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    Compositions containing opioid antagonists
    3.
    发明授权
    Compositions containing opioid antagonists 有权
    含有阿片样物质拮抗剂的组合物

    公开(公告)号：US08598207B2

    公开(公告)日：2013-12-03

    申请号：US13477742

    申请日：2012-05-22

    申请人： John D. Buehler

    发明人： John D. Buehler

    IPC分类号： A61K31/454

    CPC分类号： A61K47/10 ,  A61K9/0019 ,  A61K9/19 ,  A61K31/451 ,  A61K31/454 ,  A61K47/02 ,  A61K47/26

    摘要： Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and provide maximum levels of opioid antagonists when administered parenterally, particularly via injection. The results are achieved by a combination of processing techniques and component selection.

    摘要翻译： 公开了含有阿片样物质拮抗剂，特别是阿维莫潘及其活性代谢物的组合物，具有口服或肠胃外给药的改善的溶解度和生物利用度，可注射剂型，试剂盒及其制备和使用方法。 在优选的实施方案中，本发明提供了含有阿片样物质拮抗剂，特别是阿维莫潘及其活性代谢物的可注射制剂，其具有低易溶解性，易于制备，在储存期间是稳定的，并且当肠胃外特别是通过注射时提供最大量的阿片样物质拮抗剂。 结果通过处理技术和部件选择的组合来实现。

    COMPOSITIONS CONTAINING OPIOID ANTAGONISTS
    5.
    发明申请
    COMPOSITIONS CONTAINING OPIOID ANTAGONISTS 有权
    含有阿片样物质拮抗剂的组合物

    公开(公告)号：US20120232114A1

    公开(公告)日：2012-09-13

    申请号：US13477742

    申请日：2012-05-22

    申请人： John D. Buehler

    发明人： John D. Buehler

    IPC分类号： A61K31/445

    CPC分类号： A61K47/10 ,  A61K9/0019 ,  A61K9/19 ,  A61K31/451 ,  A61K31/454 ,  A61K47/02 ,  A61K47/26

    摘要： Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and provide maximum levels of opioid antagonists when administered parenterally, particularly via injection. The results are achieved by a combination of processing techniques and component selection.

    摘要翻译： 公开了含有阿片样物质拮抗剂，特别是阿维莫潘及其活性代谢物的组合物，具有口服或肠胃外给药的改善的溶解度和生物利用度，可注射剂型，试剂盒及其制备和使用方法。 在优选的实施方案中，本发明提供了含有阿片样物质拮抗剂，特别是阿维莫潘及其活性代谢物的可注射制剂，其具有低易溶解性，易于制备，在储存期间是稳定的，并且当肠胃外特别是通过注射时提供最大量的阿片样物质拮抗剂。 结果通过处理技术和部件选择的组合来实现。

    Methods for delivering a drug to a hospital patient for short-term use while minimizing long-term use of the drug
    7.
    发明授权
    Methods for delivering a drug to a hospital patient for short-term use while minimizing long-term use of the drug 有权
    将药物递送到医院病人短期使用，同时尽量减少长期使用药物的方法

    公开(公告)号：US08112290B2

    公开(公告)日：2012-02-07

    申请号：US12467016

    申请日：2009-05-15

    申请人： George Raymond Maurer ,  Robert Barnett Jones

    发明人： George Raymond Maurer ,  Robert Barnett Jones

    IPC分类号： G06Q50/00

    CPC分类号： A61K31/451 ,  G06F19/00 ,  G06F19/3456 ,  G06Q50/22

    摘要： Novel methods for delivering a drug to hospital patients for short-term in-hospital use while minimizing long-term use of the drug. Embodiments are provided in which hospitals are identified which may be eligible to treat patients, for example, perform certain types of surgery, and which have measures in place to limit use of the drug to short-term use. The identified hospitals are preferably registered in a storage medium, including computer readable storage media, and may be authorized to receive the shipments of the drug. The received drug may then be dispensed to the patient.

    摘要翻译： 将药物递送给医院病人进行短期住院使用的最新方法，同时尽量减少长期使用药物。 提供的实施例是哪些医院被识别为可能有资格治疗患者，例如执行某些类型的手术，并且哪些医疗措施已经将药物的使用限制为短期使用。 所识别的医院优选地登记在包括计算机可读存储介质的存储介质中，并且可以被授权接收药物的运输。 然后将所接收的药物分配给患者。

    Solid dispersions of opioid antagonists
    8.
    发明授权
    Solid dispersions of opioid antagonists 有权
    阿片样物质拮抗剂的固体分散体

    公开(公告)号：US07914776B2

    公开(公告)日：2011-03-29

    申请号：US11543619

    申请日：2006-10-05

    申请人： Virendra Kumar

    发明人： Virendra Kumar

    IPC分类号： A61K31/785 ,  C08F20/00

    CPC分类号： A61K31/445

    摘要： Solid dispersions of stable, amorphous opioid antagonists, particularly [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-piperidinyl]methyl]-1-oxo-3-phenylpropyl]amino]acetic acid, with improved water solubility and bioavailability are disclosed. Also disclosed are methods of preventing or treating a side effect associated with an opioid. In addition, methods of treating or preventing pain, ileus, and opioid bowel dysfunction are disclosed.

