JP5894283B2 - 硫酸サルブタモールを含有する組成物 - Google Patents
硫酸サルブタモールを含有する組成物 Download PDFInfo
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- JP5894283B2 JP5894283B2 JP2014535167A JP2014535167A JP5894283B2 JP 5894283 B2 JP5894283 B2 JP 5894283B2 JP 2014535167 A JP2014535167 A JP 2014535167A JP 2014535167 A JP2014535167 A JP 2014535167A JP 5894283 B2 JP5894283 B2 JP 5894283B2
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- 239000000203 mixture Substances 0.000 title claims description 30
- BNPSSFBOAGDEEL-UHFFFAOYSA-N albuterol sulfate Chemical compound OS(O)(=O)=O.CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1.CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 BNPSSFBOAGDEEL-UHFFFAOYSA-N 0.000 title claims description 26
- 239000008194 pharmaceutical composition Substances 0.000 claims description 62
- 229940071648 metered dose inhaler Drugs 0.000 claims description 46
- NPNPZTNLOVBDOC-UHFFFAOYSA-N 1,1-difluoroethane Chemical compound CC(F)F NPNPZTNLOVBDOC-UHFFFAOYSA-N 0.000 claims description 38
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims description 31
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims description 31
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims description 31
- 239000005642 Oleic acid Substances 0.000 claims description 31
- ZQPPMHVWECSIRJ-UHFFFAOYSA-N Oleic acid Natural products CCCCCCCCC=CCCCCCCCC(O)=O ZQPPMHVWECSIRJ-UHFFFAOYSA-N 0.000 claims description 31
- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 claims description 31
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 claims description 31
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 26
- 239000000443 aerosol Substances 0.000 claims description 11
- 238000012377 drug delivery Methods 0.000 claims description 11
- 239000007788 liquid Substances 0.000 claims description 7
- 208000023504 respiratory system disease Diseases 0.000 claims description 7
- 208000006673 asthma Diseases 0.000 claims description 5
- 238000000034 method Methods 0.000 claims description 5
- 239000007921 spray Substances 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 62
- 239000003380 propellant Substances 0.000 description 60
- 239000003814 drug Substances 0.000 description 48
- 229940079593 drug Drugs 0.000 description 47
- 239000004094 surface-active agent Substances 0.000 description 35
- 235000019441 ethanol Nutrition 0.000 description 21
- LVGUZGTVOIAKKC-UHFFFAOYSA-N 1,1,1,2-tetrafluoroethane Chemical compound FCC(F)(F)F LVGUZGTVOIAKKC-UHFFFAOYSA-N 0.000 description 19
- 238000009472 formulation Methods 0.000 description 15
- 239000002245 particle Substances 0.000 description 8
- 238000012387 aerosolization Methods 0.000 description 7
- 239000000725 suspension Substances 0.000 description 7
- 230000008021 deposition Effects 0.000 description 5
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 5
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 5
- 238000002156 mixing Methods 0.000 description 5
- 239000013543 active substance Substances 0.000 description 4
- 239000006185 dispersion Substances 0.000 description 4
- 238000004128 high performance liquid chromatography Methods 0.000 description 4
- 239000002904 solvent Substances 0.000 description 4
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 4
- 239000004338 Dichlorodifluoromethane Substances 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- CBENFWSGALASAD-UHFFFAOYSA-N Ozone Chemical compound [O-][O+]=O CBENFWSGALASAD-UHFFFAOYSA-N 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 150000001875 compounds Chemical class 0.000 description 3
- RWRIWBAIICGTTQ-UHFFFAOYSA-N difluoromethane Chemical compound FCF RWRIWBAIICGTTQ-UHFFFAOYSA-N 0.000 description 3
