JP4878839B2 - ゲル安定化ナノパーティクル活性物質組成物 - Google Patents
ゲル安定化ナノパーティクル活性物質組成物 Download PDFInfo
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- JP4878839B2 JP4878839B2 JP2005503259A JP2005503259A JP4878839B2 JP 4878839 B2 JP4878839 B2 JP 4878839B2 JP 2005503259 A JP2005503259 A JP 2005503259A JP 2005503259 A JP2005503259 A JP 2005503259A JP 4878839 B2 JP4878839 B2 JP 4878839B2
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- gelatin
- chloride
- active substance
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- 239000013543 active substance Substances 0.000 title claims abstract description 288
- 239000000203 mixture Substances 0.000 title claims description 325
- 239000002105 nanoparticle Substances 0.000 title claims description 148
- 229920000159 gelatin Polymers 0.000 claims abstract description 232
- 235000019322 gelatine Nutrition 0.000 claims abstract description 232
- 108010010803 Gelatin Proteins 0.000 claims abstract description 231
- 235000011852 gelatine desserts Nutrition 0.000 claims abstract description 231
- 239000008273 gelatin Substances 0.000 claims abstract description 230
- 239000002245 particle Substances 0.000 claims abstract description 163
- 239000002552 dosage form Substances 0.000 claims abstract description 133
- 239000007787 solid Substances 0.000 claims abstract description 96
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 65
- 239000000126 substance Substances 0.000 claims abstract description 31
- 239000000499 gel Substances 0.000 claims abstract description 19
- 238000001879 gelation Methods 0.000 claims abstract description 8
- 229940014259 gelatin Drugs 0.000 claims description 228
- 238000009472 formulation Methods 0.000 claims description 134
- 239000003381 stabilizer Substances 0.000 claims description 81
- DKYWVDODHFEZIM-UHFFFAOYSA-N ketoprofen Chemical compound OC(=O)C(C)C1=CC=CC(C(=O)C=2C=CC=CC=2)=C1 DKYWVDODHFEZIM-UHFFFAOYSA-N 0.000 claims description 79
- 229960000991 ketoprofen Drugs 0.000 claims description 79
- -1 antibiotic Substances 0.000 claims description 58
- 239000003814 drug Substances 0.000 claims description 57
- 238000000034 method Methods 0.000 claims description 55
- 229940079593 drug Drugs 0.000 claims description 46
- CMWTZPSULFXXJA-UHFFFAOYSA-N Naproxen Natural products C1=C(C(C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-UHFFFAOYSA-N 0.000 claims description 29
- 229960002009 naproxen Drugs 0.000 claims description 29
- CMWTZPSULFXXJA-VIFPVBQESA-N naproxen Chemical compound C1=C([C@H](C)C(O)=O)C=CC2=CC(OC)=CC=C21 CMWTZPSULFXXJA-VIFPVBQESA-N 0.000 claims description 29
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- 239000002872 contrast media Substances 0.000 claims description 19
- 125000002091 cationic group Chemical group 0.000 claims description 17
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- 239000011159 matrix material Substances 0.000 claims description 17
- 239000007909 solid dosage form Substances 0.000 claims description 17
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 16
- 235000015872 dietary supplement Nutrition 0.000 claims description 16
- 238000004519 manufacturing process Methods 0.000 claims description 16
- 239000000463 material Substances 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 16
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 15
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 15
- 230000008569 process Effects 0.000 claims description 15
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 14
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 12
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 12
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- 229960000878 docusate sodium Drugs 0.000 claims description 11
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- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical compound [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 claims description 11
- CADWTSSKOVRVJC-UHFFFAOYSA-N benzyl(dimethyl)azanium;chloride Chemical compound [Cl-].C[NH+](C)CC1=CC=CC=C1 CADWTSSKOVRVJC-UHFFFAOYSA-N 0.000 claims description 10
- 238000010521 absorption reaction Methods 0.000 claims description 9
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims description 9
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- 229920001223 polyethylene glycol Polymers 0.000 claims description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims description 7
