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公开(公告)号：US06365188B1
公开(公告)日：2002-04-02
申请号：US09081808
申请日：1998-05-20
IPC分类号： A61K914
CPC分类号： B82Y5/00 , A61K9/1694 , A61K47/6951
摘要： Process for preparing a solid mixture comprising one or more cyclodextrins and an insoluble active ingredient characterized in that said process comprises a melt-extrusion step, wherein the active ingredient is embedded into the cyclodextrin carrier.
摘要翻译： 制备包含一种或多种环糊精和不溶性活性成分的固体混合物的方法，其特征在于所述方法包括熔融挤出步骤，其中活性成分嵌入到环糊精载体中。
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公开(公告)号：US06509038B2
公开(公告)日：2003-01-21
申请号：US09194480
申请日：1998-11-19
IPC分类号： A61K936
CPC分类号： A61K9/146 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2866 , A61K31/496
摘要： The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.
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公开(公告)号：US08591948B2
公开(公告)日：2013-11-26
申请号：US11445849
申请日：2006-06-01
IPC分类号： A61K9/36 , A61K9/20 , A61K9/28 , A61K9/30 , A61K31/497
CPC分类号： A61K9/146 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2866 , A61K31/496
摘要： The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.
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公开(公告)号：US07081255B2
公开(公告)日：2006-07-25
申请号：US10218851
申请日：2002-08-14
IPC分类号： A61K9/36 , A61K9/20 , A61K9/28 , A61K9/30 , A61K31/497
CPC分类号： A61K9/146 , A61K9/1652 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2866 , A61K31/496
摘要： The present invention is concerned with novel pharmaceutical compositions of itraconazole which can be administered to a mammal suffering from a fungal infection, whereby a single such dosage form can be administered once daily, and in addition at any time of the day independently of the food taken in by said mammal. These novel compositions comprise particles obtainable by melt-extruding a mixture comprising itraconazole and an appropriate water-soluble polymer and subsequently milling said melt-extruded mixture.
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公开(公告)号：US20120201868A1
公开(公告)日：2012-08-09
申请号：US13497719
申请日：2010-09-22
IPC分类号： A61K31/427 , A61P31/18 , A61K9/14 , B82Y5/00
CPC分类号： A61K9/0019 , A61K9/51 , A61K31/352 , A61K47/10 , A61K47/26
摘要： This invention relates to the long term treatment of HIV infection by intermittently administering a parenteral formulation comprising brecanavir at relatively long time intervals. This invention further concerns pharmaceutical compositions for parenteral administration, comprising micro- or nanoparticles of brecanavir, suspended in an aqueous pharmaceutically acceptable carrier, for the treatment and prophylaxis of HIV infection.
摘要翻译： 本发明涉及通过以相当长的时间间隔间歇施用包含布雷必匹韦的胃肠外制剂来长期治疗HIV感染。 本发明进一步涉及用于肠胃外给药的药物组合物，其包含悬浮在药学上可接受的载体的水中的雷帕霉素的微粒或纳米颗粒，用于治疗和预防HIV感染。
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6.发明申请公开(公告)号：US20080287488A1
公开(公告)日：2008-11-20
申请号：US11911465
申请日：2006-04-14
申请人： Gerben Albert Eleutherius Van 'T Klooster , Piet Tom Bert Paul Wigerinck , Sandra De Meyer , Lieven Elvire Colette Baert , Herman Augustinus De Kock
发明人： Gerben Albert Eleutherius Van 'T Klooster , Piet Tom Bert Paul Wigerinck , Sandra De Meyer , Lieven Elvire Colette Baert , Herman Augustinus De Kock
IPC分类号： A61K31/427 , A61K31/428 , A61K31/47 , A61P31/18
CPC分类号： C07D417/12
摘要： A method for improving the pharmacokinetics of drugs, which are metabolized by cytochrome P450 monooxygenase is disclosed. More specifically it relates to a method for improving the pharmacokinetics of retroviral protease inhibitors and in particular for improving the pharmacokinetics of human immunodeficiency virus (HIV) protease inhibitors. A pharmaceutical composition and its use in the manufacture of a medicament for the inhibition or treatment of an HIV infection or AIDS in a human being are also part of the invention.
摘要翻译： 公开了一种改善由细胞色素P450单加氧酶代谢的药物的药代动力学的方法。 更具体地说，本发明涉及一种用于改善逆转录病毒蛋白酶抑制剂的药代动力学的方法，特别涉及改善人类免疫缺陷病毒（HIV）蛋白酶抑制剂的药代动力学。 药物组合物及其在制备用于抑制或治疗人体中的HIV感染或AIDS的药物中的用途也是本发明的一部分。
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公开(公告)号：US10953009B2
公开(公告)日：2021-03-23
申请号：US12161445
申请日：2007-01-19
IPC分类号： A61K31/505
摘要： This invention relates to the use of a parenteral formulation comprising an anti-virally effective amount of TMC278 or a pharmaceutically acceptable acid-addition salt thereof, and a carrier, for the manufacture of a medicament for the treatment of a subject being infected with HIV, wherein the formulation is to be administered intermittently at a time interval of at least one week.
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公开(公告)号：US08754093B2
公开(公告)日：2014-06-17
申请号：US13262077
申请日：2010-03-26
IPC分类号： C07D239/46 , A61K31/455
CPC分类号： A61K31/513 , A61K9/4866 , A61K31/455 , A61K45/06 , A61K47/6949 , B82Y5/00 , C07D213/82 , C07D239/48 , A61K2300/00
摘要： Etravirine (TMC125) nicotinamide co-crystal, its preparation, and use in the treatment of HIV infection.
摘要翻译： 艾司伐林（TMC125）烟酰胺共晶，其制备及用于治疗艾滋病毒感染。
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公开(公告)号：US20120028998A1
公开(公告)日：2012-02-02
申请号：US13262077
申请日：2010-03-26
IPC分类号： A61K31/505 , A61P31/18 , C07D239/48
CPC分类号： A61K31/513 , A61K9/4866 , A61K31/455 , A61K45/06 , A61K47/6949 , B82Y5/00 , C07D213/82 , C07D239/48 , A61K2300/00
摘要： Etravirine (TMC125) nicotinamide co-crystal, its preparation, and use in the treatment of HIV infection.
摘要翻译： 艾司伐林（TMC125）烟酰胺共晶，其制备及用于治疗艾滋病毒感染。
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公开(公告)号：US20090197903A1
公开(公告)日：2009-08-06
申请号：US12302366
申请日：2007-06-06
IPC分类号： A61K31/505
CPC分类号： A61K9/1652
摘要： This invention relates to a process for producing a spray-dried powder comprising microcrystalline cellulose in a solid dispersion of the anti-HIV compound etravirine (TMC125) in a water-soluble polymer.
摘要翻译： 本发明涉及在水溶性聚合物中含有抗HIV化合物依曲韦林（TMC125）的固体分散体中的微晶纤维素的喷雾干燥粉末的制造方法。
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