公开(公告)号：US06280763B1

公开(公告)日：2001-08-28

申请号：US09309075

申请日：1999-05-10

申请人： Kamal K. Midha ,  Hans E. Junginer ,  Mark Hirsh

发明人： Kamal K. Midha ,  Hans E. Junginer ,  Mark Hirsh

IPC分类号： A61F1302

CPC分类号： A61K9/7023 ,  A61K31/137 ,  A61K47/12 ,  A61K47/14 ,  A61K47/22

摘要： The invention includes an apparatus and method for transdermal delivery of bupropion base. In the method of this invention, patient is administered parenterally a bupropion base in an amount effective to alleviate withdrawal symptoms and to prevent or reduce craving of nicotine in said patient. Alternatively, an effective amount of bupropion base is delivered to alleviate depression in a patient. A transdermal delivery system includes a bupropion base. The bupropion base can be mixed with an acceptable pharmaceutical carrier.

摘要翻译： 本发明包括用于安非他酮碱的透皮递送的装置和方法。 在本发明的方法中，患者以有效缓解戒断症状并预防或减少所述患者中尼古丁的渴望的量肠胃外施用安非他酮碱。 或者，输送有效量的安非他酮碱以缓解患者的抑郁症。 透皮递送系统包括安非他酮碱。 安非他酮碱可与可接受的药物载体混合。

公开(公告)号：US06645524B2

公开(公告)日：2003-11-11

申请号：US09929838

申请日：2001-08-14

申请人： Kamal K. Midha ,  Mark Hirsh ,  Whe-Yong Lo

发明人： Kamal K. Midha ,  Mark Hirsh ,  Whe-Yong Lo

IPC分类号： A61K956

CPC分类号： A61K9/5084 ,  A61K9/2081 ,  A61K9/209

摘要： Novel pharmaceutical dosage forms provide for pulsatile delivery of an antiarrhythmic agent 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. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads, granules, or particles or may comprise a single tablet with the first, second and optional third dosage units incorporated therein, or a “coated core” dosage form. Methods of treatment using the pharmaceutical dosage forms are provided as well.

公开(公告)号：US06582737B2

公开(公告)日：2003-06-24

申请号：US09962927

申请日：2001-09-25

申请人： Mark Hirsh ,  Kamal K. Midha ,  Hans E. Junginger

发明人： Mark Hirsh ,  Kamal K. Midha ,  Hans E. Junginger

IPC分类号： A61K3578

CPC分类号： A61K9/703 ,  A61K9/7084 ,  A61K9/7092 ,  A61K31/135 ,  A61K31/465 ,  A61K31/505 ,  A61K2300/00

摘要： A kit to alleviate tobacco-smoking withdrawal symptoms in a patient is disclosed which comprises: (a) a therapeutically effective amount of nicotine, at least one active nicotine metabolite, a combination of nicotine and an active nicotine metabolite, or an azapirone, or a pharmaceutically acceptable salt thereof; (b) a transdermal delivery system consisting essentially of a bupropion base in a therapeutically effective amount; and (c) a packaging material surrounding (a) and (b).

摘要翻译： 公开了一种用于减轻患者戒烟戒烟症状的试剂盒，其包括：（a）治疗有效量的尼古丁，至少一种活性尼古丁代谢物，尼古丁和活性尼古丁代谢物的组合，或氮杂氮酮，或 其药学上可接受的盐;（b）基本上由治疗有效量的安非他酮碱组成的透皮递送系统; （c）围绕（a）和（b）的包装材料。

公开(公告)号：US06500457B1

公开(公告)日：2002-12-31

申请号：US09639584

申请日：2000-08-14

申请人： Kamal K. Midha ,  Mark Hirsh ,  Whe-Yong Lo

发明人： Kamal K. Midha ,  Mark Hirsh ,  Whe-Yong Lo

IPC分类号： A61K920

CPC分类号： A61K9/5084 ,  A61K9/2081 ,  A61K9/209

摘要： Novel pharmaceutical dosage forms provide for pulsatile delivery of an antiarrhythmic agent 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. The dosage forms may comprise capsules housing compressed tablets or drug-containing beads, granules, or particles or may comprise a single tablet with the first, second and optional third dosage units incorporated therein, or a “coated core” dosage form. Methods of treatment using the pharmaceutical dosage forms are provided as well.

公开(公告)号：US06312716B1

公开(公告)日：2001-11-06

申请号：US09562178

申请日：2000-05-02

申请人： Kamal K. Midha ,  Hans E. Junginger ,  Mark Hirsh

发明人： Kamal K. Midha ,  Hans E. Junginger ,  Mark Hirsh

IPC分类号： A61F1302

CPC分类号： A61K47/14 ,  A61K9/7023 ,  A61K31/137 ,  A61K47/12 ,  A61K47/22

摘要： The invention includes a patch and method for transdermal delivery of bupropion base. In the method of this invention, a patient is administered a bupropion base in an amount effective to alleviate withdrawal symptoms and to prevent or reduce craving of nicotine in said patient. Alternatively, an effective amount of bupropion base is delivered to alleviate depression in a patient or to treat obesity. A transdermal patch includes a bupropion base. The bupropion base can be mixed with an acceptable pharmaceutical carrier.

