TW201206908A - Pharmaceutical compositions and methods of making same - Google Patents
Pharmaceutical compositions and methods of making same Download PDFInfo
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- TW201206908A TW201206908A TW100115488A TW100115488A TW201206908A TW 201206908 A TW201206908 A TW 201206908A TW 100115488 A TW100115488 A TW 100115488A TW 100115488 A TW100115488 A TW 100115488A TW 201206908 A TW201206908 A TW 201206908A
- Authority
- TW
- Taiwan
- Prior art keywords
- pharmaceutical composition
- cyclodextrin
- composition
- modified cyclodextrin
- modified
- Prior art date
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- 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 53
- 238000000034 method Methods 0.000 title claims abstract description 16
- 239000000203 mixture Substances 0.000 claims abstract description 86
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical class O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims abstract description 77
- 239000003798 L01XE11 - Pazopanib Substances 0.000 claims abstract description 45
- 229960000639 pazopanib Drugs 0.000 claims abstract description 45
- CUIHSIWYWATEQL-UHFFFAOYSA-N pazopanib Chemical compound C1=CC2=C(C)N(C)N=C2C=C1N(C)C(N=1)=CC=NC=1NC1=CC=C(C)C(S(N)(=O)=O)=C1 CUIHSIWYWATEQL-UHFFFAOYSA-N 0.000 claims abstract description 43
- 238000009472 formulation Methods 0.000 claims abstract description 40
- 150000003839 salts Chemical class 0.000 claims abstract description 29
- 239000002253 acid Substances 0.000 claims abstract description 26
- 229920000858 Cyclodextrin Polymers 0.000 claims description 41
- 239000000243 solution Substances 0.000 claims description 34
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 28
- 239000003814 drug Substances 0.000 claims description 22
- 230000003204 osmotic effect Effects 0.000 claims description 21
- 239000007864 aqueous solution Substances 0.000 claims description 19
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 18
- 229960004853 betadex Drugs 0.000 claims description 17
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 17
- -1 methylcyclodextrin Chemical compound 0.000 claims description 15
- 239000000872 buffer Substances 0.000 claims description 14
- 239000003002 pH adjusting agent Substances 0.000 claims description 13
- 239000001116 FEMA 4028 Substances 0.000 claims description 9
- 229940097346 sulfobutylether-beta-cyclodextrin Drugs 0.000 claims description 9
- 239000003795 chemical substances by application Substances 0.000 claims description 6
- 239000012458 free base Substances 0.000 claims description 6
- NZAQRZWBQUIBSF-UHFFFAOYSA-N 4-(4-sulfobutoxy)butane-1-sulfonic acid Chemical compound OS(=O)(=O)CCCCOCCCCS(O)(=O)=O NZAQRZWBQUIBSF-UHFFFAOYSA-N 0.000 claims description 5
- 239000003607 modifier Substances 0.000 claims description 5
- 239000008363 phosphate buffer Substances 0.000 claims description 5
- 238000012360 testing method Methods 0.000 claims description 5
- YZOUYRAONFXZSI-SBHWVFSVSA-N (1S,3R,5R,6R,8R,10R,11R,13R,15R,16R,18R,20R,21R,23R,25R,26R,28R,30R,31S,33R,35R,36R,37S,38R,39S,40R,41S,42R,43S,44R,45S,46R,47S,48R,49S)-5,10,15,20,25,30,35-heptakis(hydroxymethyl)-37,39,40,41,42,43,44,45,46,47,48,49-dodecamethoxy-2,4,7,9,12,14,17,19,22,24,27,29,32,34-tetradecaoxaoctacyclo[31.2.2.23,6.28,11.213,16.218,21.223,26.228,31]nonatetracontane-36,38-diol Chemical compound O([C@@H]([C@H]([C@@H]1OC)OC)O[C@H]2[C@@H](O)[C@@H]([C@@H](O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3O)OC)O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3OC)OC)O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3OC)OC)O[C@@H]3[C@@H](CO)O[C@@H]([C@H]([C@@H]3OC)OC)O3)O[C@@H]2CO)OC)[C@H](CO)[C@H]1O[C@@H]1[C@@H](OC)[C@H](OC)[C@H]3[C@@H](CO)O1 YZOUYRAONFXZSI-SBHWVFSVSA-N 0.000 claims description 2
