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    Non-flammable topical anesthetic liquid aerosols
    11.
    发明申请
    Non-flammable topical anesthetic liquid aerosols 审中-公开
    不易燃的局部麻醉液体气溶胶

    公开(公告)号：US20050123484A1

    公开(公告)日：2005-06-09

    申请号：US10956819

    申请日：2004-10-01

    申请人： Jane Hirsh ,  Donald Tibbetts ,  Mark Hirsh

    发明人： Jane Hirsh ,  Donald Tibbetts ,  Mark Hirsh

    IPC分类号： A61K9/12 ,  A61K31/00 ,  A61K31/24 ,  A61K31/245 ,  A61K45/06 ,  A61P23/02 ,  A61L9/04

    CPC分类号： A61K31/245 ,  A61K9/12 ,  A61K31/00 ,  A61K31/24 ,  A61K45/06 ,  A61K2300/00

    摘要： A topical liquid aerosol formulation for accurate metered dose delivery has been developed which includes a concentrate comprising a local anesthetic in a non-alcohol solvent and a hydrofluorocarbon (HFC) propellant. In the preferred embodiment, the concentration of the non-alcohol solvent in the concentrate is between about 75% and 85% by weight of the formulation. In the most preferred embodiment, the non-alcohol solvent is a water-soluble polyol such as ethylene glycol, propylene glycol, glycerol, diethylene glycol, dipropylene glycol, oligoalkylene glycols, liquid polyalkylene glycols, or combinations thereof. In one embodiment, the concentration of the local anesthetic in the concentrate is between about 15% and 25% by weight. In the preferred embodiment, the hydrofluorocarbon propellant is 1,1,1,2-tetrafluoroethane 1,1,1,2,3,3,3-heptafluoropropane or combinations thereof, in a concentration between about 35% and 65% by weight of the final formulation, more preferably between about 45% and 55% by weight of the final formulation. A particularly preferred formulation includes benzocaine, tetracaine, and butylaminobenzoate, wherein the concentration of benzocaine in the concentrate is 14% by weight, the concentration of tetracaine in the concentrate is 2% by weight, and the concentration of butylaminobenzoate in the concentrate is 2% by weight. It has been found that the formulation is more stable in the substantial absence of oxygen. The formulation is preferably administered using a metered dose device for release of a controlled amount of the local anesthetic.

    摘要翻译： 已经开发了用于精确计量剂量递送的局部液体气溶胶制剂，其包括在非醇溶剂中的局部麻醉剂和氢氟烃（HFC）推进剂的浓缩物。 在优选的实施方案中，浓缩物中非醇溶剂的浓度为制剂重量的约75％至85％。 在最优选的实施方案中，非醇溶剂是水溶性多元醇，例如乙二醇，丙二醇，甘油，二甘醇，二丙二醇，低聚亚烷基二醇，液体聚亚烷基二醇或其组合。 在一个实施方案中，浓缩物中局部麻醉剂的浓度为约15重量％至25重量％。 在优选的实施方案中，氢氟烃推进剂是1,1,1,2-四氟乙烷1,1,1,2,3,3,3-七氟丙烷或其组合，其浓度为约35-65重量％ 最终制剂，更优选为最终制剂重量的约45％至55％。 特别优选的制剂包括苯佐卡因，丁卡因和丁基氨基苯甲酸酯，其中浓缩物中苯佐卡因的浓度为14重量％，浓缩物中丁卡因的浓度为2重量％，浓缩物中丁基氨基苯甲酸酯的浓度为2重量％ 重量。 已经发现，在基本不存在氧的情况下，制剂更加稳定。 制剂优选使用计量剂量装置施用以释放受控量的局部麻醉剂。

    Abuse-deterrent pharmaceutical compositions of opioids and other drugs
    16.
    发明授权
    Abuse-deterrent pharmaceutical compositions of opioids and other drugs 有权
    阿片类药物和其他药物的滥用药物组合物

    公开(公告)号：US08557291B2

    公开(公告)日：2013-10-15

    申请号：US12473073

    申请日：2009-05-27

    申请人： Roman V. Rariy ,  Alison B. Fleming ,  Jane Hirsh ,  Alexander M. Klibanov

    发明人： Roman V. Rariy ,  Alison B. Fleming ,  Jane Hirsh ,  Alexander M. Klibanov

    IPC分类号： A61K9/14 ,  A61K9/20 ,  A61K9/48

    CPC分类号： A61K47/46 ,  A61K9/1617 ,  A61K9/5026 ,  A61K31/485 ,  A61K45/06 ,  A61K47/12

    摘要： An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opioids. In a preferred embodiment, a drug is modified to increase its lipophilicity. In some embodiments the modified drug is homogeneously dispersed within spherical microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and/or organic solvent insoluble. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is passes through the GI tract.

