HRP20200571T1 - Postupak priprave formulacije suhog praška koji sadrži antikolinergik, kortikosteroid i beta-adrenergik - Google Patents
Postupak priprave formulacije suhog praška koji sadrži antikolinergik, kortikosteroid i beta-adrenergik Download PDFInfo
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- HRP20200571T1 HRP20200571T1 HRP20200571TT HRP20200571T HRP20200571T1 HR P20200571 T1 HRP20200571 T1 HR P20200571T1 HR P20200571T T HRP20200571T T HR P20200571TT HR P20200571 T HRP20200571 T HR P20200571T HR P20200571 T1 HRP20200571 T1 HR P20200571T1
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- 239000000203 mixture Substances 0.000 title claims 23
- 238000009472 formulation Methods 0.000 title claims 13
- 239000000843 powder Substances 0.000 title claims 11
- 239000003246 corticosteroid Substances 0.000 title claims 4
- 230000001078 anti-cholinergic effect Effects 0.000 title 1
- 238000004519 manufacturing process Methods 0.000 title 1
- 238000000034 method Methods 0.000 claims 10
- 239000010419 fine particle Substances 0.000 claims 8
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 6
- 239000002245 particle Substances 0.000 claims 6
- VPNYRYCIDCJBOM-UHFFFAOYSA-M Glycopyrronium bromide Chemical compound [Br-].C1[N+](C)(C)CCC1OC(=O)C(O)(C=1C=CC=CC=1)C1CCCC1 VPNYRYCIDCJBOM-UHFFFAOYSA-M 0.000 claims 5
- 239000011362 coarse particle Substances 0.000 claims 5
- 229960002462 glycopyrronium bromide Drugs 0.000 claims 5
- KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 claims 4
- 239000013543 active substance Substances 0.000 claims 4
- 229950000210 beclometasone dipropionate Drugs 0.000 claims 4
- 239000003149 muscarinic antagonist Substances 0.000 claims 4
- RATSWNOMCHFQGJ-TUYNVFRMSA-N (e)-but-2-enedioic acid;n-[2-hydroxy-5-[(1s)-1-hydroxy-2-[[(2s)-1-(4-methoxyphenyl)propan-2-yl]amino]ethyl]phenyl]formamide;dihydrate Chemical compound O.O.OC(=O)\C=C\C(O)=O.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1.C1=CC(OC)=CC=C1C[C@H](C)NC[C@@H](O)C1=CC=C(O)C(NC=O)=C1 RATSWNOMCHFQGJ-TUYNVFRMSA-N 0.000 claims 3
- 235000014113 dietary fatty acids Nutrition 0.000 claims 3
- 229940112141 dry powder inhaler Drugs 0.000 claims 3
- 239000000194 fatty acid Substances 0.000 claims 3
- 229930195729 fatty acid Natural products 0.000 claims 3
- -1 fatty acid salts Chemical class 0.000 claims 3
- 229960003610 formoterol fumarate dihydrate Drugs 0.000 claims 3
- 229940127212 long-acting beta 2 agonist Drugs 0.000 claims 3
- 235000019359 magnesium stearate Nutrition 0.000 claims 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- PZSMUPGANZGPBF-UHFFFAOYSA-N 4-[5-(dithiolan-3-yl)pentanoylamino]butanoic acid Chemical compound OC(=O)CCCNC(=O)CCCCC1CCSS1 PZSMUPGANZGPBF-UHFFFAOYSA-N 0.000 claims 2
- 229940125389 long-acting beta agonist Drugs 0.000 claims 2
- KHICUSAUSRBPJT-UHFFFAOYSA-N 2-(2-octadecanoyloxypropanoyloxy)propanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(=O)OC(C)C(=O)OC(C)C(O)=O KHICUSAUSRBPJT-UHFFFAOYSA-N 0.000 claims 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical group O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 1
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims 1