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 claims 2
- SNICXCGAKADSCV-JTQLQIEISA-N (-)-Nicotine Chemical compound CN1CCC[C@H]1C1=CC=CN=C1 SNICXCGAKADSCV-JTQLQIEISA-N 0.000 claims 1
- DURPTKYDGMDSBL-UHFFFAOYSA-N 1-butoxybutane Chemical compound CCCCOCCCC DURPTKYDGMDSBL-UHFFFAOYSA-N 0.000 claims 1
- 239000004067 bulking agent Substances 0.000 claims 1
- 239000007979 citrate buffer Substances 0.000 claims 1
- 238000010586 diagram Methods 0.000 claims 1
- 239000006210 lotion Substances 0.000 claims 1
- 229960002715 nicotine Drugs 0.000 claims 1
- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 claims 1
- 125000000020 sulfo group Chemical group O=S(=O)([*])O[H] 0.000 claims 1
- 125000001273 sulfonato group Chemical group [O-]S(*)(=O)=O 0.000 claims 1
- 229940079593 drug Drugs 0.000 description 21
- 239000002997 ophthalmic solution Substances 0.000 description 11
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 9
- 150000001875 compounds Chemical class 0.000 description 9
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 8
- 229940054534 ophthalmic solution Drugs 0.000 description 8
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 5
- 238000002360 preparation method Methods 0.000 description 5
- 239000008215 water for injection Substances 0.000 description 5
- 239000004375 Dextrin Substances 0.000 description 4
- 229920001353 Dextrin Polymers 0.000 description 4
- 235000019425 dextrin Nutrition 0.000 description 4
- CDBYLPFSWZWCQE-UHFFFAOYSA-L sodium carbonate Substances [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 description 4
- 239000011780 sodium chloride Substances 0.000 description 4
- 238000005063 solubilization Methods 0.000 description 4
- 230000007928 solubilization Effects 0.000 description 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 description 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 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 description 3
- 239000002552 dosage form Substances 0.000 description 3
- 239000003889 eye drop Substances 0.000 description 3
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- 231100001271 preclinical toxicology Toxicity 0.000 description 3
- 239000011734 sodium Substances 0.000 description 3
- 229910052708 sodium Inorganic materials 0.000 description 3
- 239000001488 sodium phosphate Substances 0.000 description 3
- 229910000162 sodium phosphate Inorganic materials 0.000 description 3
- 235000011008 sodium phosphates Nutrition 0.000 description 3
- 239000012453 solvate Substances 0.000 description 3
- 239000002904 solvent Substances 0.000 description 3
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- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 3
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 2
- LTEQMZWBSYACLV-UHFFFAOYSA-N Hexylbenzene Chemical compound CCCCCCC1=CC=CC=C1 LTEQMZWBSYACLV-UHFFFAOYSA-N 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 229910002651 NO3 Inorganic materials 0.000 description 2
- 241000283973 Oryctolagus cuniculus Species 0.000 description 2
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- KEAYESYHFKHZAL-UHFFFAOYSA-N Sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 description 2
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 2
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- 239000004480 active ingredient Substances 0.000 description 2