    摘要翻译： 已经开发了一种滥用威慑药物组合物，以减少药物不当管理的可能性，特别是阿片样物质等药物。 在优选的实施方案中，修饰药物以增加其亲油性。 在一些实施方案中，改性药物均匀地分散在由缓慢溶解或不溶于水的材料组成的球形微粒内。 在一些实施方案中，含有微粒或药物颗粒的药物涂覆有一个或多个涂层，其中至少一种涂层是不溶于水的和/或有机溶剂不溶的。 即使制剂的物理完整性受到损害（例如通过用刀片切碎或破碎）并且将所得材料置于水中，嗅到或吞咽，滥用威慑组合物也会延缓释放药物。 然而，当按照指导给药时，当组合物通过胃肠道时，药物从组合物缓慢释放。

    Abuse-deterrent drug formulations
    17.
    发明授权
    Abuse-deterrent drug formulations 有权
    滥用威慑药物制剂

    公开(公告)号：US07771707B2

    公开(公告)日：2010-08-10

    申请号：US11149867

    申请日：2005-06-10

    申请人： Jane C. Hirsh ,  Alison B. Fleming ,  Roman V. Rariy ,  Alexander M. Klibanov

    发明人： Jane C. Hirsh ,  Alison B. Fleming ,  Roman V. Rariy ,  Alexander M. Klibanov

    IPC分类号： A61K49/00 ,  A61K31/44

    CPC分类号： A61K31/485 ,  A61K9/0053 ,  A61K9/145 ,  A61K9/148 ,  A61K9/1617 ,  A61K9/1664 ,  A61K9/2013 ,  A61K9/4808 ,  A61K9/4858 ,  A61K9/5015 ,  A61K9/5042 ,  A61K31/13 ,  A61K31/20 ,  A61K45/06 ,  A61K47/12 ,  A61K2300/00

    摘要： An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

    摘要翻译： 已经开发了一种滥用威慑药物组合物，以减少药物不当管理的可能性，特别是诸如阿片类药物。 在优选的实施方案中，通过在药物和一种或多种脂肪酸之间形成盐，来修饰药物以增加其亲油性，其中一种或多种脂肪酸的浓度是活性剂的摩尔量的1至15倍 活性剂摩尔量的2〜10倍。 在一个实施方案中，改性药物均匀地分散在由缓慢溶解或不溶于水的材料组成的微粒内。 在一些实施方案中，含有微粒或药物颗粒的药物涂覆有一个或多个涂层，其中至少一个涂层是水不溶性的，优选有机溶剂不溶。 即使制剂的物理完整性受损（例如通过用刀片切碎或破碎），所述滥用威慑组合物可以立即释放大部分药物，并将所得材料置于水中，嗅到或 吞下去 然而，当按照指导给药时，由于组合物通过酶降解，胆汁酸的表面活性作用和机械侵蚀的组合被分解或逐渐溶解在胃肠道内，药物从组合物中缓慢释放。

    Stereoisomers of p-hydroxy-milnacipran, and methods of use thereof
    18.
    发明授权
    Stereoisomers of p-hydroxy-milnacipran, and methods of use thereof 有权
    对羟基米那普兰的立体异构体及其使用方法

    公开(公告)号：US07038085B2

    公开(公告)日：2006-05-02

    申请号：US10691465

    申请日：2003-10-22

    申请人： Roman V. Rariy ,  Michael Heffernan ,  Stephen L. Buchwald ,  Timothy M. Swager

    发明人： Roman V. Rariy ,  Michael Heffernan ,  Stephen L. Buchwald ,  Timothy M. Swager

    IPC分类号： C07C233/05 ,  A61K31/165

    CPC分类号： C07C237/24 ,  C07B2200/07 ,  C07C2601/02

    摘要： The present invention relates generally to the enantiomers of para-hydroxy-milnacipran or congeners thereof. Biological assays revealed that racemic para-hydroxy-milnacipran is approximately equipotent in inhibiting serotonin and norepinephrine uptake (IC50=28.6 nM for norepinephrine, IC50=21.7 nM for serotonin). Interestingly, (+)-para-hydroxy-milnacipran is a more potent inhibitor of norepinephrine uptake than serotonin uptake (IC50=10.3 nM for norepinephrine, IC50=22 nM for serotonin). In contrast, (−)-para-hydroxy-milnacipran is a more potent inhibitor of serotonin uptake compared to norepinephrin uptake (IC50=88.5 nM for norepinephrine, IC50=40.3 nM for serotonin). The invention also relates to salts and prodrug forms of the aforementioned compounds. In certain embodiments, the compounds of the present invention and a pharmaceutically acceptable excipient are combined to prepare a formulation for administration to a patient. Finally, the present invention relates to methods of treating mammals suffering from various afflictions, e.g., depression, chronic pain, or fibromyalgia, comprising administering to a mammal in need thereof a therapeutically effective amount of a compound of the present invention.

