SG176304A1 - Tamper resistant dosage form comprising a matrix and melt - extruded particulates comprising a drug - Google Patents
Tamper resistant dosage form comprising a matrix and melt - extruded particulates comprising a drug Download PDFInfo
- Publication number
- SG176304A1 SG176304A1 SG2011089273A SG2011089273A SG176304A1 SG 176304 A1 SG176304 A1 SG 176304A1 SG 2011089273 A SG2011089273 A SG 2011089273A SG 2011089273 A SG2011089273 A SG 2011089273A SG 176304 A1 SG176304 A1 SG 176304A1
- Authority
- SG
- Singapore
- Prior art keywords
- particulates
- dosage form
- drug
- melt
- extrudate
- Prior art date
Links
- 239000002552 dosage form Substances 0.000 title claims abstract description 278
- 239000003814 drug Substances 0.000 title claims abstract description 133
- 229940079593 drug Drugs 0.000 title claims abstract description 122
- 239000011159 matrix material Substances 0.000 title claims abstract description 70
- 239000000203 mixture Substances 0.000 claims description 72
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 69
- 229920000642 polymer Polymers 0.000 claims description 52
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 claims description 49
- 229960002085 oxycodone Drugs 0.000 claims description 49
- 238000000034 method Methods 0.000 claims description 47
- 239000003795 chemical substances by application Substances 0.000 claims description 43
- 229960004127 naloxone Drugs 0.000 claims description 39
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 36
- -1 poly(acrylic acid) Polymers 0.000 claims description 35
- 150000003839 salts Chemical class 0.000 claims description 29
- WVLOADHCBXTIJK-YNHQPCIGSA-N hydromorphone Chemical compound O([C@H]1C(CC[C@H]23)=O)C4=C5[C@@]12CCN(C)[C@@H]3CC5=CC=C4O WVLOADHCBXTIJK-YNHQPCIGSA-N 0.000 claims description 27
- 229960001410 hydromorphone Drugs 0.000 claims description 27
- 239000000155 melt Substances 0.000 claims description 22
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- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 18
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 18
- 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 18
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- 230000008569 process Effects 0.000 claims description 15
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- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims description 14
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- 239000001069 triethyl citrate Substances 0.000 claims description 8
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 claims description 8
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- 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
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- 230000004799 sedative–hypnotic effect Effects 0.000 claims description 3
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- VKNASXZDGZNEDA-UHFFFAOYSA-N 2-cyanoethyl 2-methylprop-2-enoate Chemical compound CC(=C)C(=O)OCCC#N VKNASXZDGZNEDA-UHFFFAOYSA-N 0.000 claims description 2
- SFPNZPQIIAJXGL-UHFFFAOYSA-N 2-ethoxyethyl 2-methylprop-2-enoate Chemical class CCOCCOC(=O)C(C)=C SFPNZPQIIAJXGL-UHFFFAOYSA-N 0.000 claims description 2
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims description 2
- 229920003144 amino alkyl methacrylate copolymer Polymers 0.000 claims description 2
