JP2010530890A5 - - Google Patents
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- JP2010530890A5 JP2010530890A5 JP2010513435A JP2010513435A JP2010530890A5 JP 2010530890 A5 JP2010530890 A5 JP 2010530890A5 JP 2010513435 A JP2010513435 A JP 2010513435A JP 2010513435 A JP2010513435 A JP 2010513435A JP 2010530890 A5 JP2010530890 A5 JP 2010530890A5
- Authority
- JP
- Japan
- Prior art keywords
- compressed tablet
- sulfate
- lubricant
- compressed
- 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.)
- Pending
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- 239000007891 compressed tablet Substances 0.000 claims 23
- 239000000314 lubricant Substances 0.000 claims 12
- 108010019625 Atazanavir Sulfate Proteins 0.000 claims 7
- 229960003796 Atazanavir sulfate Drugs 0.000 claims 7
- DQSGVVGOPRWTKI-QVFAWCHISA-N atazanavir sulfate Chemical compound [H+].[H+].[O-]S([O-])(=O)=O.C([C@H](NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)[C@@H](O)CN(CC=1C=CC(=CC=1)C=1N=CC=CC=1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C1=CC=CC=C1 DQSGVVGOPRWTKI-QVFAWCHISA-N 0.000 claims 7
- 239000008187 granular material Substances 0.000 claims 6
- JTEGQNOMFQHVDC-NKWVEPMBSA-N 4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]-1,2-dihydropyrimidin-2-one Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1 JTEGQNOMFQHVDC-NKWVEPMBSA-N 0.000 claims 5
- 229960001627 Lamivudine Drugs 0.000 claims 5
- 229960000531 abacavir sulfate Drugs 0.000 claims 5
- WMHSRBZIJNQHKT-FFKFEZPRSA-N abacavir sulfate Chemical compound OS(O)(=O)=O.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 WMHSRBZIJNQHKT-FFKFEZPRSA-N 0.000 claims 5
- 238000005550 wet granulation Methods 0.000 claims 3
- IPCSVZSSVZVIGE-UHFFFAOYSA-N Palmitic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 claims 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N Stearic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 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
- CJZGTCYPCWQAJB-UHFFFAOYSA-L Calcium stearate Chemical compound [Ca+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O CJZGTCYPCWQAJB-UHFFFAOYSA-L 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
- 208000005721 HIV Infections 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
- WXMKPNITSTVMEF-UHFFFAOYSA-M Sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 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
- UGWQMIXVUBLMAH-IVVFTGHFSA-N [(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol;4-amino-1-[(2R,5S)-2-(hydroxymethyl)-1,3-oxathiolan-5-yl]pyrimidin-2-one Chemical compound O=C1N=C(N)C=CN1[C@H]1O[C@@H](CO)SC1.C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 UGWQMIXVUBLMAH-IVVFTGHFSA-N 0.000 claims 1
- 239000011230 binding agent Substances 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
- 229940075507 glyceryl monostearate Drugs 0.000 claims 1
- 229940046813 glyceryl palmitostearate Drugs 0.000 claims 1
- 201000001820 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
- KREXGRSOTUKPLX-UHFFFAOYSA-N octadecanoic acid;zinc Chemical compound [Zn].CCCCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O KREXGRSOTUKPLX-UHFFFAOYSA-N 0.000 claims 1
- 239000003921 oil Substances 0.000 claims 1
- 235000019198 oils Nutrition 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- VBICKXHEKHSIBG-UHFFFAOYSA-N rac-1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 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
- STFSJTPVIIDAQX-LTRPLHCISA-M sodium;(E)-4-octadecoxy-4-oxobut-2-enoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCCOC(=O)\C=C\C([O-])=O STFSJTPVIIDAQX-LTRPLHCISA-M 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
Claims (15)
- 硫酸アバカビル、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。
- さらにラミブジンを含む、請求項１の圧縮錠剤。
- 硫酸アバカビル、ラミブジン、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、少なくとも１つの硫酸アバカビルまたはラミブジン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９の圧縮錠剤。
- 硫酸アタザナビル、硫酸アバカビルおよびラミブジン並びに他の治療剤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９の圧縮錠剤。
- （ｉ）少なくとも１つの硫酸アバカビルまたはラミブジン、（ｉｉ）硫酸アタザナビルおよび（ｉｉｉ）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９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、少なくとも１つの硫酸アバカビルまたはラミブジン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９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 |
|---|---|---|---|
| US94569107P | 2007-06-22 | 2007-06-22 | |
| PCT/US2008/067629 WO2009002826A2 (en) | 2007-06-22 | 2008-06-20 | Tableted compositions containing atazanavir |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2010530890A JP2010530890A (ja) | 2010-09-16 |
| JP2010530890A5 true JP2010530890A5 (ja) | 2011-07-21 |
Family
ID=39645379
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010513435A Pending JP2010530890A (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) | US20100178340A1 (ja) |
| EP (1) | EP2178512B1 (ja) |
| JP (1) | JP2010530890A (ja) |
| KR (1) | KR20100033379A (ja) |
| CN (1) | CN101778625A (ja) |
| AT (1) | ATE500820T1 (ja) |
| AU (1) | AU2008268630A1 (ja) |
| DE (1) | DE602008005462D1 (ja) |
| ES (1) | ES2359770T3 (ja) |
| MX (1) | MX2009013499A (ja) |
| WO (1) | WO2009002826A2 (ja) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10071059B2 (en) * | 2009-12-18 | 2018-09-11 | Frieslandcampina Nederland Holding B.V. | Co-processed tablet excipient composition its preparation and use |
| KR101317809B1 (ko) | 2011-06-07 | 2013-10-16 | 한미약품 주식회사 | 암세포의 성장을 억제하는 아마이드 유도체 및 비금속염 활택제를 포함하는 약학 조성물 |
| WO2013057469A1 (en) * | 2011-10-20 | 2013-04-25 | Cipla Limited | Pharmaceutical antiretroviral compositions |
| US20140315936A1 (en) * | 2011-11-18 | 2014-10-23 | Avexa Limited | Apricitabine and pi combination therapy |
| KR20140096571A (ko) | 2013-01-28 | 2014-08-06 | 한미약품 주식회사 | 1-(4-(4-(3,4-디클로로-2-플루오로페닐아미노)-7-메톡시퀴나졸린-6-일옥시)피페리딘-1-일)프로프-2-엔-1-온의 제조방법 |
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-
2008
- 2008-06-20 MX MX2009013499A patent/MX2009013499A/es active IP Right Grant
- 2008-06-20 WO PCT/US2008/067629 patent/WO2009002826A2/en active Application Filing
- 2008-06-20 DE DE602008005462T patent/DE602008005462D1/de active Active
- 2008-06-20 AT AT08771565T patent/ATE500820T1/de not_active IP Right Cessation
- 2008-06-20 KR KR1020097026606A patent/KR20100033379A/ko not_active Application Discontinuation
- 2008-06-20 JP JP2010513435A patent/JP2010530890A/ja active Pending
- 2008-06-20 EP EP08771565A patent/EP2178512B1/en not_active Not-in-force
- 2008-06-20 AU AU2008268630A patent/AU2008268630A1/en not_active Abandoned
- 2008-06-20 CN CN200880103691A patent/CN101778625A/zh active Pending
- 2008-06-20 US US12/664,806 patent/US20100178340A1/en not_active Abandoned
- 2008-06-20 ES ES08771565T patent/ES2359770T3/es active Active
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