RU2403013C2 - Твердая дисперсия, содержащая активный ингредиент с низкой температурой плавления, и содержащая ее таблетка для перорального введения - Google Patents
Твердая дисперсия, содержащая активный ингредиент с низкой температурой плавления, и содержащая ее таблетка для перорального введения Download PDFInfo
- Publication number
- RU2403013C2 RU2403013C2 RU2008129041/15A RU2008129041A RU2403013C2 RU 2403013 C2 RU2403013 C2 RU 2403013C2 RU 2008129041/15 A RU2008129041/15 A RU 2008129041/15A RU 2008129041 A RU2008129041 A RU 2008129041A RU 2403013 C2 RU2403013 C2 RU 2403013C2
- Authority
- RU
- Russia
- Prior art keywords
- tablet
- solid dispersion
- pharmaceutically acceptable
- release
- fused solid
- Prior art date
Links
- 239000007962 solid dispersion Substances 0.000 title claims abstract description 52
- 239000007935 oral tablet Substances 0.000 title claims description 5
- 229940096978 oral tablet Drugs 0.000 title claims description 5
- 230000004927 fusion Effects 0.000 title 1
- RMAQACBXLXPBSY-UHFFFAOYSA-N silicic acid Chemical compound O[Si](O)(O)O RMAQACBXLXPBSY-UHFFFAOYSA-N 0.000 claims abstract description 13
- 235000012239 silicon dioxide Nutrition 0.000 claims abstract description 13
- HEFNNWSXXWATRW-UHFFFAOYSA-N Ibuprofen Chemical compound CC(C)CC1=CC=C(C(C)C(O)=O)C=C1 HEFNNWSXXWATRW-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229960001680 ibuprofen Drugs 0.000 claims abstract description 8
- 239000003826 tablet Substances 0.000 claims description 103
- 239000004480 active ingredient Substances 0.000 claims description 41
- 238000013270 controlled release Methods 0.000 claims description 41
- 238000000034 method Methods 0.000 claims description 37
- 239000000203 mixture Substances 0.000 claims description 26
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 24
- HEFNNWSXXWATRW-JTQLQIEISA-N dexibuprofen Chemical compound CC(C)CC1=CC=C([C@H](C)C(O)=O)C=C1 HEFNNWSXXWATRW-JTQLQIEISA-N 0.000 claims description 18
- 238000002844 melting Methods 0.000 claims description 17
- 230000008018 melting Effects 0.000 claims description 16
- 229960003428 dexibuprofen Drugs 0.000 claims description 15
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 14
- 239000003795 chemical substances by application Substances 0.000 claims description 13
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims description 8
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 8
- 239000008187 granular material Substances 0.000 claims description 8
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 8
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 8
- 238000010438 heat treatment Methods 0.000 claims description 7
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 7
- 235000019359 magnesium stearate Nutrition 0.000 claims description 7
- 239000003921 oil Substances 0.000 claims description 7
- 150000005846 sugar alcohols Chemical class 0.000 claims description 7
- 229920003169 water-soluble polymer Polymers 0.000 claims description 7
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 6
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 6
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 6
- 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 6
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- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 5
- 229920002472 Starch Polymers 0.000 claims description 5
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 claims description 5
- 239000008101 lactose Substances 0.000 claims description 5
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 claims description 5
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- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 claims description 4
- 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 claims description 3
- 229930195725 Mannitol Natural products 0.000 claims description 3
- 239000002202 Polyethylene glycol Substances 0.000 claims description 3
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- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 claims description 2
- 239000000263 2,3-dihydroxypropyl (Z)-octadec-9-enoate Substances 0.000 claims description 2
- RZRNAYUHWVFMIP-GDCKJWNLSA-N 3-oleoyl-sn-glycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-GDCKJWNLSA-N 0.000 claims description 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound 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 GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims description 2
- 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 description 2
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- 159000000007 calcium salts Chemical class 0.000 claims description 2