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- 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 description 2
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 2
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- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
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- IDIIJJHBXUESQI-DFIJPDEKSA-N moxifloxacin hydrochloride Chemical compound Cl.COC1=C(N2C[C@H]3NCCC[C@H]3C2)C(F)=CC(C(C(C(O)=O)=C2)=O)=C1N2C1CC1 IDIIJJHBXUESQI-DFIJPDEKSA-N 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
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- NTTOTNSKUYCDAV-UHFFFAOYSA-N potassium hydride Chemical compound [KH] NTTOTNSKUYCDAV-UHFFFAOYSA-N 0.000 description 2
- 229910000105 potassium hydride Inorganic materials 0.000 description 2
- NMMVKSMGBDRONO-UHFFFAOYSA-N potassium;9-methyl-3-(1,2,4-triaza-3-azanidacyclopenta-1,4-dien-5-yl)pyrido[1,2-a]pyrimidin-4-one Chemical compound [K+].CC1=CC=CN(C2=O)C1=NC=C2C1=NN=N[N-]1 NMMVKSMGBDRONO-UHFFFAOYSA-N 0.000 description 2
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Landscapes
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| US20070020299A1 (en) | 2003-12-31 | 2007-01-25 | Pipkin James D | Inhalant formulation containing sulfoalkyl ether cyclodextrin and corticosteroid |
| ES2493641T3 (es) * | 2007-06-28 | 2014-09-12 | Cydex Pharmaceuticals, Inc. | Administración nasal de soluciones acuosas de corticosteroides |
| US12370352B2 (en) | 2007-06-28 | 2025-07-29 | Cydex Pharmaceuticals, Inc. | Nasal and ophthalmic delivery of aqueous corticosteroid solutions |
| US8623395B2 (en) | 2010-01-29 | 2014-01-07 | Forsight Vision4, Inc. | Implantable therapeutic device |
| US10166142B2 (en) | 2010-01-29 | 2019-01-01 | Forsight Vision4, Inc. | Small molecule delivery with implantable therapeutic device |
| TW201206908A (en) * | 2010-05-05 | 2012-02-16 | Glaxo Wellcome Mfg Pte Ltd | Pharmaceutical compositions and methods of making same |
| HUE054113T2 (hu) | 2010-08-05 | 2021-08-30 | Forsight Vision4 Inc | Injekciós készülék gyógyszerbejuttatáshoz |
| EP2640360A2 (en) | 2010-11-19 | 2013-09-25 | Forsight Vision4, Inc. | Therapeutic agent formulations for implanted devices |
| SI2755600T1 (sl) | 2011-09-16 | 2021-08-31 | Forsight Vision4, Inc. | Naprava za izmenjavo tekočine |
| RU2014137190A (ru) * | 2012-02-17 | 2016-04-10 | Фармасайкликс, Инк. | Комбинации ингибитора гистон-деацетилазы и пазопаниба и их применение |
| EP3897032B1 (en) * | 2012-03-08 | 2025-04-30 | Samsung Electronics Co., Ltd. | Method for controlling services in wireless communication system |
| AU2014236455B2 (en) | 2013-03-14 | 2018-07-12 | Forsight Vision4, Inc. | Systems for sustained intraocular delivery of low solubility compounds from a port delivery system implant |
| ES2972168T3 (es) | 2013-03-28 | 2024-06-11 | Forsight Vision4 Inc | Implante oftálmico para administración de sustancias terapéuticas |
| US11136625B2 (en) | 2013-08-28 | 2021-10-05 | Crown Bioscience, Inc. (Taicang) | Gene expression signatures predictive of subject response to a multi-kinase inhibitor and methods of using the same |
| CA2957548A1 (en) * | 2014-08-08 | 2016-02-11 | Forsight Vision4, Inc. | Stable and soluble formulations of receptor tyrosine kinase inhibitors, and methods of preparation thereof |
| BR112017009660A2 (pt) | 2014-11-10 | 2017-12-19 | Forsight Vision4 Inc | dispositivos de administração de fármacos expansíveis e métodos de utilização |
| JP6818264B2 (ja) | 2014-12-25 | 2021-01-20 | 国立大学法人京都大学 | 高密度リポタンパク質およびその細胞親和性ペプチドを融合した高密度リポタンパク質の点眼による後眼部薬物デリバリー |
