HRP20230147T1 - Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom - Google Patents

Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom Download PDF

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HRP20230147T1
HRP20230147T1 HRP20230147TT HRP20230147T HRP20230147T1 HR P20230147 T1 HRP20230147 T1 HR P20230147T1 HR P20230147T T HRP20230147T T HR P20230147TT HR P20230147 T HRP20230147 T HR P20230147T HR P20230147 T1 HRP20230147 T1 HR P20230147T1
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particles
microns
formulation according
bdp
percent
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HRP20230147TT
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Elisa MONARI
Anna Maria Cantarelli
Daniela Cocconi
Irene PASQUALI
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Chiesi Farmaceutici S.P.A.
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Application filed by Chiesi Farmaceutici S.P.A. filed Critical Chiesi Farmaceutici S.P.A.
Publication of HRP20230147T1 publication Critical patent/HRP20230147T1/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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A61K31/167Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/20Carboxylic acids, e.g. valproic acid having a carboxyl group bound to a chain of seven or more carbon atoms, e.g. stearic, palmitic, arachidic acids
    • 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
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61K31/57Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • A61K31/573Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
    • 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
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/007Pulmonary tract; Aromatherapy
    • A61K9/0073Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • 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
    • A61MDEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M15/00Inhalators
    • A61M15/0001Details of inhalators; Constructional features thereof
    • A61M15/0003Details of inhalators; Constructional features thereof with means for dispensing more than one drug
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M15/00Inhalators
    • A61M15/0028Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up
    • A61M15/003Inhalators using prepacked dosages, one for each application, e.g. capsules to be perforated or broken-up using capsules, e.g. to be perforated or broken-up
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M15/00Inhalators
    • A61M15/009Inhalators using medicine packages with incorporated spraying means, e.g. aerosol cans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61MDEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
    • A61M2202/00Special media to be introduced, removed or treated
    • A61M2202/06Solids
    • A61M2202/064Powder

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Hematology (AREA)
  • Anesthesiology (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Otolaryngology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Claims (15)