- LERNTVKEWCAPOY-VOGVJGKGSA-N C[N+]1(C)[C@H]2C[C@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)C(O)(c1cccs1)c1cccs1 Chemical compound C[N+]1(C)[C@H]2C[C@H](C[C@@H]1[C@H]1O[C@@H]21)OC(=O)C(O)(c1cccs1)c1cccs1 LERNTVKEWCAPOY-VOGVJGKGSA-N 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- GIIZNNXWQWCKIB-UHFFFAOYSA-N Serevent Chemical compound C1=C(O)C(CO)=CC(C(O)CNCCCCCCOCCCCC=2C=CC=CC=2)=C1 GIIZNNXWQWCKIB-UHFFFAOYSA-N 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- 229960005012 aclidinium bromide Drugs 0.000 claims 1
- XLAKJQPTOJHYDR-QTQXQZBYSA-M aclidinium bromide Chemical compound [Br-].C([C@@H](C(CC1)CC2)OC(=O)C(O)(C=3SC=CC=3)C=3SC=CC=3)[N+]21CCCOC1=CC=CC=C1 XLAKJQPTOJHYDR-QTQXQZBYSA-M 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 229960004436 budesonide Drugs 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 1
- XTULMSXFIHGYFS-VLSRWLAYSA-N fluticasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(F)[C@@]4(C)C=CC(=O)C=C4[C@@H](F)C[C@H]3[C@@H]2C[C@H]1C)C(=O)SCF)C(=O)C1=CC=CO1 XTULMSXFIHGYFS-VLSRWLAYSA-N 0.000 claims 1
- 229960001469 fluticasone furoate Drugs 0.000 claims 1
- 229960000289 fluticasone propionate Drugs 0.000 claims 1
- WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 claims 1
- 229960002848 formoterol Drugs 0.000 claims 1
- BPZSYCZIITTYBL-UHFFFAOYSA-N formoterol Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-UHFFFAOYSA-N 0.000 claims 1
- 229960004078 indacaterol Drugs 0.000 claims 1
- QZZUEBNBZAPZLX-QFIPXVFZSA-N indacaterol Chemical compound N1C(=O)C=CC2=C1C(O)=CC=C2[C@@H](O)CNC1CC(C=C(C(=C2)CC)CC)=C2C1 QZZUEBNBZAPZLX-QFIPXVFZSA-N 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 229940037627 magnesium lauryl sulfate Drugs 0.000 claims 1
- HBNDBUATLJAUQM-UHFFFAOYSA-L magnesium;dodecyl sulfate Chemical compound [Mg+2].CCCCCCCCCCCCOS([O-])(=O)=O.CCCCCCCCCCCCOS([O-])(=O)=O HBNDBUATLJAUQM-UHFFFAOYSA-L 0.000 claims 1
- 229960002744 mometasone furoate Drugs 0.000 claims 1
- WOFMFGQZHJDGCX-ZULDAHANSA-N mometasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(Cl)[C@@]4(C)C=CC(=O)C=C4CC[C@H]3[C@@H]2C[C@H]1C)C(=O)CCl)C(=O)C1=CC=CO1 WOFMFGQZHJDGCX-ZULDAHANSA-N 0.000 claims 1
- 150000004682 monohydrates Chemical group 0.000 claims 1
- 230000000414 obstructive effect Effects 0.000 claims 1
- 229960004286 olodaterol Drugs 0.000 claims 1
- COUYJEVMBVSIHV-SFHVURJKSA-N olodaterol Chemical compound C1=CC(OC)=CC=C1CC(C)(C)NC[C@H](O)C1=CC(O)=CC2=C1OCC(=O)N2 COUYJEVMBVSIHV-SFHVURJKSA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 208000023504 respiratory system disease Diseases 0.000 claims 1
- 229960004017 salmeterol Drugs 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
- 229960000257 tiotropium bromide Drugs 0.000 claims 1
- 229960004541 umeclidinium bromide Drugs 0.000 claims 1
- PEJHHXHHNGORMP-AVADPIKZSA-M umeclidinium bromide Chemical compound [Br-].C=1C=CC=CC=1C([C@@]12CC[N@@+](CCOCC=3C=CC=CC=3)(CC1)CC2)(O)C1=CC=CC=C1 PEJHHXHHNGORMP-AVADPIKZSA-M 0.000 claims 1
- 229960004026 vilanterol Drugs 0.000 claims 1
- DAFYYTQWSAWIGS-DEOSSOPVSA-N vilanterol Chemical compound C1=C(O)C(CO)=CC([C@@H](O)CNCCCCCCOCCOCC=2C(=CC=CC=2Cl)Cl)=C1 DAFYYTQWSAWIGS-DEOSSOPVSA-N 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds 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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
- A61K31/167—Amides, 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
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/194—Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds 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
