KR20130076818A - 약학 조성물 - Google Patents
약학 조성물 Download PDFInfo
- Publication number
- KR20130076818A KR20130076818A KR1020127030186A KR20127030186A KR20130076818A KR 20130076818 A KR20130076818 A KR 20130076818A KR 1020127030186 A KR1020127030186 A KR 1020127030186A KR 20127030186 A KR20127030186 A KR 20127030186A KR 20130076818 A KR20130076818 A KR 20130076818A
- Authority
- KR
- South Korea
- Prior art keywords
- sodium
- composition
- particles
- surfactant
- particle size
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Ceased
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 22
- 239000000203 mixture Substances 0.000 claims description 70
- 238000000034 method Methods 0.000 claims description 47
- 239000002245 particle Substances 0.000 claims description 45
- 239000003814 drug Substances 0.000 claims description 37
- -1 brij Chemical compound 0.000 claims description 35
- 229920000642 polymer Polymers 0.000 claims description 26
- 238000009472 formulation Methods 0.000 claims description 16
- 239000008187 granular material Substances 0.000 claims description 16
- 239000004094 surface-active agent Substances 0.000 claims description 15
- 239000003381 stabilizer Substances 0.000 claims description 14
- 229930006000 Sucrose Natural products 0.000 claims description 13
- 239000006185 dispersion Substances 0.000 claims description 13
- 229910052757 nitrogen Inorganic materials 0.000 claims description 13
- 239000002002 slurry Substances 0.000 claims description 13
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 13
- 229960004793 sucrose Drugs 0.000 claims description 13
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 12
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 12
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 12
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 12
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 12
- 239000002562 thickening agent Substances 0.000 claims description 12
- 229920003171 Poly (ethylene oxide) Chemical class 0.000 claims description 11
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims description 11
- GUBGYTABKSRVRQ-QKKXKWKRSA-N lactose group Chemical group OC1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@H](O)[C@@H](O)[C@@H](O)[C@H](O2)CO)[C@H](O1)CO GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims description 11
- LZZYPRNAOMGNLH-UHFFFAOYSA-M Cetrimonium bromide Chemical compound [Br-].CCCCCCCCCCCCCCCC[N+](C)(C)C LZZYPRNAOMGNLH-UHFFFAOYSA-M 0.000 claims description 9
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 9
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 9
- 229960001375 lactose Drugs 0.000 claims description 9
- 239000008101 lactose Substances 0.000 claims description 9
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 9
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 9
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 9
- 239000005720 sucrose Substances 0.000 claims description 9
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 8
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 8
- 238000011282 treatment Methods 0.000 claims description 8
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 7
- 229920002472 Starch Polymers 0.000 claims description 7
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 7
- 229960001021 lactose monohydrate Drugs 0.000 claims description 7
- 229920001223 polyethylene glycol Chemical class 0.000 claims description 7
- 235000019698 starch Nutrition 0.000 claims description 7
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims description 6
- 229920002675 Polyoxyl Polymers 0.000 claims description 6
- 239000011230 binding agent Substances 0.000 claims description 6
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 6
- 229960000913 crospovidone Drugs 0.000 claims description 6
- 235000014113 dietary fatty acids Nutrition 0.000 claims description 6
- 239000007884 disintegrant Substances 0.000 claims description 6
