SI9110156A - Nove zmesi poganjalnih plinov in njihova uporaba v pripravkih zdravil - Google Patents
Nove zmesi poganjalnih plinov in njihova uporaba v pripravkih zdravil Download PDFInfo
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- SI9110156A SI9110156A SI9110156A SI9110156A SI9110156A SI 9110156 A SI9110156 A SI 9110156A SI 9110156 A SI9110156 A SI 9110156A SI 9110156 A SI9110156 A SI 9110156A SI 9110156 A SI9110156 A SI 9110156A
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- propellant
- combination
- active ingredients
- betamimetics
- butylamino
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- 239000000203 mixture Substances 0.000 title claims abstract description 28
- 238000002360 preparation method Methods 0.000 title claims abstract description 12
- 239000003814 drug Substances 0.000 claims abstract description 15
- 150000001335 aliphatic alkanes Chemical class 0.000 claims abstract description 11
- 239000003380 propellant Substances 0.000 claims description 22
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 claims description 21
- LVGUZGTVOIAKKC-UHFFFAOYSA-N 1,1,1,2-tetrafluoroethane Chemical compound FCC(F)(F)F LVGUZGTVOIAKKC-UHFFFAOYSA-N 0.000 claims description 9
- 230000003454 betamimetic effect Effects 0.000 claims description 9
- 229940079593 drug Drugs 0.000 claims description 8
- 239000004480 active ingredient Substances 0.000 claims description 7
- 239000000808 adrenergic beta-agonist Substances 0.000 claims description 7
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 claims description 6
- 230000003266 anti-allergic effect Effects 0.000 claims description 5
- 229940065524 anticholinergics inhalants for obstructive airway diseases Drugs 0.000 claims description 5
- 239000001273 butane Substances 0.000 claims description 5
- 239000000812 cholinergic antagonist Substances 0.000 claims description 5
- 229960001022 fenoterol Drugs 0.000 claims description 5
- LSLYOANBFKQKPT-UHFFFAOYSA-N fenoterol Chemical compound C=1C(O)=CC(O)=CC=1C(O)CNC(C)CC1=CC=C(O)C=C1 LSLYOANBFKQKPT-UHFFFAOYSA-N 0.000 claims description 5
- 229960001361 ipratropium bromide Drugs 0.000 claims description 5
- KEWHKYJURDBRMN-ZEODDXGYSA-M ipratropium bromide hydrate Chemical compound O.[Br-].O([C@H]1C[C@H]2CC[C@@H](C1)[N@@+]2(C)C(C)C)C(=O)C(CO)C1=CC=CC=C1 KEWHKYJURDBRMN-ZEODDXGYSA-M 0.000 claims description 5
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 claims description 5
- 239000004094 surface-active agent Substances 0.000 claims description 5
- -1 4-amino-3-chloro-5-trifluoromethylphenyl Chemical group 0.000 claims description 4
- 239000000443 aerosol Substances 0.000 claims description 4
- 239000005557 antagonist Substances 0.000 claims description 4
- 150000001875 compounds Chemical class 0.000 claims description 4
- 150000003431 steroids Chemical class 0.000 claims description 4
- 235000021122 unsaturated fatty acids Nutrition 0.000 claims description 4
- 150000004670 unsaturated fatty acids Chemical class 0.000 claims description 4
- YFMFNYKEUDLDTL-UHFFFAOYSA-N 1,1,1,2,3,3,3-heptafluoropropane Chemical compound FC(F)(F)C(F)C(F)(F)F YFMFNYKEUDLDTL-UHFFFAOYSA-N 0.000 claims description 3
- NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 claims description 3
- 229960001609 oxitropium bromide Drugs 0.000 claims description 3
- LCELQERNWLBPSY-KHSTUMNDSA-M oxitropium bromide Chemical compound [Br-].C1([C@@H](CO)C(=O)O[C@H]2C[C@@H]3[N+]([C@H](C2)[C@@H]2[C@H]3O2)(C)CC)=CC=CC=C1 LCELQERNWLBPSY-KHSTUMNDSA-M 0.000 claims description 3
- 239000001294 propane Substances 0.000 claims description 3
- 229960002052 salbutamol Drugs 0.000 claims description 3
- XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical compound CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 claims description 2
- NPNPZTNLOVBDOC-UHFFFAOYSA-N 1,1-difluoroethane Chemical compound CC(F)F NPNPZTNLOVBDOC-UHFFFAOYSA-N 0.000 claims description 2
- RTLJQOLVPIGICL-UHFFFAOYSA-N 4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(methylsulfonylmethyl)phenol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CS(C)(=O)=O)=C1 RTLJQOLVPIGICL-UHFFFAOYSA-N 0.000 claims description 2
- KOTMQCNDGLTIHR-UHFFFAOYSA-N 4-[2-[[4-(benzimidazol-1-yl)-2-methylbutan-2-yl]amino]-1-hydroxyethyl]-3-fluorophenol Chemical compound C1=NC2=CC=CC=C2N1CCC(C)(C)NCC(O)C1=CC=C(O)C=C1F KOTMQCNDGLTIHR-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- VQDBNKDJNJQRDG-UHFFFAOYSA-N Pirbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=N1 VQDBNKDJNJQRDG-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- PRXRUNOAOLTIEF-ADSICKODSA-N Sorbitan trioleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC\C=C/CCCCCCCC)[C@H]1OC[C@H](O)[C@H]1OC(=O)CCCCCCC\C=C/CCCCCCCC PRXRUNOAOLTIEF-ADSICKODSA-N 0.000 claims description 2
- 239000004147 Sorbitan trioleate Substances 0.000 claims description 2
- WKHOPHIMYDJVSA-UHFFFAOYSA-N [3-[2-(tert-butylamino)-1-hydroxyethyl]-5-(2-methylpropanoyloxy)phenyl] 2-methylpropanoate Chemical compound CC(C)C(=O)OC1=CC(OC(=O)C(C)C)=CC(C(O)CNC(C)(C)C)=C1 WKHOPHIMYDJVSA-UHFFFAOYSA-N 0.000 claims description 2
- SCSIRWUYQVAIRL-UHFFFAOYSA-N ac1miw90 Chemical compound C1=2CC(C(=O)N(CCC)CCC)CC=2SC(N2C(C)=NN=C2CN=2)=C1C=2C1=CC=CC=C1Cl SCSIRWUYQVAIRL-UHFFFAOYSA-N 0.000 claims description 2
- 229960003060 bambuterol Drugs 0.000 claims description 2
- ANZXOIAKUNOVQU-UHFFFAOYSA-N bambuterol Chemical compound CN(C)C(=O)OC1=CC(OC(=O)N(C)C)=CC(C(O)CNC(C)(C)C)=C1 ANZXOIAKUNOVQU-UHFFFAOYSA-N 0.000 claims description 2
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone 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)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 claims description 2
- FWYVRZOREBYLCY-UHFFFAOYSA-N bepafant Chemical compound C1C=2SC=3N4C(C)=NN=C4CN=C(C=4C(=CC=CC=4)Cl)C=3C=2CC1C(=O)N1CCOCC1 FWYVRZOREBYLCY-UHFFFAOYSA-N 0.000 claims description 2
- 229960004620 bitolterol Drugs 0.000 claims description 2
- FZGVEKPRDOIXJY-UHFFFAOYSA-N bitolterol Chemical compound C1=CC(C)=CC=C1C(=O)OC1=CC=C(C(O)CNC(C)(C)C)C=C1OC(=O)C1=CC=C(C)C=C1 FZGVEKPRDOIXJY-UHFFFAOYSA-N 0.000 claims description 2
- 229960004436 budesonide Drugs 0.000 claims description 2
- 229960001386 carbuterol Drugs 0.000 claims description 2
- KEMXXQOFIRIICG-UHFFFAOYSA-N carbuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(NC(N)=O)=C1 KEMXXQOFIRIICG-UHFFFAOYSA-N 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 229960001117 clenbuterol Drugs 0.000 claims description 2
- STJMRWALKKWQGH-UHFFFAOYSA-N clenbuterol Chemical compound CC(C)(C)NCC(O)C1=CC(Cl)=C(N)C(Cl)=C1 STJMRWALKKWQGH-UHFFFAOYSA-N 0.000 claims description 2
- 239000013583 drug formulation Substances 0.000 claims description 2
- 229960000708 hexoprenaline Drugs 0.000 claims description 2
- OXLZNBCNGJWPRV-UHFFFAOYSA-N hexoprenaline Chemical compound C=1C=C(O)C(O)=CC=1C(O)CNCCCCCCNCC(O)C1=CC=C(O)C(O)=C1 OXLZNBCNGJWPRV-UHFFFAOYSA-N 0.000 claims description 2
- 229950002451 ibuterol Drugs 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 229960004398 nedocromil Drugs 0.000 claims description 2
- RQTOOFIXOKYGAN-UHFFFAOYSA-N nedocromil Chemical compound CCN1C(C(O)=O)=CC(=O)C2=C1C(CCC)=C1OC(C(O)=O)=CC(=O)C1=C2 RQTOOFIXOKYGAN-UHFFFAOYSA-N 0.000 claims description 2