- 229960001736 buprenorphine Drugs 0.000 claims description 2
- RMRJXGBAOAMLHD-IHFGGWKQSA-N buprenorphine Chemical compound C([C@]12[C@H]3OC=4C(O)=CC=C(C2=4)C[C@@H]2[C@]11CC[C@]3([C@H](C1)[C@](C)(O)C(C)(C)C)OC)CN2CC1CC1 RMRJXGBAOAMLHD-IHFGGWKQSA-N 0.000 claims description 2
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2121/00—Preparations for use in therapy
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Emergency Medicine (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
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|---|---|---|---|
| GBGB0909680.1A GB0909680D0 (en) | 2009-06-05 | 2009-06-05 | Dosage form |
| PCT/GB2010/050948 WO2010140007A2 (en) | 2009-06-05 | 2010-06-07 | Dosage form |
Publications (1)
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| SG176304A1 true SG176304A1 (en) | 2012-01-30 |
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| SG10201402810XA SG10201402810XA (en) | 2009-06-05 | 2010-06-07 | Tamper resistant dosage form comprising a matrix and melt - extruded particulates comprising a drug |
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| SG10201402810XA SG10201402810XA (en) | 2009-06-05 | 2010-06-07 | Tamper resistant dosage form comprising a matrix and melt - extruded particulates comprising a drug |
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| EP (1) | EP2437729B1 (enExample) |
| JP (1) | JP5635082B2 (enExample) |
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| CN (2) | CN102481260A (enExample) |
| AU (1) | AU2010255502B2 (enExample) |
| BR (1) | BRPI1012004A2 (enExample) |
| CA (1) | CA2764517C (enExample) |
| EA (1) | EA022801B1 (enExample) |
| ES (1) | ES2713957T3 (enExample) |
| GB (1) | GB0909680D0 (enExample) |
| IL (1) | IL216748A0 (enExample) |
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| MY (1) | MY173629A (enExample) |
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| SG (2) | SG176304A1 (enExample) |
| WO (1) | WO2010140007A2 (enExample) |
| ZA (1) | ZA201109221B (enExample) |
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| US7776314B2 (en) | 2002-06-17 | 2010-08-17 | Grunenthal Gmbh | Abuse-proofed dosage system |
| US8877241B2 (en) | 2003-03-26 | 2014-11-04 | Egalet Ltd. | Morphine controlled release system |
| US8075872B2 (en) | 2003-08-06 | 2011-12-13 | Gruenenthal Gmbh | Abuse-proofed dosage form |
| DE102005005446A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Bruchfeste Darreichungsformen mit retardierter Freisetzung |
| DE10336400A1 (de) | 2003-08-06 | 2005-03-24 | Grünenthal GmbH | Gegen Missbrauch gesicherte Darreichungsform |
| DE102004032051A1 (de) | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten, festen Darreichungsform |
| US20070048228A1 (en) | 2003-08-06 | 2007-03-01 | Elisabeth Arkenau-Maric | Abuse-proofed dosage form |
| DE10361596A1 (de) | 2003-12-24 | 2005-09-29 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| DE102004032049A1 (de) | 2004-07-01 | 2006-01-19 | Grünenthal GmbH | Gegen Missbrauch gesicherte, orale Darreichungsform |
| DE102005005449A1 (de) | 2005-02-04 | 2006-08-10 | Grünenthal GmbH | Verfahren zur Herstellung einer gegen Missbrauch gesicherten Darreichungsform |
| DE102007011485A1 (de) | 2007-03-07 | 2008-09-11 | Grünenthal GmbH | Darreichungsform mit erschwertem Missbrauch |
