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1. 发明授权

US06805881B1 Multiple unit controlled food effect-independent release pharmaceutical preparations and method for preparing the same 失效
标题翻译：多单位对照食品效应无关药物制剂及其制备方法
公开(公告)号：US06805881B1
公开(公告)日：2004-10-19
申请号：US09787229
申请日：2001-04-23
申请人： Venkata-Rangarao Kanikanti , Roland Rupp , Erich Brendel , Claus Weisemann , Ernst Chantraine
发明人： Venkata-Rangarao Kanikanti , Roland Rupp , Erich Brendel , Claus Weisemann , Ernst Chantraine
IPC分类号： A61K914
CPC分类号： A61K31/4422 , A61K9/1652
摘要： The present invention relates to orally administrable multiple-unit sustained-release dose forms having controlled agitation-independent release of active compound and processes for their production using a selected erodable hydrophilic polymer (HPC) and a limitation of the maximum size of the active compound-containing polymer particles to ≦3 mm.
摘要翻译：本发明涉及具有受控搅动独立的活性化合物释放的可口服给药的多单位缓释剂量形式及其使用选择的可侵蚀亲水性聚合物（HPC）的生产方法，以及活性化合物 - 含有聚合物颗粒至<= 3MM。

2. 发明授权

US06780436B1 Solid oral pharmaceutical formulation of modified release that contains an acid labile benzimidazole compound 有权
标题翻译：含有不稳定苯并咪唑化合物的固体口服药物制剂
公开(公告)号：US06780436B1
公开(公告)日：2004-08-24
申请号：US09660022
申请日：2000-09-12
申请人： Antonio López-Cabrera , Pedro Juan Solanas-Ibarra , Vincent Mancinelli
发明人： Antonio López-Cabrera , Pedro Juan Solanas-Ibarra , Vincent Mancinelli
IPC分类号： A61K914
CPC分类号： A61K31/444 , A61K9/5026 , A61K9/5078
摘要： The pharmaceutical formulation consists of a number of pellets that comprise an inert nucleus, a layer with the active ingredient, one or more intermediate layers that comprise at least a system of modified release, and an external layer of enteric coating. These pellets can be obtained applying the different layers by means of fluid bed coating techniques using aqueous solutions or suspensions of the components of such layers. The pharmaceutical formulations can be hard gelatin capsules or tablets and are suitable for use in the prevention and treatment of disorders related to abnormal gastric acid secretion.
摘要翻译：药物制剂由许多包含惰性核的丸粒，具有活性成分的层，至少包含调节释放系统的一个或多个中间层和肠溶衣外层构成。可以通过使用这些层的组分的水溶液或悬浮液的流化床涂覆技术施加不同层的这些颗粒。药物制剂可以是硬明胶胶囊或片剂，并且适用于预防和治疗与胃酸分泌异常相关的疾病。

3. 发明授权

US06767556B2 Pharmaceutical compositions comprising moexipril magnesium 失效
标题翻译：包含莫昔普利镁的药物组合物
公开(公告)号：US06767556B2
公开(公告)日：2004-07-27
申请号：US09809173
申请日：2001-03-16
申请人： Bernard Charles Sherman
发明人： Bernard Charles Sherman
IPC分类号： A61K914
CPC分类号： C07D217/26 , A61K9/1635 , A61K9/2095 , A61K31/472
摘要： Stable solid compositions comprising moxeipril magnesium can be made using moexipril or an acid addition salt thereof, by reacting the moxeipril or acid addition salt with an alkaline magnesium compound in the presence of a solvent, so as to convert most or all of the moexipril or acid addition salt to moexipril magnesium.
摘要翻译：包含莫昔普利镁的稳定的固体组合物可以使用莫昔普利或其酸加成盐，通过在溶剂存在下使阿昔普利或酸加成盐与碱性镁化合物反应，从而将大部分或全部的莫昔普利或酸加盐给莫昔普利镁。

4. 发明授权

US06761909B1 Particulate insulin-containing products and method of manufacture 有权
标题翻译：颗粒胰岛素产品及其制造方法
公开(公告)号：US06761909B1
公开(公告)日：2004-07-13
申请号：US09469733
申请日：1999-12-21
申请人： Jeffrey B. Etter
发明人： Jeffrey B. Etter
IPC分类号： A61K914
CPC分类号： A61K9/1617 , A61K9/14 , A61K9/1647 , A61K9/1694 , A61K38/00 , A61K48/00
摘要： Provided is a compressed anti-solvent technique for manufacture of insulin-containing powders for pulmonary delivery. The insulin is processed in a cosolvent system including two or more mutually soluble organic solvents. Also provided are powders manufacturable by the manufacture method, including powders of substantially pure insulin and powders including a biocompatible polymer for pulmonary sustained insulin release applications. Also provided are packaged products including insulin-containing powder in a container that is receivable by and operable with a dry powder inhaler to produce an aerosol including dispersed insulin-containing particles when the inhaler is actuated.
摘要翻译：提供了用于制造用于肺部输送的含胰岛素的粉末的压缩的反溶剂技术。胰岛素在包含两种或多种相互溶解的有机溶剂的助溶剂体系中进行处理。还提供了可通过制造方法制造的粉末，其包括基本上纯的胰岛素粉末和包括用于肺持续胰岛素释放应用的生物相容性聚合物的粉末。还提供包括在容器中的包含含胰岛素的粉末的包装产品，所述容器能够通过干粉吸入器接收并且可操作，以在吸入器致动时产生包含分散的含胰岛素颗粒的气溶胶。

