HRP20231641T1 - Farmaceutski pripravak koji sadrži mitotan za oralnu primjenu za liječenje adrenokortikalnog karcinoma i cushingovog sindroma - Google Patents

Farmaceutski pripravak koji sadrži mitotan za oralnu primjenu za liječenje adrenokortikalnog karcinoma i cushingovog sindroma Download PDF

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Publication number
HRP20231641T1
HRP20231641T1 HRP20231641TT HRP20231641T HRP20231641T1 HR P20231641 T1 HRP20231641 T1 HR P20231641T1 HR P20231641T T HRP20231641T T HR P20231641TT HR P20231641 T HRP20231641 T HR P20231641T HR P20231641 T1 HRP20231641 T1 HR P20231641T1
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Croatia
Prior art keywords
cyclodextrin
mitotane
oil phase
formulation
mixtures
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Application number
HRP20231641TT
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English (en)
Inventor
Malika Lahiani-Skiba
Frédéric BOUNOURE
Michael Thomas
Hervé LEFEBVRE
Mohamed Skiba
Original Assignee
Mohamed Skiba
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Publication date
Application filed by Mohamed Skiba filed Critical Mohamed Skiba
Publication of HRP20231641T1 publication Critical patent/HRP20231641T1/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
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1617Organic compounds, e.g. phospholipids, fats
    • 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
    • A61K9/107Emulsions ; Emulsion preconcentrates; Micelles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/02Halogenated hydrocarbons
    • A61K31/025Halogenated hydrocarbons carbocyclic
    • A61K31/03Halogenated hydrocarbons carbocyclic aromatic
    • 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
    • A61K47/14Esters 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
    • A61K47/30Macromolecular 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
    • A61K47/40Cyclodextrins; Derivatives 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
    • A61K47/44Oils, fats or waxes according to two or more groups of A61K47/02-A61K47/42; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
    • 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
    • A61K9/14Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/16Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
    • A61K9/1605Excipients; Inactive ingredients
    • A61K9/1629Organic macromolecular compounds
    • A61K9/1652Polysaccharides, e.g. alginate, 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
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/38Drugs for disorders of the endocrine system of the suprarenal hormones

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Dispersion Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Claims (10)

1. Formulacija suhe emulzije mitotana koja sadrži: Uljnu fazu obogaćenu mitotanom i ciklodekstrinom koja sadrži ili ne sadrži suotapalo i/ili promotora apsorpcije.
2. Formulacija prema patentnom zahtjevu 1, naznačena time što je uljna faza biljno ulje ili njihove mješavine, životinjsko ulje ili njihove mješavine i/ili morsko ulje ili njihove mješavine prisutni su u nižem sadržaju od 50% težine.
3. Formulacija prema patentnom zahtjevu 1, naznačena time što uljna faza sadrži promotore apsorpcije i/ili suotapala koja su odabrana na primjer između sljedećih spojeva: gliceril kaprilat/kaprat, makro golglicerol hidroksistearat, makrogolglicerol ricinoleat (Cremophor EL®), polioksietilen sorbitan oleat, dietilen glikol monoetil eter, propilen glikol monokaprilat, apsolutni etanol i makrogol 800 do 300, a koji su prisutni u sadržaju od 10 do 20% težine.
4. Formulacija prema patentnom zahtjevu 1, naznačena time što je ciklodekstrin odabran između a-ciklodekstrina, β-ciklodekstrina i γ-ciklodekstrina i time što su derivati ciklodekstrina odabrani između hidroksipropilnih, metiliranih, etiliranih, sulfobutiliranih eter derivata ili acetiliranih a-ciklodekstrina, β-ciklodekstrina i γ-ciklodekstrina i binarne ili ternarne smjese navedenih ciklodekstrina i navedenih derivata ciklodekstrina, i prisutni su u sadržaju većem od 45% težine.
5. Farmaceutski i veterinarski pripravak koji sadrži formulaciju suhe emulzije mitotana kao što je definirana u jednom od patentnih zahtjeva 1 do 4.
6. Pripravak prema patentnom zahtjevu 5, naznačen time što je u obliku prikladnom za davanje oralnim putem.
7. Pripravak prema patentnom zahtjevu 6, naznačen time što je predstavljen u različitim oblicima, obloženim ili ne: prašak, granulat, mini-tablete, granule (peleti), tablete, kapsule.
8. Formulacija u obliku mekih kapsula ili tvrdih kapsula koja sadrži mitotan u uljnoj fazi i ciklodekstrin, kako je definirano u bilo kojem od patentnih zahtjeva 2 do 4.
9. Pripravak prema bilo kojem od patentnih zahtjeva 6 do 7, naznačen time što se koristi u liječenju karcinoma kore nadbubrežne žlijezde, kongenitalne adrenalne hiperplazije i Cushingovog sindroma.
10. Postupak za pripremu suhe emulzije mitotana prema patentnim zahtjevima 2 do 4 za formiranje sustava davanja mitotana, što uključuje solubilizaciju mitotana u uljnoj fazi s ili bez suotapala, dodavanje ciklodekstrina u uljnu fazu s ili bez promotora apsorpcije, dodavanje vodenaste faze za dobivanje primarne U/V emulzije zatim suhe emulzije na bazi mitotana, sušenje i kalibracija zrna.
HRP20231641TT 2019-10-28 2020-10-01 Farmaceutski pripravak koji sadrži mitotan za oralnu primjenu za liječenje adrenokortikalnog karcinoma i cushingovog sindroma HRP20231641T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
FR1912084A FR3102356B1 (fr) 2019-10-28 2019-10-28 Composition pharmaceutique comprenant le mitotane pour une administration par voie orale pour le traitement du carcinome corticosurrenalien et du syndrome de cushing
PCT/IB2020/059218 WO2021084345A1 (fr) 2019-10-28 2020-10-01 Composition pharmaceutique comprenant le mitotane pour une administration par voie orale pour le traitement du carcinome corticosurrenalien et du syndrome de cushing
EP20786346.5A EP4051249B1 (fr) 2019-10-28 2020-10-01 Composition pharmaceutique comprenant le mitotane pour une administration par voie orale pour le traitement du carcinome corticosurrenalien et du syndrome de cushing

