JP2010530889A5 - - Google Patents
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- Publication number
- JP2010530889A5 JP2010530889A5 JP2010513433A JP2010513433A JP2010530889A5 JP 2010530889 A5 JP2010530889 A5 JP 2010530889A5 JP 2010513433 A JP2010513433 A JP 2010513433A JP 2010513433 A JP2010513433 A JP 2010513433A JP 2010530889 A5 JP2010530889 A5 JP 2010530889A5
- Authority
- JP
- Japan
- Prior art keywords
- compressed tablet
- lubricant
- raltegravir
- total weight
- tablet
- 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.)
- Withdrawn
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- 239000007891 compressed tablet Substances 0.000 claims 22
- 239000000314 lubricant Substances 0.000 claims 12
- YSIBYEBNVMDAPN-CMDGGOBGSA-N (e)-4-oxo-4-(3-triethoxysilylpropylamino)but-2-enoic acid Chemical compound CCO[Si](OCC)(OCC)CCCNC(=O)\C=C\C(O)=O YSIBYEBNVMDAPN-CMDGGOBGSA-N 0.000 claims 7
- 108010019625 Atazanavir Sulfate Proteins 0.000 claims 7
- 229960003796 atazanavir sulfate Drugs 0.000 claims 7
- 239000008187 granular material Substances 0.000 claims 6
- CZFFBEXEKNGXKS-UHFFFAOYSA-N raltegravir Chemical compound O1C(C)=NN=C1C(=O)NC(C)(C)C1=NC(C(=O)NCC=2C=CC(F)=CC=2)=C(O)C(=O)N1C CZFFBEXEKNGXKS-UHFFFAOYSA-N 0.000 claims 6
- 229960004742 raltegravir Drugs 0.000 claims 6
- 238000000034 method Methods 0.000 claims 3
- 238000005550 wet granulation Methods 0.000 claims 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 claims 2
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 239000003826 tablet Substances 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 235000021314 Palmitic acid Nutrition 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 235000004443 Ricinus communis Nutrition 0.000 claims 1
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- CJZGTCYPCWQAJB-UHFFFAOYSA-L calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 0.000 claims 1
- 239000008116 calcium stearate Substances 0.000 claims 1
- 235000013539 calcium stearate Nutrition 0.000 claims 1
- 239000004203 carnauba wax Substances 0.000 claims 1
- 235000013869 carnauba wax Nutrition 0.000 claims 1
- 239000007884 disintegrant Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 1
- 229940075507 glyceryl monostearate Drugs 0.000 claims 1
- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 claims 1
- 229940046813 glyceryl palmitostearate Drugs 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 239000002480 mineral oil Substances 0.000 claims 1
- 235000010446 mineral oil Nutrition 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000001788 mono and diglycerides of fatty acids Substances 0.000 claims 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 239000003921 oil Substances 0.000 claims 1
- 235000019198 oils Nutrition 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims 1
- 235000010234 sodium benzoate Nutrition 0.000 claims 1
- 239000004299 sodium benzoate Substances 0.000 claims 1
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
- XOOUIPVCVHRTMJ-UHFFFAOYSA-L zinc stearate Chemical compound [Zn+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O XOOUIPVCVHRTMJ-UHFFFAOYSA-L 0.000 claims 1
Claims (14)
- ラルテグラビル、並びに硫酸アタザナビルおよび顆粒内滑沢剤を含有する顆粒を含む圧縮錠剤であって、前記顆粒が内部領域および外部表面を有し、顆粒内滑沢剤の少なくとも一部が顆粒の内部領域に存在する圧縮錠剤。
- 圧縮錠剤の総重量に基づき、顆粒内滑沢剤を約０.１〜１０％含む、請求項１の圧縮錠剤。
- 圧縮錠剤の総重量に基づき、顆粒内滑沢剤を約０.５〜８％含む、請求項１の圧縮錠剤。
- 顆粒内滑沢剤が、ステアリン酸マグネシウム、ステアリン酸亜鉛、ステアリン酸カルシウム、ステアリン酸、パルミチン酸、フマル酸ステアリルナトリウム、安息香酸ナトリウム、ラウリル硫酸ナトリウム、モノステアリン酸グリセリン、パルミトステアリン酸グリセリン、硬化ヒマシ油、硬化植物油、鉱油、カルナウバロウ、ポリエチレングリコールおよびそれらの混合物からなる群より選択される、請求項１の圧縮錠剤。
- 圧縮錠剤の総重量に基づき、さらに崩壊剤を約１〜２０％含む、請求項１の圧縮錠剤。
- 圧縮錠剤の総重量に基づき、さらに結合剤を約０.１〜１０％含む、請求項１の圧縮錠剤。
- 圧縮錠剤の総重量に基づき、さらに賦形剤を約５〜９０％含む、請求項１の圧縮錠剤。
- 圧縮錠剤の総重量に基づき、さらに顆粒外滑沢剤を約０.１〜３％含む、請求項１の圧縮錠剤。
- ラルテグラビル、硫酸アタザナビル、顆粒内滑沢剤、および顆粒外滑沢剤を含む圧縮錠剤であって、硫酸アタザナビルおよび顆粒内滑沢剤を顆粒内で混合し、顆粒外滑沢剤を顆粒外で加えることを特徴とする湿式造粒法によって製造される圧縮錠剤。