| AR108177A1 (es) | 2016-04-05 | 2018-07-25 | Forsight Vision4 Inc | Dispositivos de suministro de fármacos oculares implantables |
| EP3612223B1 (en) * | 2017-04-17 | 2024-07-31 | National Institute Of Biological Sciences, Beijing | Treating male senescence |
| TWI770246B (zh) * | 2017-08-02 | 2022-07-11 | 昊運股份有限公司 | 新穎化合物及包含其之醫藥組成物 |
| NZ805649A (en) * | 2018-06-07 | 2024-11-29 | Pfizer | Aqueous formulation comprising 1-(4-{ [4-(dimethylamino)piperidin-1-yl]carbonyl} phenyl)-3- [4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea |
| CN113350351A (zh) * | 2020-03-13 | 2021-09-07 | 青晓制药公司 | 帕唑帕尼的应用、药物组合物、注射液及制备方法和应用 |
| USD1033637S1 (en) | 2022-01-24 | 2024-07-02 | Forsight Vision4, Inc. | Fluid exchange device |
| US20240050429A1 (en) * | 2022-08-10 | 2024-02-15 | Qx Therapeutics, Inc. | Pazopanib pharmaceutical composition, injection and preparation method and use thereof |
Family Cites Families (12)
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| SE8904296D0 (sv) * | 1989-12-21 | 1989-12-21 | Pharmacia Ab | Transdermal system |
| US7893040B2 (en) * | 2005-07-22 | 2011-02-22 | Oculis Ehf | Cyclodextrin nanotechnology for ophthalmic drug delivery |
| US20080293691A1 (en) * | 2005-11-29 | 2008-11-27 | Smithkline Beecham Corporation | Treatment Method |
| AR059066A1 (es) * | 2006-01-27 | 2008-03-12 | Amgen Inc | Combinaciones del inhibidor de la angiopoyetina -2 (ang2) y el inhibidor del factor de crecimiento endotelial vascular (vegf) |
| CA2650922C (en) * | 2006-04-18 | 2015-09-29 | Ekr Therapeutics, Inc. | Pre-mixed, ready-to-use pharmaceutical compositions |
| ES2830024T3 (es) * | 2007-10-19 | 2021-06-02 | Novartis Ag | Composiciones y métodos para el tratamiento del edema macular |
| JP5608099B2 (ja) * | 2008-01-30 | 2014-10-15 | ジェネンテック， インコーポレイテッド | ピラゾロピリミジンｐｉ３ｋ阻害剤化合物および使用方法 |
| JP2012533562A (ja) * | 2009-07-16 | 2012-12-27 | グラクソ ウェルカム マニュファクチュアリング ピーティーイー リミテッド | 治療法 |
| US20120232102A1 (en) * | 2009-09-30 | 2012-09-13 | Chun-Fang Xu | Methods Of Administration And Treatment |
| UY33164A (es) * | 2010-01-06 | 2011-08-31 | Glaxo Wellcome Mfg Pte Ltd | Metodo de tratamiento |
| TW201206908A (en) * | 2010-05-05 | 2012-02-16 | Glaxo Wellcome Mfg Pte Ltd | Pharmaceutical compositions and methods of making same |
| US20130023550A1 (en) * | 2010-05-05 | 2013-01-24 | Glaxo Wellcome Manufacturing Pte, Ltd | Pharmaceutical compositions and methods of making same |
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| AR081364A1 (es) | 2012-08-29 |
| US20120028918A1 (en) | 2012-02-02 |
| US20150231265A1 (en) | 2015-08-20 |
| AU2011247995A1 (en) | 2012-12-13 |
| MX2012012837A (es) | 2013-01-24 |
| EP2566331A1 (en) | 2013-03-13 |
| BR112012028291A2 (pt) | 2015-09-15 |
| EP2566331A4 (en) | 2013-09-18 |
| HK1175947A1 (en) | 2013-07-19 |
| IL222751A0 (en) | 2012-12-31 |
| US20110281901A1 (en) | 2011-11-17 |
| JP2013525501A (ja) | 2013-06-20 |
| CA2798386A1 (en) | 2011-11-10 |
| SG185087A1 (en) | 2012-12-28 |
| NZ603411A (en) | 2014-10-31 |
| EP2566331B1 (en) | 2014-09-03 |
| EA201291168A1 (ru) | 2013-06-28 |
| UY33367A (es) | 2011-10-31 |
| KR20130071434A (ko) | 2013-06-28 |
| CO6640262A2 (es) | 2013-03-22 |
| WO2011140343A1 (en) | 2011-11-10 |
| JP5835717B2 (ja) | 2015-12-24 |
| ZA201208265B (en) | 2013-07-31 |
| PH12012502159A1 (en) | 2013-02-04 |
| AU2011247995B2 (en) | 2014-07-31 |
| MA34286B1 (fr) | 2013-06-01 |
| CR20120556A (es) | 2013-02-20 |
| CN102970871A (zh) | 2013-03-13 |
| PE20130217A1 (es) | 2013-03-21 |
| DOP2012000281A (es) | 2013-05-31 |
| ES2519615T3 (es) | 2014-11-07 |
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