JP2014528470A - 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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- 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 abstract description 25
- 239000003380 propellant Substances 0.000 claims abstract description 66
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 62
- 239000003814 drug Substances 0.000 claims abstract description 53
- 229940079593 drug Drugs 0.000 claims abstract description 52
- 229940071648 metered dose inhaler Drugs 0.000 claims abstract description 46
- 239000004094 surface-active agent Substances 0.000 claims abstract description 41
- NPNPZTNLOVBDOC-UHFFFAOYSA-N 1,1-difluoroethane Chemical compound CC(F)F NPNPZTNLOVBDOC-UHFFFAOYSA-N 0.000 claims abstract description 40
- WRIDQFICGBMAFQ-UHFFFAOYSA-N (E)-8-Octadecenoic acid Natural products CCCCCCCCCC=CCCCCCCC(O)=O WRIDQFICGBMAFQ-UHFFFAOYSA-N 0.000 claims abstract description 31
- LQJBNNIYVWPHFW-UHFFFAOYSA-N 20:1omega9c fatty acid Natural products CCCCCCCCCCC=CCCCCCCCC(O)=O LQJBNNIYVWPHFW-UHFFFAOYSA-N 0.000 claims abstract description 31
- QSBYPNXLFMSGKH-UHFFFAOYSA-N 9-Heptadecensaeure Natural products CCCCCCCC=CCCCCCCCC(O)=O QSBYPNXLFMSGKH-UHFFFAOYSA-N 0.000 claims abstract description 31
- 239000005642 Oleic acid Substances 0.000 claims abstract description 31
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- 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
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- 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
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- 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
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- 150000001298 alcohols Chemical class 0.000 description 1
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- 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
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- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
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- 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
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- 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
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- 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
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- 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
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- 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
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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
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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]
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- 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
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- 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
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- 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
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- 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
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- 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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Abstract
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 (14)
- 極性賦形剤を含まない医薬組成物であって、
(a)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、
(b)オレイン酸を含む界面活性剤成分と、
(c)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。 - 成分(a)、(b)、及び(c)から実質的になる、請求項1に記載の医薬組成物。
- 加圧容器から送達するための医薬組成物であって、
(a)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、
(b)オレイン酸を含む界面活性剤成分と、
(c)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。 - 成分(a)、(b)、及び(c)から完全になる、請求項1又は3に記載の医薬組成物。
- 前記噴射剤成分が1、1−ジフルオロエタン(R−152a)から完全になる、請求項1〜4のいずれか一項に記載の医薬組成物。
- 前記界面活性剤成分がオレイン酸から完全になる、請求項1〜5のいずれか一項に記載の医薬組成物。
- 請求項1〜6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7に記載の密封容器。
- 請求項8に記載の加圧容器を装着した、定量噴霧式吸入器(MDI)。
- 呼吸器疾患を患うか又は患う可能性のある患者の治療方法であって、治療又は予防に有効な量の請求項1〜6のいずれか一項に記載の医薬組成物を患者に投与することを含む、方法。
- 前記呼吸器疾患が喘息である、請求項10に記載の方法。
- 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、請求項10又は11に記載の方法。
- 請求項1〜6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前記薬物成分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、秤量した前記薬物成分を導入する工程と、
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前記噴射剤成分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前記界面活性剤成分を導入する工程と、
を含む、方法。 - 前記液体噴射剤が前記界面活性剤と混合され、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13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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JP2019529428A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
JP2019529431A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
JP2019529432A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
JP2019529430A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
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GB2545025A (en) * | 2015-12-04 | 2017-06-07 | Mexichem Fluor Sa De Cv | Pharmaceutical composition |
BR122020022602B1 (pt) * | 2015-12-04 | 2024-03-05 | Mexichem Fluor S.A. De C.V. | 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 |
WO2024033941A1 (en) * | 2022-08-10 | 2024-02-15 | Cipla Limited | A pharmaceutical composition of salbutamol and pharmaceutical green propellant |
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JP2019529428A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
JP2019529431A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
JP2019529432A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
JP2019529430A (ja) * | 2016-09-19 | 2019-10-17 | メキシケム フロー エセ・ア・デ・セ・ヴェ | 医薬組成物 |
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CA2851026A1 (en) | 2013-04-18 |
CN103874489A (zh) | 2014-06-18 |
WO2013054137A1 (en) | 2013-04-18 |
MX335944B (es) | 2016-01-04 |
CA2851026C (en) | 2016-01-05 |
AU2012322455B2 (en) | 2015-07-02 |
BR112014008602B1 (pt) | 2022-05-24 |
EP2766006B1 (en) | 2015-11-25 |
GB201117619D0 (en) | 2011-11-23 |
CN103874489B (zh) | 2016-01-20 |
US9517216B2 (en) | 2016-12-13 |
BR112014008602A2 (pt) | 2017-04-18 |
ES2556586T3 (es) | 2016-01-19 |
US20140230812A1 (en) | 2014-08-21 |
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US10039828B2 (en) | 2018-08-07 |
EP2766006A1 (en) | 2014-08-20 |
ZA201402321B (en) | 2015-03-25 |
US20170165367A1 (en) | 2017-06-15 |
AU2012322455A1 (en) | 2014-04-17 |
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