Device for delivery of TRPV1 agonists
    1.
    发明申请
    Device for delivery of TRPV1 agonists 审中-公开
    TRPV1激动剂输送装置

    公开(公告)号:US20060204561A1

    公开(公告)日:2006-09-14

    申请号:US11354349

    申请日:2006-02-14

    IPC分类号: A61K36/81 A61K31/16 A61F13/02

    摘要: Described here are drug delivery devices including an occlusive backing layer and a drug depot containing a TRPV1 agonist and a non-hydrophilic solvent. The drug depot may take various forms, such as an adhesive polymeric matrix, liquid reservoir, or microreservoir droplets. Methods of making and using the drug delivery devices are also described.

    摘要翻译: 这里描述了药物递送装置,其包括闭塞背衬层和含有TRPV1激动剂和非亲水溶剂的药物贮库。 药物库可以采取各种形式,例如粘合剂聚合物基质,液体储存器或微储层液滴。 还描述了制备和使用药物递送装置的方法。

    TRPV1 agonist compounds and methods for making and using the same
    2.
    发明申请
    TRPV1 agonist compounds and methods for making and using the same 有权
    TRPV1激动剂化合物及其制备和使用方法

    公开(公告)号:US20060240097A1

    公开(公告)日:2006-10-26

    申请号:US11411328

    申请日:2006-04-25

    IPC分类号: A61K31/24 A61K9/48 C07C235/72

    摘要: Described here are TRPV1 agonist compounds and their methods of synthesis and use. In addition to specifically identified compounds, capsaicin prodrugs, gemini dimers, and mutual prodrugs are also described. Formulations of the TRPV1 agonist compounds may be in the form of a liquid, tablets, capsules, gel, cream, emulsion, a patch, or the like. Methods for treating medical conditions using the compounds, compositions, or prodrugs described, are also provided.

    摘要翻译: 这里描述的是TRPV1激动剂化合物及其合成和使用方法。 除了具体鉴定的化合物之外,还描述了辣椒素前药,双子二聚体和共同前药。 TRPV1激动剂化合物的制剂可以是液体,片剂,胶囊,凝胶,霜剂,乳剂,贴剂等的形式。 还提供了使用所述化合物,组合物或前药治疗医学病症的方法。

    Oils of capsaicinoids and methods of making and using the same
    4.
    发明申请
    Oils of capsaicinoids and methods of making and using the same 有权
    辣椒素油及其制作和使用方法

    公开(公告)号:US20060233901A1

    公开(公告)日:2006-10-19

    申请号:US11394495

    申请日:2006-03-31

    IPC分类号: A61K36/81

    摘要: Oils of capsaicinoids and methods of making and using them are described. In some variations, the oils of capsaicinoids comprise at least 40% w/w capsaicinoid and a solvent capable of solubilizing the capsaicinoid, wherein the oil of capsaicinoid is substantially free of capsaicinoid crystals or capsaicinoid precipitates. In other variations, the oils of capsaicinoids consist essentially of at least 40% w/w capsaicinoid and a solvent capable of solubilizing the capsaicinoid. The solvent may be a semi-volatile solvent, a non-volatile solvent, or a volatile solvent, and the oil may comprise at least 50% w/w capsaicinoid, 60% w/w capsaicinoid, 70% w/w capsaicinoid, 80% w/w capsaicinoid, 90% w/w capsaicinoid, or 95% w/w capsaicinoid. The oil of capsaicinoid may also include a crystallization inhibitor.