- 硫酸アタザナビルが１つの層中にあって、ラルテグラビルが別の層中にあることを特徴とする多層錠剤の形態である、請求項１の圧縮錠剤。
- 硫酸アタザナビルおよびラルテグラビルが同一の層中にあることを特徴とする一体型（monolith）錠剤の形態である、請求項１の圧縮錠剤。
- ラルテグラビル、硫酸アタザナビルおよび顆粒内滑沢剤を顆粒内で混合することを特徴とする湿式造粒法によって製造される、請求項１の圧縮錠剤。
- 硫酸アタザナビルおよび顆粒内滑沢剤を顆粒内で混合し、ラルテグラビルを顆粒外で加えることを特徴とする湿式造粒法によって製造される、請求項１の圧縮錠剤。
- 請求項１の圧縮錠剤を含むＨＩＶ感染治療剤。
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US94570607P | 2007-06-22 | 2007-06-22 | |
| PCT/US2008/067624 WO2009002823A2 (en) | 2007-06-22 | 2008-06-20 | Tableted compositions containing atazanavir |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010530889A JP2010530889A (ja) | 2010-09-16 |
| JP2010530889A5 true JP2010530889A5 (ja) | 2011-07-21 |
Family
ID=39645408
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010513433A Withdrawn JP2010530889A (ja) | 2007-06-22 | 2008-06-20 | アタザナビルを含む錠剤組成物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20100178339A1 (ja) |
| EP (1) | EP2178511B1 (ja) |
| JP (1) | JP2010530889A (ja) |
| KR (1) | KR20100033378A (ja) |
| CN (1) | CN101801348A (ja) |
| AT (1) | ATE499927T1 (ja) |
| AU (1) | AU2008268627A1 (ja) |
| DE (1) | DE602008005316D1 (ja) |
| ES (1) | ES2360336T3 (ja) |
| MX (1) | MX2009013462A (ja) |
| WO (1) | WO2009002823A2 (ja) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE602008005462D1 (de) * | 2007-06-22 | 2011-04-21 | Bristol Myers Squibb Co | Tablettierte atazanavirhaltige zusammensetzungen |
| AU2010313571B2 (en) | 2009-10-26 | 2014-07-31 | Merck Sharp & Dohme Llc | Solid pharmaceutical compositions containing an integrase inhibitor |
| WO2011127244A2 (en) * | 2010-04-09 | 2011-10-13 | Bristol-Myers Squibb Company | ATAZANAVIR SULFATE FORMULATIONS WITH IMPROVED pH EFFECT |
| WO2012041488A1 (en) | 2010-09-28 | 2012-04-05 | Ratiopharm Gmbh | Dry processing of atazanavir |
| EP2677868B1 (en) * | 2011-02-21 | 2020-01-15 | Hetero Research Foundation | Pharmaceutical compositions of maraviroc and process for the preparation thereof |
| CA2833006A1 (en) * | 2011-04-22 | 2012-10-26 | Merck Sharp & Dohme Corp. | Taste-masked formulations of raltegravir |
| US20140038992A1 (en) * | 2011-04-25 | 2014-02-06 | Hetero Research Foundation | Methods of administering raltegravir and raltegravir compositions |
| US9968607B2 (en) * | 2011-04-25 | 2018-05-15 | Hetero Research Foundation | Pharmaceutical compositions of raltegravir, methods of preparation and methods of use therof |
| WO2014064711A2 (en) * | 2012-10-22 | 2014-05-01 | Hetero Research Foundation | Methods of administering raltegravir and raltegravir compositions |
| ES2693580T3 (es) * | 2013-10-07 | 2018-12-12 | Bristol-Myers Squibb Holdings Ireland | Formulación de tratamiento del VIH de atazanavir y cobicistat |
| KR101497508B1 (ko) * | 2013-12-20 | 2015-03-03 | 한국유나이티드제약 주식회사 | 펠라고니움 시도이데스 추출물 및 규산 화합물을 포함하는 고형 제제 및 이의 제조 방법 |
| CN105237526B (zh) * | 2014-06-20 | 2018-01-23 | 朱靖华 | 一种抗艾滋病毒药物及其制备方法 |
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-
2008
- 2008-06-20 KR KR1020097026605A patent/KR20100033378A/ko not_active Application Discontinuation
- 2008-06-20 AU AU2008268627A patent/AU2008268627A1/en not_active Abandoned
- 2008-06-20 AT AT08780880T patent/ATE499927T1/de not_active IP Right Cessation
- 2008-06-20 WO PCT/US2008/067624 patent/WO2009002823A2/en active Application Filing
- 2008-06-20 MX MX2009013462A patent/MX2009013462A/es active IP Right Grant
- 2008-06-20 JP JP2010513433A patent/JP2010530889A/ja not_active Withdrawn
- 2008-06-20 US US12/664,793 patent/US20100178339A1/en not_active Abandoned
- 2008-06-20 ES ES08780880T patent/ES2360336T3/es active Active
- 2008-06-20 DE DE602008005316T patent/DE602008005316D1/de active Active
- 2008-06-20 EP EP08780880A patent/EP2178511B1/en not_active Not-in-force
- 2008-06-20 CN CN200880103525A patent/CN101801348A/zh active Pending
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