摘要翻译： 本发明包括用于安非他酮碱的透皮递送的贴剂和方法。 在本发明的方法中，患者以有效减轻戒断症状的量并且预防或减少所述患者中的尼古丁的渴望量施用安非他酮碱。 或者，递送有效量的安非他酮碱以缓解患者的抑郁症或治疗肥胖症。 透皮贴剂包括安非他酮碱。 安非他酮碱可与可接受的药物载体混合。

公开(公告)号：US07387792B2

公开(公告)日：2008-06-17

申请号：US11041474

申请日：2005-01-24

申请人： Jane C. Hirsh ,  Kamal K. Midha ,  Mark Hirsh ,  Whe-Yong Lo

发明人： Jane C. Hirsh ,  Kamal K. Midha ,  Mark Hirsh ,  Whe-Yong Lo

IPC分类号： A61K9/20 ,  A61K9/22 ,  A61K9/24 ,  A61K9/46

CPC分类号： A61K9/209 ,  A61K9/0056

摘要： New pharmaceutical compositions in unit dosage form are disclosed for both intraoral and oral administration to a patient, said unit dosage form configured to be placed intraorally of said patient, which comprises: (a) as a first portion, at least one discrete molded triturate tablet comprising a therapeutically effective amount of at least one pharmaceutically active ingredient capable of intraoral administration; and (b) as a second portion located around the said first portion, a therapeutically effective amount of at least one pharmaceutically active ingredient capable of oral administration and which is releasable and orally ingestible by the patient after the molded triturate tablet has disintegrated or has dissolved intraorally.

摘要翻译： 公开了单位剂量形式的新的药物组合物，用于向患者进行口内和口服给药，所述单位剂型被配置为置于所述患者的口内，其包括：（a）作为第一部分，至少一个离散的模制成型的片剂 包括治疗有效量的至少一种能口内给药的药物活性成分; 和（b）作为位于所述第一部分周围的第二部分，治疗有效量的至少一种能够口服给药的药学活性成分，并且其在模制的特定片剂崩解或溶解之后由患者可释放和口服摄入 口语

公开(公告)号：US20050255048A1

公开(公告)日：2005-11-17

申请号：US11128947

申请日：2005-05-13

申请人： Mark Hirsh ,  Jane Hirsh ,  Ira Skolnik ,  Mark Trumbore

发明人： Mark Hirsh ,  Jane Hirsh ,  Ira Skolnik ,  Mark Trumbore

IPC分类号： A61K9/12 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/496 ,  A61K31/58 ,  A61K31/65 ,  A61K31/704 ,  A61K31/7048

CPC分类号： A61K31/58 ,  A61K9/0014 ,  A61K9/06 ,  A61K9/122 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/496 ,  A61K31/65 ,  A61K31/704 ,  A61K31/7048 ,  A61K45/06 ,  A61K2300/00

摘要： A topical spray or foam, methods of making the formulation, and methods of use thereof, has been developed. In one preferred embodiment, the composition includes one or more active agents and exhibits both antibacterial activity and antifungal activity. Excipients such as chemical disinfectants, anti-pruritic agents to minimize itching, and skin protective compounds may be added. The composition may be formulated to be dispensed as a spray or foam and the spray or foam may be administered either by a hand pump or by an aerosolizing propellant. A second single phase formulation has also been developed. The formulation comprises a first drug which is water soluble or hydrophilic and a second drug which is lipid soluble or hydrophobic, wherein at least one of the drugs is bound to an ion-exchange resin. The use of binding resins, such as ion-exchange resins, allows drugs with incompatible solvent requirements to be prepared in a single-phase formulation.

摘要翻译： 已经开发了局部喷雾或泡沫，制备方法及其使用方法。 在一个优选的实施方案中，组合物包含一种或多种活性剂并且表现出抗菌活性和抗真菌活性。 可以加入赋形剂如化学消毒剂，抗瘙痒剂以最小化瘙痒和皮肤保护性化合物。 组合物可以配制成以喷雾或泡沫的形式分配，并且喷雾或泡沫可以通过手泵或雾化推进剂施用。 还开发了第二个单相制剂。 该制剂包含水溶性或亲水性的第一药物和脂溶性或疏水性的第二药物，其中至少一种药物与离子交换树脂结合。 使用结合树脂，例如离子交换树脂，可以在单相制剂中制备具有不相容溶剂要求的药物。

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

IPC分类号： A61K9/24 ,  A61K9/20 ,  A61K9/22 ,  A61K9/28 ,  A61K9/14

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：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：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。