FI119676B - Pulver för användning i en torrpulverinhalator - Google Patents

Pulver för användning i en torrpulverinhalator Download PDF

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Publication number
FI119676B
FI119676B FI973151A FI973151A FI119676B FI 119676 B FI119676 B FI 119676B FI 973151 A FI973151 A FI 973151A FI 973151 A FI973151 A FI 973151A FI 119676 B FI119676 B FI 119676B
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FI
Finland
Prior art keywords
particles
powder
additive
carrier
active
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Application number
FI973151A
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English (en)
Finnish (fi)
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FI973151A0 (sv
FI973151A (sv
Inventor
John Nicholas Staniforth
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Vectura Ltd
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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
    • 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
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7012Compounds having a free or esterified carboxyl group attached, directly or through a carbon chain, to a carbon atom of the saccharide radical, e.g. glucuronic acid, neuraminic acid
    • 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
    • A61K9/12Aerosols; Foams
    • 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
    • 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
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Dispersion Chemistry (AREA)
  • Pulmonology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Otolaryngology (AREA)
  • Medicinal Preparation (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Manufacturing Of Micro-Capsules (AREA)

Claims (42)

1. Pulver för användning i en torrpulverinhalator, varvid pulvret inkluderar aktiva partiklar, bärarpartiklar för att bära de aktiva partiklarna och partiklar av tillsatsma-terial fästade till bärarpartiklarnas ytor, varvid tillsatsmaterialets syfte är att främja 5 frisättning av de aktiva partiklarna frän bärarpartiklama vid utlösning av inhalatorn, kännetecknat av att tillsatsmaterialet innefattar ett ytaktivt material och inkluderar en kombination av material, varvid väsentligen samtliga bärarpartiklar har en aerodynamisk diameter som ligger mellan 20 pm och 1000 pm och massmedia-nen vad gäller tillsatspartiklarnas aerodynamiska diameter inte är mer än 10 pm.
2. Pulver enligt patentkrav 1, varvid pulvret inkluderar inte mer än 10 vikt% till- satsmaterial baserad pä pulvrets vikt.
3. Pulver enligt patentkrav 2, varvid pulvret inkluderar inte mer än 5 vikt% till-satsmaterial baserad pä pulvrets vikt.
4. Pulver enligt patentkrav 3, varvid pulvret inkluderar inte mer än 4 vikt% till-15 satsmaterial baserad pä pulvrets vikt.
5. Pulver enligt patentkrav 4, varvid pulvret inkluderar inte mer än 2 vikt% till-satsmaterial baserad pa pulvrets vikt. • "**: 6. Pulver enligt nägot av de föregäende patentkraven, varvid tillsatsmaterialet är ett fysiologisi godtagbart material. • · ..... 20 7. Pulver enligt nägot av de föregäende patentkraven, varvid tillsatsmaterialet I. ** innefattar partiklar av ytaktivt material, varvid det ytaktiva materialet valts ur grup- • · pen som bestär av: lecitin; fettsyror i fast fas säsom palmitinsyra, stearinsyra, eru- • · · *·* * kasyra, behensyra, och derivat därav; magnesiumstearat; natriumstearylfumarat; natriumstearyllaktylat; fosfatidylkoliner; fosfatidylglyceroler; liposomala formule- • · :.v 25 ringar; laurinsyra eller laurinsyrasalter; triglycerider; och sockerestrar. • · · • · • · *" 8. Pulver enligt nägot av de föregäende patentkraven, varvid tillsatsmaterialet ·.!:* valts ur gruppen som bestär av: en eller flera vattenlösliga substanser; en fosfoli- • · · pid eller ett derivat därav; palmitinsyra, stearinsyra, erukasyra, behensyra, mag- nesiumstearat, natriumstearylfumarat, natriumstearyllaktylat, en fosfatidyl koi in, en .···. 30 fosfatidylglycerol, en liposomal formulering, laurinsyra eller ett laurinsyrasalt, en • · triglycerid, eller en sockerester; en eller flera föreningar som valts bland aminosy-ror och derivat därav, och peptider och polypeptider som har en molekylvikt frän 0,25 till 1000 Kda, och derivat därav; och dipolara joner.
9. Pulver enligt patentkrav 7 eller 8, varvid tillsatsmaterialet innefattar lecitin.
10. Pulver enligt patentkrav 9, varvid tillsatsmaterialet innefattar sojalecitin.
11. Pulver enligt patentkrav 7 eller 8, varvid tillsatsmaterialet innefattar magnesi-5 umstearat i en mängd som utgör mindre än 1,5 vikt%. t
12. Pulver enligt patentkrav 8, varvid tillsatsmaterialet inkluderar en aminosyra.
13. Pulver enligt patentkrav 12, varvid tillsatsmaterialet inkluderar leucin.
14. Pulver enligt patentkrav 8, varvid tillsatsmaterialet bestär av zwitterjoner.
15. Pulver enligt nägot av de föregäende patentkraven, varvid tillsatsmaterialet 10 inkluderar en mangfald ytaktiva material.
16. Pulver enligt nägot av föregaende patentkrav, varvid pulvret bestär av inte mindre än 0,1 vikt% tillsatspartiklar baserad pä bärarpartiklamas vikt.
