HRP20240525T1 - Pripravak na bazi lipida za oralnu primjenu antagonista bradikininskog b2-receptora - Google Patents
Pripravak na bazi lipida za oralnu primjenu antagonista bradikininskog b2-receptora Download PDFInfo
- Publication number
- HRP20240525T1 HRP20240525T1 HRP20240525TT HRP20240525T HRP20240525T1 HR P20240525 T1 HRP20240525 T1 HR P20240525T1 HR P20240525T T HRP20240525T T HR P20240525TT HR P20240525 T HRP20240525 T HR P20240525T HR P20240525 T1 HRP20240525 T1 HR P20240525T1
- Authority
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- Croatia
- Prior art keywords
- weight
- propylene glycol
- liquid pharmaceutical
- pharmaceutical preparation
- liquid
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims 2
- 229940123765 Bradykinin B2 receptor antagonist Drugs 0.000 title 1
- 239000003359 bradykinin B2 receptor antagonist Substances 0.000 title 1
- 150000002632 lipids Chemical class 0.000 title 1
- 239000007788 liquid Substances 0.000 claims 26
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 18
- 239000000825 pharmaceutical preparation Substances 0.000 claims 10
- GHHURQMJLARIDK-UHFFFAOYSA-N 2-hydroxypropyl octanoate Chemical compound CCCCCCCC(=O)OCC(C)O GHHURQMJLARIDK-UHFFFAOYSA-N 0.000 claims 8
- 101800004538 Bradykinin Proteins 0.000 claims 7
- QXZGBUJJYSLZLT-UHFFFAOYSA-N H-Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg-OH Natural products NC(N)=NCCCC(N)C(=O)N1CCCC1C(=O)N1C(C(=O)NCC(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CO)C(=O)N2C(CCC2)C(=O)NC(CC=2C=CC=CC=2)C(=O)NC(CCCN=C(N)N)C(O)=O)CCC1 QXZGBUJJYSLZLT-UHFFFAOYSA-N 0.000 claims 7
- 102100035792 Kininogen-1 Human genes 0.000 claims 7
- QXZGBUJJYSLZLT-FDISYFBBSA-N bradykinin Chemical compound NC(=N)NCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)NCC(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CO)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)CCC1 QXZGBUJJYSLZLT-FDISYFBBSA-N 0.000 claims 7
- 239000004359 castor oil Substances 0.000 claims 7
- 235000019438 castor oil Nutrition 0.000 claims 7
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims 7
- 229920002675 Polyoxyl Polymers 0.000 claims 6
- 239000002775 capsule Substances 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 239000002464 receptor antagonist Substances 0.000 claims 4
- 229940044551 receptor antagonist Drugs 0.000 claims 4
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical group [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 229910052805 deuterium Inorganic materials 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000012453 solvate Substances 0.000 claims 3
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000004014 plasticizer Substances 0.000 claims 2
- 239000007901 soft capsule Substances 0.000 claims 2
- 239000000600 sorbitol Substances 0.000 claims 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 206010019860 Hereditary angioedema Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical group [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- 206010030113 Oedema Diseases 0.000 claims 1
- 229920002690 Polyoxyl 40 HydrogenatedCastorOil Polymers 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 229910052739 hydrogen Chemical group 0.000 claims 1
- 239000001257 hydrogen Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
Classifications
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—Organic macromolecular compounds
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
-
- 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
- A61K9/107—Emulsions ; Emulsion preconcentrates; Micelles
- A61K9/1075—Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4816—Wall or shell material
- A61K9/4825—Proteins, e.g. gelatin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- 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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Dispersion Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Claims (15)
1. Tekući farmaceutski pripravak za oralnu primjenu koji sadrži antagonist bradikininskog (BK) B2 receptora koji ima kemijsku strukturu u skladu s Formulom 1, ili njegov stereoizomer, sol ili solvat:
[image]
pri čemu je R deuterij ili vodik;
pri čemu je antagonist BK B2 receptora otopljen u tekućem nosaču koji sadrži propilen glikol monokaprilat, polioksil ricinusovo ulje i propilen glikol.