- 238000004090 dissolution Methods 0.000 description 3
- 238000002474 experimental method Methods 0.000 description 3
- 239000000945 filler Substances 0.000 description 3
- 230000006870 function Effects 0.000 description 3
- 238000000338 in vitro Methods 0.000 description 3
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 description 3
- 229940029284 trichlorofluoromethane Drugs 0.000 description 3
- CDOOAUSHHFGWSA-OWOJBTEDSA-N (e)-1,3,3,3-tetrafluoroprop-1-ene Chemical compound F\C=C\C(F)(F)F CDOOAUSHHFGWSA-OWOJBTEDSA-N 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 2
- FXRLMCRCYDHQFW-UHFFFAOYSA-N 2,3,3,3-tetrafluoropropene Chemical compound FC(=C)C(F)(F)F FXRLMCRCYDHQFW-UHFFFAOYSA-N 0.000 description 2
- LCGLNKUTAGEVQW-UHFFFAOYSA-N Dimethyl ether Chemical compound COC LCGLNKUTAGEVQW-UHFFFAOYSA-N 0.000 description 2
- 239000002202 Polyethylene glycol Substances 0.000 description 2
- ATUOYWHBWRKTHZ-UHFFFAOYSA-N Propane Chemical compound CCC ATUOYWHBWRKTHZ-UHFFFAOYSA-N 0.000 description 2
- 239000002253 acid Substances 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 238000004378 air conditioning Methods 0.000 description 2
- 229910052782 aluminium Inorganic materials 0.000 description 2
- XAGFODPZIPBFFR-UHFFFAOYSA-N aluminium Chemical compound [Al] XAGFODPZIPBFFR-UHFFFAOYSA-N 0.000 description 2
- 239000010419 fine particle Substances 0.000 description 2
- 239000011521 glass Substances 0.000 description 2
- NNPPMTNAJDCUHE-UHFFFAOYSA-N isobutane Chemical compound CC(C)C NNPPMTNAJDCUHE-UHFFFAOYSA-N 0.000 description 2
- 210000004072 lung Anatomy 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 229910052751 metal Inorganic materials 0.000 description 2
- 239000002184 metal Substances 0.000 description 2
- 239000003595 mist Substances 0.000 description 2
- 239000004033 plastic Substances 0.000 description 2
- 229920003023 plastic Polymers 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 230000001105 regulatory effect Effects 0.000 description 2
- 210000002345 respiratory system Anatomy 0.000 description 2
- 238000004062 sedimentation Methods 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000000126 substance Substances 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 238000010792 warming Methods 0.000 description 2
- 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 description 1
- OWNWYCOLFIFTLK-UHFFFAOYSA-N 4-[2-(tert-butylamino)-1-hydroxyethyl]-2-(hydroxymethyl)phenol;hydron;chloride Chemical compound Cl.CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 OWNWYCOLFIFTLK-UHFFFAOYSA-N 0.000 description 1
- HIQIXEFWDLTDED-UHFFFAOYSA-N 4-hydroxy-1-piperidin-4-ylpyrrolidin-2-one Chemical compound O=C1CC(O)CN1C1CCNCC1 HIQIXEFWDLTDED-UHFFFAOYSA-N 0.000 description 1
- 239000004215 Carbon black (E152) Substances 0.000 description 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
- 229920001213 Polysorbate 20 Polymers 0.000 description 1
- 206010070834 Sensitisation Diseases 0.000 description 1
- 239000004147 Sorbitan trioleate Substances 0.000 description 1
- 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 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 230000007059 acute toxicity Effects 0.000 description 1
- 231100000403 acute toxicity Toxicity 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 238000005054 agglomeration Methods 0.000 description 1
- 230000002776 aggregation Effects 0.000 description 1
- 238000013019 agitation Methods 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 238000004458 analytical method Methods 0.000 description 1
- 239000012298 atmosphere Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 238000009835 boiling Methods 0.000 description 1
