FI118512B - Flutikasonpropionatformulationer - Google Patents

Flutikasonpropionatformulationer Download PDF

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Publication number
FI118512B
FI118512B FI964634A FI964634A FI118512B FI 118512 B FI118512 B FI 118512B FI 964634 A FI964634 A FI 964634A FI 964634 A FI964634 A FI 964634A FI 118512 B FI118512 B FI 118512B
Authority
FI
Finland
Prior art keywords
formulation
sorbitan monolaurate
formulation according
polyoxyethylene
fluticasone propionate
Prior art date
Application number
FI964634A
Other languages
English (en)
Finnish (fi)
Other versions
FI964634A (sv
FI964634A0 (sv
Inventor
David Alexander Tainsh
Trevor Leslie Ilott
Dorothy Jill Snell
Li Fong Lam
Original Assignee
Glaxo Wellcome Australia Ltd
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 Glaxo Wellcome Australia Ltd filed Critical Glaxo Wellcome Australia Ltd
Publication of FI964634A publication Critical patent/FI964634A/sv
Publication of FI964634A0 publication Critical patent/FI964634A0/sv
Application granted granted Critical
Publication of FI118512B publication Critical patent/FI118512B/sv

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Classifications

    • 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
    • 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
    • A61K9/0078Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a nebulizer such as a jet nebulizer, ultrasonic nebulizer, e.g. in the form of aqueous drug solutions or dispersions
    • 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
    • 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
    • A61K47/02Inorganic compounds
    • 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
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Dispersion Chemistry (AREA)
  • Otolaryngology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biochemistry (AREA)
  • Organic Chemistry (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Inorganic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Claims (16)

1. Suspensionsformulation, som lärapar sig för ne-bulisering för administration av en verksam formulations- 5 mängd till lungorna, kännetecknad av att den omfattar (a) fluticasonpropionat som är väsentligen helt och hället till sin partikelstorlek under 12 μπι,- (b) ett eller flera ytaktiva airmen; 10 (c) ett eller flera buffertmedel; (d) vatten.
2. Formulation enligt patentkrav 1, kännetecknad av att fluticasonpropionatets partikelstorlek är 1 - 6 μη.
3. Formulation enligt patentkrav 1 eller 2, kän netecknad av att 0,5 - 10 vikt-% fluticasonpropionat är närvarande beräknat pä den totala mängden fasta ingre-dienser i formulationen.
4. Formulation enligt nägot av patentkraven 1-3, 20 kännetecknad av att formulationen innehäller tvä ytaktiva ämnen.
,·. 5. Formulation enligt nägot av patentkraven 1-4, kännetecknad av att 0,25 - 0,75 vikt-% ytaktivt ämne • · * ! är närvarande beräknat pä den totala mängden fasta ingre- • * · *···* 25 dienser i formulationen.
«·· ···· 6. Formulation enligt nägot av de föregäende pa- tentkraven, kännetecknad av att som ytaktiva ämnen V : kommer sorbitantrioleat, sorbitanmonooleat, sorbitanmono- laurat, polyoxieten(20)sorbitanmonolaurat, polyoxieten- 30 (20) sorbi tanmonooleat, naturligt lecitin, oleylpolyoxie- ten(2)eter, stearylpolyoxieten(2)eter, laurylpolyoxieten- ·* (4)eter, blockpolymerer av oxieten och oxipropen, synte- • t · *·|#* tiskt lecitin, dietenglykoldioleat, tetrahydrofuryloleat, • · etyloleat, glycerylmonooleat, polyetenglykol 400 och gly- * 35 cerylmonolaurat pä fräga. • · • · 118512
7. Formulation enligt patentkrav 6, känneteck-n a d av att de ytaktiva ämnena är sorbitanmonolaurat och polyoxieten(20)sorbitanmonolaurat.
8. Formulation enligt patentkrav 7, känneteck- 5 nad av att sorbitanmonolaurat och polyoxieten(20)sorbi- tanmonolaurat är närvarande i förhällandet 1:7,5 - 1:8,25.
9. Formulation enligt nägot av de föregäende pa-tentkraven, kännetecknad av att den är buff rad tili ett pH-värde pä cirka 5-7.
10. Formulation enligt nägot av de föregäende pa- tentkraven, kännetecknad av att den är isoton.
11. Formulation enligt nägot av de föregäende pa-tentkraven, kännetecknad av att den omfattar (a) 0,25 - 1,1 mg/ml fluticasonpropionat (mikroni- 15 serat); (b) 0,06 - 0,09 mg/ml polyoxieten(20)sorbitanmonolaurat ; (c) 0,0075 - 0,0125 mg/ml sorbitanmonolaurat,- (d) 9,25 - 9,5 mg/ml mononatriumfosfatdihydrat; 20 (e) 1,6 - 1,85 mg/ml vattenfritt tväbasiskt natri- umfosfat; (f) 4,7 - 4,9 mg/ml natriumklorid; och « II1I (g) vatten. • · * I
12. Formulation enligt patentkrav 11, kanne- **"1 25 tecknad av att den omfattar ca ··· ··1! (a) 0,26 mg/ml fluticasonproprionat (mikronise- *.!.1 rat) ; • tt V : (b) 0,07 mg/ml polyoxieten(20) sorbitanmonolaurat,- (c) 0,009 mg/ml sorbitanmonolaurat; 30 (d) 9,4 mg/ml mononatriumfosfatdihydrat; :'**· (e) 1,75 mg/ml vattenfritt tväbasiskt natriumfos- • · · f at; • · 1 *;]t1 (f) 4,8 mg/ml natriumklorid; och • · **··1 (g) vatten. • · • · · • · · • I · 118512
13. Formulation enligt patentkrav 11, kanne -tecknad av att den omfattar ca (a) 1,05 mg/ml fluticasonpropionat (mikroniserat); (b) 0,08 mg/ml polyoxieten(20)sorbitanmonolaurat; 5 (c) 0,01 mg/ml sorbitanmonolaurat; (d) 9,4 mg/ml mononatriumfosfatdihydrat; (e) 1,75 mg/ml vattenfritt tväbasiskt natriumfos- fat; (f) 4,8 mg/ml natriumklorid; och 10 (g) vatten.
14. Förfarande för framställning av en formulation enligt nägot av de föregäende patentkraven, känneteck-nat av att fluticasonpropionat bringas i kontakt med en lösning av ytaktivt ämne och den som resultat erhällna 15 lösningen av läkemedel och ytaktivt ämne blandas med for-mulationens övriga ingredienser.
15. Behällare, kännetecknad av att den inne-häller en formulation enligt nägot av patentkraven 1 - 13.
16. Användning av en formulation enligt nägot av 20 patentkraven 1-13 i en nebulisator för bildande av ett flertal droppar bestäende av nämnda formulation, vilka droppar är lämpliga för inhalation. ···· ·· · « · · • 1 • · » t · • · · ··· « • · · Ml» • · 1 • · · *·· • · · I f · • · · ·1 • · • ·· ΦΦ1 • · • Φ • Φ · • ··· • · · • · · ··· • · • t • · · • · · « « 1 • 1· • ·
FI964634A 1994-05-21 1996-11-20 Flutikasonpropionatformulationer FI118512B (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB9410222A GB9410222D0 (en) 1994-05-21 1994-05-21 Medicaments
GB9410222 1994-05-21
PCT/EP1995/001913 WO1995031964A1 (en) 1994-05-21 1995-05-19 Fluticasone propionate formulations
EP9501913 1995-05-19

