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1.发明授权Methods of treating mammals using nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors 失效使用人类免疫缺陷病毒（HIV）蛋白酶抑制剂的纳米晶体制剂治疗哺乳动物的方法公开(公告)号：US06221400B1
公开(公告)日：2001-04-24
申请号：US09225498
申请日：1999-01-06
申请人： Gary G. Liversidge , David A. Engers , Mary E. Roberts , Stephen B. Ruddy , Sui-Ming Wong , Shuqian Xu
发明人： Gary G. Liversidge , David A. Engers , Mary E. Roberts , Stephen B. Ruddy , Sui-Ming Wong , Shuqian Xu
IPC分类号： A61K914
CPC分类号： B82Y5/00 , A61K9/146 , A61K9/2077 , A61K9/5161 , A61K31/192 , A61K31/366 , A61K31/427 , A61K31/472 , A61K31/4725 , A61K31/551 , A61K31/635 , A61K38/55
摘要： The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.
摘要翻译： 本发明描述了包含纤维素表面稳定剂的纳米颗粒HIV蛋白酶抑制剂的制剂。 纳米颗粒制剂在体外具有增加的溶出速率，体内吸收速率增加，进食/禁食率变异性降低，吸收变异性降低。 本发明还涉及制备新配方的方法。 特别地，描述了HIV 1型（HIV-1）和2型（HIV-2）蛋白酶抑制剂的纳米颗粒制剂。
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2.发明授权Methods of making nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors using cellulosic surface stabilizers 有权使用纤维素表面稳定剂制备人类免疫缺陷病毒（HIV）蛋白酶抑制剂的纳米晶体制剂的方法
公开(公告)号：US6068858A
公开(公告)日：2000-05-30
申请号：US225493
申请日：1999-01-06
申请人： Gary G. Liversidge , David A. Engers , Mary E. Roberts , Stephen B. Ruddy , Sui-Ming Wong , Shuqian Xu
发明人： Gary G. Liversidge , David A. Engers , Mary E. Roberts , Stephen B. Ruddy , Sui-Ming Wong , Shuqian Xu
IPC分类号： A61K9/14 , A61K9/20 , A61K9/51 , A61K31/192 , A61K31/366 , A61K31/427 , A61K31/472 , A61K31/4725 , A61K31/551 , A61K31/635 , A61K38/55
CPC分类号： A61K9/5161 , A61K31/192 , A61K31/366 , A61K31/427 , A61K31/472 , A61K31/4725 , A61K31/551 , A61K31/635 , A61K9/146 , A61K9/2077 , A61K9/5192
摘要： The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increased rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HV-2) protease inhibitors are described.
摘要翻译： 本发明描述了包含纤维素表面稳定剂的纳米颗粒HIV蛋白酶抑制剂的制剂。 纳米颗粒制剂在体外具有增加的溶出速率，体内吸收速率增加，进食/禁食率变异性降低，吸收变异性降低。 本发明还涉及制备新配方的方法。 特别地，描述了HIV 1型（HIV-1）和2型（HV-2）蛋白酶抑制剂的纳米颗粒制剂。
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3.发明授权X-ray contrast compositions containing iodophenoxyalkanes and pharmaceutically acceptable clays 失效含有碘苯氧基烷烃和药学上可接受的粘土的X射线对比组合物
公开(公告)号：US5476646A
公开(公告)日：1995-12-19
申请号：US230580
申请日：1994-04-21
CPC分类号： A61K49/04 , A61K49/0404 , A61K49/0409 , A61K49/0442 , A61K49/0461 , B82Y5/00 , Y10S424/90 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising a nonionic x-ray producing agent in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译： 公开了用于口服或逆行检查胃肠道的X射线造影剂组合物，其包含与药学上可接受的载体中的药学上可接受的粘土组合的非离子X射线产生剂; 以及它们用于胃肠道诊断放射学的方法。
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4.发明授权