- GTLACDSXYULKMZ-UHFFFAOYSA-N pentafluoroethane Chemical compound FC(F)C(F)(F)F GTLACDSXYULKMZ-UHFFFAOYSA-N 0.000 claims description 2
- 150000003904 phospholipids Chemical group 0.000 claims description 2
- 229960005414 pirbuterol Drugs 0.000 claims description 2
- 229960002288 procaterol Drugs 0.000 claims description 2
- FKNXQNWAXFXVNW-BLLLJJGKSA-N procaterol Chemical compound N1C(=O)C=CC2=C1C(O)=CC=C2[C@@H](O)[C@@H](NC(C)C)CC FKNXQNWAXFXVNW-BLLLJJGKSA-N 0.000 claims description 2
- 229960002720 reproterol Drugs 0.000 claims description 2
- WVLAAKXASPCBGT-UHFFFAOYSA-N reproterol Chemical compound C1=2C(=O)N(C)C(=O)N(C)C=2N=CN1CCCNCC(O)C1=CC(O)=CC(O)=C1 WVLAAKXASPCBGT-UHFFFAOYSA-N 0.000 claims description 2
- 229960004017 salmeterol Drugs 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 150000004671 saturated fatty acids Chemical class 0.000 claims description 2
- 235000019337 sorbitan trioleate Nutrition 0.000 claims description 2
- 229960000391 sorbitan trioleate Drugs 0.000 claims description 2
- 229950007862 sulfonterol Drugs 0.000 claims description 2
- 229960000195 terbutaline Drugs 0.000 claims description 2
- RVCSYOQWLPPAOA-DHWZJIOFSA-M trospium chloride Chemical compound [Cl-].[N+]12([C@@H]3CC[C@H]2CC(C3)OC(=O)C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CCCC1 RVCSYOQWLPPAOA-DHWZJIOFSA-M 0.000 claims description 2
- IMZMKUWMOSJXDT-UHFFFAOYSA-N cromoglycic acid Chemical compound O1C(C(O)=O)=CC(=O)C2=C1C=CC=C2OCC(O)COC1=CC=CC2=C1C(=O)C=C(C(O)=O)O2 IMZMKUWMOSJXDT-UHFFFAOYSA-N 0.000 claims 2
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical group CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 claims 1
- BQTXJHAJMDGOFI-NJLPOHDGSA-N Dexamethasone 21-(4-Pyridinecarboxylate) Chemical compound O=C([C@]1(O)[C@@]2(C)C[C@H](O)[C@]3(F)[C@@]4(C)C=CC(=O)C=C4CC[C@H]3[C@@H]2C[C@H]1C)COC(=O)C1=CC=NC=C1 BQTXJHAJMDGOFI-NJLPOHDGSA-N 0.000 claims 1
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical compound [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims 1
- 230000001078 anti-cholinergic effect Effects 0.000 claims 1
- UKXSKSHDVLQNKG-UHFFFAOYSA-N benzilic acid Chemical compound C=1C=CC=CC=1C(O)(C(=O)O)C1=CC=CC=C1 UKXSKSHDVLQNKG-UHFFFAOYSA-N 0.000 claims 1
- 238000007796 conventional method Methods 0.000 claims 1
- 229960000265 cromoglicic acid Drugs 0.000 claims 1
- 235000010445 lecithin Nutrition 0.000 claims 1
- 229940067606 lecithin Drugs 0.000 claims 1
- 239000000787 lecithin Substances 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000003848 thrombocyte activating factor antagonist Substances 0.000 claims 1
- 239000007789 gas Substances 0.000 abstract description 5
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 description 8
- 239000000126 substance Substances 0.000 description 4
- 239000000725 suspension Substances 0.000 description 3
- 239000000043 antiallergic agent Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000005507 spraying Methods 0.000 description 2
- DDMOUSALMHHKOS-UHFFFAOYSA-N 1,2-dichloro-1,1,2,2-tetrafluoroethane Chemical compound FC(F)(Cl)C(F)(F)Cl DDMOUSALMHHKOS-UHFFFAOYSA-N 0.000 description 1
- 239000004338 Dichlorodifluoromethane Substances 0.000 description 1
- 208000027771 Obstructive airways disease Diseases 0.000 description 1
- CBENFWSGALASAD-UHFFFAOYSA-N Ozone Chemical compound [O-][O+]=O CBENFWSGALASAD-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000002411 adverse Effects 0.000 description 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 description 1
- 239000000470 constituent Substances 0.000 description 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 1
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 1
