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    Abuse-deterrent drug formulations
    11.
    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。

    Foamable microemulsion compositions for topical administration
    14.
    发明授权
    Foamable microemulsion compositions for topical administration 失效
    用于局部给药的可发泡微乳液组合物

    公开(公告)号：US08652443B2

    公开(公告)日：2014-02-18

    申请号：US12371155

    申请日：2009-02-13

    申请人： Ravi K. Varanasi ,  Roman V. Rariy

    发明人： Ravi K. Varanasi ,  Roman V. Rariy

    IPC分类号： A61K9/00 ,  A61K9/12 ,  A61K9/107

    CPC分类号： A61K9/0014 ,  A61K9/122 ,  A61K9/124 ,  A61K31/164

    摘要： Described are ethanol-free foamable microemulsions for topical application, and method of making them. The propellants used in the compositions may be environmentally-friendly hydrofluoroalkanes. The foam compositions may also comprise one or more of a variety of active ingredients, including anti-inflammatory agents, anesthetics, and keratolytic agents.

    摘要翻译： 描述了用于局部应用的无乙醇泡沫微乳液及其制备方法。 在组合物中使用的推进剂可以是环保的氢氟烷烃。 泡沫组合物还可以包含一种或多种各种活性成分，包括抗炎剂，麻醉剂和角质分解剂。

    STABILIZED TRANSDERMAL BUPROPION PREPARATIONS
    19.
    发明申请
    STABILIZED TRANSDERMAL BUPROPION PREPARATIONS 审中-公开
    稳定的转基因制剂

    公开(公告)号：US20080044462A1

    公开(公告)日：2008-02-21

    申请号：US11697484

    申请日：2007-04-06

    申请人： Mark W. Trumbore ,  Roman V. Rariy ,  Jane C. Hirsh ,  Mark Hirsh

    发明人： Mark W. Trumbore ,  Roman V. Rariy ,  Jane C. Hirsh ,  Mark Hirsh

    IPC分类号： A61K31/205 ,  A61K9/70 ,  A61K31/381

    CPC分类号： A61K9/06 ,  A61K9/0014 ,  A61K9/7023 ,  A61K31/135 ,  A61K31/137 ,  A61K31/138 ,  A61K31/381 ,  A61K31/4525 ,  A61K31/465

    摘要： Pharmaceutical compositions for transdermal administration containing a fatty acid salt, a dicarboxylic acid salt, an alkyl sulfonic acid salt, an aryl sulfonic acid salt, or an alkyl aryl sulfonic acid salt of an unstable active agent, such as bupropion free base or a derivative of burpropion free base, such as bupropion free base or derivative of bupropion free base, paroxetine, fluvoxamine, fluoxetine, sertraline, venlafaxine, duloxetine, and metabolites and derivatives thereof are described herein. The composition may also contain one or more antioxidants. The compositions can be prepared by forming the bupropion salt followed by addition of the antioxidant. Alternatively, bupropion can be combined first with the antioxidant followed by addition of the acid to form the salt. The compositions can be administered as a gel, cream, lotion, ointment, or patch and typically contain a pharmaceutically acceptable carrier and optionally one or more pharmaceutically acceptable excipients. The compositions described herein are expected to be more stable than bupropion free base and should exhibit excellent dermal penetration.

    摘要翻译： 用于透皮给药的药物组合物，其含有不稳定活性剂的脂肪酸盐，二羧酸盐，烷基磺酸盐，芳基磺酸盐或烷基芳基磺酸盐，例如安非他酮游离碱或 如安非他酮游离碱或安非他酮游离碱衍生物，帕罗西汀，氟伏沙明，氟西汀，舍曲林，文拉法辛，度洛西汀及其代谢产物及其衍生物等无刺激性游离碱。 组合物还可以含有一种或多种抗氧化剂。 可以通过形成安非他酮盐然后添加抗氧化剂来制备组合物。 或者，安非他酮可以首先与抗氧化剂组合，然后加入酸形成盐。 组合物可以作为凝胶，霜剂，洗剂，软膏剂或贴片施用，并且通常含有药学上可接受的载体和任选的一种或多种药学上可接受的赋形剂。 预期本文所述的组合物比安非他酮游离碱更稳定，并且应显示出优异的皮肤渗透性。