    摘要翻译: 描述了辣椒素的油以及制造和使用它们的方法。 在一些变型中,辣椒素类油包含至少40%w / w辣椒素和能够溶解辣椒素的溶剂,其中辣椒素类油基本上不含辣椒素晶体或辣椒素沉淀物。 在其它变体中,辣椒素类油基本上由至少40%w / w辣椒素和能够溶解辣椒素的溶剂组成。 溶剂可以是半挥发性溶剂,非挥发性溶剂或挥发性溶剂,并且油可以包含至少50%w / w辣椒素,60%w / w辣椒素,70%w / w辣椒素,80 %w / w辣椒素,90%w / w辣椒素,或95%w / w辣椒素。 辣椒素油也可以包括结晶抑制剂。

    Pharmaceutical compositions of benzodiazepines and method of use thereof
    7.
    发明授权
    Pharmaceutical compositions of benzodiazepines and method of use thereof 失效
    苯并二氮杂的药物组合物及其使用方法

    公开(公告)号:US08609651B2

    公开(公告)日:2013-12-17

    申请号:US11897028

    申请日:2007-08-27

    IPC分类号: A01N43/62

    摘要: The present invention includes benzodiazepine compositions formulated for intranasal administration, comprising a binary solvent system comprising a first solvent in which the benzodiazepine is soluble, the first solvent capable of penetrating nasal mucosal tissue, and a second solvent in which the benzodiazepine in less soluble. The compositions of the present invention may be used to treat a variety of disorders including, but not limited to, panic attacks, muscle spasms, anxiety, and seizures. In one aspect, the present invention relates to a fast-acting, clonazepam composition for transnasal administration that can be used for the treatment of seizure clusters.

    摘要翻译: 本发明包括配制用于鼻内给药的苯并二氮杂类组合物,其包含二元溶剂系统,其包含其中可溶于苯并二氮杂的第一溶剂,能够渗透鼻粘膜组织的第一溶剂和其中苯二氮卓类溶解度较低的第二溶剂。 本发明的组合物可用于治疗各种障碍,包括但不限于恐慌发作,肌肉痉挛,焦虑和癫痫发作。 一方面,本发明涉及可用于治疗癫痫发作簇的用于经鼻给药的快速作用的氯硝西泮组合物。

    Manganese (II) chelates
    8.
    发明授权
    Manganese (II) chelates 失效
    锰(II)螯合物

    公开(公告)号:US5155224A

    公开(公告)日:1992-10-13

    申请号:US370478

    申请日:1989-06-23

    摘要: The process of this invention for preparing Mn(II) chelate comprises forming the Mn(II) chelate by mixing manganese (II) oxide (insoluble) with an aqueous suspension comprising a molar equivalent or molar excess of the insoluble protonated chelating compound at a temperature of from 20.degree.to 50.degree. C. When the reaction is carried out with a protonated chelating agent in the absence of base, a precipitate of the protonated Mn(II) chelate is formed. A low osmolarity MN(II) chelate solution can be formed from the precipitates by dissolving them in an aqueous solution of base. When the initial chelate forming reaction is carried out in a solution containing a molar equivalent or excess of sodium hydroxide, a low osmolarity solution of the Mn(II) chelate is directly formed with most chelating agents. Preferred chelating compounds for this process include DPDP, DTPA, DCTA, EDTP, DOTA, DOXA, DO3A and EDTA. The Nm(II) chelate precipitates and low osmolarity solutions formed by the above processes are also aspects of this invention.

    摘要翻译: 本发明制备Mn(II)螯合物的方法包括通过将锰(II)氧化物(不溶性)与包含摩尔当量或摩尔过量的不溶性质子化螯合化合物的水悬浮液在温度下混合形成Mn(II)螯合物 为20〜50℃。当不存在碱时,用质子化螯合剂进行反应时,形成质子化的Mn(II)螯合物的沉淀物。 通过将沉淀物溶解在碱的水溶液中,可以从沉淀物形成低摩尔渗透浓度的MN(II)螯合溶液。 当初始螯合物形成反应在含有摩尔当量或过量氢氧化钠的溶液中进行时,Mn(II)螯合物的低渗透压溶液与大多数螯合剂直接形成。 用于该方法的优选螯合化合物包括DPDP,DTPA,DCTA,EDTP,DOTA,DOXA,DO3A和EDTA。 通过上述方法形成的Nm(II)螯合物沉淀物和低摩尔渗压浓度溶液也是本发明的一个方面。