- 229940088679 drug related substance Drugs 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 238000005457 optimization Methods 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 235000003441 saturated fatty acids Nutrition 0.000 description 1
- 238000004062 sedimentation Methods 0.000 description 1
- 239000008347 soybean phospholipid Substances 0.000 description 1
- 150000005846 sugar alcohols Polymers 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
Classifications
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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
- A61K9/0012—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
- A61K9/008—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
-
- 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
- A61K9/10—Dispersions; Emulsions
- A61K9/12—Aerosols; Foams
- A61K9/124—Aerosols; Foams characterised by the propellant
-
- C—CHEMISTRY; METALLURGY
- C09—DYES; PAINTS; POLISHES; NATURAL RESINS; ADHESIVES; COMPOSITIONS NOT OTHERWISE PROVIDED FOR; APPLICATIONS OF MATERIALS NOT OTHERWISE PROVIDED FOR
- C09K—MATERIALS FOR MISCELLANEOUS APPLICATIONS, NOT PROVIDED FOR ELSEWHERE
- C09K3/00—Materials not provided for elsewhere
- C09K3/30—Materials not provided for elsewhere for aerosols
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Dispersion Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- Materials Engineering (AREA)
- Pulmonology (AREA)
- Otolaryngology (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Materials For Medical Uses (AREA)
- Cosmetics (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Abstract
Nove koristne zmesi poganjalnih plinov vsebujejo dve ali več komponent, od katerih je vsaj ena delno fluoriran nižji alkan in jih lahko uporabljamo v pripravkih zdravil.ŕ
Description
Boehringer Ingelheim KG
Nove zmesi poganjalnih plinov in njihova uporaba v pripravkih zdravil
Izum se nanaša na nove zmesi poganjalnih plinov v katerih so, kot značilni sestavni deli, vsebovani delno fluorirani nižji alkani, kot npr. 1,1,1,2,3,3,3-heptafluorpropan (TG 227), na uporabo teh zmesi poganjalnih plinov v pripravkih zdravil, ki so primerni za izdelavo aerosolov, kot tudi na same pripravke zdravil.
Aerosole praškastih (mikroniziranih) zdravilnih snovi velikokrat uporabljajo pri terapiji, npr. pri terapiji obstruktivnih obolenj dihalnih poti. Dokler ne izdelujejo aerosolov z razprševanjem zdravilnih praškov ali s pršenjem raztopin, uporabljajo suspenzije zdravilnih snovi v utekočinjenih poganjalnih plinih. Kot take so primerne zlasti zmesi iz TG 11 (triklorfluormetan), TG 12 (diklordifluormetan) in TG 114 (l,2-diklor-l,l,2,2-tetrafluoretan), v danem primeru ob dodatku nižji alkanov, npr. butana, pentana ali tudi DME (dimetileter). Zmesi te vrste so npr. znane iz nemškega patentnega spisa 1178975. Uporaba klorfluorogljikovodikov, je zaradi njihovega negativnega vpliva na zemeljsko atmosfero (uničevanje ozonskega sloja, efekt tople grede) postala problematična, tako da iščemo druge poganjalne pline oz. zmesi poganjalnih plinov, ki navedenih negativnih učinkov ne povzročajo ali pa jih vsaj v neznatni meri.
-r
Pri iskanju vendar naletimo na precejšnje težave, ker morajo poganjalni plini, ki naj jih terapevtsko uporabimo, izpolniti številne kriterije, ki jih ni lahko uskladiti med seboj, npr. glede na toksičnost, stabilnost, parni tlak, gostoto, topilnost.
Kot smo sedaj ugotovili, so iz dveh ali več komponent obstoječe zmesi poganjalnih plinov, ki vsebujejo vsaj en delno fluoriran nižji alkan in v danem primeru eno ali več spojin iz skupine TG 11, TG 12, TG 114, nižjega alkana in dimetiletra, zlasti primerne za uporabo v terapevtsko uporabnih pripravkih.
