HRP20240072T1 - Nanočestice koje sadrže takrolimus - Google Patents

Nanočestice koje sadrže takrolimus Download PDF

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Publication number
HRP20240072T1
HRP20240072T1 HRP20240072TT HRP20240072T HRP20240072T1 HR P20240072 T1 HRP20240072 T1 HR P20240072T1 HR P20240072T T HRP20240072T T HR P20240072TT HR P20240072 T HRP20240072 T HR P20240072T HR P20240072 T1 HRP20240072 T1 HR P20240072T1
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Croatia
Prior art keywords
film according
buccal film
mucoadhesive buccal
nanoparticles
cellulose
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Application number
HRP20240072TT
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English (en)
Inventor
Wolfgang Beier
Elke Horstkotte
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Nucleus Medical Gmbh
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Publication date
Application filed by Nucleus Medical Gmbh filed Critical Nucleus Medical Gmbh
Publication of HRP20240072T1 publication Critical patent/HRP20240072T1/hr

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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
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/145Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic compounds
    • 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
    • A61K9/141Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
    • A61K9/146Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
    • 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
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/436Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/5123Organic compounds, e.g. fats, sugars
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5138Organic macromolecular compounds; Dendrimers obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5146Organic macromolecular compounds; Dendrimers obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyamines, polyanhydrides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5107Excipients; Inactive ingredients
    • A61K9/513Organic macromolecular compounds; Dendrimers
    • A61K9/5161Polysaccharides, e.g. alginate, chitosan, cellulose derivatives; Cyclodextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/50Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
    • A61K9/51Nanocapsules; Nanoparticles
    • A61K9/5192Processes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7007Drug-containing films, membranes or sheets
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/70Web, sheet or filament bases ; Films; Fibres of the matrix type containing drug
    • A61K9/7023Transdermal patches and similar drug-containing composite devices, e.g. cataplasms
    • A61K9/703Transdermal patches and similar drug-containing composite devices, e.g. cataplasms characterised by shape or structure; Details concerning release liner or backing; Refillable patches; User-activated patches
    • A61K9/7038Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer
    • A61K9/7046Transdermal patches of the drug-in-adhesive type, i.e. comprising drug in the skin-adhesive layer the adhesive comprising macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection

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  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Nanotechnology (AREA)
  • Optics & Photonics (AREA)
  • Physics & Mathematics (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (9)

1. Mukoadhezivni bukalni film koji sadrži najmanje jedan sloj matrice koji sadrži najmanje jedan polimer i nanočestice koje sadrže takrolimus ili njegovu sol, pri čemu nanočestice imaju veličinu čestica od oko 10 do oko 400 nm.
2. Mukoadhezivni bukalni film prema patentnom zahtjevu 1, pri čemu nanočestice imaju indeks polidisperznosti od ~ oko 0,4.
3. Mukoadhezivni bukalni film prema bilo kojem od patentnih zahtjeva 1-2, pri čemu nanočestice dalje sadrže najmanje jedan agens za stabilizaciju i/ili surfaktant.
4. Mukoadhezivni bukalni film prema patentnom zahtjevu 3, pri čemu nanočestice dalje sadrže najmanje jedan agens za stabilizaciju, pri čemu najmanje jedan agens za stabilizaciju sadrži polivinil pirolidon, vinil pirolidon-/vinilacetat-kopolimer, polietilenglikol i/ili derivat celuloze kao što je hidroksipropilmetil celuloza (HPMC), hidroksipropilmetil celuloza ftalat (HPMCP), hidroksipropilmetil celuloza acetat sukcinat (HPMCAS), hidroksipropil celuloza (HPC) i/ili karboksimetil celuloza (CMC).
5. Mukoadhezivni bukalni film prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu najmanje jedan polimer sadrži hidroksipropilmetil celulozu, hidroksipropil celulozu, hidroksietil celulozu, škrob od graška, pululan, poli(met)akrilat, polivinil kaprolaktam-polivinil acetat-polietilen glikol graft kopolimer, kitozan, arapsku gumu, dekstran, dekstrin, alginat, polivinilalkohol, polivinilpirolidon i/ili vinil pirolidon-vinilacetat-kopolimer.
6. Mukoadhezivni bukalni film prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu najmanje jedan sloj matrice dalje sadrži najmanje jedno pomoćno sredstvo izabrano iz grupe koja sadrži boje, arome, zaslađivače, agense za maskiranje okusa, emulgatore, pojačivače, regulatore pH, humektante, konzervanse i/ili antioksidanse.
7. Mukoadhezivni bukalni film prema bilo kojem od prethodnih patentnih zahtjeva, pri čemu mukoadhezivni bukalni film sadrži jedan zaštitni sloj, koji je poželjno nepropustan za takrolimus na jednoj strani najmanje jednog sloja matrice.
8. Mukoadhezivni bukalni film prema bilo kojem od prethodnih patentnih zahtjeva, za primjenu kao medikament, posebno za primjenu u profilaksi i/ili liječenju odbacivanja presađenog čvrstog organa.
9. Mukoadhezivni bukalni film prema bilo kojem od patentnih zahtjeva 1-7, za primjenu kao medikament za liječenje pedijatrijskih pacijenata, posebno za primjenu u profilaksi i/ili liječenju odbacivanja presađenog čvrstog organa.
HRP20240072TT 2018-12-04 2019-12-04 Nanočestice koje sadrže takrolimus HRP20240072T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE102018130848 2018-12-04
EP19816295.0A EP3846783B8 (en) 2018-12-04 2019-12-04 Nanoparticles comprising tacrolimus
PCT/EP2019/083691 WO2020115140A1 (en) 2018-12-04 2019-12-04 Nanoparticles comprising tacrolimus