- A61K31/573—Compounds 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/007—Pulmonary tract; Aromatherapy
- A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
- A61K9/0075—Sprays 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/141—Intimate 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
- A61K9/145—Intimate 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
- A61K9/1623—Sugars or sugar alcohols, e.g. lactose; Derivatives thereof; Homeopathic globules
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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Claims (15)
1. Postupak priprave formulacije praška za inhalaciju za upotrebu u inhalatoru za suhi prašak, rečena formulacija praška sadrži:
(A) nosač, koji sadrži:
(a) frakciju grubih čestica fiziološki prihvatljivog nosača koji ima srednju veličinu čestica od najmanje 175 µm; te
(b) frakciju finih čestica, koja se sastoji od smjese od 90 do 99.5 posto po masi čestica fiziološki prihvatljivog ekscipijensa i 0.5 do 10 posto po masi soli masne kiseline, gdje najmanje 90% svih rečenih finih čestica ima volumni promjer manji od 15 mikrona,
gdje je maseni omjer rečenih finih čestica prema rečenim grubim česticama 5:95 do 30:70; te
(B) mikronizirane čestice antimuskarinskog lijeka, dugodjelujućeg β2-agonista (LABA) te, opcionalno, kortikosteroida za inhalaciju (ICS), kao aktivnih tvari, gdje rečeni postupak obuhvaća:
(i) miješanje rečenog nosača, rečenog dugodjelujućeg β2-agonista, te, opcionalno, rečenog kortikosteroida za inhalaciju u posudi miješalice s potresivanjem pri brzini rotacije ne manjoj od 16 r.p.m. u vremenu ne kraćem od 60 minuta, da se dobije prva smjesa; te
(ii) dodavanje rečenog antimuskarinskog lijeka u rečenu prvu smjesu, da se dobije druga smjesa, te miješanje rečene druge smjese pri brzini rotacije ne većoj od 16 r.p.m. u vremenu ne dužem od 40 minuta,
gdje je
dugodjelujući β2-agonist odabran iz skupine koju čine formoterol, salmeterol, indakaterol, olodaterol i vilanterol;
antimuskarinski lijek odabran je iz skupine koju čine glikopironijev bromid ili klorid, tiotropijev bromid, umeklidinijev bromid, te aklidinijev bromid;
kortikosteroid za inhalaciju odabran je iz skupine koju čine beklometazon-dipropionat i njegov oblik monohidrata, budezonid, flutikazon-propionat, flutikazon-furoat, te mometazon-furoat.
2. Postupak prema patentnom zahtjevu 1, koji dalje obuhvaća: (iii) daljnje miješanje formulacije dobivene u (ii), da se postigne homogena distribucija rečenih aktivnih tvari.
3. Postupak prema patentnom zahtjevu 1, naznačeno time da antimuskarinski lijek je glikopironijev bromid, ICS je beklometazon-dipropionat, LABA je formoterol-fumarat dihidrat.
4. Postupak prema patentnom zahtjevu 1, naznačeno time da je sol masne kiseline odabrana iz skupine koju čine magnezijev stearat; natrijev stearil-fumarat; natrijev stearil-laktilat; natrijev lauril-sulfat, te magnezijev lauril-sulfat.
5. Postupak prema patentnom zahtjevu 4, naznačeno time da sol masne kiseline jest magnezijev stearat.
6. Postupak prema bilo kojem od prethodnih patentnih zahtjeva, naznačeno time da je u koraku i) miješanje provedeno pri 16-32 r.p.m., u vremenu između 60 i 120 minuta.
7. Postupak prema bilo kojem od prethodnih patentnih zahtjeva, naznačeno time da je u koraku ii) miješanje provedeno u vremenu između 20 i 40 minuta.