Kot delno fluorirani nižji alkani v smislu izuma, so predvsem primerni TG 227 (1,1,1,2,3,3,3-heptafluor-propan, TG 125 (pentafluoretan), TG 134a (1,1,1,2tetrafluoretan) in TG 152a (1,1-difluoretan). Od alkanov pridejo zlasti v poštev propan, butan in pentan, zlasti n-spojine. Za optimiranje lastnosti zmesi poganjalnega plina lahko koristijo dodatki dosedaj v glavnem uporabljenih poganjalnih plinov TG 11, TG 12 in TG 114, ker imajo relativno visoko gostoto. Pripravki zdravil, pripravljeni na osnovi novih zmesi poganjalnih plinov, vsebujejo poleg učinkovine (npr. v suspendirani obliki), v splošnem eno, v ta namen uporabno površinsko aktivno snov, npr. ester polialkohola, npr. sorbitanester z višjimi nasičenimi ali nenasičenimi maščobnimi kislinami, npr. sorbitantrioleat ali polietoksisorbitanester višje, zlasti nenasičene maščobne kisline ali fosfolipid, npr. licitin. Pomožna snov je lahko v zmesi raztopljena ali neraztopljena.
Da ustavimo sedimentacijo suspendiranih delcev zdravil, je ugodno, da uporabimo take zmesi utekočinjenih poganjalnih plinov, katerih gostota se ne razlikuje znatno od gostote suspendirane snovi. Vendar so uporabne tudi zmesi z večjimi razlikami med gostoto zdravila in gostoto utekočinjene zmesi poganjalnega plina. Pokazalo se je namreč, da lahko razmešane suspenzije, s stresanjem, zlahka spet enakomerno porazdelimo v tukaj predlaganem suspenzijskem mediju.
Količinska razmerja posameznih sestavin zmesi poganjalnega plina, lahko variirajo v širokih mejah. Delež (vsakokrat v masnih odstotkih), znaša za TG 227 10 do 99 %, za TG 125 20 do 75 %, za TG 134a 20 do 75 %, za TG 152a 25 do 80 %. Zmes lahko razen tega vsebuje 0 do 50 % propana in/ali butana in/ali pentana in/ali DME in 0 do % TG 11, TG 12 in/ali TG 114. Znotraj navedenih mej, izberemo sestavine tako, da dajo skupaj 100 %. Prednostne so zmesi poganjalnih plinov, ki vsebujejo 30 do 95 % TG 227.
Delež suspendiranega zdravila v gotovem pripravku znaša med 0,001 in 5 %, prednostno 0,005 do 3 %, zlasti 0,01 do 2 %. Površinsko aktivne snovi dodamo v količinah od 0,01 do 10 %, prednostno 0,05 do 5 %, zlasti 0,1 do 3 % (tukaj so tako kot pri zdravilih navedeni masni odstotki gotovega pripravka). Kot zdravila so lahko v novih pripravkih vse substance, ki so primerne za inhalacijsko, v danem primeru tudi za intranazalno uporabo. Gre torej zlasti za betamimetike, antiholinergike, steroide, antialergike, PAF-antagoniste, kot tudi za kombinacije iz takih učinkovin.
Posebej kot primere navajamo:
Kot betamimetike:
Bambuterol
Bitolterol
Carbuterol
Clenbuterol
Fenoterol
Hexoprenalin
Ibuterol
Pirbuterol
Procaterol
Reproterol
Salbutamol
Salmeterol
Sulfonterol
Terbutalin
Tulobuterol l-(2-fluor-4-hidroksifenil)-2-[4-(l-benzimidazolil)-2-metil-2-butilamino]etanol eritro-5’-hidroksi-8’-(l-hidroksi-2-izopropilaminobutil)-2H-l,4-benzoksazin-3(4H)-on l-(4-amino-3-klor-5-trifluormetilfenil)-2-terc.butilamino)etanol l-(4-etoksikarbonilamino-3-cian-5-fluorfenil)-2-(terc.butilamino)etanol.