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 7
- 239000002202 Polyethylene glycol Substances 0.000 claims description 7
- 235000019441 ethanol Nutrition 0.000 claims description 7
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims description 6
- 229960000686 benzalkonium chloride Drugs 0.000 claims description 6
- 235000010980 cellulose Nutrition 0.000 claims description 6
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- 235000014113 dietary fatty acids Nutrition 0.000 claims description 6
- 239000000194 fatty acid Substances 0.000 claims description 6
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- 229960003174 lansoprazole Drugs 0.000 claims description 6
- MJIHNNLFOKEZEW-UHFFFAOYSA-N lansoprazole Chemical compound CC1=C(OCC(F)(F)F)C=CN=C1CS(=O)C1=NC2=CC=CC=C2N1 MJIHNNLFOKEZEW-UHFFFAOYSA-N 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- 239000008299 semisolid dosage form Substances 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- NLXLAEXVIDQMFP-UHFFFAOYSA-N Ammonia chloride Chemical compound [NH4+].[Cl-] NLXLAEXVIDQMFP-UHFFFAOYSA-N 0.000 claims description 5
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- 229910019142 PO4 Inorganic materials 0.000 claims description 5
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 5
- 235000010443 alginic acid Nutrition 0.000 claims description 5
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- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 5
- 239000010452 phosphate Substances 0.000 claims description 5
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 5
- 150000003904 phospholipids Chemical class 0.000 claims description 5
- AISMNBXOJRHCIA-UHFFFAOYSA-N trimethylazanium;bromide Chemical compound Br.CN(C)C AISMNBXOJRHCIA-UHFFFAOYSA-N 0.000 claims description 5
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 4
- YJHSJERLYWNLQL-UHFFFAOYSA-N 2-hydroxyethyl(dimethyl)azanium;chloride Chemical compound Cl.CN(C)CCO YJHSJERLYWNLQL-UHFFFAOYSA-N 0.000 claims description 4
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims description 4
- 244000215068 Acacia senegal Species 0.000 claims description 4
- 241000416162 Astragalus gummifer Species 0.000 claims description 4
- 229920000084 Gum arabic Polymers 0.000 claims description 4
- 229920001615 Tragacanth Polymers 0.000 claims description 4
- XTXRWKRVRITETP-UHFFFAOYSA-N Vinyl acetate Chemical compound CC(=O)OC=C XTXRWKRVRITETP-UHFFFAOYSA-N 0.000 claims description 4
- 235000010489 acacia gum Nutrition 0.000 claims description 4
- 239000000205 acacia gum Substances 0.000 claims description 4
- 229940072056 alginate Drugs 0.000 claims description 4
- 150000001412 amines Chemical class 0.000 claims description 4
- JBIROUFYLSSYDX-UHFFFAOYSA-M benzododecinium chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)CC1=CC=CC=C1 JBIROUFYLSSYDX-UHFFFAOYSA-M 0.000 claims description 4
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 claims description 4
- 229940107161 cholesterol Drugs 0.000 claims description 4
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims description 4
- MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 claims description 4
- WHBIGIKBNXZKFE-UHFFFAOYSA-N delavirdine Chemical compound CC(C)NC1=CC=CN=C1N1CCN(C(=O)C=2NC3=CC=C(NS(C)(=O)=O)C=C3C=2)CC1 WHBIGIKBNXZKFE-UHFFFAOYSA-N 0.000 claims description 4
- DDXLVDQZPFLQMZ-UHFFFAOYSA-M dodecyl(trimethyl)azanium;chloride Chemical compound [Cl-].CCCCCCCCCCCC[N+](C)(C)C DDXLVDQZPFLQMZ-UHFFFAOYSA-M 0.000 claims description 4
- 235000013399 edible fruits Nutrition 0.000 claims description 4
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- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims description 4
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- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 4
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- HICYUNOFRYFIMG-UHFFFAOYSA-N n,n-dimethyl-1-naphthalen-1-ylmethanamine;hydrochloride Chemical compound [Cl-].C1=CC=C2C(C[NH+](C)C)=CC=CC2=C1 HICYUNOFRYFIMG-UHFFFAOYSA-N 0.000 claims description 4
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- 102000004169 proteins and genes Human genes 0.000 claims description 4
- 108090000623 proteins and genes Proteins 0.000 claims description 4
- BNRNXUUZRGQAQC-UHFFFAOYSA-N sildenafil Chemical compound CCCC1=NN(C)C(C(N2)=O)=C1N=C2C(C(=CC=1)OCC)=CC=1S(=O)(=O)N1CCN(C)CC1 BNRNXUUZRGQAQC-UHFFFAOYSA-N 0.000 claims description 4
