MODIFIED DOSAGE FORMS OF TACROLIMUS
    32.
    发明申请
    MODIFIED DOSAGE FORMS OF TACROLIMUS 审中-公开
    改良剂量剂型

    公开(公告)号:US20100086592A1

    公开(公告)日:2010-04-08

    申请号:US12530011

    申请日:2008-03-25

    IPC分类号: A61K9/24 A61K31/436 A61K9/16

    摘要: The present invention provides a modified release dosage form of tacrolimus that releases two or more amount of tacrolimus upon oral administration, the first amount of tacrolimus releases from the immediate release dosage unit substantially immediately within 0-2 hours followed by a time interval ranging from about 1-10 hours during which substantially no amount of tacrolimus is released from the dosage form, after which a second amount of tacrolimus is released wherein said second amount is released from the delayed release dosage unit either immediately e.g. within 0-2 hours or over a period of time ranging from about 2-12 hours from its initial release from the delayed release dosage unit. The dosage form may further comprise additional amount of tacrolimus to provide additional pulse of tacrolimus. The dosage forms of tacrolimus exhibit improved bioavailability and reduced flux or fluctuation over existing composition of tacrolimus. A method of preparing the dosage forms is also described.

    摘要翻译: 本发明提供了他克莫司的释放剂量形式,其口服给药释放两种或更多量的他克莫司,第一批量的他克莫司基本上立即在0-2小时内立即从即时释放剂量单位释放,之后是从约 1-10小时,其中基本上没有量的他克莫司从剂型中释放出来,之后第二量的他克莫司被释放,其中所述第二量从延迟释放剂量单位释放, 在0-2小时内或超过延迟释放剂量单位从其初始释放约2-12小时的时间段内。 剂型还可包含额外量的他克莫司以提供他克莫司的额外脉冲。 他克莫司的剂型表现出改善的生物利用度和减少通量或波动超过现有组合的他克莫司。 还描述了制备剂型的方法。

    Controlled release compositions comprising Nimesulide
    33.
    发明申请
    Controlled release compositions comprising Nimesulide 审中-公开
    包含尼美舒利的控制释放组合物

    公开(公告)号:US20080160082A1

    公开(公告)日:2008-07-03

    申请号:US11978162

    申请日:2007-10-26

    IPC分类号: A61K9/22 A61K31/18

    摘要: A controlled release pharmaceutical composition for peroral administration including a single unit fast release fraction and a single unit extended release fraction which includes nimesulide as an active drug upto 99% w/w of the composition, one or more release controlling materials from 0.1% to 99% w/w of the composition and pharmaceutical excipients from 0% to 90% w/w of the composition. The nimesulide is present in the fast release fraction and in the extended release fraction.

    摘要翻译: 用于口服给药的控释药物组合物,包括单一单位快速释放级分和单一单位延长释放级分,其包含尼泊洛尔作为组合物高达99%w / w的活性药物,一种或多种释放控制材料为0.1%至99 %w / w的组合物和药物赋形剂的组合物的0%至90%w / w。 尼美舒利存在于快速释放部分和延长释放部分中。

    Controlled Release Pharmaceutical Composition Comprising An Acid-Insoluble And A Bioadhesive Polymer
    34.
    发明申请
    Controlled Release Pharmaceutical Composition Comprising An Acid-Insoluble And A Bioadhesive Polymer 审中-公开
    包含酸不溶性和生物粘合聚合物的控制释放药物组合物

    公开(公告)号:US20070219175A1

    公开(公告)日:2007-09-20

    申请号:US10551058

    申请日:2005-01-05

    IPC分类号: A61K31/43

    摘要: Rapidly disintegrating oral controlled release pharmaceutical compositions and process for preparation of such compositions are provided. The compositions preferably comprise antibiotic(s) as active ingredient, more preferably amoxicillin either alone or in combination with other antibiotic(s). The controlled release compositions comprise at least one active ingredient, and a polymer system comprising of at least two polymers which retard the release of the active ingredient in the stomach while providing rapid release of the said active ingredient in the alkaline contents of small intestine, optionally with other pharmaceutically acceptable excipients. The compositions provide therapeutically effective levels of the active ingredient for extended periods of time, and possess bioadhesive properties.