- SYELZBGXAIXKHU-UHFFFAOYSA-N dodecyldimethylamine N-oxide Chemical compound CCCCCCCCCCCC[N+](C)(C)[O-] SYELZBGXAIXKHU-UHFFFAOYSA-N 0.000 claims description 6
- 150000002148 esters Chemical class 0.000 claims description 6
- 239000000194 fatty acid Substances 0.000 claims description 6
- 229930195729 fatty acid Natural products 0.000 claims description 6
- 150000004665 fatty acids Chemical class 0.000 claims description 6
- 150000002334 glycols Chemical class 0.000 claims description 6
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims description 6
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims description 6
- 239000011734 sodium Substances 0.000 claims description 6
- 229910052708 sodium Inorganic materials 0.000 claims description 6
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims description 6
- 229920000858 Cyclodextrin Polymers 0.000 claims description 5
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 5
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 5
- 239000000945 filler Substances 0.000 claims description 5
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 5
- 229920000609 methyl cellulose Polymers 0.000 claims description 5
- 235000010981 methylcellulose Nutrition 0.000 claims description 5
- 239000001923 methylcellulose Substances 0.000 claims description 5
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 5
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- 239000008107 starch Substances 0.000 claims description 5
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound 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 description 4
- 239000005913 Maltodextrin Substances 0.000 claims description 4
- 229920002774 Maltodextrin Polymers 0.000 claims description 4
- 239000002202 Polyethylene glycol Chemical class 0.000 claims description 4
- 229920003090 carboxymethyl hydroxyethyl cellulose Polymers 0.000 claims description 4
- 239000004359 castor oil Substances 0.000 claims description 4
- 235000019438 castor oil Nutrition 0.000 claims description 4
- 125000002091 cationic group Chemical group 0.000 claims description 4
- 229940097362 cyclodextrins Drugs 0.000 claims description 4
- 235000013681 dietary sucrose Nutrition 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 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 description 4
- 235000010445 lecithin Nutrition 0.000 claims description 4
- 239000000787 lecithin Substances 0.000 claims description 4
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- 229940035034 maltodextrin Drugs 0.000 claims description 4
- 230000008569 process Effects 0.000 claims description 4
- CMCBDXRRFKYBDG-UHFFFAOYSA-N 1-dodecoxydodecane Chemical compound CCCCCCCCCCCCOCCCCCCCCCCCC CMCBDXRRFKYBDG-UHFFFAOYSA-N 0.000 claims description 3
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims description 3
- IEORSVTYLWZQJQ-UHFFFAOYSA-N 2-(2-nonylphenoxy)ethanol Chemical compound CCCCCCCCCC1=CC=CC=C1OCCO IEORSVTYLWZQJQ-UHFFFAOYSA-N 0.000 claims description 3
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-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
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical class NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims description 3
- QXNVGIXVLWOKEQ-UHFFFAOYSA-N Disodium Chemical class [Na][Na] QXNVGIXVLWOKEQ-UHFFFAOYSA-N 0.000 claims description 3
- PIICEJLVQHRZGT-UHFFFAOYSA-N Ethylenediamine Chemical class NCCN PIICEJLVQHRZGT-UHFFFAOYSA-N 0.000 claims description 3
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 3
- 150000001298 alcohols Chemical class 0.000 claims description 3
- 150000001412 amines Chemical class 0.000 claims description 3
- 239000000908 ammonium hydroxide Substances 0.000 claims description 3
- 239000003833 bile salt Substances 0.000 claims description 3
- 229940093761 bile salts Drugs 0.000 claims description 3
- 125000003178 carboxy group Chemical class [H]OC(*)=O 0.000 claims description 3
