-05-27 Способ образования наночастиц циклоспорина а/циклодекстрина

Country Status (16)

Country Link
US (2) US20160346347A1 (ru)
EP (1) EP3302424A1 (ru)
JP (1) JP2018521117A (ru)
KR (1) KR20180028992A (ru)
CN (1) CN108024951A (ru)
AU (1) AU2016272700A1 (ru)
BR (1) BR112017025631A2 (ru)
CA (1) CA2986297A1 (ru)
CO (1) CO2017012573A2 (ru)
EA (1) EA201792674A1 (ru)
IL (1) IL255720A (ru)
MA (1) MA50637A (ru)
MX (1) MX2017015250A (ru)
PH (1) PH12017502155A1 (ru)
RU (1) RU2017146716A (ru)
WO (1) WO2016193810A1 (ru)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10231937B2 (en) 2014-06-24 2019-03-19 The Trustees Of Princeton University Process for encapsulating soluble biologics, therapeutics, and imaging agents
WO2019055539A1 (en) * 2017-09-12 2019-03-21 Prudhomme Robert K CELLULOSIC POLYMER NANOPARTICLES AND METHODS OF FORMING THE SAME
US11731099B2 (en) 2018-07-20 2023-08-22 The Trustees Of Princeton University Method for controlling encapsulation efficiency and burst release of water soluble molecules from nanoparticles and microparticles produced by inverse flash nanoprecipitation
CN109646684B (zh) * 2019-02-18 2021-05-28 天津医科大学总医院 环孢菌素h环糊精及其用途
EP3993807A1 (en) 2019-07-01 2022-05-11 Oculis SA Method for stabilizing the ph of an aqueous composition comprising a drug
CN112724200B (zh) * 2019-10-28 2022-09-27 上海云泽生物科技有限公司 一种稳定环孢霉素a的稀释液及其应用
CN111514115A (zh) * 2020-04-26 2020-08-11 天津大学 一种自身免疫性肝炎治疗纳米颗粒的合成方法
EP4356929A1 (en) 2022-10-19 2024-04-24 Universität Rostock Antifibrotic formulation for ophthalmic treatment
KR20240115545A (ko) * 2023-01-19 2024-07-26 주식회사 스카이테라퓨틱스 사이클로스포린 나노 분자회합체, 이를 포함하는 점안 조성물 및 그의 제조방법

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2577049B2 (ja) * 1987-06-04 1997-01-29 三共株式会社 シクロスポリン製剤
WO1993023010A1 (en) * 1992-05-13 1993-11-25 Sandoz Ltd. Ophthalmic compositions containing a cyclosporin
DE10036871A1 (de) * 2000-07-28 2002-02-14 Pharmasol Gmbh Dispersionen zur Formulierung wenig oder schwer löslicher Wirkstoffe
WO2006062875A1 (en) * 2004-12-08 2006-06-15 Merck & Co., Inc. Ophthalmic nanoparticulate formulation of a cyclooxygenase-2 selective inhibitor
US7893040B2 (en) 2005-07-22 2011-02-22 Oculis Ehf Cyclodextrin nanotechnology for ophthalmic drug delivery

Also Published As

Publication number Publication date
RU2017146716A (ru) 2019-07-02
MA50637A (fr) 2020-08-05
BR112017025631A2 (pt) 2018-08-07
IL255720A (en) 2018-02-28
CO2017012573A2 (es) 2018-03-28
AU2016272700A1 (en) 2017-12-14
KR20180028992A (ko) 2018-03-19
WO2016193810A8 (en) 2018-01-18
PH12017502155A1 (en) 2018-05-28
CA2986297A1 (en) 2016-12-08
CN108024951A (zh) 2018-05-11
EP3302424A1 (en) 2018-04-11
MX2017015250A (es) 2018-04-11
WO2016193810A1 (en) 2016-12-08
US20180161449A1 (en) 2018-06-14
US20160346347A1 (en) 2016-12-01
JP2018521117A (ja) 2018-08-02

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