公开(公告)号：US5472682A
公开(公告)日：1995-12-05
申请号：US249424
申请日：1994-05-26
申请人： Stephen B. Ruddy , Mary E. Roberts , Gregory L. McIntire , Eugene R. Cooper , Kimberly G. Estep
发明人： Stephen B. Ruddy , Mary E. Roberts , Gregory L. McIntire , Eugene R. Cooper , Kimberly G. Estep
IPC分类号： A61K49/04 , C07C69/017 , C07C69/63 , C07C69/74 , C07C309/65 , A61K31/22
CPC分类号： C07C69/74 , A61K49/04 , A61K49/0404 , A61K49/0409 , A61K49/0433 , C07C309/65 , C07C69/017 , C07C69/63
摘要： Disclosed are x-ray contrast compositions of the formula ##STR1## wherein X is ##STR2## or --SO.sub.2 --; Z is H, halo, methyl, ethyl, n-propyl, C.sub.4 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl or aryl each of which may be optionally substituted with halo, fluoro-lower-alkyl, lower-alkoxy, hydroxy, carboxy or lower-alkoxy carbonyl; lower-alkenyl, lower-alkynyl, lower-alkylene or lower-alkoxy-carbonyloxy;n is 1-5;y is 0-4; andw is 1-4;in combination with a pharmaceutically acceptable clay; and method for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译： 公开了下式的X射线造影剂组合物，其中X是或-SO 2; Z是H，卤素，甲基，乙基，正丙基，C 4 -C 20烷基，环烷基，低级烷氧基，氰基，其中烷基和环烷基可被卤素或卤代低级烷基取代; R是C 1 -C 25烷基，环烷基或芳基，其各自可以任选被卤素，氟 - 低级 - 烷基，低级 - 烷氧基，羟基，羧基或低级 - 烷氧基羰基取代; 低级烯基，低级炔基，低级亚烷基或低级烷氧基 - 羰基氧基; n为1-5; y为0-4; w为1-4; 与药学上可接受的粘土组合; 及其用于胃肠道诊断放射学的方法。
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5.发明授权Compositions of iodophenoxy alkanes and iodophenyl ethers and pharmaceutically acceptable clays for visualization of the gastrointestinal tract 失效碘苯氧基烷烃和碘苯基醚的组合物和用于胃肠道可视化的药学上可接受的粘土
公开(公告)号：US5531979A
公开(公告)日：1996-07-02
申请号：US247438
申请日：1994-05-23
IPC分类号： A61K49/00 , A61K49/04 , C07C43/225 , C07C43/247 , C07C255/54
CPC分类号： A61K49/0404 , A61K49/04 , A61K49/0409 , A61K49/0433 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkanes and iodophenyl ethers as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译： 公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含碘苯氧基烷烃和碘苯基醚作为x射线产生剂与药学上可接受的载体中的药学上可接受的粘土的组合; 以及它们用于胃肠道诊断放射学的方法。
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公开(公告)号：US5718919A
公开(公告)日：1998-02-17
申请号：US393648
申请日：1995-02-24
申请人： Stephen B. Ruddy , Mary E. Roberts
发明人： Stephen B. Ruddy , Mary E. Roberts
IPC分类号： A61K9/14 , A61K31/192 , A61K9/16
CPC分类号： A61K9/146 , A61K31/192 , Y10S977/775 , Y10S977/915
摘要： There is described a composition comprised of nanoparticles of a therapeutic agent having a surface modifier adsorbed on the surface thereof. The present composition is characterized in that the therapeutic agent is ibuprofen or fenoprofen which is substantially enriched in the R(-) enantiomer.