2. Tekući farmaceutski pripravak prema zahtjevu 1, naznačen time što je antagonist BK B2 receptora spoj u skladu s Formulom 1, ili njegova sol ili solvat, pri čemu je R deuterij.
3. Tekući farmaceutski pripravak prema zahtjevu 1 ili 2, naznačen time što je količina propilen glikol monokaprilata u tekućem nosaču 40-60 tež.%, temeljeno na težini tekućeg nosača.
4. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što količina polioksilnog ricinusovog ulja u tekućem nosaču iznosi 30-50 tež.%, temeljeno na težini tekućeg nosača.
5. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je količina propilen glikola 2,5-15 tež.%, temeljeno na težini tekućeg nosača.
6. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je propilen glikol monokaprilat propilen glikol monokaprilat tipa II (USP/NF).
7. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je polioksil ricinusovo ulje polioksil 40 hidrogenirano ricinusovo ulje (USP/NF).
8. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što je sadržaj propilen glikol monokaprilata 50 tež.%, sadržaj polioksilnog ricinusovog ulja je 40 tež.%, a sadržaj propilen glikola je 10 tež.% , na temelju kombinirane težine propilen glikol monokaprilata, polioksil ricinusovog ulja i propilen glikola u tekućem nosaču.
9. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što ima sadržaj antagonista BK B2 receptora u rasponu od 5 mg do 100 mg po g, kao što je od 5 mg do 65 mg po g, ili kao što je od 20 mg do 70 mg po g tekućeg farmaceutskog pripravka.
10. Tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva, naznačen time što uglavnom sadrži:
(a) temeljeno na ukupnoj težini tekućeg farmaceutskog pripravka, 0,5 do 6,5 tež.%, kao što je 5 tež.%, spoja u skladu s Formulom 1, ili njegovog stereoizomera, soli ili solvata, pri čemu je R deuterij;
(b) temeljeno na ukupnoj težini tekućeg farmaceutskog pripravka, 93,5 do 99,5 tež.% tekućeg nosača, pri čemu navedeni tekući nosač uglavnom sadrži:
(i) 50 dijelova (težinski) propilen glikol monokaprilata, kao što je propilen glikol monokaprilat tipa II (USP/NF);
(ii) 40 dijelova (težinski) polioksilnog ricinusovog ulja, kao što je 40 udjela hidrogeniranog ricinusovog ulja (USP/NF);
(iii) 5 do 10 dijelova (težinski) propilen glikola; i izborno (iv) do 5 dijelova (težinski) vode;
i izborno
(c) ostatak je jedna ili više dodatnih pomoćnih tvari otopljenih ili raspršenih u tekućem nosaču.
11. Kapsula za oralnu primjenu, naznačena time što sadrži tekući farmaceutski pripravak prema bilo kojem od prethodnih zahtjeva.
12. Kapsula prema zahtjevu 11, naznačena time što je kapsula meka kapsula.
13. Meka kapsula prema zahtjevu 12, naznačena time što sadrži stijenku kapsule koja sadrži želatinu, vodu i najmanje jedan plastifikator odabran između propilen glikola, glicerola, sorbitola, sorbitana, smjesa plastifikatora na bazi sorbitola, ili bilo koje njihove kombinacije.
14. Tekući farmaceutski pripravak prema bilo kojem od zahtjeva 1 do 10, ili kapsula prema bilo kojem od zahtjeva 11 do 13, za upotrebu u akutnom ili kroničnom liječenju subjekta koji pati od bolesti ili stanja koje reagira na modulaciju BK B2 receptora.