| US8821928B2 (en) | 2007-06-04 | 2014-09-02 | Egalet Ltd. | Controlled release pharmaceutical compositions for prolonged effect |
| CN105534936B (zh) * | 2007-08-13 | 2020-07-31 | Ohemo 生命科学股份有限公司 | 抗滥用药物、使用方法和制备方法 |
| TWI454288B (zh) | 2008-01-25 | 2014-10-01 | Gruenenthal Chemie | 藥物劑型 |
| ES2599031T3 (es) | 2008-05-09 | 2017-01-31 | Grünenthal GmbH | Proceso para la preparación de una formulación de polvo intermedia y una forma de dosificación solida final utilizando un paso de congelación por pulverización |
| NZ594207A (en) | 2009-02-06 | 2013-03-28 | Egalet Ltd | Immediate release composition resistant to abuse by intake of alcohol |
| AU2010265213B2 (en) | 2009-06-24 | 2012-08-23 | Egalet Ltd. | Controlled release formulations |
| BR112012001466A2 (pt) | 2009-07-22 | 2020-08-11 | Grünenthal GmbH | forma de dosagem resistente à falsificação para opioides sensíveis à oxidação, seu processo de fabricação, e embalagem |
| ES2534908T3 (es) | 2009-07-22 | 2015-04-30 | Grünenthal GmbH | Forma de dosificación de liberación controlada extruida por fusión en caliente |
| SG184523A1 (en) * | 2010-05-10 | 2012-11-29 | Euro Celtique Sa | Pharmaceutical compositions comprising hydromorphone and naloxone |
| MX340188B (es) | 2010-05-10 | 2016-06-30 | Euro-Celtique S A * | Elaboracion de granulos sin activos y tabletas que comprenden los mismos. |
| WO2011141490A1 (en) | 2010-05-10 | 2011-11-17 | Euro-Celtique S.A. | Combination of active loaded granules with additional actives |
| CA2808219C (en) | 2010-09-02 | 2019-05-14 | Gruenenthal Gmbh | Tamper resistant dosage form comprising inorganic salt |
| WO2012028318A1 (en) | 2010-09-02 | 2012-03-08 | Grünenthal GmbH | Tamper resistant dosage form comprising an anionic polymer |
| WO2012061780A1 (en) | 2010-11-04 | 2012-05-10 | Abbott Gmbh & Co. Kg | Method for producing monolithic tablets |
| WO2012061779A1 (en) * | 2010-11-04 | 2012-05-10 | Abbott Gmbh & Co. Kg | Drug formulations |
| GB201020895D0 (en) * | 2010-12-09 | 2011-01-26 | Euro Celtique Sa | Dosage form |
| SG191208A1 (en) * | 2010-12-28 | 2013-07-31 | Euro Celtique Sa | A combination of an opioid agonist and an opioid antagonist in the treatment of parkinson's disease |
| JP6063462B2 (ja) | 2011-07-29 | 2017-01-18 | グリュネンタール・ゲゼルシャフト・ミト・ベシュレンクテル・ハフツング | 即時薬剤放出を提供するタンパーレジスタント錠剤 |
| BR112014002022A2 (pt) | 2011-07-29 | 2017-02-21 | Gruenenthal Gmbh | comprimido resistente à violação proporcionando liberação de fármaco imediata |
| US20140341984A1 (en) * | 2011-09-16 | 2014-11-20 | Purdue Pharma L.P. | Tamper resistant pharmaceutical formulations |
| CA2850853A1 (en) * | 2011-10-06 | 2013-04-11 | Grunenthal Gmbh | Tamper-resistant oral pharmaceutical dosage form comprising opioid agonist and opioid antagonist |
| KR20140096062A (ko) | 2011-11-17 | 2014-08-04 | 그뤼넨탈 게엠베하 | 약리학적 활성 성분, 오피오이드 길항제 및/또는 혐오제, 폴리알킬렌 옥사이드 및 음이온성 중합체를 포함하는 탬퍼-저항성 경구 약제학적 투여형 |
| BR112014019988A8 (pt) | 2012-02-28 | 2017-07-11 | Gruenenthal Gmbh | Forma de dosagem resistente a socamento compreendendo um composto farmacologicamente ativo e um polímero aniônico |
| LT2838512T (lt) * | 2012-04-18 | 2018-11-12 | GrĆ¼nenthal GmbH | Pažeidimui atspari ir dozės atpalaidavimo nuokrypiui atspari farmacinė vaisto forma |
| US10064945B2 (en) | 2012-05-11 | 2018-09-04 | Gruenenthal Gmbh | Thermoformed, tamper-resistant pharmaceutical dosage form containing zinc |