1. Formulacija suhog praška za upotrebu u inhalatoru za suhi prašak (DPI) sadrži sljedeće: (a) udio fino usitnjenih čestica koje se sastoje od smjese sastavljene od 90 do 99.5 posto po masi fiziološki prihvatljivog ekscipijensa i 0.5 do 10 posto po masi magnezijeva stearata, gdje spomenuta smjesa ima prosječni promjer čestica manji od 20 mikrona, (b) udio grubo usitnjenih čestica koje se sastoje od fiziokoški prihvatljivog ekscipijensa koji ima prosječni promjer čestica između 200 i 400 mikrona, pri čemu je omjer fino usitnjenih čestica i grubo usitnjenih čestica između 1:99 i 30:70 posto po masi, te (c) formoterol-fumarat dihidrat u kombinaciji s beklometazon-dipropionatom (BDP) kao aktivni sastojci oba u obliku usitnjenih čestica; gdje je doza od 6-12 µg formoterol-fumarat dihidrata koja se isporučuje po aplikaciji i doza od 100 ili 200 µg BDP koja se isporučuje se po aplikaciji i usitnjene čestice formoterol-fumarat dihidrata imaju sljedeću raspodjelu čestica: i) ne više od 10% spomenutih čestica ima volumni promjer manji od 0.8 mikrona ii) ne više od 50% spomenutih čestica ima volumni promjer manji od 1.7 mikrona, te (iii) najmanje 90% spomenutih čestica ima prosječni volumni promjer manji od 5.0 mikrona, gdje su spomenute čestice formoterol-fumarat dihidrata naznačene time da je specifična površina od 5 do 7.5 m2/g i veličina čestica BDP u rasponu definiranom kao d(v,0.9) - d(v,0.1)]/d(v,0.5), jest između 1.2 i 2.2 m2/g i da je dalje naznačeno time da je specifična površina između 5.5 i 7.0 m2/g, pri čemu je specifična površina određena Brunaer-Tellerovom (BET) metodom adsorpcije dušika, te gdje: i) ne više od 10% spomenutih čestica ima volumni promjer manji od 0.6 mikrona ii) ne više od 50% spomenutih čestica ima volumni promjer između 1.5 i 2.0 mikrona, te (iii) najmanje 90% spomenutih čestica ima prosječni volumni promjer jednak ili manji od 4.7 mikrona, a veličina čestica aktivnih sastojaka određena je metodom laserske difrakcije upotrebom Malevernovog instrumenta, gdje fiziološki prihvatljiv akscipijens jest α-laktoza monohidrat.
2. Formulacija prema patentom zahtjevu 1, naznačena time da d(v,0.1) čestica BDP jest između 0.8 i 1.0 mikrona, d(v,0.5) u rasponu između1.5 i 2.0 mikrona i d(v,0.9) između 2.5 i 4.7 mikrona.
3. Formulacija prema patentom zahtjevu 2, naznačena time da veličina čestica BDP jest u rasponu između 1.3 i 2.1.
4. Formulacija prema patentnim zahtjevima 1-3, naznačena time da specifična površina čestica BDP jest između 5.9 i 6.8 m2/g.
5. Formulacija prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time da omjer fino usitnjenih čestica a) i grubo usitnjenih čestica b) jest između 2:98 i 20:80 posto po masi.
6. Formulacija prema patentom zahtjevu 5, naznačena time da omjer jest 10:90 posto po masi.
7. Formulacija prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time da udio fino usitnjenih čestica a) ima prosječnu veličinu čestica jednaku ili manju od 10 mikrona.
8. Formulacija prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time da je veličina čestica grubo usitnjenih čestica b) jest između 212 i 355 mikrona.
9. Formulacija prema bilo kojem od prethodnih patentnih zahtjeva, naznačena time da usitnjene čestice formoterol-fumarat hihidrata imaju promjer koji je manji od 6 mikrona.
10. Formulacija prema patentnim zahtjevima 1-9, pri čemu su usitnjene čestice formoterol-fumarat dihidrata naznačno time da je specifična površina od 5.2 do 6.5 m2/g.
11. Formulacija prema patentom zahtjevu 10, pri čemu su usitnjene čestica formoterol-fumarat dihidrata naznačeno time da je specifična površina od 5.5 do 5.8 m2/g.
12. Formulacija prema patentom zahtjevu 1, sastoji se od sljedećeg: (a) udio fino usitnjenih čestica koji se sastoji od smjese 98 posto po masi α-laktoza monohidrata i 2 posto po masi magnezijeva stearata, a spomenuta smjesa ima prosječni promjer čestica jednak ili manji od 6 mikrona, (b) udio grubo usitnjenih čestica koji se sastoji od α-laktoza monohidrata koji ima prosječni promjer čestica između 212 i 355 mikrona, u kojem omjer fino usitnjenih čestica ili grubo usitnjenih jest 10:90 posto po masi, te (c) formoterol-fumarat dihidrat u kombinaciji s beklometazon-dipropionatom (BDP) kao aktivni sastojci, a oba jesu u obliku usitnjenih čestica, pri čemu se isporučuje doza od 6-12 µg formoterol-fumarat dihidrata po aplikaciji i isporučuje se doza od 100 ili 200 µg BDP po aplikaciji, te i) ne više od 10% spomenutih čestica BDP ima volumni promjer manji od 0.7 mikrona, ii) ne više od 50% spomenutih čestica ima volumni promjer između 1.6 i 1.9 mikrona, te (iii) najmanje 90% spomenutih čestica ima volumni promjer manji od 4.0 mikrona.
13. Inhalator za suhi prašak je napunjen formulacijom suhog praška iz bilo kojeg od patentnih zahtjeva 1-12.
14. Formulacija prema bilo kojem od patentnih zahtjeva 1-12 za upotrebu u prevenciji i/ili liječenju upalne opstruktivne bolesti dišnih puteva.
15. Formulacija prema patentom zahtjevu 14, naznačena time da bolest jest astma ili kronična opstruktivna bolest pluća (COPD).
HRP20230147TT 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom HRP20230147T1 (hr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12152392 2012-01-25
EP18181331.2A EP3412277B1 (en) 2012-01-25 2013-01-23 Dry powder formulation comprising a corticosteroid and a beta-adrenergic for administration by inhalation

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HRP20230147T1 true HRP20230147T1 (hr) 2023-03-31

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Family Applications (5)