- 210000003123 bronchiole Anatomy 0.000 description 1
- 239000001273 butane Substances 0.000 description 1
- 230000007665 chronic toxicity Effects 0.000 description 1
- 231100000160 chronic toxicity Toxicity 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- -1 containers Substances 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 229940087091 dichlorotetrafluoroethane Drugs 0.000 description 1
- 239000013536 elastomeric material Substances 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
- 229940093471 ethyl oleate Drugs 0.000 description 1
- 238000005429 filling process Methods 0.000 description 1
- 239000004446 fluoropolymer coating Substances 0.000 description 1
- 150000002334 glycols Chemical class 0.000 description 1
- 239000012456 homogeneous solution Substances 0.000 description 1
- 229930195733 hydrocarbon Natural products 0.000 description 1
- 150000002430 hydrocarbons Chemical class 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- 239000001282 iso-butane Substances 0.000 description 1
- 229940074928 isopropyl myristate Drugs 0.000 description 1
- 238000005339 levitation Methods 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 description 1
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 description 1
- 229910052755 nonmetal Inorganic materials 0.000 description 1
- 229940068886 polyethylene glycol 300 Drugs 0.000 description 1
- 229920001451 polypropylene glycol Polymers 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 239000001294 propane Substances 0.000 description 1
- 230000001681 protective effect Effects 0.000 description 1
- 239000003507 refrigerant Substances 0.000 description 1
- 230000001846 repelling effect Effects 0.000 description 1
- QEVHRUUCFGRFIF-MDEJGZGSSA-N reserpine Chemical compound O([C@H]1[C@@H]([C@H]([C@H]2C[C@@H]3C4=C(C5=CC=C(OC)C=C5N4)CCN3C[C@H]2C1)C(=O)OC)OC)C(=O)C1=CC(OC)=C(OC)C(OC)=C1 QEVHRUUCFGRFIF-MDEJGZGSSA-N 0.000 description 1
- 230000008313 sensitization Effects 0.000 description 1
- 238000000926 separation method Methods 0.000 description 1
- 229920002545 silicone oil Polymers 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 238000000527 sonication Methods 0.000 description 1
- 229960000391 sorbitan trioleate Drugs 0.000 description 1
- 235000019337 sorbitan trioleate Nutrition 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000723 toxicological property Toxicity 0.000 description 1
- PHYFQTYBJUILEZ-IUPFWZBJSA-N triolein Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(OC(=O)CCCCCCC\C=C/CCCCCCCC)COC(=O)CCCCCCC\C=C/CCCCCCCC PHYFQTYBJUILEZ-IUPFWZBJSA-N 0.000 description 1
- 239000000080 wetting agent Substances 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
- 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
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/137—Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine or methadone
-
- 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
-
- 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
- A61M—DEVICES FOR INTRODUCING MEDIA INTO, OR ONTO, THE BODY; DEVICES FOR TRANSDUCING BODY MEDIA OR FOR TAKING MEDIA FROM THE BODY; DEVICES FOR PRODUCING OR ENDING SLEEP OR STUPOR
- A61M15/00—Inhalators
- A61M15/009—Inhalators using medicine packages with incorporated spraying means, e.g. aerosol cans
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
- B65B—MACHINES, APPARATUS OR DEVICES FOR, OR METHODS OF, PACKAGING ARTICLES OR MATERIALS; UNPACKING
- B65B3/00—Packaging plastic material, semiliquids, liquids or mixed solids and liquids, in individual containers or receptacles, e.g. bags, sacks, boxes, cartons, cans, or jars