    摘要翻译: 提供快速崩解的口服释药药物组合物和制备这些组合物的方法。 组合物优选包含抗生素作为活性成分,更优选单独或与其它抗生素组合使用阿莫西林。 控释组合物包含至少一种活性成分和包含至少两种聚合物的聚合物体系,所述聚合物延缓了胃中活性成分的释放,同时提供所述活性成分在小肠的碱性成分中的快速释放,任选地 与其它药学上可接受的赋形剂。 该组合物延长时间段提供治疗有效水平的活性成分,并且具有生物粘合性质。

    Pharmaceutical compositions comprising of proton pump inhibitor and prokinetic agent
    35.
    发明申请
    Pharmaceutical compositions comprising of proton pump inhibitor and prokinetic agent 审中-公开
    包含质子泵抑制剂和促动力剂的药物组合物

    公开(公告)号:US20070160664A1

    公开(公告)日:2007-07-12

    申请号:US11482186

    申请日:2006-07-06

    IPC分类号: A61K31/4439 A61K9/64 A61K9/24

    摘要: Oral pharmaceutical compositions and process for preparation thereof are provided comprising at least one gastric acid suppressing agent, preferably a proton pump inhibitor or its pharmaceutically acceptable salts, esters, hydrates, derivatives or prodrugs, and one or more prokinetic agent or its pharmaceutically acceptable salts, esters, hydrates, derivatives or prodrugs, optionally with other pharmaceutically acceptable excipients, characterized in that the gastric acid suppressing agent is present in a delayed release form and the prokinetic agent is present in a bimodal release form such as an immediate release form to provide an initial loading dose, and a delayed release form to provide a dose with a lag time; with the proviso that the prokinetic agent is not formulated using a hydrophilic rate controlling polymer and is not present in a sustained release form. Method of treatment of gastro esophageal reflux disease, reflux esophagitis, peptic ulcer, gastric ulcer, and other gastric acid related disorders by administering to a patient such a pharmaceutical composition in need thereof is also provided.

    摘要翻译: 提供了口服药物组合物及其制备方法,其包含至少一种胃酸抑制剂,优选质子泵抑制剂或其药学上可接受的盐,酯,水合物,衍生物或前药,以及一种或多种促动力剂或其药学上可接受的盐, 酯,水合物,衍生物或前药,任选地与其它药学上可接受的赋形剂,其特征在于所述胃酸抑制剂以延迟释放形式存在,并且促动力剂以双峰释放形式存在,例如立即释放形式,以提供 初始加载剂量和延迟释放形式以提供具有滞后时间的剂量; 条件是促动剂不是使用亲水性速率控制聚合物配制的,并且不以缓释形式存在。 还提供了通过向患者施用这种有此需要的药物组合物来治疗胃食管反流病,反流性食管炎,消化性溃疡,胃溃疡和其它胃酸相关疾病的方法。

    Pharmaceutical compositions containing cyclosporin
    36.
    发明授权
    Pharmaceutical compositions containing cyclosporin 失效
    含有环孢菌素的药物组合物

    公开(公告)号:US6008191A

    公开(公告)日:1999-12-28

    申请号:US136663

    申请日:1998-08-19

    摘要: A novel homogenous alcohol free, free flowing, clear and transparent pharmaceutical composition containing Cyclosporin is disclosed. The amount of Cyclosporin is easily measurable at a wide range of temperature of 15.degree. to 45.degree. C. The composition comprises a Cyclosporin in a hydrophillic carrier medium comprising propylene glycol, a transesterification product of a natural vegetable oil triglyceride and a polyalkylene polyol--such as Apricot Kernel Oil Polyethylene glycol 6 esters--such as Labrafil M1944 and polyethylene hydrogenated castor oils--such as Cremophor RH 40 and Glycerol Triacetate or Triacetin.