Application Number Title Priority Date Filing Date
HRP20230147TT HRP20230147T1 (hr) 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom
HRP20221431TT HRP20221431T1 (hr) 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom
HRP20221433TT HRP20221433T1 (hr) 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom
HRP20221432TT HRP20221432T1 (hr) 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom
HRP20181550TT HRP20181550T1 (hr) 2012-01-25 2018-09-28 Formulacija suhog praška koja sadrži kortikosteroid i beta-adrenergik za davanje inhalacijom

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Application Number Title Priority Date Filing Date
HRP20221431TT HRP20221431T1 (hr) 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom
HRP20221433TT HRP20221433T1 (hr) 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom
HRP20221432TT HRP20221432T1 (hr) 2012-01-25 2013-01-23 Formulacija suhog praška koja sadrži antikolinergik, kortikosteroid i beta-adrenergik za davanje inhalacijom
HRP20181550TT HRP20181550T1 (hr) 2012-01-25 2018-09-28 Formulacija suhog praška koja sadrži kortikosteroid i beta-adrenergik za davanje inhalacijom

Country Status (38)

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US (3) US10028964B2 (hr)
EP (7) EP3527197B1 (hr)
JP (1) JP6104282B2 (hr)
KR (3) KR101895279B1 (hr)
CN (2) CN105726548B (hr)
AR (1) AR089805A1 (hr)
AU (1) AU2013211656B2 (hr)
BR (1) BR112014017481A8 (hr)
CA (1) CA2862548C (hr)
CL (1) CL2014001966A1 (hr)
CO (1) CO7010836A2 (hr)
CY (1) CY1120684T1 (hr)
DK (5) DK3527199T3 (hr)
EA (2) EA031566B1 (hr)
ES (5) ES2928688T3 (hr)
FI (1) FI3412277T3 (hr)
GE (1) GEP201706767B (hr)
HK (1) HK1200021A1 (hr)
HR (5) HRP20230147T1 (hr)
HU (5) HUE040525T2 (hr)
IL (1) IL233784A0 (hr)
LT (5) LT3412277T (hr)
MA (1) MA35859B1 (hr)
MX (2) MX355729B (hr)
MY (1) MY165888A (hr)
NZ (1) NZ627837A (hr)
PE (1) PE20141703A1 (hr)
PH (1) PH12014501565A1 (hr)
PL (5) PL3412277T3 (hr)
PT (5) PT2806855T (hr)
RS (5) RS63761B1 (hr)
SG (1) SG11201404350PA (hr)
SI (2) SI3412277T1 (hr)
TN (1) TN2014000322A1 (hr)
TW (1) TWI559940B (hr)
UA (1) UA115543C2 (hr)
WO (1) WO2013110632A1 (hr)
ZA (1) ZA201405464B (hr)

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CA2962531C (en) 2014-10-08 2023-05-23 Eratech S.R.L. Composition comprising at least one dry powder obtained by spray drying to increase the stability of the formulation
CN109789107B (zh) * 2016-09-29 2021-12-03 广东东阳光药业有限公司 药物组合物
PL3621590T3 (pl) * 2017-05-11 2022-01-17 Chiesi Farmaceutici S.P.A. Sposób wytwarzania preparatu suchego proszku zawierającego środek antycholinergiczny, kortykosteroid i środek beta-adrenergiczny
US11931368B2 (en) 2017-09-29 2024-03-19 Crititech, Inc. Glucocorticoid “nintedanib” particles and their use
PT3833964T (pt) * 2018-08-07 2023-08-17 Norton Waterford Ltd Aplicação de espetroscopia de raman para o fabrico de pós de inalação
US20210370007A1 (en) 2018-10-30 2021-12-02 Chiesi Farmaceuticl S.p.A. Apparatus to administer drugs to mechanically ventilated patients
EP4034079A1 (en) 2019-09-24 2022-08-03 Chiesi Farmaceutici S.p.A. Novel carrier particles for dry powder formulations for inhalation
AU2021324395A1 (en) 2020-08-14 2023-03-16 Norton (Waterford) Limited An inhalable formulation of fluticasone propionate and albuterol sulfate
WO2023117967A1 (en) * 2021-12-21 2023-06-29 Chiesi Farmaceutici S.P.A. Dry powder formulations filled in an inhaler with improved resistance to humidity

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