- 239000004359 castor oil Substances 0.000 claims description 2
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- 238000001816 cooling Methods 0.000 claims description 2
- 229920001577 copolymer Polymers 0.000 claims description 2
- 238000001035 drying Methods 0.000 claims description 2
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims description 2
- 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 2
- 229940049654 glyceryl behenate Drugs 0.000 claims description 2
- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 claims description 2
- 229940046813 glyceryl palmitostearate Drugs 0.000 claims description 2
- 238000000227 grinding Methods 0.000 claims description 2
- 229940057948 magnesium stearate Drugs 0.000 claims description 2
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 claims description 2
- 229920002689 polyvinyl acetate Polymers 0.000 claims description 2
- 239000011118 polyvinyl acetate Substances 0.000 claims description 2
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims description 2
- 239000000600 sorbitol Substances 0.000 claims description 2
- 235000010356 sorbitol Nutrition 0.000 claims description 2
- -1 sucrose fatty acid ester Chemical class 0.000 claims description 2
- 244000303965 Cyamopsis psoralioides Species 0.000 claims 1
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- 239000003463 adsorbent Substances 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
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- 229920002554 vinyl polymer Polymers 0.000 claims 1
- 239000003814 drug Substances 0.000 abstract description 11
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- FUFJGUQYACFECW-UHFFFAOYSA-L calcium hydrogenphosphate Chemical compound [Ca+2].OP([O-])([O-])=O FUFJGUQYACFECW-UHFFFAOYSA-L 0.000 description 3
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- GDVKFRBCXAPAQJ-UHFFFAOYSA-A dialuminum;hexamagnesium;carbonate;hexadecahydroxide Chemical compound [OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[OH-].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Mg+2].[Al+3].[Al+3].[O-]C([O-])=O GDVKFRBCXAPAQJ-UHFFFAOYSA-A 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
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Images
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
- A61K9/14—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
- A61K9/143—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 inorganic compounds
-
- 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
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
- A61K9/209—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat containing drug in at least two layers or in the core and in at least one outer layer
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Inorganic Chemistry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR10-2005-0124386 | 2005-12-16 | ||
| KR20050124386 | 2005-12-16 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2008129041A RU2008129041A (ru) | 2010-01-27 |
| RU2403013C2 true RU2403013C2 (ru) | 2010-11-10 |
Family
ID=38163142
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2008129041/15A RU2403013C2 (ru) | 2005-12-16 | 2006-12-18 | Твердая дисперсия, содержащая активный ингредиент с низкой температурой плавления, и содержащая ее таблетка для перорального введения |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20080292702A1 (enExample) |
| EP (1) | EP1968542B1 (enExample) |
| JP (1) | JP2009519326A (enExample) |
| CN (1) | CN101330904B (enExample) |
| AU (1) | AU2006325658B2 (enExample) |
| BR (1) | BRPI0619868A8 (enExample) |
| CA (1) | CA2633266C (enExample) |
| ES (1) | ES2429097T3 (enExample) |
| IL (1) | IL191804A0 (enExample) |
| NO (1) | NO339674B1 (enExample) |
| NZ (1) | NZ569813A (enExample) |
| RU (1) | RU2403013C2 (enExample) |
| WO (1) | WO2007069874A1 (enExample) |
| ZA (1) | ZA200806138B (enExample) |
Cited By (1)
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| RU2685294C1 (ru) * | 2018-05-10 | 2019-04-17 | Общество с ограниченной ответственностью "ДИНОН" (ООО "ДИНОН") | Поглотитель, способ его приготовления (варианты) и способ удаления диоксида углерода из газовых смесей |
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| MXPA06002731A (es) | 2003-09-11 | 2006-06-05 | Xenoport Inc | Tratamiento y/o prevencion de incontinencia urinaria utilizando profarmacos de analogos de gaba. |
| KR101005391B1 (ko) * | 2008-07-22 | 2010-12-30 | 한국콜마 주식회사 | 덱시부프로펜 함유 서방출성 시럽제 및 그의 제조방법 |
| KR101067224B1 (ko) * | 2008-07-22 | 2011-09-22 | 한국콜마 주식회사 | 이부프로펜 함유 서방출성 시럽제 및 그의 제조방법 |
| CN101961306B (zh) * | 2009-07-24 | 2011-11-09 | 北京化工大学 | 一种低熔点药物固体分散体的制备方法 |