Publications (3)

Publication Number Publication Date
FI964634A FI964634A (sv) 1996-11-20
FI964634A0 FI964634A0 (sv) 1996-11-20
FI118512B true FI118512B (sv) 2007-12-14

Family

ID=10755515

Family Applications (1)

Application Number Title Priority Date Filing Date
FI964634A FI118512B (sv) 1994-05-21 1996-11-20 Flutikasonpropionatformulationer

Country Status (29)

Country Link
US (1) US5993781A (sv)
EP (1) EP0760649B1 (sv)
JP (1) JPH10500420A (sv)
KR (2) KR100361413B1 (sv)
CN (1) CN1098680C (sv)
AT (1) ATE207734T1 (sv)
AU (1) AU710821B2 (sv)
BR (1) BR9507746A (sv)
CA (1) CA2190763A1 (sv)
CY (1) CY2294B1 (sv)
CZ (1) CZ285966B6 (sv)
DE (1) DE69523587T2 (sv)
DK (1) DK0760649T3 (sv)
ES (1) ES2164767T3 (sv)
FI (1) FI118512B (sv)
GB (1) GB9410222D0 (sv)
HK (1) HK1004192A1 (sv)
HU (1) HU223316B1 (sv)
IL (1) IL113794A (sv)
MX (1) MX9605650A (sv)
NO (1) NO313785B1 (sv)
NZ (1) NZ287425A (sv)
PL (1) PL180318B1 (sv)
PT (1) PT760649E (sv)
RU (1) RU2161485C2 (sv)
SI (1) SI0760649T1 (sv)
TW (1) TW438604B (sv)
WO (1) WO1995031964A1 (sv)
ZA (1) ZA954101B (sv)

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Also Published As

Publication number Publication date
HU9603227D0 (en) 1997-01-28
CZ285966B6 (cs) 1999-12-15
HK1004192A1 (en) 1998-11-20
EP0760649A1 (en) 1997-03-12
PL180318B1 (pl) 2001-01-31
HUT76552A (en) 1997-09-29
KR100361413B1 (ko) 2003-02-19
CN1148804A (zh) 1997-04-30
DE69523587D1 (de) 2001-12-06
KR970703130A (ko) 1997-07-03
BR9507746A (pt) 1997-08-19
ATE207734T1 (de) 2001-11-15
IL113794A (en) 2000-10-31
NO313785B1 (no) 2002-12-02
ES2164767T3 (es) 2002-03-01
WO1995031964A1 (en) 1995-11-30
MX9605650A (es) 1998-05-31
RU2161485C2 (ru) 2001-01-10
FI964634A (sv) 1996-11-20
AU2614595A (en) 1995-12-18
IL113794A0 (en) 1995-08-31
EP0760649B1 (en) 2001-10-31
CZ342396A3 (en) 1997-07-16
TW438604B (en) 2001-06-07
DE69523587T2 (de) 2002-06-27
CA2190763A1 (en) 1995-11-30
PT760649E (pt) 2002-04-29
NO964938L (no) 1996-11-20
JPH10500420A (ja) 1998-01-13
HU223316B1 (hu) 2004-05-28
CN1098680C (zh) 2003-01-15
DK0760649T3 (da) 2002-01-28
AU710821B2 (en) 1999-09-30
CY2294B1 (en) 2003-07-04
GB9410222D0 (en) 1994-07-06
US5993781A (en) 1999-11-30
ZA954101B (en) 1996-01-29
NZ287425A (en) 1998-05-27
KR970703132A (ko) 1997-07-03
FI964634A0 (sv) 1996-11-20
SI0760649T1 (en) 2002-04-30
PL317225A1 (en) 1997-03-17
NO964938D0 (no) 1996-11-20

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