- 150000007942 carboxylates Chemical class 0.000 claims description 3
- 229920001577 copolymer Polymers 0.000 claims description 3
- 229960003964 deoxycholic acid Drugs 0.000 claims description 3
- 239000003937 drug carrier Substances 0.000 claims description 3
- 238000000227 grinding Methods 0.000 claims description 3
- 229920003063 hydroxymethyl cellulose Polymers 0.000 claims description 3
- 229940031574 hydroxymethyl cellulose Drugs 0.000 claims description 3
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims description 3
- 229920000847 nonoxynol Polymers 0.000 claims description 3
- 229920002113 octoxynol Polymers 0.000 claims description 3
- 229940066429 octoxynol Drugs 0.000 claims description 3
- 239000003921 oil Substances 0.000 claims description 3
- JRZJOMJEPLMPRA-UHFFFAOYSA-N olefin Natural products CCCCCCCC=C JRZJOMJEPLMPRA-UHFFFAOYSA-N 0.000 claims description 3
- NFHFRUOZVGFOOS-UHFFFAOYSA-N palladium;triphenylphosphane Chemical group [Pd].C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1.C1=CC=CC=C1P(C=1C=CC=CC=1)C1=CC=CC=C1 NFHFRUOZVGFOOS-UHFFFAOYSA-N 0.000 claims description 3
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- 229920000136 polysorbate Polymers 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 150000003242 quaternary ammonium salts Chemical class 0.000 claims description 3
- NRHMKIHPTBHXPF-TUJRSCDTSA-M sodium cholate Chemical compound [Na+].C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 NRHMKIHPTBHXPF-TUJRSCDTSA-M 0.000 claims description 3
- FHHPUSMSKHSNKW-SMOYURAASA-M sodium deoxycholate Chemical compound [Na+].C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 FHHPUSMSKHSNKW-SMOYURAASA-M 0.000 claims description 3
- 159000000000 sodium salts Chemical class 0.000 claims description 3
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- 235000019329 dioctyl sodium sulphosuccinate Nutrition 0.000 claims 3
- 229960000878 docusate sodium Drugs 0.000 claims 3
- 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 3
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- 150000003973 alkyl amines Chemical class 0.000 claims 2
- 239000002280 amphoteric surfactant Substances 0.000 claims 2
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- 239000003925 fat Substances 0.000 claims 2
- PSZYNBSKGUBXEH-UHFFFAOYSA-M naphthalene-1-sulfonate Chemical compound C1=CC=C2C(S(=O)(=O)[O-])=CC=CC2=C1 PSZYNBSKGUBXEH-UHFFFAOYSA-M 0.000 claims 2
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| US10646452B2 (en) * | 2013-03-15 | 2020-05-12 | New Jersey Institute Of Technology | System and method for fabrication of uniform polymer films containing nano and micro particles via continuous drying process |
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| WO2015071841A1 (en) | 2013-11-12 | 2015-05-21 | Druggability Technologies Holdings Limited | Complexes of dabigatran and its derivatives, process for the preparation thereof and pharmaceutical compositions containing them |
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| AU2017364077A1 (en) | 2016-11-22 | 2019-06-20 | Elektrofi, Inc. | Particles comprising a therapeutic or diagnostic agent and suspensions and methods of use thereof |
| AU2018306303A1 (en) * | 2017-07-25 | 2020-02-20 | Elektrofi, Inc. | Formation of particles including agents |
| US20230040901A1 (en) * | 2018-01-04 | 2023-02-09 | PlantTec Medical GmbH | Pharmaceutical composition for inhibiting postoperative adhesions |
| ES2732498B2 (es) * | 2018-05-21 | 2020-04-27 | Consejo Superior Investigacion | Uso de efavirenz para el tratamiento de enfermedades de almacenamiento lipidico. |
| US12115262B2 (en) | 2018-05-24 | 2024-10-15 | Elektrofi, Inc. | Particles comprising a therapeutic or diagnostic agent and suspensions and methods of use thereof |
| CN112236141A (zh) * | 2018-06-11 | 2021-01-15 | 大塚制药株式会社 | 包含德拉马尼的组合物 |
| AU2020214626B2 (en) | 2019-01-31 | 2025-10-16 | Elektrofi, Inc. | Particle formation and morphology |
