SI2600830T1 - Formulacija suhega praška, obsegajoča fosfodiesterazni inhibitor - Google Patents

Formulacija suhega praška, obsegajoča fosfodiesterazni inhibitor Download PDF

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Publication number
SI2600830T1
SI2600830T1 SI201131448T SI201131448T SI2600830T1 SI 2600830 T1 SI2600830 T1 SI 2600830T1 SI 201131448 T SI201131448 T SI 201131448T SI 201131448 T SI201131448 T SI 201131448T SI 2600830 T1 SI2600830 T1 SI 2600830T1
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Slovenia
Prior art keywords
inhalable
powder according
dry powder
inhalable powder
formulation
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SI201131448T
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English (en)
Inventor
Daniela Cocconi
Francesca Schiaretti
Roberto Bilzi
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Chiesi Farmaceutici S.P.A.
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Publication of SI2600830T1 publication Critical patent/SI2600830T1/sl

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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
    • A61K31/33Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated 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
    • A61K9/007Pulmonary 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
    • 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
    • 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
    • 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

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

Claims (18)

  1. FORMULACIJA SUHEGA PRAŠKA, OBSEGAJOČA FOSFODIESTERAZNI INHIBITOR PATENTNI ZAHTEVKI
    1. Inhalabilna formulacija suhega praška, ki obsega mikronizirane delce spojine s splošno formulo (I) kot (-) enantiomer, kjer:
    n je 0 ali 1; Ri in R2 sta lahko enaka ali različna in sta izbrana iz skupine, ki jo sestavljajo: - linearen ali razvejen CrCe alkil, opcijsko substituiran z enim ali več atomi halogena; - OR3, kjer je R3 linearen ali razvejen Ci-C6 alkil, opcijsko substituiran z enim ali več atomi halogena ali C3-C7 cikloalkilnimi skupinami; in - HNSO2R4, kjer je R4 linearen ali razvejen C1-C4 alkil, opcijsko substituiran z enim ali več atomi halogena, kjer je vsaj eden od R1 in R2 HNSO2R4; in grobe delce nosilca, narejene iz fiziološko sprejemljive farmakološko inertne snovi z masnim premerom 150 do 400 mikronov; kjer se omenjena spojina daje v terapevtsko učinkovitem enkratnem odmerku, ki je med 300 pg in 2000 pg.
  2. 2. Inhalabilen prašek po zahtevku 1, kjer je enkratni odmerek med 300 pg in 600 M9·
  3. 3. Inhalabilen prašek po zahtevku 2, kjer je enkratni odmerek 400 pg ali 600 pg.
  4. 4. Inhalabilen prašek po katerem koli od zahtevkov 1 do 3, kjer je spojina s formulo (I) 1 -(3-ciklopropilmetoksi-4-difluorometoksi-fenil)-2-(3,5-dikloro-1 -oksi-piridin-4-il)-etil ester (-)-3-ciklopropilmetoksi-4-metansulfonilamino-benzojske kisline (C2).
  5. 5. Inhalabilen prašek po katerem koli od zahtevkov 1 do 4, kjer je fiziološko sprejemljiva farmakološko inertna snov kristalinični sladkor, izbran iz skupine, ki jo sestavljajo glukoza, arabinoza, maltoza, saharoza, dekstroza in laktoza ali polialkohol, izbran iz skupine, ki jo sestavljajo manitol, maltitol, laktitol in sorbitol.
  6. 6. Inhalabilen prašek po zahtevku 5, kjer je sladkor laktoza.
  7. 7. Inhalabilen prašek po zahtevku 6, kjer je sladkor α-laktoza monohidrat.
  8. 8. Inhalabilen prašek po katerem koli od zahtevkov 1 do 7, kjer imajo grobi delci nosilca masni premer, ki je med 212 in 355 mikroni.
  9. 9. Inhalabilen prašek po katerem koli od predhodnih zahtevkov, ki nadalje obsega eno ali več aditivnih snovi, izbranih iz skupine, ki jo sestavljajo aminokisline, v vodi topna površinsko aktivna sredstva, maziva in drsila.
  10. 10. Inhalabilen prašek po zahtevku 9, kjer je aditivna snov mazivo.
  11. 11. Inhalabilen prašek po zahtevku 10, kjer je aditivna snov magnezijev stearat.
  12. 12. Inhalabilen prašek po zahtevku 11, kjer je magnezijev stearat prisoten v količini, ki je med 0,01 in 2 mas. % glede na celotno maso formulacije.
  13. 13. Inhalabilen prašek po zahtevku 12, kjer je količina magnezijevega stearata med 0,02 in 1 % m/m.
  14. 14. Inhalabilen prašek po katerem koli od predhodnih zahtevkov, ki nadalje obsega na drobno razdeljene delce fiziološko sprejemljive farmakološko inertne snovi z MMD, ki je enak ali manjši kot 15 mikronov.
  15. 15. Inhalator za suh prašek, ki obsega inhalabilno formulacijo suhega praška po katerem koli od zahtevkov 1 do 14.
  16. 16. Inhalabilna formulacija suhega praška po katerem koli od zahtevkov 1 do 14, za uporabo za preprečevanje in/ali zdravljenje respiratorne bolezni.
  17. 17. Inhalabilna formulacija suhega praška po zahtevku 16, kjer je bolezen astma in kronična obstrukcijska pljučna bolezen (COPD).
  18. 18. Ovojnina, ki obsega inhalabilno formulacijo suhega praška po katerem koli od zahtevkov 1 do 14 in inhalator za suh prašek.
SI201131448T 2010-08-03 2011-07-27 Formulacija suhega praška, obsegajoča fosfodiesterazni inhibitor SI2600830T1 (sl)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10171748 2010-08-03
EP11741172.8A EP2600830B1 (en) 2010-08-03 2011-07-27 Dry powder formulation comprising a phosphodiesterase inhibitor
PCT/EP2011/062872 WO2012016889A2 (en) 2010-08-03 2011-07-27 Dry powder formulation comprising a phosphodiesterase inhibitor

