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1. 发明授权

US08703202B2 Coated tablets 有权
标题翻译：涂层片剂
公开(公告)号：US08703202B2
公开(公告)日：2014-04-22
申请号：US11492373
申请日：2006-07-24
申请人： Michael Vachon , Mishra K. Awadhesh , Robert A. Snow , Pol-Henri Guivarc'h
发明人： Michael Vachon , Mishra K. Awadhesh , Robert A. Snow , Pol-Henri Guivarc'h
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20 , A61K31/19 , A61K31/216 , A61K9/48
CPC分类号： A61K9/14 , A61K9/145 , A61K9/146 , A61K9/148 , A61K9/16 , A61K9/1623 , A61K9/1629 , A61K9/167 , A61K9/1676 , A61K9/19 , A61K9/20 , A61K9/2077 , A61K9/282 , A61K9/284 , A61K9/2866 , A61K9/48 , A61K31/192 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/505 , A61K31/66 , A61K2300/00
摘要： Disclosed is a pharmaceutically acceptable oral dosage form comprising fenofibrate, phospholipid, a buffer salt, a water-soluble bulking agent selected from maltodextrin, mannitol, and combinations thereof, a cellulosic additive, beads or crystals of a pharmaceutically acceptable water-soluble excipient support material, a polyvinylpyrrolidone or crospovidone, croscarmellose sodium, granular mannitol, sodium dodecyl sulfate, silicon dioxide, and a stearate, wherein the fenofibrate is in the form of microparticles, and wherein at least a portion of the phospholipid is coated on the surfaces of the fenofibrate microparticles, the phospholipid coated microparticles are embedded in a matrix comprising the water-soluble bulking agent, phospholipid that is not coated on the microparticles, the buffer salt and the cellulosic additive, and the matrix is coated on up to 100% of the surfaces of the beads or crystals of the excipient support material.
摘要翻译：公开了包含非诺贝特，磷脂，缓冲盐，选自麦芽糖糊精，甘露糖醇及其组合的水溶性填充剂的药学上可接受的口服剂型，纤维素添加剂，药学上可接受的水溶性赋形剂载体材料的珠粒或晶体，聚乙烯吡咯烷酮或交聚维酮，交联羧甲基纤维素钠，颗粒状甘露醇，十二烷基硫酸钠，二氧化硅和硬脂酸盐，其中非诺贝特为微粒形式，并且其中至少一部分磷脂被涂覆在非诺贝特微粒，将包含磷脂的微粒嵌入包含水溶性填充剂的基质，未涂覆在微粒上的磷脂，缓冲盐和纤维素添加剂，并且将基质涂覆在至多100％的表面上赋形剂载体材料的珠粒或晶体。

2. 发明授权

US06604698B2 Media milling 有权
公开(公告)号：US06604698B2
公开(公告)日：2003-08-12
申请号：US09852054
申请日：2001-05-10
申请人： Frank H. Verhoff , Robert A. Snow , Gary W. Pace
发明人： Frank H. Verhoff , Robert A. Snow , Gary W. Pace
IPC分类号： B02C1716
CPC分类号： A61K9/14 , A61K9/145 , B02C17/161 , Y10S977/775 , Y10S977/797 , Y10S977/90
摘要： This invention describes a process for preparing a dispersion of solid particles of a milled substrate in a fluid carrier comprising the steps of (a) providing a plurality of large size milling media to the milling chamber of a media mill and forming a depth filter therefrom on an exit screen or separator in the milling chamber; (b) adding to said milling chamber a plurality of small size milling media optionally containing additional large size milling media, a conglomerate of a solid substance comprising a substrate to be milled and optionally one or more than one surface active substance, and a fluid carrier; (c) milling said conglomerate in said milling chamber to produce very small milled substrate product particles; and (d) separating said milled substrate particles suspended in said fluid carrier from the media through said depth filter; wherein the exit screen comprises openings of size S0; the large size media have a size distribution S1 of which all are larger than S0; the small size media have a size distribution S2 which are smaller than S0; the very small milled substrate particles have a size distribution S3 and are smaller than all of the small media; and the large size media and the small size media are essentially retained in the milling chamber.