- B65B3/003—Filling medical containers such as ampoules, vials, syringes or the like
-
- B—PERFORMING OPERATIONS; TRANSPORTING
- B65—CONVEYING; PACKING; STORING; HANDLING THIN OR FILAMENTARY MATERIAL
- B65B—MACHINES, APPARATUS OR DEVICES FOR, OR METHODS OF, PACKAGING ARTICLES OR MATERIALS; UNPACKING
- B65B31/00—Packaging articles or materials under special atmospheric or gaseous conditions; Adding propellants to aerosol containers
- B65B31/003—Adding propellants in fluid form to aerosol containers
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- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Mechanical Engineering (AREA)
- Emergency Medicine (AREA)
- Otolaryngology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Anesthesiology (AREA)
- Dispersion Chemistry (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Description
1,1−ジフルオロエタン(R−152a)から実質的になる噴射剤成分と、
オレイン酸を含む界面活性剤成分と、
硫酸サルブタモールからなる薬物成分と、
を含む組成物が提供される。
1,1−ジフルオロエタン(R−152a)から実質的になる噴射剤成分と、
オレイン酸を含む界面活性剤成分と、
硫酸サルブタモールからなる薬物成分と、
から実質的になる医薬組成物が提供される。
1,1−ジフルオロエタン(R−152a)からなる噴射剤成分と、
オレイン酸からなる界面活性剤成分と、
硫酸サルブタモールからなる薬物成分と、
を含む医薬組成物を提供する。
1,1−ジフルオロエタン(R−152a)からなる噴射剤成分と、
オレイン酸からなる界面活性剤成分と、
硫酸サルブタモールからなる薬物成分と、
を含む医薬組成物を保持する加圧容器を提供する。
1,1−ジフルオロエタン(R−152a)からなる噴射剤成分と、
オレイン酸からなる界面活性剤成分と、
硫酸サルブタモールからなる薬物成分と、
を含む医薬組成物を保持する加圧容器を有する薬剤送達装置、特に定量噴霧式吸入器を提供する。
R−134a又はR−152aのいずれかを含む定量噴霧式吸入器(MDI)における硫酸サルブタモールのインビトロエアロゾル化性能を調査すべく多数の実験を行った。硫酸サルブタモールの粒径は5μm未満であり、吸入による薬物送達に好適なものであった。
R−134a及びR−152aにおける様々な界面活性剤の溶解性を調査すべく多数の実験を行った。各噴射剤における界面活性剤の見かけ上の溶解を、プラスチックでコーティングした耐圧性の透明なガラス製エアロゾル瓶に既知量の界面活性剤を加えることにより周囲温度(19.5〜25.0℃)にて試験した。次いで、定量弁を瓶に加締めた。合計10グラムの各噴射剤を、界面活性剤濃度が0〜5%w/wの範囲となるように各エアロゾル瓶に充填した。噴射剤の添加後、内容物を10分間超音波処理し、溶解したか目視により観察した。
Claims (15)
- (a)1,1−ジフルオロエタン(R−152a)96.5〜99.94重量%と、
(b)オレイン酸0.05〜2.5重量%と、
(c)硫酸サルブタモール0.01〜1.0重量%と、
を含んでなる、医薬組成物。 - 前記医薬組成物は極性賦形剤を含まない、請求項1に記載の医薬組成物。
- 前記医薬組成物の少なくとも99重量%が成分(a)、(b)、及び(c)からなる、請求項1又は2に記載の医薬組成物。
- 成分(a)、(b)、及び(c)から完全になる、請求項1又は2に記載の医薬組成物。
- 請求項1〜4のいずれか一項に記載の医薬組成物を含む、密封容器。
- 定量噴霧式吸入器(MDI)と共に使用するための加圧容器である、請求項5に記載の密封容器。
- 請求項6に記載の加圧容器を装着した、定量噴霧式吸入器(MDI)。
- 1,1−ジフルオロエタン(R−152a)96.5〜99.94重量%、オレイン酸0.05〜2.5重量%、および硫酸サルブタモール0.01〜1.0重量%の、呼吸器疾患を患うか又は患う可能性のある患者の治療のための医薬組成物の製造における使用。
- 前記呼吸器疾患が喘息である、請求項8に記載の使用。
- 前記医薬組成物が定量噴霧式吸入器(MDI)を使用して患者に送達されるように適合されてなる、請求項8又は9に記載の使用。
- 呼吸器疾患を患うか又は患う可能性のある患者の治療のための、請求項1〜4のいずれか一項に記載の医薬組成物。
- 前記呼吸器疾患が喘息である、請求項11に記載の医薬組成物。
- 前記医薬組成物が定量噴霧式吸入器(MDI)を使用して患者に送達されるように適合されてなる、請求項11又は12に記載の医薬組成物。
- 請求項1〜4のいずれか一項に記載の医薬組成物の製造方法であって、
薬剤送達装置を使用して硫酸サルブタモールが最終的にエアロゾルスプレーとして放出されることになる開放容器に、秤量した硫酸サルブタモールを導入する工程と、
前記容器にバルブ装置を装着する工程と、
加圧下で前記バルブを通して前記容器に1,1−ジフルオロエタンを液形態で導入する工程と、
加圧下で前記バルブを通して前記容器にオレイン酸を導入する工程と、
を含む、方法。 - 前記液体1,1−ジフルオロエタンが前記オレイン酸と混合され、得られた液体混合物が前記バルブを介して加圧下で前記容器に導入される、請求項14に記載の方法。
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PCT/GB2012/052544 WO2013054137A1 (en) | 2011-10-12 | 2012-10-12 | Compositions comprising salbutamol sulphate |
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GB201306984D0 (en) * | 2013-04-17 | 2013-05-29 | Mexichem Amanco Holding Sa | Composition |
US11559505B2 (en) * | 2015-12-04 | 2023-01-24 | Mexichem Fluor S.A. De C.V. | Pharmaceutical composition |
GB2545025A (en) * | 2015-12-04 | 2017-06-07 | Mexichem Fluor Sa De Cv | Pharmaceutical composition |
WO2018051131A1 (en) * | 2016-09-19 | 2018-03-22 | Mexichem Fluor S.A. De C.V. | Pharmaceutical composition |
GEP20217239B (en) | 2016-09-19 | 2021-03-25 | Mexichem Fluor Sa De Cv | Pharmaceutical composition |
JP6781830B2 (ja) * | 2016-09-19 | 2020-11-04 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
CN115252552A (zh) * | 2016-09-19 | 2022-11-01 | 墨西哥氟石股份公司 | 药物组合物 |