17. Pulver enligt nägot av de föregäende patentkraven, varvid partiklar av till-satsmaterial bildar en diskontinuerlig beläggning pä bärarpartiklamas ytor. ·:··: 15 18. Pulver enligt patentkrav 17, varvid tillsatsmaterialet, medan det bildar en dis- : .·. kontinuerlig beläggning pä bärarpartiklamas ytor, mättar bärarpartiklamas ytor. • ·· · ' ’ 19. Pulver enligt nägot av de föregäende patentkraven, varvid bärarpartiklarna : V innefattar ett eller flera kristallina sockerarter. • · • · • · ·
20. Pulver enligt patentkrav 19, varvid bärarpartiklarna är partiklar av laktos.
21. Pulver enligt nägot av de föregäende patentkraven, varvid massmedianen • · v.: vad gäller de aktiva partiklarnas aerodynamiska diameter inte är mer än 10 μίτι. ·♦· • · *** 22. Pulver enligt nägot av de föregäende patentkraven, varvid de aktiva partik- ···:* lama innefattar material som vanligen administreras oralt genom inhalation för ··· behandling av respiratoriska sjukdomar. • · • · ♦
24. Pulver enligt patentkrav 23, varvid de aktiva partiklarna inkluderar salbuta- *·)·* 25 23. Pulver enligt patentkrav 22, varvid de aktiva partiklarna inkluderar en β2- • · *·♦·’ agonist. mol, ett salt av salbutamol, salmeterol och/eller ett sait av salmeterol.
25. Pulver enligt patentkrav 22, varvid de aktiva partiklama inkluderar en steroid.
26. Pulver enigt patentkrav 25, varvid steroiden är beklometason-dipropionat el-ler flutikason.
27. Pulver enligt nägot av de föregaende patentkraven, varvid de aktiva partik- larna inte är benägna att frisättas frän bärarpartiklarna innan inhalatom utlöses.
28. Pulver enligt nägot av de föregäende patentkraven, varvid pulvret har en homogenitet efter vibration mätt som en procentuell variationskoefficient av mind-re än cirka 5 %, när den mäts med användning av förfarandet som beskrivits i Ex- 10 empel 12.
29. Förfarande för framställning av ett pulver enligt nagot av patentkraven 1 tili 28, varvid nämnda förfarande inkluderar stegen att man blandar bärarpartiklar som har en storlek som är lämplig för användning i en torrpulverinhalator med par-tiklar av tillsatsmaterial som fäster tili bärarpartiklarnas ytor, och att man blandar 15 de resulterande partiklarna med aktiva partiklar pä sä sätt att de aktiva partiklarna fäster tili bärarpartiklarnas ytor och/eller tillsatspartiklarnas ytor, kännetecknat av att tillsatsmaterialet innefattar ett ytaktivt material och inkluderar en kombination av material, och varvid väsentligen samtliga bärarpartiklar har en aerodynamisk • · diameter som ligger mellan 20 pm och 1000 pm och massmedianen vad gäller till- **' | 20 satspartiklarnas aerodynamiska diameter inte är mer än 10 pm. • ·
30. Förfarande enligt patentkrav 29, vidare innefattande steget att man ur ett prov av bärarpartiklar väljer ett fördelaktigt storleksintervall av bärarpartiklar före blandningssteget.
31. Förfarande enligt patentkrav 29 eller 30, varvid förfarandet vidare innefattar :.v 25 steget att man ur ett prov av tillsatspartiklar väljer ett fördelaktigt storleksintervall • · · av tillsatspartiklar före blandningssteget. • · · *"j 32. Förfarande enligt patentkrav 29 eller 30, varvid tillsatsmaterialet tillsatts i form av en suspension. • · • · · .*!:* 33. Förfarande enligt nagot av patentkraven 29 tili 32, varvid tillsatsmaterialet • ♦ *···* 30 och bärarpartiklarna blandas i mellan 0,1 timme och 0,5 timme.
34. Förfarande enligt nägot av patentkraven 29 tili 33, varvid bärarpartiklarna blandas med tillsatsmaterialet genom användning av en trumlingsblandare.
35. Förfarande enligt nägot av patentkraven 29 till 34, varvid förfarandet ytterli-gare inkluderar steget att man behandlar bärarpartiklarna för att avlägsna smä korn frän bärarpartiklarnas ytor, utan att väsentligen förändra storleken pä bärar- 5 partiklarna under behandlingen.
36. Förfarande enligt patentkrav 35, varvid blandningssteget är före behand-lingssteget.
37. Förfarande enligt patentkrav 35 eller patentkrav 36, varvid de sma kornen äter fäster tili ytorna pä bärarpartiklarna. 10 38. Förfarande enligt nägot av patentkraven 35 tili 37, varvid behandlingssteget är ett malningssteg.
39. Förfarande enligt patentkrav 38, varvid malningssteget utförs i en kulkvarn.
40. Förfarande enligt patentkrav 39, varvid partiklarna mals genom användning av plastkulor. 15 41. Förfarande enligt patentkrav 38, varvid behandlingssteget utförs i en ätercir- kulerande "low fluid energy”-kvam. .* 42. Förfarande enligt nägot av patentkraven 38 tili 41, varvid partiklarna mals i • · · ··· \ mellan cirka 0,25 timmar och 6 timmar. « · ·· · • · · ♦ « • · ·· • · • ♦· ··· • · · » · · • · • · · • · · • · ··· • · • · ··· m 9 9 99 9 9999 999 9 9 9 9 999 • • · • · · • · · 9 9 999 9 9 9 9 999
FI973151A 1995-01-31 1997-07-30 Pulver för användning i en torrpulverinhalator FI119676B (sv)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
GBGB9501841.2A GB9501841D0 (en) 1995-01-31 1995-01-31 Improvements in and relating to carrier particles for use in dry powder inhalers
GB9501841 1995-01-31
GBGB9521937.4A GB9521937D0 (en) 1995-01-31 1995-10-26 Improvementsin and relating to carrier particles for use in dry powder inhailers
GB9521937 1995-10-26
GB9600215 1996-01-31
PCT/GB1996/000215 WO1996023485A1 (en) 1995-01-31 1996-01-31 Carrier particles for use in dry powder inhalers