| JP7781743B2 (ja) | 2019-09-13 | 2025-12-08 | エレクトロフィ,インコーポレイテッド | 疾患の処置のための治療用生物学的作用剤の送達のための組成物及び方法 |
| WO2021110697A1 (en) * | 2019-12-02 | 2021-06-10 | Astrazeneca Ab | Solid pharmaceutical formulations of 6-(2-chloro-6-methylpyridin-4-yl)-5-(-4-fluorophenyl)-1,2,4-triazin-3-amine |
| JP2023522627A (ja) | 2020-04-17 | 2023-05-31 | エレクトロフィ,インコーポレイテッド | 連続的な液滴形成及び脱水によって粒子を形成する方法 |
| WO2021216475A1 (en) * | 2020-04-20 | 2021-10-28 | Poviva Corp. | Compositions and methods for enhanced delivery of antiviral agents |
| CN112245400B (zh) * | 2020-11-10 | 2023-01-20 | 蓝龙药业(北京)有限公司 | 一种依法韦仑微片剂、制备方法及其应用 |
| CN114404377B (zh) * | 2022-01-10 | 2023-07-25 | 安徽贝克生物制药有限公司 | 一种阿巴卡韦、拉米夫定、依非韦伦复方片及其制备方法 |
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| UA72207C2 (uk) | 1998-04-07 | 2005-02-15 | Брістол- Майєрс Сквібб Фарма Компані | Фармацевтична композиція ефавіренцу з добавкою дезінтегруючих агентів у вигляді швидкорозчинних капсул або таблеток та спосіб її виготовлення |
| EP1332757B1 (en) * | 1998-05-27 | 2012-06-13 | Merck Sharp & Dohme Corp. | Efavirenz compressed tablet formulation |
| CO5070643A1 (es) | 1998-05-27 | 2001-08-28 | Merck & Co Inc | Formulacion en tabletas comprimidas |
| WO2003045327A2 (en) * | 2001-11-27 | 2003-06-05 | Bristol-Myers Squibb Company | Efavirenz tablet formulation having unique biopharmaceutical characteristics |
| WO2007002823A2 (en) * | 2005-06-29 | 2007-01-04 | Wyeth | Formulations of conjugated estrogens and bazedoxifene |
| US20080026062A1 (en) * | 2006-07-31 | 2008-01-31 | Isaac Farr | Pharmaceutical compositions including nano-sized active agent |
| TWI405590B (zh) * | 2007-04-06 | 2013-08-21 | Activus Pharma Co Ltd | 微粉碎化有機化合物粒子之製法 |
| EP2076248A2 (en) * | 2007-08-17 | 2009-07-08 | Teva Pharmaceutical Industries Ltd. | Methods and compositions for controlling the bioavailability of poorly soluble drugs |
| JP4606444B2 (ja) * | 2007-08-21 | 2011-01-05 | アピ株式会社 | アントシアニン含有経口投与用組成物及びその製造方法 |
| US8846096B2 (en) * | 2008-12-12 | 2014-09-30 | Creighton University | Nanoparticles and methods of use |
| US10952965B2 (en) * | 2009-05-15 | 2021-03-23 | Baxter International Inc. | Compositions and methods for drug delivery |
| GB201006038D0 (en) * | 2010-04-12 | 2010-05-26 | Unilever Plc | Improvements relating to antiviral compositions |
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2011
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- 2011-04-20 JP JP2013505533A patent/JP2013525337A/ja active Pending
- 2011-04-20 KR KR1020127030186A patent/KR20130076818A/ko not_active Ceased
- 2011-04-20 EP EP11716002A patent/EP2560617A2/en not_active Withdrawn
- 2011-04-20 RU RU2012149115/15A patent/RU2012149115A/ru not_active Application Discontinuation
- 2011-04-20 NZ NZ602955A patent/NZ602955A/en not_active IP Right Cessation
- 2011-04-20 WO PCT/GB2011/000620 patent/WO2011131943A2/en not_active Ceased
- 2011-04-20 CN CN2011800201397A patent/CN102985072A/zh active Pending
- 2011-04-20 CA CA2796494A patent/CA2796494A1/en not_active Abandoned
- 2011-04-20 BR BR112012026843A patent/BR112012026843A2/pt not_active IP Right Cessation
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2012
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- 2012-10-18 GT GT201200284A patent/GT201200284A/es unknown
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2013
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| WO2011131943A8 (en) | 2012-11-29 |
| GT201200284A (es) | 2014-08-26 |
| CN102985072A (zh) | 2013-03-20 |
| EP2560617A2 (en) | 2013-02-27 |
| ZA201207670B (en) | 2013-05-29 |
| WO2011131943A3 (en) | 2011-12-29 |
| NZ602955A (en) | 2015-02-27 |
| AU2011244783B2 (en) | 2015-11-12 |
| AU2011244783A1 (en) | 2012-11-01 |
| JP2013525337A (ja) | 2013-06-20 |
| RU2012149115A (ru) | 2014-05-27 |
| US20130302415A1 (en) | 2013-11-14 |
| BR112012026843A2 (pt) | 2016-07-12 |
| CA2796494A1 (en) | 2011-10-27 |
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