Kot antiholinergike:
Ipratropiumbromid
Oxitropiumbromid
Trospiumchlorid
N-/3-fluoretilnortropinestermetobromid benzilne kisline
Kot steroide:
Budesonid
Beclometason (oz. 17,21-dipropionat)
Dexamethason-21-izonikotinat
Flunisolid
Kot antialergike:
Dinatriumcromoglikat
Nedocromil
Kot PAF-antagoniste: WEB 2086 WEB 2170 WEB 2347
Učinkovine lahko tudi kombiniramo, npr. betamimetike in antiholinergike ali betamimetike in antialergike.
-5Primeri za pripravke v smislu izuma (podatek v masnih odstotkih):
| 0,10 % Oxitropiumbromida 0,01 % sojalecitina 4,0 % pentana 95,89 % TG 227 | 2·) | 0,3 % Fenoterola 0,1 % sojalecitina 10,0 % pentana 70,0 % TG 227 19,6 % TG 134a |
| 0,1 % Ipratropiumbromida 0,1 % sojalecitina 25,0 % pentana 10,1 % TG 227 64,7 % TG 134a | 4·) | 0,3 % Fenoterola 0,1 % sojalecitina 30,0 % TG 11 49,6 % TG 134a 20,0 % TG 227 |
| 1,5 % Dinatriumcromoglicata 0,1 % Tweena 20 97,0 % TG 227 1,4 % butana | 6·) | 0,3 % Salbutamola 0,2 % Špana 85 20,0 % pentana 30,0 % TG 227 49,5 % TG 134a |
| 0,15 % Fenoterola 0,06 % Ipratropiumbromida 0,10 % sojalecitina 40,00 % TG 11 39,69 %TG 134a | 8·) | 0,1 % Ipratropiumbromida 0,1 % sojalecitina 20,3 % TG 125 25,5 % TG 152a 54,0 % TG 227 |
20,00 % TG 227
Claims (12)
- PATENTNI ZAHTEVKI1. Zmesi poganjalnih plinov iz dveh ali več komponent, ki vsebujejo vsaj en nižji delno fluoriran alkan in v danem primeru eno ali več spojin iz skupine TG 11, TG 12, TG 114, nižjega alkana in DME.
- 2. Zmes poganjalnih plinov po zahtevku 1, označena s tem, daje delno fluoriran nižji alkan spojina iz skupine 1,1-difluoretana, 1,1,1,2-tetrafluoretana, pentafluoretana,1,1,1,2,3,3,3-heptafluorpropana in daje nižji alkan, propan, butan ali pentan.
- 3. Zmesi poganjalnih plinov po zahtevku 1, označene s tem, da dodatno vsebujejo vsaj eno površinsko aktivno snov.
- 4. Zmesi poganjalnih plinov po zahtevku 2, označene s tem, da je površinsko aktivna snov fosfolipid, sorbitanester z višjo nasičeno ali nenasičeno maščobno kislino ali polietoksisorbitanester višje, prednostno nenasičene maščobne kisline.
- 5. Zmes poganjalnih plinov po zahtevku 2, označena s tem, daje površinsko aktivna snov lecitin, polietoksietilensorbitanoleat ali sorbitantrioleat.
- 6. Pripravki zdravil za izdelavo praškastih aerosolov na osnovi zmesi poganjalnih plinov po zahtevku 1, 2, 3 ali 4, označeni s tem, da kot učinkovino vsebujejo betamimetik, antiholinergik, steroid, antialergik ali PAF-antagonist ali kombinacijo takih spojin.
- 7. Pripravki zdravil po zahtevku 5, označeni s tem, da uporabimo, kot betamimetikBambuterolBitolterolCarbuterolClenbuterolFenoterolHexoprenalinIbuterolPirbuterolProcaterolReproterolSalbutamolSalmeterolSulfonterolTerbutalinTulobuterol l-(2-fluor-4-hidroksifenil)-2-[4-(l-benzimidazolil)-2-metil-2-butilamino]etanol eritro-5’-hidroksi-8’-(l-hidroksi-2-izopropilaminobutil)-2H-l,4-benzoksazin-3(4H)-on l-(4-amino-3-klor-5-trifluormetilfenil)-2-terc.butilamino)etanol l-(4-etoksikarbonilamino-3-cian-5-fluorfenil)-2-(terc.butilamino)etanol.kot antiholinergike:IpratropiumbromidOxitropiumbromidTrospiumchloridN-/3-fluoretilnortropinestermetobromid benzilne kisline kot steroide:BudesonidBeclometason (oz. 17,21-dipropionat)Dexametason-21-izonikotinatFlunisolid kot antialergike:DinatriumcromoglikatNedocromil kot PAF-antagoniste: WEB 2086 WEB 2170 WEB 2347.-2'
- 8. Pripravki zdravil po zahtevku 5, označeni s tem, da obsegajo kombinacijo učinkovin enega od v zahtevku 6 navedenih betamimetikov in enega od v zahtevku 6 navedenih antiholinergikov.
