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公开(公告)号：US20180028529A1
公开(公告)日：2018-02-01
申请号：US15727134
申请日：2017-10-06
IPC分类号： A61K31/485 , A61K9/50 , A61K9/00 , A61K9/14 , A61K9/48
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.
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公开(公告)号：US08758813B2
公开(公告)日：2014-06-24
申请号：US13870690
申请日：2013-04-25
发明人： Jane Hirsh , Alison Fleming , Roman Rariy , Alexander M. Klibanov
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 opioids. In one 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. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised 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，特别是阿片样物质等药物。 在一个实施方案中，通过在药物和一种或多种脂肪酸之间形成盐，使药物被修饰以增加其亲油性，其中一种或多种脂肪酸的浓度是活性剂摩尔量的1至15倍。 即使药物的物理完整性受损，并且所得材料被放置在水中，嗅到或吞咽，滥用威慑组合物可防止即时释放大部分药物。 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。
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3.发明授权公开(公告)号：US09592200B2
公开(公告)日：2017-03-14
申请号：US14946275
申请日：2015-11-19
IPC分类号： A61K9/14 , A61K31/485 , A61K9/16 , A61K9/20 , A61K9/48 , A61K9/50 , A61K31/13 , A61K31/20 , A61K45/06 , A61K47/12
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 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。
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4.发明申请公开(公告)号：US20150265596A1
公开(公告)日：2015-09-24
申请号：US14717232
申请日：2015-05-20
发明人： Jane Hirsh , Alexander M. Klibanov , Timothy M. Swager , Stephen L. Buchwald , Whe Yong Lo , Alison B. Fleming , Roman V. Rariy
IPC分类号： A61K31/485 , 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。
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公开(公告)号：US10525053B2
公开(公告)日：2020-01-07
申请号：US15727134
申请日：2017-10-06
IPC分类号： A61K31/485 , A61K9/14 , A61K31/20 , A61K47/12 , A61K9/16 , A61K9/20 , A61K31/13 , A61K9/48 , A61K9/50 , A61K45/06 , A61K9/00
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.
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公开(公告)号：US20180028528A1
公开(公告)日：2018-02-01
申请号：US15725818
申请日：2017-10-05
发明人： Jane Hirsh , Alexander M. Klibanov , Timothy M. Swager , Stephen L. Buchwald , Whe Yong Lo , Alison B. Fleming , Roman V. Rariy
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 tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.
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公开(公告)号：US20170182032A1
公开(公告)日：2017-06-29
申请号：US15457153
申请日：2017-03-13
IPC分类号： A61K31/485 , A61K9/48 , A61K9/50 , A61K9/00 , A61K9/14
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 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.
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公开(公告)号：US09248195B2
公开(公告)日：2016-02-02
申请号：US14054513
申请日：2013-10-15
IPC分类号： A61K9/14 , A61K9/20 , A61K9/48 , A61K47/46 , A61K9/16 , A61K9/50 , A61K31/485 , A61K45/06 , A61K47/12
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.
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