| JP2015521988A (ja) | 2012-07-06 | 2015-08-03 | イガレット・リミテッド | 制御放出用乱用防止性医薬組成物 |
| US9730885B2 (en) | 2012-07-12 | 2017-08-15 | Mallinckrodt Llc | Extended release, abuse deterrent pharmaceutical compositions |
| CA2881144A1 (en) * | 2012-11-09 | 2014-05-09 | Purdue Pharma | Pharmaceutical compositions comprising hydromorphone and naloxone |
| US10751287B2 (en) | 2013-03-15 | 2020-08-25 | Purdue Pharma L.P. | Tamper resistant pharmaceutical formulations |
| MX2015016254A (es) | 2013-05-29 | 2016-04-20 | Gruenenthal Gmbh | Forma de dosificacion resistente al uso indebido con perfil de liberacion bimodal. |
| AU2014273227B2 (en) * | 2013-05-29 | 2019-08-15 | Grunenthal Gmbh | Tamper-resistant dosage form containing one or more particles |
| AU2014289187B2 (en) | 2013-07-12 | 2019-07-11 | Grunenthal Gmbh | Tamper-resistant dosage form containing ethylene-vinyl acetate polymer |
| CA3042642A1 (en) | 2013-08-12 | 2015-02-19 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded immediate release abuse deterrent pill |
| JP6232135B2 (ja) | 2013-11-13 | 2017-11-15 | ユーロ−セルティーク エス．エイ． | 疼痛およびオピオイドによる腸機能障害症候群の治療のためのヒドロモルホンおよびナロキソン |
| WO2015071248A1 (en) | 2013-11-15 | 2015-05-21 | Synthon B.V. | Abuse-proofed extended release pharmaceutical composition comprising tapentadol |
| HK1224189A1 (zh) | 2013-11-26 | 2017-08-18 | Grünenthal GmbH | 通过低温研磨制备粉状药物组合物 |
| AU2014364800A1 (en) * | 2013-12-17 | 2016-07-07 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| US9492444B2 (en) | 2013-12-17 | 2016-11-15 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| WO2015095391A1 (en) | 2013-12-17 | 2015-06-25 | Pharmaceutical Manufacturing Research Services, Inc. | Extruded extended release abuse deterrent pill |
| WO2015089530A1 (de) * | 2013-12-20 | 2015-06-25 | G.L. PHARMA GmbH | Orale darreichungsform mit verzögerter freisetzung enthaltend morphin und naloxon |
| CA2847781C (en) * | 2014-03-28 | 2019-03-12 | Purdue Pharma | Reducing drug liking in a subject |
| WO2015173195A1 (en) | 2014-05-12 | 2015-11-19 | Grünenthal GmbH | Tamper resistant immediate release capsule formulation comprising tapentadol |
| US9872835B2 (en) | 2014-05-26 | 2018-01-23 | Grünenthal GmbH | Multiparticles safeguarded against ethanolic dose-dumping |
| PL3164117T3 (pl) | 2014-07-03 | 2024-03-11 | SpecGx LLC | Preparaty zapewniające natychmiastowe uwalnianie i powstrzymujące przed nadużywaniem, zawierające polisacharydy inne niż celuloza |
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| US20160310428A1 (en) | 2015-04-24 | 2016-10-27 | Grunenthal Gmbh | Tamper-resistant fixed dose combination providing fast release of two drugs from different particles |
| WO2016170093A1 (en) | 2015-04-24 | 2016-10-27 | Grünenthal GmbH | Tamper-resistant fixed dose combination providing fast release of two drugs from particles and a matrix |
| BR112017022856A2 (pt) | 2015-04-24 | 2018-07-17 | Gruenenthal Gmbh | combinação de dose fixa inviolável que proporciona rápida liberação de duas drogas a partir de partículas |
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| WO2017009865A1 (en) * | 2015-07-10 | 2017-01-19 | Sun Pharma Advanced Research Company Ltd. | Multiple pill abuse-resistant immediate release solid dosage form of hydrocodone |