15. Tekući farmaceutski pripravak za upotrebu prema zahtjevu 14, ili kapsula za upotrebu prema zahtjevu 14, naznačena time što je bolest ili stanje koje reagira na modulaciju BK B2 receptora edem, kao što je nasljedni angioedem.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP21189990 | 2021-08-05 | ||
PCT/EP2022/072049 WO2023012322A1 (en) | 2021-08-05 | 2022-08-05 | Lipid-based composition for oral administration of bradykinin b2-receptor antagonists |
EP22760986.4A EP4203919B1 (en) | 2021-08-05 | 2022-08-05 | Lipid-based composition for oral administration of bradykinin b2-receptor antagonists |
Publications (1)
Publication Number | Publication Date |
---|---|
HRP20240525T1 true HRP20240525T1 (hr) | 2024-07-05 |
Family
ID=77226756
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HRP20240525TT HRP20240525T1 (hr) | 2021-08-05 | 2022-08-05 | Pripravak na bazi lipida za oralnu primjenu antagonista bradikininskog b2-receptora |
Country Status (23)
Country | Link |
---|---|
US (1) | US20240350418A1 (hr) |
EP (1) | EP4203919B1 (hr) |
JP (1) | JP2024528195A (hr) |
KR (1) | KR20240039185A (hr) |
CN (1) | CN118076342A (hr) |
AU (1) | AU2022323749A1 (hr) |
BR (1) | BR112024002215A2 (hr) |
CA (1) | CA3227476A1 (hr) |
CO (1) | CO2024001171A2 (hr) |
DK (1) | DK4203919T3 (hr) |
ES (1) | ES2978563T3 (hr) |
FI (1) | FI4203919T3 (hr) |
HR (1) | HRP20240525T1 (hr) |
HU (1) | HUE066306T2 (hr) |
IL (1) | IL310321A (hr) |
LT (1) | LT4203919T (hr) |
MX (1) | MX2024001711A (hr) |
PL (1) | PL4203919T3 (hr) |
PT (1) | PT4203919T (hr) |
RS (1) | RS65427B1 (hr) |
SI (1) | SI4203919T1 (hr) |
TW (1) | TW202320774A (hr) |
WO (1) | WO2023012322A1 (hr) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN117224522B (zh) * | 2023-11-15 | 2024-02-23 | 北京协和药厂有限公司 | 药物组合物及其制备方法、药物制剂 |
Family Cites Families (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ES2218554T3 (es) | 1994-10-27 | 2004-11-16 | Fujisawa Pharmaceutical Co., Ltd. | Piridopirimidonas, quinolinas y n-heterociclos condensados que son antagonistas de bradiquinina. |
FR2737892B1 (fr) | 1995-08-17 | 1997-10-24 | Fournier Ind & Sante | Nouveaux composes de benzenesulfonamide, procede de preparation et utilisation en therapeutique |
GB9602029D0 (en) | 1996-02-01 | 1996-04-03 | Fujisawa Pharmaceutical Co | New heterocyclic compounds |
DE19609827A1 (de) | 1996-03-13 | 1997-09-18 | Hoechst Ag | Aminoalkyl- und Acylaminoalkylether, Verfahren zu deren Herstellung und ihre Verwendung als Bradykinin-Rezeptorantagonisten |
DE19610784A1 (de) | 1996-03-19 | 1997-09-25 | Hoechst Ag | Fluoralkyl- und Fluoralkoxysubstituierte heterocyclische Bradykinin-Antagonisten, Verfahren zu ihrer Herstellung und ihre Verwendung |
AUPN952696A0 (en) | 1996-04-29 | 1996-05-23 | Fujisawa Pharmaceutical Co., Ltd. | New heterocyclic compounds |
DE19712960A1 (de) | 1997-03-27 | 1998-10-01 | Hoechst Ag | Benzyloxy-substituierte, anellierte N-Heterocyclen, Verfahren zu ihrer Herstellung und ihre Verwendung als Bradykininrezeptorantagonisten |
CA2319730A1 (en) | 1998-06-08 | 1999-12-16 | Advanced Medicine, Inc. | Bradykinin antagonists |