8. Formulacija praška za upotrebu u bilo kojem inhalatoru za suhi prašak koja sadrži:
(A) nosač, koji sadrži:
(a) frakciju grubih čestica fiziološki prihvatljivog nosača koji ima srednju veličinu čestica od najmanje 175 µm; te
(b) frakciju finih čestica koja se sastoji od smjese od 90 do 99.5 posto po masi čestica fiziološki prihvatljivog ekscipijensa i 0.5 do 10 posto po masi magnezijeva stearata, gdje najmanje 90% svih rečenih finih čestica ima volumni promjer manji od 15 mikrona,
gdje je maseni omjer rečenih finih čestica prema rečenim grubim česticama 5:95 do 30:70; te
(B) mikronizirane čestice glikopironijeva bromida, formoterol-fumarat dihidrata, te, opcionalno, beklometazon-dipropionata, kao aktivnih tvari, gdje se rečena formulacija dobiva postupkom koji obuhvaća:
(i) miješanje rečenog nosača, rečenog formoterol-fumarat dihidrata, te, opcionalno, rečenog beklometazon-dipropionata u posudi miješalice s potresivanjem pri brzini rotacije ne manjoj od 16 r.p.m. u vremenu ne kraćem od 60 minuta, da se dobije prva smjesa; te
(ii) dodavanje rečenog glikopironijeva bromida u rečenu prvu smjesu, da se dobije druga smjesa, te miješanje rečene druge smjese pri brzini rotacije ne većoj od 16 r.p.m. u vremenu ne dužem od 40 minuta; te gdje je srednja frakcija finih čestica glikopironijeva bromida viša od 25%.
9. Prašak prema patentnom zahtjevu 8, naznačeno time da postupak dalje obuhvaća:
(iii) daljnje miješanje formulacije dobivene u (ii), da se postigne homogena distribucija rečenih aktivnih tvari.
10. Formulacija praška prema patentnom zahtjevu 8 ili 9, naznačeno time da srednja frakcija finih čestica jest između 28 i 40%.
11. Formulacija praška prema bilo kojem od patentnih zahtjeva 8 do 10, naznačeno time da fiziološki prihvatljiv ekscipijens jest alfa-laktoza monohidrat.
12. Formulacija praška prema bilo kojem od patentnih zahtjeva 8 do 11, naznačeno time da grube čestice imaju maseni promjer između 210 i 360 µm.
13. Inhalator za suhi prašak napunjen formulacijom suhog praška iz bilo kojeg od patentnih zahtjeva 8 do 12.
14. Formulacija suhog praška iz bilo kojeg od patentnih zahtjeva 8 do 12 za upotrebu u prevenciji i/ili liječenju upalne i/ili opstruktivne bolesti dišnih puteva.
15. Formulacija suhog praška za upotrebu prema patentnom zahtjevu 14, naznačeno time da bolest jest astma ili kronična opstruktivna plućna bolest (COPD).
Applications Claiming Priority (3)
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| EP15194661 | 2015-11-16 | ||
| EP16801984.2A EP3377109B1 (en) | 2015-11-16 | 2016-11-14 | A process for preparing a dry powder formulation comprising an anticholinergic, a corticosteroid and a beta-adrenergic |
| PCT/EP2016/077566 WO2017085007A1 (en) | 2015-11-16 | 2016-11-14 | A process for preparing a dry powder formulation comprising an anticholinergic, a corticosteroid and a beta-adrenergic |
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| Publication Number | Publication Date |
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| HRP20200571T1 true HRP20200571T1 (hr) | 2020-07-10 |
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| HRP20211599TT HRP20211599T1 (hr) | 2015-11-16 | 2016-11-14 | Postupak priprave formulacije suhog praška koji sadrži antikolinergik, kortikosteroid i beta-adrenergik |