Publications (1)

Publication Number Publication Date
SI2600830T1 true SI2600830T1 (sl) 2018-05-31

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US (2) US9132121B2 (sl)
EP (2) EP2600830B1 (sl)
JP (1) JP6004233B2 (sl)
KR (1) KR101805958B1 (sl)
CN (2) CN103052379A (sl)
AR (1) AR082443A1 (sl)
AU (1) AU2011287711B2 (sl)
BR (1) BR112013002506A2 (sl)
CA (1) CA2807256C (sl)
CL (1) CL2013000293A1 (sl)
CO (1) CO6690744A2 (sl)
CY (1) CY1120605T1 (sl)
DK (1) DK2600830T3 (sl)
EA (2) EA027692B1 (sl)
ES (1) ES2664175T3 (sl)
GE (1) GEP20156343B (sl)
HR (1) HRP20180717T1 (sl)
HU (1) HUE037620T2 (sl)
IL (1) IL224517B (sl)
LT (1) LT2600830T (sl)
MA (1) MA34449B1 (sl)
ME (1) ME03022B (sl)
MX (1) MX346424B (sl)
MY (1) MY179703A (sl)
NO (1) NO2600830T3 (sl)
NZ (1) NZ606548A (sl)
PE (2) PE20171256A1 (sl)
PL (1) PL2600830T3 (sl)
PT (1) PT2600830T (sl)
RS (1) RS57061B1 (sl)
SG (1) SG187258A1 (sl)
SI (1) SI2600830T1 (sl)
TR (1) TR201807012T4 (sl)
UA (1) UA112296C2 (sl)
WO (1) WO2012016889A2 (sl)
ZA (1) ZA201300870B (sl)

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SI3587400T1 (sl) 2013-10-22 2024-05-31 Chiesi Farmaceutici S.P.A. Postopek za pripravo zaviralca pde4
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KR101859750B1 (ko) * 2017-09-13 2018-05-21 제일에스엠피(주) 고정식 열 저장 운반장치
WO2023117985A1 (en) 2021-12-21 2023-06-29 Chiesi Farmaceutici S.P.A. Dry powder formulations filled in an inhaler with improved resistance to humidity
WO2023208982A1 (en) 2022-04-27 2023-11-02 Chiesi Farmaceutici S.P.A. Crystal form of a pde4 inhibitor
WO2024027901A1 (en) 2022-08-02 2024-02-08 Chiesi Farmaceutici S.P.A. Predictive biomarker of clinical response to a pde4 inhibitor
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WO2024062005A1 (en) 2022-09-22 2024-03-28 Chiesi Farmaceutici S.P.A. Capsule inhaler for the administration of a phosphodiesterase-4 inhibitor
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Publication number Publication date
ME03022B (me) 2018-10-20
PE20130601A1 (es) 2013-05-30
KR101805958B1 (ko) 2017-12-07
EA201390049A1 (ru) 2013-05-30
PT2600830T (pt) 2018-04-02
US20150342936A1 (en) 2015-12-03
DK2600830T3 (en) 2018-03-12
US9132121B2 (en) 2015-09-15
MA34449B1 (fr) 2013-08-01
EP3246016A1 (en) 2017-11-22
CY1120605T1 (el) 2019-12-11
ZA201300870B (en) 2014-04-30
MX346424B (es) 2017-03-21
BR112013002506A2 (pt) 2016-05-31
ES2664175T3 (es) 2018-04-18
CO6690744A2 (es) 2013-06-17
AR082443A1 (es) 2012-12-05
PL2600830T3 (pl) 2018-08-31
AU2011287711B2 (en) 2016-10-27
EP2600830B1 (en) 2018-02-21
HRP20180717T1 (hr) 2018-07-13
KR20130094784A (ko) 2013-08-26
JP2013532705A (ja) 2013-08-19
MY179703A (en) 2020-11-11
EA201690541A1 (ru) 2016-07-29
IL224517B (en) 2018-04-30
WO2012016889A3 (en) 2012-04-19
LT2600830T (lt) 2018-04-10
US20120031403A1 (en) 2012-02-09
AU2011287711A1 (en) 2013-02-21
WO2012016889A2 (en) 2012-02-09
HUE037620T2 (hu) 2018-09-28
JP6004233B2 (ja) 2016-10-05
MX2013001172A (es) 2013-03-07
RS57061B1 (sr) 2018-06-29
EA027692B1 (ru) 2017-08-31
SG187258A1 (en) 2013-03-28
EA024922B1 (ru) 2016-11-30
CL2013000293A1 (es) 2013-05-03
CN106890165A (zh) 2017-06-27
CA2807256A1 (en) 2012-02-09
NZ606548A (en) 2015-02-27
US9308200B2 (en) 2016-04-12
NO2600830T3 (sl) 2018-07-21
EP2600830A2 (en) 2013-06-12
TR201807012T4 (tr) 2018-06-21
UA112296C2 (uk) 2016-08-25
GEP20156343B (en) 2015-08-10
CN103052379A (zh) 2013-04-17
CA2807256C (en) 2018-08-28
PE20171256A1 (es) 2017-08-28

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