3. 发明授权

US06465016B2 Cyclosporiine particles 有权
公开(公告)号：US06465016B2
公开(公告)日：2002-10-15
申请号：US09750218
申请日：2000-12-29
申请人： Indu Parikh , Robert A. Snow
发明人： Indu Parikh , Robert A. Snow
IPC分类号： A61K914
CPC分类号： B82Y5/00 , A61K9/145
摘要： Pharmaceutical compositions containing solid cyclic oligopeptide cyclosporine microparticles are prepared by applying energy input to solid cyclic oligopeptide cyclosporine in the presence of phospholipid and one or more non-ionic, anionic or cationic second surface modifiers. The microparticles consist essentially of a solid cyclic oligopeptide cyclosporine core coated with a combination of phospholipid and at least one second surface modifier. The combination of phospholipid and second surface modifier(s) provide volume-weighted mean particle size values of solid cyclic oligopeptide cyclosporine particles that are about 50% smaller than cyclic oligopeptide cyclosporine particles produced in the presence of the phospholipid and without the presence of the second surface modifier(s) using the same energy input.

4. 发明授权

US5932188A Therapeutic and diagnostic imaging compositions and methods 失效
标题翻译：治疗和诊断成像组合物和方法
公开(公告)号：US5932188A
公开(公告)日：1999-08-03
申请号：US963125
申请日：1997-10-28
申请人： Robert A. Snow , David L. Ladd , John L. Toner
发明人： Robert A. Snow , David L. Ladd , John L. Toner
IPC分类号： A61K47/48 , A61K49/00 , A61K51/00 , A61K51/04 , C08G65/34 , C08G65/48 , C08G69/40 , A61B5/055 , C07F5/00
CPC分类号： A61K47/48215 , A61K47/48192 , A61K47/48207 , A61K51/0497 , A61K2123/00
摘要： This invention provides therapeutic and diagnostic imaging compositions and methods featuring a polymer comprising units containing a poly(alkylene oxide) moiety linked to the residue of a chelating agent, said polymer having a cytotoxic agent associated therewith.
摘要翻译：本发明提供治疗和诊断成像组合物和方法，其特征在于包含含有与螯合剂残基连接的聚（环氧烷）部分的单元的聚合物，所述聚合物具有与其相关的细胞毒性剂。

5. 发明授权

US5817292A MR imaging compositions and methods 失效
标题翻译： MR成像组合物和方法
公开(公告)号：US5817292A
公开(公告)日：1998-10-06
申请号：US960746
申请日：1992-10-14
申请人： Robert A. Snow , David L. Ladd , John L. Toner
发明人： Robert A. Snow , David L. Ladd , John L. Toner
IPC分类号： A61K49/06 , A61K49/12 , A61K49/00
CPC分类号： A61K49/128
摘要： This invention provides compositions useful in MR imaging comprising a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, the polymer having a paramagetic metal ion associated therewith.
摘要翻译：本发明提供了可用于MR成像的组合物，其包含包含与聚（环氧烷）部分连接的螯合剂残基的单元的聚合物，所述聚合物具有与其相关的参与性金属离子。

6. 发明授权

US5529915A Lyophilized polyethylene oxide modified protein and polypeptide complexes with cyclodextrin 失效
公开(公告)号：US5529915A
公开(公告)日：1996-06-25
申请号：US372621
申请日：1995-01-12
申请人： Christopher P. Phillips , Robert A. Snow
发明人： Christopher P. Phillips , Robert A. Snow
IPC分类号： A61K47/40 , A61K47/48 , C07K7/08 , C07K14/54 , C07K14/77 , C07K17/08 , C12N9/02 , C12N9/08 , C12N9/96 , C12N11/08 , A61K31/715 , A61K38/28
CPC分类号： B82Y5/00 , A61K47/48215 , A61K47/48969 , C07K14/5406 , C07K14/77 , C07K7/083 , C12N9/0065 , C12N9/0089 , C12N9/96
摘要： Disclosed are lyophilized biologically active proteinaceous compositions containing low diol polyalkylene oxide, such as polyethylene glycol, covalently attached to a biologically active proteinaceous substance and combined with the cryoprotectant cyclodextrin.