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- KGIGUEBEKRSTEW-UHFFFAOYSA-N 2-vinylpyridine Chemical compound C=CC1=CC=CC=N1 KGIGUEBEKRSTEW-UHFFFAOYSA-N 0.000 claims description 3
- HRPVXLWXLXDGHG-UHFFFAOYSA-N Acrylamide Chemical compound NC(=O)C=C HRPVXLWXLXDGHG-UHFFFAOYSA-N 0.000 claims description 3
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims description 3
- 229920001661 Chitosan Polymers 0.000 claims description 3
- IAYPIBMASNFSPL-UHFFFAOYSA-N Ethylene oxide Chemical compound C1CO1 IAYPIBMASNFSPL-UHFFFAOYSA-N 0.000 claims description 3
- 241000282412 Homo Species 0.000 claims description 3
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- 235000019485 Safflower oil Nutrition 0.000 claims description 3
- 235000021355 Stearic acid Nutrition 0.000 claims description 3
- NJSSICCENMLTKO-HRCBOCMUSA-N [(1r,2s,4r,5r)-3-hydroxy-4-(4-methylphenyl)sulfonyloxy-6,8-dioxabicyclo[3.2.1]octan-2-yl] 4-methylbenzenesulfonate Chemical compound C1=CC(C)=CC=C1S(=O)(=O)O[C@H]1C(O)[C@@H](OS(=O)(=O)C=2C=CC(C)=CC=2)[C@@H]2OC[C@H]1O2 NJSSICCENMLTKO-HRCBOCMUSA-N 0.000 claims description 3
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- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims description 3
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Images
Classifications
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0087—Galenical forms not covered by A61K9/02 - A61K9/7023
- A61K9/0095—Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches
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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
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
- A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
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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
- A61K9/141—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
- A61K9/146—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 macromolecular compounds
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- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Physiology (AREA)
- Nutrition Science (AREA)
- Zoology (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Yarns And Mechanical Finishing Of Yarns Or Ropes (AREA)
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| US60/409,587 | 2002-09-11 | ||
| PCT/US2003/028380 WO2005000265A2 (en) | 2002-09-11 | 2003-09-11 | Gel-stabilized nanoparticulate active agent compositions |
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| JP2006514688A JP2006514688A (ja) | 2006-05-11 |
| JP2006514688A5 JP2006514688A5 (enExample) | 2010-09-16 |
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- 2003-09-11 DK DK03816299.6T patent/DK1553927T3/da active
- 2003-09-11 DE DE60334924T patent/DE60334924D1/de not_active Expired - Lifetime
- 2003-09-11 EP EP03816299A patent/EP1553927B9/en not_active Expired - Lifetime
- 2003-09-11 WO PCT/US2003/028380 patent/WO2005000265A2/en not_active Ceased
- 2003-09-11 AT AT03816299T patent/ATE487470T1/de active
- 2003-09-11 AU AU2003304237A patent/AU2003304237A1/en not_active Abandoned
- 2003-09-11 PT PT03816299T patent/PT1553927E/pt unknown
- 2003-09-11 SI SI200331901T patent/SI1553927T1/sl unknown
- 2003-09-11 US US10/659,706 patent/US7713551B2/en not_active Expired - Lifetime
- 2003-09-11 JP JP2005503259A patent/JP4878839B2/ja not_active Expired - Fee Related
- 2003-09-11 ES ES03816299T patent/ES2355723T3/es not_active Expired - Lifetime
- 2003-09-11 CA CA2498207A patent/CA2498207C/en not_active Expired - Fee Related
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- 2010-11-26 CY CY20101101084T patent/CY1110949T1/el unknown
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Also Published As
| Publication number | Publication date |
|---|---|
| ES2355723T3 (es) | 2011-03-30 |
| DE60334924D1 (de) | 2010-12-23 |
| WO2005000265A2 (en) | 2005-01-06 |
| AU2003304237A1 (en) | 2005-01-13 |
| EP1553927B9 (en) | 2011-09-21 |
| AU2003304237A8 (en) | 2005-01-13 |
| US7713551B2 (en) | 2010-05-11 |
| WO2005000265A3 (en) | 2005-05-12 |
| JP2006514688A (ja) | 2006-05-11 |
| CY1110949T1 (el) | 2015-06-10 |
| DK1553927T3 (da) | 2011-01-31 |
| ATE487470T1 (de) | 2010-11-15 |
| EP1553927A2 (en) | 2005-07-20 |
| US20050031691A1 (en) | 2005-02-10 |
| CA2498207A1 (en) | 2005-01-06 |
| EP1553927B1 (en) | 2010-11-10 |
| PT1553927E (pt) | 2010-11-22 |
| CA2498207C (en) | 2012-03-13 |
| SI1553927T1 (sl) | 2010-12-31 |
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