| CA2998259A1 (en) | 2015-09-10 | 2017-03-16 | Grunenthal Gmbh | Protecting oral overdose with abuse deterrent immediate release formulations |
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| EP3698776A1 (en) | 2019-02-19 | 2020-08-26 | Grünenthal GmbH | Tamper-resistant dosage form with immediate release and resistance against solvent extraction |
| WO2023072929A1 (de) * | 2021-10-27 | 2023-05-04 | Rheinisch Westfälische Technische Hochschule (Rwth) Aachen | Umhüllte wirkstoffformulierung zu kontrollierten in vivo-aufnahme von co2 |
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| DE102005047561A1 (de) | 2005-10-04 | 2007-04-05 | Bayer Healthcare Ag | Feste, oral applizierbare pharmazeutische Darreichungsformen mit schneller Wirkstofffreisetzung |
| EP1962808B1 (en) | 2005-12-14 | 2010-09-29 | F. Hoffmann-La Roche AG | Hcv prodrug formulation |
| EP1813276A1 (en) | 2006-01-27 | 2007-08-01 | Euro-Celtique S.A. | Tamper resistant dosage forms |
| US7799790B2 (en) * | 2006-07-20 | 2010-09-21 | Helm Ag | Amorphous aripiprazole and process for the preparation thereof |
| EP1935405A1 (en) | 2006-12-22 | 2008-06-25 | LEK Pharmaceuticals D.D. | Orally disintegrating tablets |
| DE102007011485A1 (de) | 2007-03-07 | 2008-09-11 | Grünenthal GmbH | Darreichungsform mit erschwertem Missbrauch |
| GB2447898B (en) | 2007-03-24 | 2011-08-17 | Reckitt Benckiser Healthcare | A tablet having improved stability with at least two actives |
| WO2010055019A1 (en) * | 2008-11-12 | 2010-05-20 | Akzo Nobel Coatings International B.V. | Polymer dispersions of narrow particle size distribution |
| DE102009015702A1 (de) | 2009-03-31 | 2010-10-07 | Ratiopharm Gmbh | Tabletten enthaltend Dapoxetin und Trockenverarbeitungsverfahren zu deren Herstellung |
| GB201020895D0 (en) | 2010-12-09 | 2011-01-26 | Euro Celtique Sa | Dosage form |
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2009
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2010
- 2010-06-07 SG SG2011089273A patent/SG176304A1/en unknown
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- 2010-06-07 NZ NZ596879A patent/NZ596879A/xx not_active IP Right Cessation
- 2010-06-07 MX MX2011012929A patent/MX2011012929A/es active IP Right Grant
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Also Published As
| Publication number | Publication date |
|---|---|
| CN102481260A (zh) | 2012-05-30 |
| ES2713957T3 (es) | 2019-05-24 |
| EP2437729A2 (en) | 2012-04-11 |
| JP2012528845A (ja) | 2012-11-15 |
| EA201171389A1 (ru) | 2012-05-30 |
| CN106667919A (zh) | 2017-05-17 |
| US9814679B2 (en) | 2017-11-14 |
| KR20120026595A (ko) | 2012-03-19 |
| AU2010255502B2 (en) | 2016-09-22 |
| MY173629A (en) | 2020-02-12 |
| MX2011012929A (es) | 2012-04-20 |
| KR101816130B1 (ko) | 2018-01-08 |
| WO2010140007A9 (en) | 2012-01-19 |
| WO2010140007A3 (en) | 2011-11-17 |
| SG10201402810XA (en) | 2014-08-28 |
| EP2437729B1 (en) | 2019-01-23 |
| JP5635082B2 (ja) | 2014-12-03 |
| CA2764517C (en) | 2017-07-04 |
| NZ596879A (en) | 2013-06-28 |
| ZA201109221B (en) | 2012-08-29 |
| BRPI1012004A2 (pt) | 2016-05-10 |
| GB0909680D0 (en) | 2009-07-22 |
| EA022801B1 (ru) | 2016-03-31 |
| CA2764517A1 (en) | 2010-12-09 |
| WO2010140007A2 (en) | 2010-12-09 |
| IL216748A0 (en) | 2012-02-29 |
| AU2010255502A1 (en) | 2012-01-12 |
| US20120135075A1 (en) | 2012-05-31 |
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