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    Abuse-Deterrent Pharmaceutical Compositions of Opiods and Other Drugs
    1.
    发明申请
    Abuse-Deterrent Pharmaceutical Compositions of Opiods and Other Drugs 有权
    鸦片和其他药物的滥用威慑药物组合物

    公开(公告)号：US20130045960A1

    公开(公告)日：2013-02-21

    申请号：US13551455

    申请日：2012-07-17

    申请人： Jane Hirsh ,  Alexander M. Klibanov ,  Timothy M. Swager ,  Stephen L. Buchwald ,  Whe Yong Lo ,  Alison Fleming ,  Roman V. Rariy

    发明人： Jane Hirsh ,  Alexander M. Klibanov ,  Timothy M. Swager ,  Stephen L. Buchwald ,  Whe Yong Lo ,  Alison Fleming ,  Roman V. Rariy

    IPC分类号： A61K31/555 ,  A61K31/485 ,  C07D489/08 ,  A61P25/36 ,  C07F3/06

    CPC分类号： A61K31/485 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1682 ,  A61K9/1694 ,  A61K9/4858 ,  A61K9/50 ,  A61K9/5052 ,  A61K9/5084 ,  A61K31/20 ,  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 opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. 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 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，修饰药物以增加其亲油性。 在优选实施方案中，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。 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，当按照指导施用时，通过酶降解，胆汁酸的表面活性作用和机械侵蚀的组合，组合物被分解或逐渐溶解在胃肠道内，药物从组合物中缓慢释放。

    ABUSE-DETERRENT PHARMACEUTICAL COMPOSITIONS OF OPIOIDS AND OTHER DRUGS
    2.
    发明申请
    ABUSE-DETERRENT PHARMACEUTICAL COMPOSITIONS OF OPIOIDS AND OTHER DRUGS 审中-公开
    阿片类药物和其他药物的滥用药物组合物

    公开(公告)号：US20080199530A1

    公开(公告)日：2008-08-21

    申请号：US12112993

    申请日：2008-04-30

    申请人： Jane Hirsh ,  Alison Fleming ,  Roman V. Rariy

    发明人： Jane Hirsh ,  Alison Fleming ,  Roman V. Rariy

    IPC分类号： A61K9/16

    CPC分类号： A61K31/485 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1682 ,  A61K9/1694 ,  A61K9/4858 ,  A61K9/50 ,  A61K9/5052 ,  A61K9/5084 ,  A61K31/20 ,  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 opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments 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, but enzymatically degradable by enzymes present in the human gastrointestinal tract. 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 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，修饰药物以增加其亲油性。 在优选实施方案中，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，但是通过存在于人胃肠道中的酶可酶促降解。 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，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。

    Abuse-deterrent pharmaceutical compositions of opiods and other drugs
    4.
    发明授权
    Abuse-deterrent pharmaceutical compositions of opiods 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：US07399488B2

    公开(公告)日：2008-07-15

    申请号：US10614866

    申请日：2003-07-07

    申请人： Jane Hirsh ,  Alexander M. Kibanov ,  Timothy M. Swager ,  Stephen L. Buchwald ,  Whe Yong Lo ,  Alison B. Fleming ,  Roman V. Rariy

    发明人： Jane Hirsh ,  Alexander M. Kibanov ,  Timothy M. Swager ,  Stephen L. Buchwald ,  Whe Yong Lo ,  Alison B. Fleming ,  Roman V. Rariy

    IPC分类号： A61K9/14 ,  A61K9/50

    CPC分类号： A61K31/485 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1682 ,  A61K9/1694 ,  A61K9/4858 ,  A61K9/50 ,  A61K9/5052 ,  A61K9/5084 ,  A61K31/20 ,  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 opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments 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, but enzymatically degradable by enzymes present in the human gastrointestinal tract. 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 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，修饰药物以增加其亲油性。 在优选实施方案中，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，但是通过存在于人胃肠道中的酶可酶促降解。 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，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。

    SUSTAINED RELEASE COMPOSITIONS OF DRUGS
    5.
    发明申请
    SUSTAINED RELEASE COMPOSITIONS OF DRUGS 审中-公开
    持续发布药物组合物

    公开(公告)号：US20080260819A1

    公开(公告)日：2008-10-23

    申请号：US12112937

    申请日：2008-04-30

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

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

    IPC分类号： A61K9/52 ,  A61K9/00 ,  A61K9/26

    CPC分类号： A61K31/485 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1682 ,  A61K9/1694 ,  A61K9/4858 ,  A61K9/50 ,  A61K9/5052 ,  A61K9/5084 ,  A61K31/20 ,  A61K47/12

    摘要： A sustained release pharmaceutical composition has been developed. The composition resists dose dumping when broken, crushed or chewed, which enhances the safety of the dosage form should it be accidentally or intentionally physically compromised. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments 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 coated with one or more coating layers. The sustained release composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chewing or crushing) and the resulting material is placed in 0.1N HCl. 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 diffusion, surfactant action of bile acids, mechanical erosion, and in some embodiments, enzymatic degradation.

    摘要翻译： 持续释放的药物组合物已被开发出来。 当破碎，粉碎或咀嚼时，组合物抵抗剂量倾倒，如果意外或故意身体受损，则可提高剂型的安全性。 在优选的实施方案中，修饰药物以增加其亲油性。 在优选实施方案中，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，含有涂覆有一个或多个涂层的微粒的药物。 即使制剂的物理完整性受损（例如通过咀嚼或破碎），并将所得材料置于0.1N HCl中，持续释放组合物延缓了药物的释放。 然而，当按照指导施用时，当组合物通过扩散，胆汁酸的表面活性作用，机械侵蚀，以及在一些实施方案中的酶降解的组合被分解或逐渐溶解在胃肠道内时，药物缓慢地从组合物中释放 。

    Abuse-deterrent pharmaceutical compositions of opioids and other drugs
    6.
    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 PHARMACEUTICAL COMPOSITIONS OF OPIOIDS AND OTHER DRUGS
    7.
    发明申请
    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：US20090297617A1

    公开(公告)日：2009-12-03

    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： A61K9/50 ,  A61K31/485

    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损（例如通过用刀片切碎或破碎），所述滥用威慑组合物也会延缓药物的释放，并将所得物质置于水中，嗅到或吞咽。 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。

    Foamable microemulsion compositions for topical administration
    10.
    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。