    摘要翻译： 稳定的无定形阿片样物质拮抗剂的固体分散体，特别是[[2（S） - [[4（R） - （3-羟基苯基）-3（R），4-二甲基 - 哌啶基]甲基] -1-氧代-3- 苯基丙基]氨基]乙酸，其具有改善的水溶性和生物利用度。 还公开了预防或治疗与阿片样物质相关的副作用的方法。 此外，公开了治疗或预防疼痛，肠梗阻和阿片样物质肠功能障碍的方法。

    USE OF AN OPIOID RECEPTOR ANTAGONIST FOR THE TREATMENT OR PREVENTION OF GASTROINTESTINAL TRACT DISORDERS
    9.
    发明申请
    USE OF AN OPIOID RECEPTOR ANTAGONIST FOR THE TREATMENT OR PREVENTION OF GASTROINTESTINAL TRACT DISORDERS 审中-公开
    使用阿片受体拮抗剂治疗或预防胃肠疾病

    公开(公告)号：US20110071163A1

    公开(公告)日：2011-03-24

    申请号：US12884985

    申请日：2010-09-17

    申请人： Richard M. WOODWARD

    发明人： Richard M. WOODWARD

    IPC分类号： A61K31/497 ,  C07D403/12 ,  A61P1/00

    CPC分类号： A61K31/497

    摘要： The disclosure relates to a method of treating or preventing a condition in a subject associated with the activation of an opioid receptor in the periphery by administering an effective amount of 5-(2-methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide (Compound I). In particular, the disclosure relates to a method of treating or preventing opioid-induced constipation or opioid-induced bowel dysfunction in a human without reducing centrally-mediated opioid analgesia or producing central opioid withdrawal symptoms by administering an effective amount of Compound I. The disclosure further relates to the use of Compound I for the preparation of a medicament for the treatment or prevention of a condition in a subject associated with the activation of an opioid receptor in the periphery.

    摘要翻译： 本公开内容涉及通过施用有效量的5-（2-甲氧基-4 - {[2-（四氢 - 吡喃-2-基） - 哌嗪-1-基） 吡啶-4-基） - 乙基氨基] - 甲基} - 苯氧基） - 吡嗪-2-甲酰胺（化合物I）。 特别地，本公开涉及一种治疗或预​​防人类阿片样物质诱发的便秘或阿片样物质诱导的肠功能障碍的方法，而不会通过施用有效量的化合物I而减少中枢介导的阿片样镇痛或产生中枢阿片样物质戒断症状。 进一步涉及化合物I用于制备用于治疗或预防与周围阿片受体活化相关的受试者中的病症的药物的用途。

    COMPOSITIONS CONTAINING OPIOID ANTAGONISTS
    10.
    发明申请
    COMPOSITIONS CONTAINING OPIOID ANTAGONISTS 审中-公开
    含有阿片样物质拮抗剂的组合物

    公开(公告)号：US20100240690A1

    公开(公告)日：2010-09-23

    申请号：US12728622

    申请日：2010-03-22

    申请人： John D. Buehler

    发明人： John D. Buehler

    IPC分类号： A61K31/451 ,  A61K31/454 ,  A61K31/485 ,  A61K31/473 ,  A61K31/4545 ,  A61K31/4535 ,  A61P25/04 ,  A61P17/04 ,  A61P1/00 ,  A61P1/08 ,  A61P1/06

    CPC分类号： A61K47/10 ,  A61K9/0019 ,  A61K9/19 ,  A61K31/451 ,  A61K31/454 ,  A61K47/02 ,  A61K47/26

    摘要： Compositions containing opioid antagonists, particularly alvimopan and its active metabolite, with improved solubility and bioavailability for oral or parenteral administration, injectable dosage formulations, kits, and methods of making and using same are disclosed. In preferred embodiments, invention provides injectable formulations containing opioid antagonists, particularly alvimopan and its active metabolite, having low solubility that may be readily prepared, are stable during storage, and provide maximum levels of opioid antagonists when administered parenterally, particularly via injection. The results are achieved by a combination of processing techniques and component selection.

    摘要翻译： 公开了含有阿片样物质拮抗剂，特别是阿维莫潘及其活性代谢物的组合物，具有口服或肠胃外给药的改善的溶解度和生物利用度，可注射剂型，试剂盒及其制备和使用方法。 在优选的实施方案中，本发明提供了含有阿片样物质拮抗剂，特别是阿维莫潘及其活性代谢物的可注射制剂，其具有低易溶解性，易于制备，在储存期间是稳定的，并且当肠胃外特别是通过注射时提供最大量的阿片样物质拮抗剂。 结果通过处理技术和部件选择的组合来实现。