7. 发明授权

US4463080A Polymeric mordants 失效
标题翻译：聚合媒染剂
公开(公告)号：US4463080A
公开(公告)日：1984-07-31
申请号：US511425
申请日：1983-07-06
申请人： Robert A. Snow , Gerald W. Klein
发明人： Robert A. Snow , Gerald W. Klein
IPC分类号： C08F20/00 , C08F12/00 , C08F12/26 , C08F20/34 , C08F20/52 , C08F20/60 , C08F26/00 , C08F26/06 , G03C7/00 , G03C8/56 , G03C5/54 , G03C1/40
CPC分类号： G03C8/56 , Y10S430/142 , Y10T428/31855 , Y10T428/31931
摘要： Photographic elements and diffusion transfer assemblages are described which contain a novel polymeric mordant comprising recurring units having the formula ##STR1## wherein A represents recurring units derived from an .alpha.,.beta.-ethylenically unsaturated monomer;B represents recurring units derived from a monomer containing at least two ethylenically unsaturated groups;QN.sup..sym. represents a moiety containing a quaternized nitrogen group;R.sup.1 represents an alkoxy group having from 1 to about 8 carbon atoms or an alkylenedioxy group having from 1 to about 4 carbon atoms, the group being appended to an aromatic group of A;R.sup.2 represents an alkoxy group having from 1 to about 8 carbon atoms or an alkylenedioxy group having from 1 to about 4 carbon atoms, the group being appended to an aromatic group of QN.sup..sym. ;each n and m independently represents an integer from 0 to 5, with the proviso that the polymer contains recurring units having at least two alkoxy groups or one alkylenedioxy group;each R.sup.3 independently represents hydrogen or an alkyl group having from 1 to about 6 carbon atoms;X.sup..crclbar. represents an anion;x is from about 0 to about 80 mole percent;y is from about 20 to about 100 mole percent; andz is from about 0 to about 10 mole percent.
摘要翻译：描述了摄影元件和扩散转移组合物，其包含新型聚合物媒染剂，其包含具有下式的重复单元：其中A表示衍生自α，β-烯属不饱和单体的重复单元; B表示衍生自含有至少两个烯属不饱和基团的单体的重复单元; QN（+）表示含有季铵化氮基团的部分; R1表示具有1至约8个碳原子的烷氧基或具有1至约4个碳原子的亚烷基二氧基，该基团附加至A的芳族基团; R2表示具有1至约8个碳原子的烷氧基或具有1至约4个碳原子的亚烷基二氧基，该基团附加到QN（+）的芳族基团上; 每个n和m独立地表示0至5的整数，条件是聚合物含有具有至少两个烷氧基或一个亚烷基二氧基的重复单元; 每个R 3独立地表示氢或具有1至约6个碳原子的烷基; X（ - ）表示阴离子; x为约0至约80mol％; y为约20至约100摩尔％; 且z为约0至约10摩尔％。

8. 发明申请

US20120064160A1 Fibrate-statin Combinations with Reduced Fed-fasted Effects 审中-公开
标题翻译：抑制他汀类药物组合减少禁食效应
公开(公告)号：US20120064160A1
公开(公告)日：2012-03-15
申请号：US13295708
申请日：2011-11-14
申请人： Pol-Henri Guivarc'h , Indu Parikh , Robert A. Snow
发明人： Pol-Henri Guivarc'h , Indu Parikh , Robert A. Snow
IPC分类号： A61K9/28 , A61K31/225 , A61K31/40 , A61K31/505 , A61P3/00 , A61K31/4418 , A61K31/47 , A61K9/14 , A61P3/06 , A61K31/366 , A61K31/405
CPC分类号： A61K45/06 , A61K9/145 , A61K9/1623 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/505 , A61K31/66 , Y10S424/824 , Y10S977/906 , A61K2300/00
摘要： This invention discloses an orally administered pharmaceutical composition for the treatment of elevated levels of cholesterol and related conditions comprising a statin and fenofibrate in the form of microparticles of solid fenofibrate that are stabilized by phospholipid as a surface active substance, wherein a therapeutically effective amount of the composition provides the statin and a quantity of fenofibrate to a fasted human patient that is greater than 80% of the quantity of fenofibrate provided by the same amount of the composition when administered to the same patient who has been fed a high fat meal.
摘要翻译：本发明公开了一种口服给药的药物组合物，用于治疗胆固醇水平升高和相关病症，包括以磷脂作为表面活性物质稳定的固体非诺贝特微粒形式的他汀类药物和非诺贝特，其中治疗有效量的组合物向给予高脂肪膳食的同一患者施用时，对禁食的患者提供了他汀类药物和一定量的非诺贝特，其大于由相同量的组合物提供的非诺贝特量的80％。