- 9. Pripravek zdravila po zahtevku 5, označen s tem, da obsega kombinacijo učinkovin enega od v zahtevku 6 navedenih betamimetikov in dinatrijev kromoglikat.
- 10. Pripravek zdravila po zahtevku 5, označen s tem, da vsebuje kombinacijo učinkovin enega od v zahtevku 6 navedenih betamimetikov in enega od v zahtevku 6 navedenih PAF-antagonistov.
- 11. Pripravek zdravila po zahtevku 5, označen s tem, da obsega kombinacija učinkovin dinatrijev kromoglikat in enega od v zahtevku 6 navedenih PAFantagonistov.
- 12. Postopek za pripravo pripravkov zdravil, po zahtevkih 5 do 10, označen s tem, da po običajnih metodah suspendiramo mikronizirane učinkovine zdravil v utekočinjeno zmes poganjalnega plina, po zahtevku 1,2,3 ali 4.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE4003272A DE4003272A1 (de) | 1990-02-03 | 1990-02-03 | Neue treibgasmischungen und ihre verwendung in arzneimittelzubereitungen |
| YU15691A YU49203B (sh) | 1990-02-03 | 1991-01-30 | Nove smeše potisnih gasova za farmaceutske preparate za inhaliranje |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SI9110156A true SI9110156A (sl) | 1998-04-30 |
| SI9110156B SI9110156B (sl) | 1999-04-30 |
Family
ID=6399400
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SI9110156A SI9110156B (sl) | 1990-02-03 | 1991-01-30 | Nove zmesi poganjalnih plinov in njihova uporaba v pripravkih zdravil |
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| Country | Link |
|---|---|
| US (1) | US6413497B1 (sl) |
| EP (1) | EP0514415B1 (sl) |
| JP (1) | JP3497161B2 (sl) |
| AT (1) | ATE165863T1 (sl) |
| AU (1) | AU650001B2 (sl) |
| CA (1) | CA2075058C (sl) |
| CZ (1) | CZ286691B6 (sl) |
| DE (2) | DE4003272A1 (sl) |
| DK (1) | DK0514415T3 (sl) |
| ES (1) | ES2117964T3 (sl) |
| FI (1) | FI102905B (sl) |
| HK (1) | HK1010786A1 (sl) |
| HR (1) | HRP940735B1 (sl) |
| HU (2) | HU9202509D0 (sl) |
| IE (2) | IE910351A1 (sl) |
| IL (1) | IL97028A (sl) |
| NO (1) | NO302419B1 (sl) |
| NZ (1) | NZ236973A (sl) |
| PT (1) | PT96634B (sl) |
| SI (1) | SI9110156B (sl) |
| SK (1) | SK280426B6 (sl) |
| WO (1) | WO1991011495A1 (sl) |
| YU (1) | YU49203B (sl) |
| ZA (1) | ZA91754B (sl) |
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| MX3864E (es) | 1975-05-27 | 1981-08-26 | Syntex Corp | Un proceso para prepara el compuesto cristalino 6-fluiro-11b 21-dihiroxi-16 17-isopropilidendioxipregna-1 4-dien-3 20-diona |
| US4405598A (en) | 1976-01-30 | 1983-09-20 | Fisons, Limited | Composition for treating asthma |
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| JPS5325284A (en) * | 1976-08-19 | 1978-03-08 | Daikin Ind Ltd | Aerosol composition |
| US4352789A (en) | 1980-03-17 | 1982-10-05 | Minnesota Mining And Manufacturing Company | Aerosol compositions containing finely divided solid materials |
| JPS5734174A (en) * | 1980-08-11 | 1982-02-24 | Toyo Aerosol Kogyo Kk | Powdered aerosol composition |
| GB8613811D0 (en) * | 1986-06-06 | 1986-07-09 | Phares Pharm Res Nv | Composition & method |
| GB8501015D0 (en) | 1985-01-16 | 1985-02-20 | Riker Laboratories Inc | Drug |
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| DE3784594T2 (de) | 1986-08-11 | 1994-01-05 | Innovata Biomed Ltd | Mikrokapseln enthaltende pharmazeutische Zusammensetzungen. |