CA2364178C (en) | 2000-12-05 | 2006-01-10 | Yasuhiro Katsu | N-benzenesulfonyl l-proline compounds as bradykinin antagonists |
TW200824686A (en) * | 2006-10-31 | 2008-06-16 | Wyeth Corp | Formulations of phospholipase enzyme inhibitors |
TWI407960B (zh) | 2007-03-23 | 2013-09-11 | Jerini Ag | 小分子緩激肽b2受體調節劑 |
AR073304A1 (es) | 2008-09-22 | 2010-10-28 | Jerini Ag | Moduladores del receptor de bradiquinina b2 de molecula pequena |
MX2015012650A (es) | 2013-03-14 | 2016-06-21 | Shire Human Genetic Therapies | Metodos para el tratamiento de angioedema mediado receptores debradicinina b2. |
CN111433196B (zh) | 2017-11-24 | 2023-06-06 | 法瓦里斯荷兰有限责任公司 | 缓激肽b2受体拮抗剂及其用途 |
-
2022
- 2022-08-05 MX MX2024001711A patent/MX2024001711A/es unknown
- 2022-08-05 PL PL22760986.4T patent/PL4203919T3/pl unknown
- 2022-08-05 HU HUE22760986A patent/HUE066306T2/hu unknown
- 2022-08-05 WO PCT/EP2022/072049 patent/WO2023012322A1/en active Application Filing
- 2022-08-05 EP EP22760986.4A patent/EP4203919B1/en active Active
- 2022-08-05 AU AU2022323749A patent/AU2022323749A1/en active Pending
- 2022-08-05 BR BR112024002215A patent/BR112024002215A2/pt unknown
- 2022-08-05 ES ES22760986T patent/ES2978563T3/es active Active
- 2022-08-05 JP JP2024506610A patent/JP2024528195A/ja active Pending
- 2022-08-05 RS RS20240456A patent/RS65427B1/sr unknown
- 2022-08-05 DK DK22760986.4T patent/DK4203919T3/da active
- 2022-08-05 KR KR1020247007280A patent/KR20240039185A/ko unknown
- 2022-08-05 CN CN202280067108.5A patent/CN118076342A/zh active Pending
- 2022-08-05 US US18/681,298 patent/US20240350418A1/en active Pending
- 2022-08-05 SI SI202230031T patent/SI4203919T1/sl unknown
- 2022-08-05 FI FIEP22760986.4T patent/FI4203919T3/fi active
- 2022-08-05 TW TW111129507A patent/TW202320774A/zh unknown
- 2022-08-05 IL IL310321A patent/IL310321A/en unknown
- 2022-08-05 PT PT227609864T patent/PT4203919T/pt unknown
- 2022-08-05 HR HRP20240525TT patent/HRP20240525T1/hr unknown
- 2022-08-05 CA CA3227476A patent/CA3227476A1/en active Pending
- 2022-08-05 LT LTEPPCT/EP2022/072049T patent/LT4203919T/lt unknown
-
2024
- 2024-02-05 CO CONC2024/0001171A patent/CO2024001171A2/es unknown
Also Published As
Publication number | Publication date |
---|---|
FI4203919T3 (fi) | 2024-05-03 |
CA3227476A1 (en) | 2023-02-09 |
CN118076342A (zh) | 2024-05-24 |
MX2024001711A (es) | 2024-03-05 |
KR20240039185A (ko) | 2024-03-26 |
EP4203919B1 (en) | 2024-01-31 |
LT4203919T (lt) | 2024-05-10 |
EP4203919A1 (en) | 2023-07-05 |
IL310321A (en) | 2024-03-01 |
TW202320774A (zh) | 2023-06-01 |
PL4203919T3 (pl) | 2024-06-10 |
WO2023012322A1 (en) | 2023-02-09 |
CO2024001171A2 (es) | 2024-05-20 |
RS65427B1 (sr) | 2024-05-31 |
BR112024002215A2 (pt) | 2024-04-30 |
ES2978563T3 (es) | 2024-09-16 |
SI4203919T1 (sl) | 2024-08-30 |
PT4203919T (pt) | 2024-04-23 |
AU2022323749A1 (en) | 2024-02-08 |
US20240350418A1 (en) | 2024-10-24 |
HUE066306T2 (hu) | 2024-07-28 |
DK4203919T3 (da) | 2024-04-29 |
JP2024528195A (ja) | 2024-07-26 |
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