| HRP20200571TT HRP20200571T1 (hr) | 2015-11-16 | 2020-04-08 | Postupak priprave formulacije suhog praška koji sadrži antikolinergik, kortikosteroid i beta-adrenergik |
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| HRP20211599TT HRP20211599T1 (hr) | 2015-11-16 | 2016-11-14 | Postupak priprave formulacije suhog praška koji sadrži antikolinergik, kortikosteroid i beta-adrenergik |
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| US (3) | US10086003B2 (hr) |
| EP (2) | EP3689379B1 (hr) |
| JP (1) | JP6942126B2 (hr) |
| KR (1) | KR20180082442A (hr) |
| CN (1) | CN108348614B (hr) |
| AR (1) | AR106687A1 (hr) |
| AU (1) | AU2016357988B2 (hr) |
| CA (1) | CA3005291C (hr) |
| CL (1) | CL2018001297A1 (hr) |
| CO (1) | CO2018005139A2 (hr) |
| DK (2) | DK3689379T3 (hr) |
| EA (1) | EA037346B1 (hr) |
| ES (2) | ES2890409T3 (hr) |
| GE (1) | GEP20207178B (hr) |
| HK (1) | HK1256859A1 (hr) |
| HR (2) | HRP20211599T1 (hr) |
| HU (2) | HUE050343T2 (hr) |
| IL (1) | IL259327B (hr) |
| MA (1) | MA52437A (hr) |
| MX (1) | MX2018005979A (hr) |
| MY (1) | MY198321A (hr) |
| PE (1) | PE20181377A1 (hr) |
| PH (1) | PH12018501023B1 (hr) |
| PL (2) | PL3689379T3 (hr) |
| PT (2) | PT3377109T (hr) |
| SA (1) | SA518391574B1 (hr) |
| SG (2) | SG10201912090UA (hr) |
| SI (2) | SI3689379T1 (hr) |
| TW (1) | TWI729025B (hr) |
| UA (1) | UA125173C2 (hr) |
| WO (1) | WO2017085007A1 (hr) |
| ZA (1) | ZA201803167B (hr) |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| EP3621589B1 (en) | 2017-05-11 | 2021-07-07 | Chiesi Farmaceutici S.p.A. | A process for preparing a dry powder formulation comprising an anticholinergic, a corticosteroid and a beta-adrenergic |
| BR112019023378A2 (pt) * | 2017-05-11 | 2020-06-16 | Chiesi Farmaceutici S.P.A. | Processo para preparar uma formulação em pó para inalação para uso em um inalador de pó seco |
| WO2019060595A1 (en) * | 2017-09-20 | 2019-03-28 | Teva Branded Pharmaceutical Products R&D, Inc. | INHALABLE DRY POWDER MEDICINAL PRODUCT COMPRISING GLYCOPYRRONIUM |
| CN112823009A (zh) * | 2019-08-28 | 2021-05-18 | 上海谷森医药有限公司 | 糠酸氟替卡松脂质体制剂及其制备方法 |
| WO2021143785A1 (zh) * | 2020-01-15 | 2021-07-22 | 四川海思科制药有限公司 | 一种含茚达特罗的吸入气雾剂药物组合物及其制备方法 |
| CN111467498A (zh) * | 2020-05-14 | 2020-07-31 | 王兆霖 | 药物组合物制剂 |
| CN117064869A (zh) * | 2023-09-27 | 2023-11-17 | 山东京卫制药有限公司 | 一种胶囊型吸入粉雾剂及其制备方法 |
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| PE20011227A1 (es) * | 2000-04-17 | 2002-01-07 | Chiesi Farma Spa | Formulaciones farmaceuticas para inhaladores de polvo seco en la forma de aglomerados duros |
| GB0015043D0 (en) | 2000-06-21 | 2000-08-09 | Glaxo Group Ltd | Medicament dispenser |
| PT1658872E (pt) | 2002-07-31 | 2011-05-12 | Chiesi Farma Spa | Inalador de p? |
| WO2005004852A1 (en) * | 2003-07-11 | 2005-01-20 | Glaxo Group Limited | Pharmaceutical formulations |
| GB0410399D0 (en) * | 2004-05-10 | 2004-06-16 | Arakis Ltd | The treatment of respiratory disease |
| KR101863523B1 (ko) | 2010-04-21 | 2018-05-31 | 키에시 파르마슈티시 엣스. 피. 에이. | 정전하가 감소된 입자를 제공하는 방법 |
| US9393202B2 (en) | 2013-04-26 | 2016-07-19 | Chiesi Farmaceutici S.P.A | Particle size reduction of an antimuscarinic compound |
| WO2015004243A1 (en) * | 2013-07-11 | 2015-01-15 | Chiesi Farmaceutici S.P.A. | Dry powder formulation comprising an anticholinergic, a corticosteroid and a beta-adrenergic for administration by inhalation |
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