    摘要翻译： 本发明一般涉及对羟基 - 米那普兰或其同系物的对映异构体。 生物测定显示外消旋的对羟基 - 米那普仑在抑制5-羟色胺和去甲肾上腺素摄取方面几乎是等量的（对于5-羟色胺，对于去甲肾上腺素为IC 50 N = 28.7nM，对于5-羟色胺为131.7nM） 。 有趣的是，（+） - 对羟基 - 米那普仑是去甲肾上腺素摄取的更有效的抑制剂，而不是5-羟色胺摄取（去甲肾上腺素（IC 50）= 22nM 用于5-羟色胺）。 相比之下，与去甲肾上腺素摄取相比，（ - ） - 对羟基 - 米那普仑是一种更有效的5-羟色胺摄取抑制剂，对于去甲肾上腺素，IC 50 <= 50> = 对于5-羟色胺为40.3nM）。 本发明还涉及上述化合物的盐和前药形式。 在某些实施方案中，将本发明的化合物和药学上可接受的赋形剂混合以制备用于给予患者的制剂。 最后，本发明涉及治疗患有各种痛苦，例如抑郁症，慢性疼痛或纤维肌痛的哺乳动物的方法，包括向有需要的哺乳动物施用治疗有效量的本发明化合物。

    Compositions for topical enzymatic debridement
    19.
    发明申请
    Compositions for topical enzymatic debridement 审中-公开
    用于局部酶清创的组合物

    公开(公告)号：US20050281806A1

    公开(公告)日：2005-12-22

    申请号：US11147567

    申请日：2005-06-08

    申请人： Mark Trumbore ,  Roman Rariy ,  Mark Hirsh ,  Jane Hirsh ,  Julie Saunders

    发明人： Mark Trumbore ,  Roman Rariy ,  Mark Hirsh ,  Jane Hirsh ,  Julie Saunders

    IPC分类号： A61K9/00 ,  A61K9/12 ,  A61K33/18 ,  A61K33/36 ,  A61K33/38 ,  A61K36/48 ,  A61K38/46 ,  A61K38/48 ,  A61K47/44 ,  A61K35/78

    CPC分类号： A61K9/0014 ,  A61K9/12 ,  A61K33/18 ,  A61K33/38 ,  A61K36/48 ,  A61K38/482 ,  A61K38/4826 ,  A61K38/4873 ,  A61K38/4886 ,  A61K47/44 ,  A61L15/34 ,  A61L15/38 ,  A61L15/48 ,  A61K2300/00

    摘要： Formulations are described for the treatment by enzymatic debridement of wounds and ulcers. The formulations have a clear, transparent composition that allows for easy visualization of the wound, and are non-staining for easy clean up. These formulations can also exhibit increased enzymatic debridement activity, improved post-treatment lubricity and coating occlusivity, and stability. The formulations, optionally containing non-animal source biologics, may be in the form of lotions, aerosols to provide a spray, or a foam. A non-reactive substrate may be used as a composition carrier. A non-aqueous lotion formulation having improved enzymatic activity is provided. The non-aqueous lotion viscosity is adjusted to achieve high enzymatic activity while maintaining the application benefits of high viscosity non-aqueous lotions. The lotion formulation may be delivered in a patch.

    摘要翻译： 描述了用于通过创伤和溃疡的酶清除治疗的制剂。 制剂具有清晰，透明的组合物，其允许容易地观察伤口，并且是无污染的以便于清洁。 这些制剂还可以表现出增加的酶清除活性，改善的后处理润滑性和涂层封闭性以及稳定性。 任选地含有非动物源生物制剂的制剂可以是洗剂，提供喷雾剂或泡沫剂的气溶胶的形式。 非反应性底物可以用作组合物载体。 提供了具有改善的酶活性的非水性乳液制剂。 调节非水性乳液粘度以达到高酶活性，同时保持高粘度非水性乳液的应用益处。 洗剂制剂可以在贴剂中递送。