摘要翻译： 描述了由表面改性剂吸收在其表面上的具有治疗剂的纳米颗粒组成的组合物。 本发明的组合物的特征在于治疗剂是基本上富含R（ - ）对映异构体的布洛芬或非诺洛芬。
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7.发明授权
公开(公告)号：US5593657A
公开(公告)日：1997-01-14
申请号：US386027
申请日：1995-02-09
IPC分类号： A61K49/04
CPC分类号： A61K49/0404 , Y10S514/941 , Y10S977/773 , Y10S977/927 , Y10S977/928
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising nanoparticles of a barium salt having associated with its surface non-ionic and anionic stabilizers; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译： 公开了用于口腔或逆行检查胃肠道的x射线造影剂组合物，其包含与其表面非离子和阴离子稳定剂相关联的钡盐纳米颗粒; 以及它们用于胃肠道诊断放射学的方法。
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8.发明授权Compositions of iodophenoxy alkylene ethers and pharmaceutically acceptable clays for visualization of the gastrointestinal tract 失效碘苯氧基亚烷基醚的组合物和用于胃肠道可视化的药学上可接受的粘土
公开(公告)号：US5492687A
公开(公告)日：1996-02-20
申请号：US237502
申请日：1994-05-03
IPC分类号： A61K49/04 , C07C43/225
CPC分类号： A61K49/0404 , A61K49/04 , A61K49/0409 , A61K49/0461 , C07C43/225
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkylene ethers and pharmaceutically acceptable clays in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译： 公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含药学上可接受的载体中的碘苯氧基亚烷基醚和药学上可接受的粘土; 以及它们用于胃肠道诊断放射学的方法。
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9.发明授权Nanocrystalline formulations of human immunodeficiency virus (HIV) protease inhibitors using cellulosic surface stabilizers 失效使用纤维素表面稳定剂的人类免疫缺陷病毒（HIV）蛋白酶抑制剂的纳米晶体制剂
公开(公告)号：US6045829A
公开(公告)日：2000-04-04
申请号：US890602
申请日：1997-07-09
申请人： Gary G. Liversidge , David A. Engers , Mary E. Roberts , Stephen B. Ruddy , Sui-Ming Wong , Shuqian Xu
发明人： Gary G. Liversidge , David A. Engers , Mary E. Roberts , Stephen B. Ruddy , Sui-Ming Wong , Shuqian Xu
IPC分类号： C12N9/99 , A61K9/14 , A61K9/18 , A61K9/20 , A61K9/51 , A61K31/192 , A61K31/366 , A61K31/427 , A61K31/472 , A61K31/4725 , A61K31/496 , A61K31/551 , A61K31/635 , A61K38/55 , A61K45/08 , A61K47/38
CPC分类号： B82Y5/00 , A61K31/192 , A61K31/366 , A61K31/427 , A61K31/472 , A61K31/4725 , A61K31/551 , A61K31/635 , A61K38/55 , A61K9/146 , A61K9/2077 , A61K9/5161
摘要： The present invention describes formulations of nanoparticulate HIV protease inhibitors comprising a cellulosic surface stabilizer. The nanoparticulate formulations have an increased rate of dissolution in vitro, an increase rate of absorption in vivo, a decreased fed/fasted ratio variability, and a decreased variability in absorption. The present invention is also directed to methods of making the novel formulations. In particular, nanoparticulate formulations of HIV type 1 (HIV-1) and type 2 (HIV-2) protease inhibitors are described.
摘要翻译： 本发明描述了包含纤维素表面稳定剂的纳米颗粒HIV蛋白酶抑制剂的制剂。 纳米颗粒制剂在体外具有增加的溶出速率，体内吸收的增加速率，减少的进食/禁食率变异性以及降低的吸收变异性。 本发明还涉及制备新配方的方法。 特别地，描述了HIV 1型（HIV-1）和2型（HIV-2）蛋白酶抑制剂的纳米颗粒制剂。
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10.发明授权Compositions of iodobenzoic acid derivatives and pharmaceutically acceptable clays for visualization of the gastrointestinal tract 失效碘苯甲酸衍生物的组合物和用于胃肠道可视化的药学上可接受的粘土
公开(公告)号：US5484585A
公开(公告)日：1996-01-16
申请号：US239090
申请日：1994-05-05
IPC分类号： A61K49/04
CPC分类号： A61K49/0409 , A61K49/04 , A61K49/0404 , A61K49/0433 , Y10S514/941 , Y10S514/942
摘要： Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodobenzoic acid derivatives as the x-ray producing agents in combination with a pharmaceutically acceptable clay in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.
摘要翻译： 公开了用于口服或逆行检查胃肠道的x射线造影剂组合物，其包含碘代苯甲酸衍生物作为x射线产生剂与药学上可接受的载体中的药学上可接受的粘土的组合; 以及它们用于胃肠道诊断放射学的方法。
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