-
公开(公告)号：US10646485B2
公开(公告)日：2020-05-12
申请号：US16218801
申请日：2018-12-13
发明人： Said Saim , Alison B. Fleming , Ravi K. Varanasi
摘要： The present disclosure relates to cured pharmaceutical compositions designed to reduce the potential for improper administration of drugs that are subject to abuse, the process of curing such composition in order to improve the dissolution stability, method of using the same for treatment of pain.
-
公开(公告)号：US20130337061A1
公开(公告)日：2013-12-19
申请号：US13970350
申请日：2013-08-19
发明人： Roman V. Rariy , Michael Heffernan
IPC分类号： A61K31/4178 , A61K31/381 , A61K31/164 , A61K9/28 , A61K31/138
CPC分类号： A61K31/4178 , A61K9/209 , A61K9/28 , A61K9/2846 , A61K9/2866 , A61K9/2886 , A61K9/4808 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/164 , A61K31/381 , A61K45/06 , A61K2300/00
摘要： Pharmaceutical compositions are provided for the pharmacological treatment of breathing disorders and, more specifically, to compositions containing agents having serotonin receptor modulating activity for the alleviation of sleep apnea (central and obstructive) and other sleep-related breathing disorders wherein the active ingredients are released such as to extend effective blood plasma concentrations across the period of sleep.
-
公开(公告)号：US20100260834A1
公开(公告)日：2010-10-14
申请号：US12823628
申请日：2010-06-25
IPC分类号： A61K9/50 , A61K31/485 , A61K9/48 , A61P25/04
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 drag, 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到损害（例如通过用刀片切碎或破碎）并且将所得材料放置在水中，嗅到或or or or or or or or or or or or or or or or or or or or or or or or or or 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。
-
4.发明授权Compositions containing both sedative and non-sedative antihistamines and sleep aids 有权含有镇静和非镇静抗组胺药和睡眠辅助剂的组合物公开(公告)号：US07585520B2
公开(公告)日：2009-09-08
申请号：US10943311
申请日：2004-09-17
申请人： Mark Hirsh , Jane Hirsh , Whe-Yong Lo
发明人： Mark Hirsh , Jane Hirsh , Whe-Yong Lo
CPC分类号： A61K45/06 , A61K9/209 , A61K9/5084 , A61K31/00 , A61K2300/00
摘要： Compositions containing both a sedative compound and a non-sedative antihistamine are provided. More particularly, compositions for administration at bedtime containing a sedating antihistamine or other sedating compound in immediate release form and a non-sedating antihistamine in delayed-release form are described. Alternatively, a composition, for administrating upon awakening, containing a non-sedating antihistamine in immediate release form, and a sedating antihistamine or other sedative in delayed-release form is described. Methods of inhibiting the release of histamines by administration of the compositions to a mammalian subject are also provided. The dosage forms may comprise other medications, such as leukotriene receptor antagonists, to enhance the suppression of histamine symptoms.
摘要翻译： 提供了含有镇静化合物和非镇静抗组胺剂的组合物。 更具体地，描述了在睡前给药的组合物，其含有立即释放形式的镇静抗组胺药或其他镇静化合物和延迟释放形式的非镇静抗组胺药。 或者，描述了用于在觉醒时施用含有立即释放形式的非镇静抗组胺剂的组合物，以及缓释形式的镇静抗组胺药或其他镇静剂。 还提供了通过将哺乳动物受试者施用组合物来抑制组胺释放的方法。 剂型可以包含其他药物，例如白三烯受体拮抗剂，以增强组胺症状的抑制。
-
公开(公告)号：US20080200508A1
公开(公告)日：2008-08-21
申请号：US11793392
申请日：2005-12-20
申请人： Roman V. Rariy , Michael Heffernan
发明人： Roman V. Rariy , Michael Heffernan
IPC分类号： A61K31/4525 , A61K31/4164 , A61P25/00 , A61P43/00
CPC分类号： A61K31/4178 , A61K9/209 , A61K9/28 , A61K9/2846 , A61K9/2866 , A61K9/2886 , A61K9/4808 , A61K31/135 , A61K31/137 , A61K31/138 , A61K31/164 , A61K31/381 , A61K45/06 , A61K2300/00
摘要： Pharmaceutical compositions are provided for the pharmacological treatment of breathing disorders and, more specifically, to compositions containing agents having serotonin receptor modulating activity for the alleviation of sleep apnea (central and obstructive) and other sleep-related breathing disorders wherein the active ingredients are released such as to extend effective blood plasma concentrations across the period of sleep.