| DE3815480A1 (de) | 1988-05-06 | 1989-11-16 | Boehringer Ingelheim Kg | Synergistische kombinationen und ihre verwendung als therapeutika |
| US5225183A (en) * | 1988-12-06 | 1993-07-06 | Riker Laboratories, Inc. | Medicinal aerosol formulations |
| DE3905726A1 (de) * | 1989-02-24 | 1990-08-30 | Hoechst Ag | Druckgaspackung und treibmittel fuer aerosole |
| US5118494A (en) * | 1990-03-23 | 1992-06-02 | Minnesota Mining And Manufacturing Company | Use of soluble fluorosurfactants for the preparation of metered-dose aerosol formulations |
| MX9203481A (es) * | 1990-10-18 | 1992-07-01 | Minnesota Mining & Mfg | Formulaciones. |
| US5190029A (en) * | 1991-02-14 | 1993-03-02 | Virginia Commonwealth University | Formulation for delivery of drugs by metered dose inhalers with reduced or no chlorofluorocarbon content |
| US6013245A (en) * | 1995-01-26 | 2000-01-11 | Glaxo Group Limited | Aerosol formulation containing beclomethasone dipropionate and 1,1,1,2,3,3,3-heptafluoro-n-propane as propellant |
| US6039932A (en) * | 1996-09-27 | 2000-03-21 | 3M Innovative Properties Company | Medicinal inhalation aerosol formulations containing budesonide |
| US6004537A (en) * | 1998-12-18 | 1999-12-21 | Baker Norton Pharmaceuticals, Inc. | Pharmaceutical solution aerosol formulations containing fluoroalkanes, budesonide and formoterol |
-
1990
- 1990-02-03 DE DE4003272A patent/DE4003272A1/de not_active Ceased
-
1991
- 1991-01-24 IL IL9702891A patent/IL97028A/en not_active IP Right Cessation
- 1991-01-30 YU YU15691A patent/YU49203B/sh unknown
- 1991-01-30 SI SI9110156A patent/SI9110156B/sl unknown
- 1991-01-31 AU AU72113/91A patent/AU650001B2/en not_active Expired
- 1991-01-31 ES ES91903275T patent/ES2117964T3/es not_active Expired - Lifetime
- 1991-01-31 DK DK91903275T patent/DK0514415T3/da active
- 1991-01-31 CA CA002075058A patent/CA2075058C/en not_active Expired - Lifetime
- 1991-01-31 AT AT91903275T patent/ATE165863T1/de not_active IP Right Cessation
- 1991-01-31 EP EP91903275A patent/EP0514415B1/de not_active Revoked
- 1991-01-31 WO PCT/EP1991/000177 patent/WO1991011495A1/de not_active Application Discontinuation
- 1991-01-31 JP JP50368691A patent/JP3497161B2/ja not_active Expired - Lifetime
- 1991-01-31 DE DE59108979T patent/DE59108979D1/de not_active Revoked
- 1991-01-31 NZ NZ236973A patent/NZ236973A/en unknown
- 1991-01-31 HU HU922509Q patent/HU9202509D0/hu unknown
- 1991-01-31 HU HU9202509A patent/HU218784B/hu unknown
- 1991-02-01 IE IE035191A patent/IE910351A1/en not_active IP Right Cessation
- 1991-02-01 ZA ZA91754A patent/ZA91754B/xx unknown
- 1991-02-01 IE IE035091A patent/IE910350A1/en not_active IP Right Cessation
- 1991-02-01 PT PT96634A patent/PT96634B/pt not_active IP Right Cessation
- 1991-02-04 CZ CS1991264A patent/CZ286691B6/cs not_active IP Right Cessation
- 1991-02-04 SK SK264-91A patent/SK280426B6/sk not_active IP Right Cessation
-
1992
- 1992-07-31 NO NO923039A patent/NO302419B1/no not_active IP Right Cessation
- 1992-08-03 FI FI923490A patent/FI102905B/fi active
-
1994
- 1994-10-24 HR HRP-156/91A patent/HRP940735B1/xx not_active IP Right Cessation
-
1998
- 1998-11-05 HK HK98111767A patent/HK1010786A1/xx not_active IP Right Cessation
-
2000
- 2000-05-05 US US09/566,105 patent/US6413497B1/en not_active Expired - Fee Related
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