    摘要翻译: 公开了一种新颖的均匀无醇,自由流动,透明和透明的含有环孢菌素的药物组合物。 环孢菌素的量可以在15°至45℃的宽温度范围内容易地测量。该组合物包含在亲水载体介质中的环孢菌素,其包含丙二醇,天然植物油甘油三酯的转酯化产物和聚亚烷基多元醇 作为杏仁油聚乙二醇6酯,例如Labrafil M1944和聚乙烯氢化蓖麻油,例如Cremophor RH 40和甘油三乙酸酯或三醋精。

    Antimicrobials
    39.
    发明授权
    Antimicrobials 有权
    抗生素

    公开(公告)号:US08841306B2

    公开(公告)日:2014-09-23

    申请号:US13130440

    申请日:2009-11-18

    摘要: The present invention relates to novel phenyl oxazolidinone compounds of formula I, their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The invention also relates to the processes for the synthesis of novel compounds of formula I or their pharmaceutically acceptable analogs, tautomeric forms, stereoisomers, polymorphs, prodrugs, metabolites, salts or solvates thereof. The present invention also provides pharmaceutical compositions comprising novel compounds of formula I and methods of using them. The compounds of the present invention are useful as antimicrobial agents, effective against a number of aerobic and/or anaerobic Gram positive and/or Gram negative pathogens such as multi drug resistant species of Staphylococcus, Streptococcus, Enterococcus, Bacterioides, Clostridia, H. influenza, Moraxella, acid-fast organisms such as Mycobacterium tuberculosis as well as Linezolid resistant species of Staphylococcus and Enterococcus.

    摘要翻译: 本发明涉及式I的新型苯基恶唑烷酮化合物,其药学上可接受的类似物,互变异构形式,立体异构体,多晶型物,前药,代谢物,盐或溶剂化物。 本发明还涉及合成新型式I化合物或其药学上可接受的类似物,互变异构体形式,立体异构体,多晶型物,前药,代谢物,盐或溶剂合物的方法。 本发明还提供了包含新颖的式I化合物和使用它们的方法的药物组合物。 本发明的化合物可用作抗微生物剂,对许多需氧和/或厌氧革兰氏阳性和/或革兰氏阴性病原体有效,如葡萄球菌,链球菌,肠球菌,细菌,梭菌,流感嗜血杆菌 ,莫拉氏菌,耐酸菌,如结核分枝杆菌,以及耐盐霉菌属的霉菌和肠球菌。

    Manufacturability evaluation of injection molded plastic models using a CAD based DFX evaluation system
    40.
    发明授权
    Manufacturability evaluation of injection molded plastic models using a CAD based DFX evaluation system 有权
    使用基于CAD的DFX评估系统的注塑模型的可制造性评估

    公开(公告)号:US08219230B2

    公开(公告)日:2012-07-10

    申请号:US12797002

    申请日:2010-06-09

    IPC分类号: G06F19/00 B29C45/00

    摘要: A method of automatic manufacturability evaluation of plastic models comprises generation of a likely pulling direction, recognition of common features on plastic parts, and then applying manufacturability rules The manufacturability rules can be specified and customized through user specified rule parameters and depend upon the geometric parameters of the recognized features. A system comprises a user interface for selection and customization of DFX (Design for ‘X’) rules for evaluation of a design. The system includes a user interface integrated with a CAD system for receiving the CAD data and displaying the results to the user. Geometry analysis engines are integrated into the system, for extracting the various features and corresponding parameters required as input to the manufacturability rules. The system further involves extensible interfaces for rules and analysis engines which allows users to write their own customized rules and engines and integrate these into the CAD based DFX evaluation system.

    摘要翻译: 塑料模型的自动制造性评估方法包括产生可能的拉动方向,识别塑料部件上的共同特征,然后应用可制造性规则可制造性规则可以通过用户指定的规则参数来指定和定制,并且取决于几何参数 公认的功能。 系统包括用于选择和定制DFX(用于'X'的设计)用于评估设计的规则的用户界面。 该系统包括与CAD系统集成的用于接收CAD数据并将结果显示给用户的用户界面。 几何分析引擎集成到系统中,用于提取作为可制造性规则输入所需的各种功能和相应参数。 该系统还涉及规则和分析引擎的可扩展接口,允许用户编写自己的定制规则和引擎,并将其集成到基于CAD的DFX评估系统中。