摘要翻译： 提供药物组合物用于呼吸障碍的药理学治疗，更具体地，涉及含有具有5-羟色胺受体调节活性用于缓解睡眠呼吸暂停（中枢和阻塞性）和其它睡眠相关呼吸障碍的药剂的组合物，其中活性成分被释放 以延长整个睡眠期的有效血浆浓度。
-
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。
-
公开(公告)号：US07309799B2
公开(公告)日：2007-12-18
申请号：US11097466
申请日：2005-04-01
IPC分类号： C07C211/00 , C07C231/00
CPC分类号： C07D209/48 , C07D307/00
摘要： One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.
摘要翻译： 本发明的一个方面涉及合成米那普仑或其同系物的方法。 本发明的另一方面涉及用于合成对映体富集的米那普仑或其同系物的不对称方法。 本发明还涉及用于合成对映体富集的米那普仑或其同系物的非对称或非对称方法中的中间体的方法。
-
公开(公告)号：US20070232695A1
公开(公告)日：2007-10-04
申请号：US11534552
申请日：2006-09-22
申请人： Mark Hirsh , Jane Hirsh , Mark Trumbore
发明人： Mark Hirsh , Jane Hirsh , Mark Trumbore
IPC分类号： A61K31/325
CPC分类号： A61K31/325 , A61K9/006 , A61K9/0063 , A61K31/245 , A61K45/06 , A61K2300/00
摘要： A composition for anesthetizing oral or buccal tissues, especially periodontal pockets, is provided. The composition has a high concentration of topical anesthetic carried in a non-aqueous liquid vehicle containing a gelling agent. The anesthetics are optionally stabilized in the solution by ion-exchange complexation. The composition can anesthetize the gingivae for an extended period, such as 30 minutes or longer. Preferred anesthetics include tetracaine, benzocaine, butamben, and mixtures of these.
摘要翻译： 提供了用于麻醉口腔或颊组织，特别是牙周袋的组合物。 该组合物在含有胶凝剂的非水液体载体中携带高浓度的局部麻醉剂。 麻醉剂任选地通过离子交换络合稳定在溶液中。 组合物可以长时间麻醉牙龈，例如30分钟或更长时间。 优选的麻醉剂包括丁卡因，苯佐卡因，丁苯丁酸及其混合物。
-
公开(公告)号：US20060003004A1
公开(公告)日：2006-01-05
申请号：US11192697
申请日：2005-07-29
申请人： Jane Hirsh , Roman Rariy , Michael Heffernan
发明人： Jane Hirsh , Roman Rariy , Michael Heffernan
IPC分类号： A61K9/22
CPC分类号： A61K9/4808 , A61K9/2054 , A61K9/2059 , A61K9/2846
摘要： A once-a-day oral milnacipran pulsatile release composition has been developed that releases the drug in spaced apart “pulses”. The dosage forms are comprised of first, second and optional third dosage units, with each dosage unit having a different drug release profile. This dosage form provides in vivo drug plasma levels characterized by Cmax below 3000 ng/ml, preferably below 2000 ng/ml, and most preferably below 1000 ng/ml. The composition provides pulsatile release of milnacipran to produce a therapeutic effect over approximately 24 hours, when administered to a patient in need, resulting in diminished incidence or decreased intensity of common milnacipran side effects such as sleep disturbance, nausea, vomiting, headache, tremulousness, anxiety, panic attacks, palpitations, urinary retention, orthostatic hypotension, diaphoresis, chest pain, rash, weight gain, back pain, constipation, vertigo, increased sweating, agitation, hot flushes, tremors, fatigue, somnolence, dyspepsia, dysoria, nervousness, dry mouth, abdominal pain, irritability, and insomnia.
摘要翻译： 已经开发了一种每天一次的口服米那普仑脉动释放组合物，其释放药物以间隔开的“脉冲”。 剂型由第一，第二和任选的第三剂量单位组成，每个剂量单位具有不同的药物释放曲线。 该剂型提供体内药物血浆水平，其特征在于低于3000ng / ml，优选低于2000ng / ml，最优选低于1000ng / ml的C max。 当给予需要的患者时，组合物提供米那普仑的脉动释放以产生约24小时的治疗效果，导致常见的米那普仑副作用的发生率降低或强度降低，例如睡眠障碍，恶心，呕吐，头痛，惊恐， 焦虑，惊恐发作，心悸，尿潴留，直立性低血压，透气，胸痛，皮疹，体重增加，背痛，便秘，眩晕，出汗增加，激动，潮红，震颤，疲劳，嗜睡，消化不良， 口干，腹痛，烦躁不安和失眠。
-
公开(公告)号：US20050281748A1
公开(公告)日：2005-12-22
申请号：US11149867
申请日：2005-06-10
申请人： Jane Hirsh , Alison Fleming , Roman Rariy , Alexander Klibanov
发明人： Jane Hirsh , Alison Fleming , Roman Rariy , Alexander 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 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），所述滥用威慑物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。
-
-
-
-
-
-
-
-
-
搜索结果
66 条记录 (耗时 0.031 秒)