Publications (1)

Publication Number Publication Date
HRP20231641T1 true HRP20231641T1 (hr) 2024-03-15

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ID=69810998

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20231641TT HRP20231641T1 (hr) 2019-10-28 2020-10-01 Farmaceutski pripravak koji sadrži mitotan za oralnu primjenu za liječenje adrenokortikalnog karcinoma i cushingovog sindroma

Country Status (16)

Country Link
US (1) US20240058277A1 (hr)
EP (1) EP4051249B1 (hr)
JP (1) JP2023500494A (hr)
KR (1) KR20220088904A (hr)
CN (1) CN114599347B (hr)
AU (1) AU2020377140A1 (hr)
CA (1) CA3153794A1 (hr)
ES (1) ES2966481T3 (hr)
FR (1) FR3102356B1 (hr)
HR (1) HRP20231641T1 (hr)
HU (1) HUE064738T2 (hr)
MX (1) MX2022004255A (hr)
PL (1) PL4051249T4 (hr)
RS (1) RS64962B1 (hr)
WO (1) WO2021084345A1 (hr)
ZA (1) ZA202205923B (hr)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4146648A (en) * 1977-07-14 1979-03-27 Bristol-Myers Company Chemotherapeutic composition
IL101007A (en) * 1992-02-18 1997-08-14 Pharmos Ltd Dry stable compositions prepared by lyophilization
ATE446087T1 (de) * 2006-01-23 2009-11-15 Yissum Res Dev Co Mikrokügelchen mit nanokapseln, die ein lipophiles arzneimittel enthalten
EP2255786A1 (en) 2009-05-25 2010-12-01 HRA Pharma LLC Self-microemulsifying mitotane composition
US20130317117A1 (en) 2010-11-24 2013-11-28 Pharmaceutics International, Inc. Self micro-emulsifying drug delivery system with increased bioavailability
CN105250221B (zh) * 2014-07-14 2018-06-19 天津药物研究院 一种利可瑞特干乳剂及其制备方法

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US20240058277A1 (en) 2024-02-22
WO2021084345A1 (fr) 2021-05-06
JP2023500494A (ja) 2023-01-06
PL4051249T3 (pl) 2024-04-08
CN114599347A (zh) 2022-06-07
EP4051249C0 (fr) 2023-09-13
AU2020377140A1 (en) 2022-06-09
CN114599347B (zh) 2024-07-12
HUE064738T2 (hu) 2024-04-28
EP4051249A1 (fr) 2022-09-07
MX2022004255A (es) 2022-05-06
KR20220088904A (ko) 2022-06-28
EP4051249B1 (fr) 2023-09-13
FR3102356B1 (fr) 2021-09-17
RS64962B1 (sr) 2024-01-31
CA3153794A1 (en) 2021-05-06
FR3102356A1 (fr) 2021-04-30
ZA202205923B (en) 2023-04-26
PL4051249T4 (pl) 2024-04-08
ES2966481T3 (es) 2024-04-22

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