5. 发明授权

US06759059B1 Fentanyl composition for the treatment of acute pain 有权
标题翻译：芬太尼组合物用于治疗急性疼痛
公开(公告)号：US06759059B1
公开(公告)日：2004-07-06
申请号：US09787887
申请日：2001-06-08
申请人： Anders Pettersson , Christer Nystrom , Hans Lennernas , Bo Lennernas , Thomas Hedner
发明人： Anders Pettersson , Christer Nystrom , Hans Lennernas , Bo Lennernas , Thomas Hedner
IPC分类号： A61K914
CPC分类号： A61K31/445 , A61K9/006 , G06F19/00
摘要： A pharmaceutical composition for the treatment of acute pain by sublingual administration is described. The composition comprises an essentially water-free, ordered mixture of fentanyl or a pharmaceutically acceptable salt thereof in the form of microparticles which are adhered to the surface of carrier particles which are substantially larger than the particles of fentanyl, and are essentially water-soluble. In a preferred embodiment, the composition also contains a bioadhesion and/or mucoadhesion promoting agent. The invention also relates to the preparation of the composition, and to the use of the composition for the treatment of acute pain.
摘要翻译：描述了通过舌下给药治疗急性疼痛的药物组合物。该组合物包含基本上无水的有限量的芬太尼或其药物上可接受的盐的微粒形式的混合物，其粘附到载体颗粒的表面上，其基本上大于芬太尼颗粒，并且基本上是水溶性的。在优选的实施方案中，组合物还含有生物粘附和/或粘膜粘着促进剂。本发明还涉及组合物的制备以及该组合物用于治疗急性疼痛的用途。

6. 发明授权

US06749867B2 Delivery system for omeprazole and its salts 失效
标题翻译：奥美拉唑及其盐的输送系统
公开(公告)号：US06749867B2
公开(公告)日：2004-06-15
申请号：US09991059
申请日：2001-11-21
申请人： Joseph R. Robinson , James W. McGinity
发明人： Joseph R. Robinson , James W. McGinity
IPC分类号： A61K914
CPC分类号： A61K31/4439 , A61K9/2009 , A61K9/2054 , A61K9/282 , A61K9/2846 , A61K9/2866
摘要： The present invention provides a time-release dosage form for delivering an acid-labile pharmaceutical, such as omeprazole, into the upper portion of the gastrointestinal tract downstream of the stomach. The dosage form includes a drug-containing core surrounded by an inert time-release coating that delays release of the drug from the core until expiration of a certain time period after administration, generally 0.5-5.0 hours or 1-3 hours. When the gastrointestinal fluid contacts the core, the drug is released rapidly into the GI tract. The dosage form does not contain an enteric coating. The dosage form can also include one or more additional coatings exterior to the time-release coating to provide delivery of an immediately released loading dose of the acid-labile drug or another drug.
摘要翻译：本发明提供了用于将酸不稳定药物（例如奥美拉唑）输送到胃下游胃肠道上部的时间释放剂型。剂型包括由惰性时间释放涂层包围的药物核心，其延迟药物从核心释放直到给药后一定时间段通常为0.5-5.0小时或1-3小时。当胃肠液接触核心时，药物迅速释放到胃肠道。剂型不含肠溶衣。剂型还可以包括一个或多个在时间释放涂层外部的附加涂层，以提供立即释放的负载剂量的酸不稳定药物或另一种药物的递送。

