IPC분류정보
국가/구분 |
United States(US) Patent
등록
|
국제특허분류(IPC7판) |
|
출원번호 |
US-0536998
(2009-08-06)
|
등록번호 |
US-8211405
(2012-07-03)
|
우선권정보 |
GB-0326632.7 (2003-11-14) |
발명자
/ 주소 |
- Mueller-Walz, Rudi
- Steiner, Roland
|
출원인 / 주소 |
|
대리인 / 주소 |
Mintz Levin Cohn Ferris Glovsky and Popeo, P.C.
|
인용정보 |
피인용 횟수 :
3 인용 특허 :
4 |
초록
▼
A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magne
A dry powder suitable for inhalation in a dry powder inhaler, the powder comprising a carrier, an active agent and at least 0.5% by weight of magnesium stearate, the powder being further characterized in that the less than 10% of the surface of the carrier material is covered with particles of magnesium stearate. The invention is also directed to a method of making dry powders by blending together the ingredients mentioned in a diffusion blender for a period time that is less than 60 minutes.
대표청구항
▼
1. A method of making a dry powder formulation for inhalation, the dry powder formulation comprising active particles and carrier particles for supporting the active particles, and magnesium stearate in an amount of at least 0.5% by weight of the formulation, the method comprising the step of blendi
1. A method of making a dry powder formulation for inhalation, the dry powder formulation comprising active particles and carrier particles for supporting the active particles, and magnesium stearate in an amount of at least 0.5% by weight of the formulation, the method comprising the step of blending the magnesium stearate with a carrier material in a low energy blender, wherein the energy consumption of said blender is from 0.10 to 1 kilowatt per 100 liters, for a period of less than 30 minutes to form a mixture in which particles of magnesium stearate are disposed on the surface of the carrier particles, wherein the coverage of the magnesium stearate on the surface of the carrier particles is less than 5%, and wherein said dry powder formulation is prepared without high shear mixing or milling steps. 2. The method according to claim 1, further comprising the step of: blending the mixture of magnesium stearate and carrier material with an active substance in blender. 3. The method of claim 1, wherein the magnesium stearate is present in an amount of from 0.5 to 2% by weight. 4. The method of claim 1, wherein the magnesium stearate is present in an amount of from 0.6 to 1% by weight. 5. The method of claim 1, wherein the active particles comprise an active substance selected from the group consisting of beta-mimetics, anticholinergics, corticosteroids, leukotrienantagonists, phosphodiesterase inhibitors, PAF-inhibitors, potassium channel openers, analgesics, potency agents, macromolecules, pharmaceutically acceptable salts thereof and mixtures thereof. 6. The method of claim 1, wherein the carrier particles comprise a carrier material selected from monosaccharides, disaccharides, sugar alcohols, polylactic acid, or mixtures thereof. 7. The method of claim 6, wherein the carrier is lactose mono-hydrate. 8. The method of claim 5, wherein the beta-mimetic is selected from the group consisting of Levalbuterol, Terbutalin, Reproterol, Salbutamol, Salmeterol, Formoterol, Fenoterol, Clenbuterol, Bambuterol, Tulobuterol, Broxaterol, Epinephrin, Isoprenaline and Hexoprenaline. 9. The method of claim 5, wherein the anticholinergic is selected from the group consisting of Tiotropium, Ipratropium, Oxitropium and Glycopyrronium. 10. The method of claim 5, wherein the corticosteroid is selected from the group consisting of Butixocart, Rofleponide, Budesonide, Ciclosenide, Mometasone, Fluticasone, Beclomethasone, Loteprednol and Triamcinolone. 11. The method of claim 5, wherein the leukotrienantagonist is selected from the group consisting of Andolast, Iralukast, Pranlukast, Imitrodast, Seratrodast, Zileuton, Zafirlukast and Montelukast. 12. The method of claim 5, wherein the phosphodiesterase-inhibitor is selected from Filaminast or Piclamilast. 13. The method of claim 5, wherein the PAF-inhibitor is selected from the group consisting of Apafant, Forapafant and Israpafant. 14. The method of claim 5, wherein the potassium channel opener is selected from Amiloride or Furosemide. 15. The method of claim 5, wherein the analgesic is selected from the group consisting of Morphine, Fentanyl, Pentazocine, Buprenorphine, Pethidine, Tilidine, Methadone and Heroin. 16. The method of claim 5, wherein the potency agent is selected from the group consisting of Sildenafil, Alprostadil and Phentolamine. 17. The method of claim 5, wherein the macromolecule is selected from the group consisting of proteins, peptides, oligopeptides, polypeptides, polyamino acids, nucleic acids, polynucleotides, oligo-nucleotides and high molecular weight polysaccharides. 18. The method of claim 6, wherein the monosaccharide or disaccharide is selected from the group consisting of glucose, lactose, lactose monohydrate, sucrose, trehalose and mixtures thereof. 19. The method of claim 6, wherein the sugar alcohol is selected from mannitol, xylitol, or a mixture thereof.
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