Publications (3)

Publication Number Publication Date
FI973151A0 FI973151A0 (sv) 1997-07-30
FI973151A FI973151A (sv) 1997-09-30
FI119676B true FI119676B (sv) 2009-02-13

Family

ID=10768844

Family Applications (1)

Application Number Title Priority Date Filing Date
FI973151A FI119676B (sv) 1995-01-31 1997-07-30 Pulver för användning i en torrpulverinhalator

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US (5) US6153224A (sv)
EP (6) EP2213279A3 (sv)
JP (1) JP4042867B2 (sv)
KR (1) KR100500694B1 (sv)
CN (1) CN1303974C (sv)
AT (3) ATE256450T1 (sv)
AU (1) AU699131B2 (sv)
BG (1) BG101858A (sv)
BR (3) BRPI9612950B8 (sv)
CA (1) CA2211874C (sv)
CZ (1) CZ294259B6 (sv)
DE (2) DE69631119T2 (sv)
DK (3) DK1666023T3 (sv)
EA (1) EA000352B1 (sv)
EE (1) EE9700176A (sv)
ES (3) ES2278828T3 (sv)
FI (1) FI119676B (sv)
GB (2) GB9501841D0 (sv)
GE (1) GEP19991687B (sv)
HK (1) HK1084897A1 (sv)
HU (1) HU229965B1 (sv)
IS (1) IS4531A (sv)
MX (1) MX9705847A (sv)
NO (1) NO324037B1 (sv)
NZ (1) NZ300654A (sv)
PL (1) PL186757B1 (sv)
PT (3) PT806938E (sv)
SI (2) SI1666023T1 (sv)
SK (1) SK282630B6 (sv)
TR (1) TR199700722T1 (sv)
UA (1) UA61051C2 (sv)
WO (1) WO1996023485A1 (sv)
ZA (1) ZA96721B (sv)

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