9. 发明授权

US06696084B2 Spray drying process and compositions of fenofibrate 有权
标题翻译：喷雾干燥工艺和非诺贝特组合物
公开(公告)号：US06696084B2
公开(公告)日：2004-02-24
申请号：US09838593
申请日：2001-04-20
申请人： Gary W. Pace , Awadesh K. Mishra , Robert A. Snow , Indu Parikh , Pol-Henri W. Guivarc'h
发明人： Gary W. Pace , Awadesh K. Mishra , Robert A. Snow , Indu Parikh , Pol-Henri W. Guivarc'h
IPC分类号： A61K914
CPC分类号： A61K31/66 , A61K9/145 , A61K9/1623 , A61K31/216 , A61K31/22 , A61K31/365 , A61K31/40 , A61K31/405 , A61K31/44 , A61K31/505 , A61K45/06 , A61K31/215 , A61K2300/00
摘要： The present invention relates to a novel spray drying process for the preparation of pharmaceutical compositions containing small particles of phospholipid-stabilized fenofibrate. This invention also relates to spray dried powdered compositions prepared according to this process, and to dosage forms of fenofibrate (capsules, tablets, powders, granules, and dispersions) prepared from these powdered compositions. The powdered compositions and dosage forms are useful in the treatment of dyslipidemia and dyslipoproteinemia and have the advantage that they provide reduced in vivo variability in the bioavailability of fenofibrate active species among fed and fasted patients when administered orally.
摘要翻译：本发明涉及一种用于制备含有磷脂稳定的非诺贝特的小颗粒的药物组合物的新型喷雾干燥方法。本发明还涉及根据该方法制备的喷雾干燥的粉末组合物，以及由这些粉末状组合物制备的非诺贝特（胶囊，片剂，粉末，颗粒剂和分散体）的剂型。粉末组合物和剂型可用于治疗血脂异常和血脂异常，并且具有这样的优点：当口服给药时，它们在进食和禁食患者中提供非诺贝特活性物质的生物利用度的体内变异性降低。

10. 发明授权

US06634576B2 Milled particles 有权
公开(公告)号：US06634576B2
公开(公告)日：2003-10-21
申请号：US09940864
申请日：2001-08-29
申请人： Frank Verhoff , Gary W. Pace , Robert A. Snow , Fay Millar
发明人： Frank Verhoff , Gary W. Pace , Robert A. Snow , Fay Millar
IPC分类号： B02C1214
CPC分类号： A61K9/14
摘要： A process for milling a solid substrate in the milling chamber of a dispersion or media mill in the presence of a two or more compositions of milling media bodies is disclosed wherein all milling media bodies contribute to the grinding of the solid substrate and wherein at least one composition of media bodies provides fragments of milling media bodies that are retained with the milled solid substrate particles in the form of a synergetic commixture produced in the milling process. More specifically, a process is disclosed for preparing a synergetic commixture comprising small particles of a solid substrate and small particulates of a first material of a desired size comprising the steps of (a) providing to the milling chamber of a media mill a contents comprising a pre-mix of a solid substrate, a fluid carrier, a plurality of milling bodies of a first material having a fracture toughness Kc1, and a plurality of milling bodies of a second material having a fracture toughness Kc2; (b) operating the media mill to grind the solid substrate and degrade at least a portion of the milling bodies of first material to produce a dispersion in the fluid carrier comprising a synergetic commixture of small particulates of the first material and small particles of the solid substrate having a desired size equal to or less than a size Sp; (c) separating the dispersion from any milling bodies and solid substrate particles having a size larger than Sp; and (d) optionally removing the fluid carrier from the dispersion to form a synergetic commixture free of fluid and comprising the particles and the small particulates, wherein KC2 is greater than KC1.

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