    Pharmaceutical compositions of clonazepam and method of use thereof
    9.
    发明授权
    Pharmaceutical compositions of clonazepam and method of use thereof 失效
    氯硝西泮的药物组合物及其使用方法

    公开(公告)号:US08716279B2

    公开(公告)日:2014-05-06

    申请号:US11897002

    申请日:2007-08-27

    IPC分类号: A01N43/62

    摘要: The present invention includes benzodiazepine compositions formulated for intranasal administration, comprising a binary solvent system comprising a first solvent in which the benzodiazepine is soluble, the first solvent capable of penetrating nasal mucosal tissue, and a second solvent in which the benzodiazepine in less soluble. The compositions of the present invention may be used to treat a variety of disorders including, but not limited to, panic attacks, muscle spasms, anxiety, and seizures. In one aspect, the present invention relates to a fast-acting, clonazepam composition for transnasal administration that can be used for the treatment of seizure clusters.

    摘要翻译: 本发明包括配制用于鼻内给药的苯并二氮杂类组合物,其包含二元溶剂系统,其包含其中可溶于苯并二氮杂的第一溶剂,能够渗透鼻粘膜组织的第一溶剂和其中苯二氮卓类溶解度较低的第二溶剂。 本发明的组合物可用于治疗各种障碍,包括但不限于恐慌发作,肌肉痉挛,焦虑和癫痫发作。 一方面,本发明涉及可用于治疗癫痫发作簇的用于经鼻给药的快速作用的氯硝西泮组合物。

    Novel manganese(II) DTPA chelate
    10.
    发明授权
    Novel manganese(II) DTPA chelate 失效
    新型锰(II)DTPA螯合物

    公开(公告)号:US4978763A

    公开(公告)日:1990-12-18

    申请号:US370483

    申请日:1989-06-23

    摘要: The process of this invention for preparing Mn(II) chelate comprises forming the Mn(II) chelate by mixing manganese(II) oxide (insoluble) with an aqueous suspension comprising a molar equivalent or molar excess of the insoluble protonated chelating compound at a temperature of from 20.degree. to 50.degree. C. When the reaction is carried out with a protonated chelating agent in the absence of base, a precipitate of the protonated Mn(II) chelate is formed. A low osmolarity Mn(II) chelate solution can be formed from the precipitates by dissolving them in an aqueous solution of base. When the initial chelate forming reaction is carried out in a solution containing a molar equivalent or excess of sodium hydroxide, a low osmolarity solution of the Mn(II) chelate is directly formed with most chelating agents. Preferred chelating compounds for this process include DPDP, DTPA, DCTA, EDTP, DOTA, DOXA, DO3A and EDTA. The Mn(II) chelate precipitates and low osmolarity solutions formed by the above processes are also aspects of this invention.

    摘要翻译: 本发明制备Mn(II)螯合物的方法包括通过将锰(II)氧化物(不溶性)与包含摩尔当量或摩尔过量的不溶性质子化螯合化合物的水悬浮液在温度下混合形成Mn(II)螯合物 为20〜50℃。当不存在碱时,用质子化螯合剂进行反应时,形成质子化的Mn(II)螯合物的沉淀物。 通过将它们溶解在碱的水溶液中,可以通过沉淀物形成低摩尔渗透浓度的Mn(II)螯合溶液。 当初始螯合物形成反应在含有摩尔当量或过量氢氧化钠的溶液中进行时,Mn(II)螯合物的低渗透压溶液与大多数螯合剂直接形成。 用于该方法的优选螯合化合物包括DPDP,DTPA,DCTA,EDTP,DOTA,DOXA,DO3A和EDTA。 通过上述方法形成的Mn(II)螯合物沉淀物和低摩尔渗压浓度溶液也是本发明的一个方面。