| CN102144982B (zh) * | 2011-03-30 | 2012-12-12 | 江苏神龙药业有限公司 | 一种米诺膦酸片及其制备方法 |
| CN102406940B (zh) * | 2011-11-01 | 2013-07-03 | 温州大学 | 一种纳米级片状羧甲基淀粉钠在固体分散体中的应用 |
| WO2013154511A1 (en) * | 2012-04-13 | 2013-10-17 | Mahmut Bilgic | Film tablet formulations comprising dexibuprofen |
| UY36046A (es) | 2014-03-26 | 2015-10-30 | Millennium Pharm Inc | Formulaciones farmacéuticas, procesos para la preparación y métodos de uso |
| JP6647902B2 (ja) * | 2015-10-30 | 2020-02-14 | 株式会社ファンケル | 徐放性顆粒剤 |
| CN106265522A (zh) * | 2016-08-30 | 2017-01-04 | 铜陵翔宇商贸有限公司 | 布洛芬‑pvp共沉淀物及其制备方法 |
| JP7147262B2 (ja) * | 2017-05-23 | 2022-10-05 | 大正製薬株式会社 | 固形製剤 |
| JP7109255B2 (ja) * | 2017-05-23 | 2022-07-29 | ライオン株式会社 | 粉砕物の製造方法及び錠剤の製造方法 |
| EP3658123A4 (en) * | 2017-07-24 | 2021-04-28 | Acryspharm LLC | PHARMACEUTICAL COMPOSITIONS WITH A HIGH DRUG LOAD |
| CN112263567B (zh) * | 2020-10-19 | 2022-05-03 | 南京易亨制药有限公司 | 一种布洛芬缓释胶囊及制备方法 |
| CN117363320B (zh) * | 2023-12-07 | 2024-02-13 | 黑龙江省鑫博鑫交通科技有限公司 | 一种公路用融雪剂及其制备方法 |
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| RU2197228C2 (ru) * | 1995-09-29 | 2003-01-27 | Басф Аг | Твердые лекарственные формы, получаемые экструзией содержащего изомальт расплава полимера и активного вещества |
| RU2246294C2 (ru) * | 1999-12-09 | 2005-02-20 | Дзе Бутс Компани ПЛС | Терапевтические средства |
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| JPS56120616A (en) * | 1980-02-27 | 1981-09-22 | Kaken Pharmaceut Co Ltd | Ibuprofen-containing granule, its preparation, and internal medicine comprising it |
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| US4806359A (en) * | 1987-04-22 | 1989-02-21 | Mcneilab, Inc. | Iburprofen sustained release matrix and process |
| DE19509807A1 (de) * | 1995-03-21 | 1996-09-26 | Basf Ag | Verfahren zur Herstellung von Wirkstoffzubereitungen in Form einer festen Lösung des Wirkstoffs in einer Polymermatrix sowie mit diesem Verfahren hergestellte Wirkstoffzubereitungen |
| IE80467B1 (en) * | 1995-07-03 | 1998-07-29 | Elan Corp Plc | Controlled release formulations for poorly soluble drugs |
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| GB0113839D0 (en) * | 2001-06-07 | 2001-08-01 | Boots Co Plc | Therapeutic agents |
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2006
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- 2006-12-18 CA CA2633266A patent/CA2633266C/en not_active Expired - Fee Related
- 2006-12-18 ZA ZA200806138A patent/ZA200806138B/xx unknown
- 2006-12-18 WO PCT/KR2006/005526 patent/WO2007069874A1/en not_active Ceased
- 2006-12-18 US US12/097,299 patent/US20080292702A1/en not_active Abandoned
- 2006-12-18 NZ NZ569813A patent/NZ569813A/en not_active IP Right Cessation
- 2006-12-18 ES ES06824193T patent/ES2429097T3/es active Active
- 2006-12-18 RU RU2008129041/15A patent/RU2403013C2/ru not_active IP Right Cessation
- 2006-12-18 EP EP06824193.4A patent/EP1968542B1/en not_active Not-in-force
- 2006-12-18 JP JP2008545503A patent/JP2009519326A/ja active Pending
- 2006-12-18 CN CN2006800474904A patent/CN101330904B/zh not_active Expired - Fee Related
- 2006-12-18 BR BRPI0619868A patent/BRPI0619868A8/pt not_active IP Right Cessation
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2008
- 2008-05-29 IL IL191804A patent/IL191804A0/en unknown
- 2008-07-15 NO NO20083151A patent/NO339674B1/no not_active IP Right Cessation
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| RU2197228C2 (ru) * | 1995-09-29 | 2003-01-27 | Басф Аг | Твердые лекарственные формы, получаемые экструзией содержащего изомальт расплава полимера и активного вещества |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2685294C1 (ru) * | 2018-05-10 | 2019-04-17 | Общество с ограниченной ответственностью "ДИНОН" (ООО "ДИНОН") | Поглотитель, способ его приготовления (варианты) и способ удаления диоксида углерода из газовых смесей |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2006325658A1 (en) | 2007-06-21 |
| EP1968542A4 (en) | 2010-06-02 |
| CA2633266C (en) | 2011-08-02 |
| IL191804A0 (en) | 2008-12-29 |
| JP2009519326A (ja) | 2009-05-14 |
| HK1126671A1 (en) | 2009-09-11 |
| NO339674B1 (no) | 2017-01-23 |
| AU2006325658B2 (en) | 2010-04-08 |
| BRPI0619868A2 (pt) | 2011-10-25 |
| ZA200806138B (en) | 2009-11-25 |
| CA2633266A1 (en) | 2007-06-21 |
| BRPI0619868A8 (pt) | 2016-06-07 |
| ES2429097T3 (es) | 2013-11-13 |
| NZ569813A (en) | 2011-07-29 |
| CN101330904B (zh) | 2012-04-18 |
| RU2008129041A (ru) | 2010-01-27 |
| EP1968542A1 (en) | 2008-09-17 |
| EP1968542B1 (en) | 2013-08-14 |
| NO20083151L (no) | 2008-09-05 |
| WO2007069874A1 (en) | 2007-06-21 |
| US20080292702A1 (en) | 2008-11-27 |
| CN101330904A (zh) | 2008-12-24 |
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