BR112019005168A2 (pt) * | 2016-09-19 | 2019-06-11 | Mexichem Fluor Sa De Cv | composição farmacêutica, recipiente vedado, inalador de dose medida, e, métodos para tratar um paciente que sofre ou susceptível de sofrer de um distúrbio respiratório, para melhoria da estabilidade de uma composição farmacêutica e do desempenho de aerossolização de uma composição farmacêutica e para reduzir o potencial de aquecimento global de uma composição farmacêutica |
GB2573297A (en) * | 2018-04-30 | 2019-11-06 | Mexichem Fluor Sa De Cv | Pharmaceutical composition |
GB2584686A (en) * | 2019-06-11 | 2020-12-16 | Mexichem Fluor Sa De Cv | Methods |
FR3130554A1 (fr) | 2021-12-20 | 2023-06-23 | Aptar France Sas | Composition pharmaceutique comprenant du salbutamol |
FR3137830A1 (fr) | 2022-07-13 | 2024-01-19 | Aptar France Sas | Composition pharmaceutique comprenant du salbutamol |
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Family Cites Families (23)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
GB8828477D0 (en) | 1988-12-06 | 1989-01-05 | Riker Laboratories Inc | Medical aerosol formulations |
US5439670A (en) | 1989-11-28 | 1995-08-08 | Riker Laboratories, Inc. | Medicinal aerosol formulations |
IL97065A (en) * | 1990-02-02 | 1994-01-25 | Fisons Plc | Repellent preparations for aerosol |
DE4003272A1 (de) | 1990-02-03 | 1991-08-08 | Boehringer Ingelheim Kg | Neue treibgasmischungen und ihre verwendung in arzneimittelzubereitungen |
US7105152B1 (en) | 1991-12-18 | 2006-09-12 | 3M Innovative Properties Company | Suspension aerosol formulations |
DE69233319T2 (de) * | 1991-12-18 | 2005-02-17 | Minnesota Mining & Manufacturing Company, St. Paul | Aerosolzusammensetzungen für Arzneimittelsuspensionen |
ATE236617T1 (de) | 1994-12-22 | 2003-04-15 | Astrazeneca Ab | Aerosol-arzneiformulierungen |
PT820322E (pt) | 1995-04-14 | 2002-10-31 | Smithkline Beecham Corp | Inalador com dosimetro para propionato de fluticasona |
ATE239447T1 (de) | 1997-09-29 | 2003-05-15 | Inhale Therapeutic Syst | In verneblern verwendbare, stabilisierte zubereitungen |
US6103266A (en) | 1998-04-22 | 2000-08-15 | Tapolsky; Gilles H. | Pharmaceutical gel preparation applicable to mucosal surfaces and body tissues |
US6451285B2 (en) | 1998-06-19 | 2002-09-17 | Baker Norton Pharmaceuticals, Inc. | Suspension aerosol formulations containing formoterol fumarate and a fluoroalkane propellant |
DE59904648D1 (de) | 1998-08-04 | 2003-04-24 | Jago Res Ag Muttenz | Medizinische aerosolformulierungen |
GB2392164B (en) | 1999-09-11 | 2004-04-07 | Glaxo Group Ltd | Pharmaceutical formulation of fluticasone propionate |
US6432415B1 (en) | 1999-12-17 | 2002-08-13 | Axrix Laboratories, Inc. | Pharmaceutical gel and aerosol formulations and methods to administer the same to skin and mucosal surfaces |
CN1144582C (zh) | 2000-11-28 | 2004-04-07 | 中国药科大学 | 治疗呼吸系统疾病的无氟里昂药用气雾剂 |
GB2389530B (en) | 2002-06-14 | 2007-01-10 | Cipla Ltd | Pharmaceutical compositions |
GB0323685D0 (en) | 2003-10-09 | 2003-11-12 | Jagotec Ag | Improvements in or relating to organic compounds |
GB0323684D0 (en) | 2003-10-09 | 2003-11-12 | Jagotec Ag | Improvements in or relating to organic compounds |
CN1559389A (zh) * | 2004-03-05 | 2005-01-05 | 山东京卫制药有限公司 | 硫酸左旋沙丁胺醇气雾剂及其制备工艺 |
US20060018840A1 (en) | 2004-06-28 | 2006-01-26 | Nektar Therapeutics | Aerosolizable formulation comprising nicotine |
WO2007020204A2 (en) | 2005-08-12 | 2007-02-22 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Hfc solution formulations for inhalation containing salbutamol hydrochloride or salbutamol citrate |
CN101428010A (zh) * | 2008-12-12 | 2009-05-13 | 国家纳米技术与工程研究院 | 一种硫酸沙丁胺醇细粉的制备方法 |
GB0915106D0 (en) | 2009-08-28 | 2009-10-07 | Glaxo Group Ltd | Process |
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