7. 发明授权

US06746693B2 Pharmaceutical excipient having improved compressibility 有权
标题翻译：药物赋形剂具有改善的压缩性
公开(公告)号：US06746693B2
公开(公告)日：2004-06-08
申请号：US10266518
申请日：2002-10-08
申请人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
发明人： John N. Staniforth , Bob E. Sherwood , Edward A. Hunter
IPC分类号： A61K914
CPC分类号： A61K9/2013 , A61K9/2009 , A61K9/2018 , A61K9/2036 , A61K9/205 , A61K9/2054 , Y10S977/906
摘要： A microcrystalline cellulose-based excipient having improved compressibility, whether utilized in direct compression, dry granulation or wet granulation formulations, is disclosed. The excipient is an agglomerate of microcrystalline cellulose particles and from about 0.1% to about 20% silicon dioxide particles, by weight of microcrystalline cellulose, wherein the microcrystalline cellulose and silicon dioxide are in intimate association with each other. The silicon dioxide utilized in the novel excipient has a particle size from 1 nanometer to about 100 microns. Most preferably, the silicon dioxide is a grade of colloidal silicon dioxide. An extra low moisture excipient is provided which exhibits improved compressibility as compared to conventional microcrystalline cellulose, while providing a moisture content of of from about 0.5 to 2.5% LOD, preferably between about 0.5 and about 1.8%, more preferably between 0.8 and 1.5%, and most preferably between about 0.8 and about 1.2%.
摘要翻译：公开了具有改进的压缩性的微晶纤维素基赋形剂，无论是用于直接压片，干法制粒还是湿法制粒。赋形剂是微晶纤维素颗粒的聚集物和约0.1％至约20％的微晶纤维素重量的二氧化硅颗粒，其中微晶纤维素和二氧化硅彼此紧密结合。在新型赋形剂中使用的二氧化硅具有1纳米至约100微米的粒度。最优选地，二氧化硅是胶体二氧化硅的等级。提供了与常规微晶纤维素相比显示出改善的可压缩性的特别低的水分赋形剂，同时提供约0.5至2.5％LOD，优选约0.5至约1.8％，更优选0.8至1.5％的水分含量，最优选在约0.8至约1.2％之间。

8. 发明授权

US06743442B2 Melt-extruded orally administrable opioid formulations 失效
公开(公告)号：US06743442B2
公开(公告)日：2004-06-01
申请号：US09777616
申请日：2001-02-06
申请人： Benjamin Oshlack , Mark Chasin , Hua-Pin Huang , David Sackler
发明人： Benjamin Oshlack , Mark Chasin , Hua-Pin Huang , David Sackler
IPC分类号： A61K914
CPC分类号： A61K9/1635 , A61K9/145 , A61K9/1617 , A61K9/1652 , A61K9/1694 , A61K9/2018 , A61K9/2027 , A61K9/2077 , A61K9/2081 , A61K9/2095 , Y10S514/951 , Y10S514/962
摘要： Bioavailable sustained release oral opioid analgesic dosage forms, comprising a plurality of multiparticulates produced via melt extrusion techniques are disclosed.

9. 发明授权

US06740341B1 Taste masking rapid release coating system 有权
标题翻译：味道掩蔽快速涂层系统
公开(公告)号：US06740341B1
公开(公告)日：2004-05-25
申请号：US09449851
申请日：1999-11-24
申请人： Kris E. Holt , Rajendra K. Khankari , John Hontz
发明人： Kris E. Holt , Rajendra K. Khankari , John Hontz
IPC分类号： A61K914
CPC分类号： A61K9/0056 , A61K9/5073 , Y10S514/974
摘要： The present invention relates to a core containing a drug encased in a spacing layer and a taste masking layer which provides effective taste masking for in-mouth disintegrable dosage forms containing highly objectionable tasting drugs, as well as dosage forms containing these cores.
摘要翻译：本发明涉及含有间隔层中的药物的核心和掩味层，其对含有高度令人讨厌的品尝药物的口腔内可分解剂型以及含有这些核心的剂型提供有效的掩味。

10. 发明授权

US06737044B1 Aerosol composition 有权
标题翻译：气溶胶组成
公开(公告)号：US06737044B1
公开(公告)日：2004-05-18
申请号：US09647331
申请日：2001-01-30
申请人： Paul Alfred Dickinson , Simon John Warren
发明人： Paul Alfred Dickinson , Simon John Warren
IPC分类号： A61K914
CPC分类号： A61K9/008 , A61K31/137 , A61K31/58 , Y10S514/826 , Y10S514/951
摘要： An aerosol composition comprising a propellant and a first particulate material comprising particle having a median aerodynamic diameter within the range 0.05 to 11 &mgr;m, such as a medicament suitable for pulmonary inhalation, and a second particulate material comprising particles having a median volume diameter within the range 15 to 200 &mgr;m. The presence of the second particulate material provides good suspension properties, particularly where the propellant is a hydrofluoro alkane.
摘要翻译：一种气溶胶组合物，其包含推进剂和包含中等空气动力学直径在0.05至11μm范围内的颗粒的第一颗粒材料，例如适合于肺部吸入的药物，以及第二颗粒材料，其包含中等体积直径在该范围内的颗粒 15到200个妈妈第二颗粒材料的存在提供了良好的悬浮性能，特别是当推进剂是氢氟烷烃时。

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