Publications (1)

Publication Number Publication Date
HRP20240072T1 true HRP20240072T1 (hr) 2024-05-10

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HRP20240072TT HRP20240072T1 (hr) 2018-12-04 2019-12-04 Nanočestice koje sadrže takrolimus

Country Status (18)

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US (2) US11311479B2 (hr)
EP (2) EP3662894B1 (hr)
JP (1) JP2022513697A (hr)
KR (1) KR20210100142A (hr)
CN (1) CN113242732A (hr)
AU (1) AU2019392718A1 (hr)
CA (1) CA3063417C (hr)
DK (2) DK3662894T3 (hr)
ES (2) ES2894112T3 (hr)
FI (1) FI3846783T3 (hr)
HR (1) HRP20240072T1 (hr)
HU (2) HUE056067T2 (hr)
IL (1) IL283458A (hr)
PL (2) PL3662894T3 (hr)
PT (1) PT3846783T (hr)
SG (1) SG11202105778PA (hr)
SI (2) SI3662894T1 (hr)
WO (1) WO2020115140A1 (hr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113425716A (zh) * 2021-05-27 2021-09-24 南京诺亚药业有限公司 一种他克莫司药物组合物及其制备方法
EP4104816A1 (en) * 2021-06-14 2022-12-21 Nucleus Medical GmbH Non-nanoparticulate applications forms of macrolides
AU2023232910A1 (en) * 2022-03-11 2024-09-12 Lts Lohmann Therapie-Systeme Ag Transmucosal therapeutic system containing a macrolide immunosuppressant
WO2024052883A1 (en) * 2022-09-10 2024-03-14 Pattanaik Smita Buccomucoadhesive patch-based drug delivery system for tacrolimus
EP4410287A1 (en) * 2023-02-06 2024-08-07 Nucleus Medical GmbH A macrolide for use in a method of preventing or treating an immunological disease or disorder
WO2024165562A1 (en) * 2023-02-06 2024-08-15 Nucleus Medical Gmbh A macrolide for use in a method of preventing or treating an immunological disease or disorder

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007502823A (ja) * 2003-08-15 2007-02-15 キューエルティー・ユーエスエイ・インコーポレーテッド 接着性および生体侵食性の経粘膜薬物送達システム
EP1835889A1 (en) * 2004-12-15 2007-09-26 Elan Pharma International Limited Nanoparticulate tacrolimus formulations
CN101652141A (zh) * 2007-03-29 2010-02-17 万能药生物有限公司 他克莫司的调节释放剂型
MA34586B1 (fr) * 2010-08-25 2013-10-02 Medis Lab Particules cristallines de tacrolimus micronise a surface modifiee et compositions pharmaceutiques associees
EP2958555A2 (en) * 2013-02-21 2015-12-30 Massachusetts Institute of Technology Targeted buccal delivery of agents
JP2018510859A (ja) * 2015-03-17 2018-04-19 レオン−ナノドラッグズ ゲーエムベーハー 安定化されたボロン酸化合物を含むナノ粒子
DE102016101232A1 (de) 2016-01-25 2017-07-27 Instillo Gmbh Verfahren zum Herstellen von Emulsionen

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Publication number Publication date
CN113242732A (zh) 2021-08-10
DK3662894T3 (da) 2021-09-20
KR20210100142A (ko) 2021-08-13
CA3063417A1 (en) 2020-06-04
US20220079872A1 (en) 2022-03-17
PT3846783T (pt) 2024-01-19
HUE056067T2 (hu) 2022-01-28
PL3662894T3 (pl) 2022-01-10
WO2020115140A1 (en) 2020-06-11
US20200170934A1 (en) 2020-06-04
EP3846783B8 (en) 2023-11-22
ES2894112T3 (es) 2022-02-11
ES2969096T3 (es) 2024-05-16
DK3846783T3 (da) 2024-01-15
EP3846783A1 (en) 2021-07-14
HUE065588T2 (hu) 2024-06-28
SI3662894T1 (sl) 2021-11-30
EP3662894A1 (en) 2020-06-10
AU2019392718A1 (en) 2021-06-10
US11311479B2 (en) 2022-04-26
PL3846783T3 (pl) 2024-04-02
FI3846783T3 (fi) 2024-01-15
SI3846783T1 (sl) 2024-03-29
EP3662894B1 (en) 2021-07-28
JP2022513697A (ja) 2022-02-09
CA3063417C (en) 2023-01-03
EP3846783B1 (en) 2023-10-18
SG11202105778PA (en) 2021-06-29
IL283458A (en) 2021-07-29
US11904048B2 (en) 2024-02-20

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