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：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：US20120189557A1

公开(公告)日：2012-07-26

申请号：US13409608

申请日：2012-03-01

申请人： Jane C. Hirsh ,  Ronald M. Gurge ,  Mark Hirsh ,  Mark W. Trumbore

发明人： Jane C. Hirsh ,  Ronald M. Gurge ,  Mark Hirsh ,  Mark W. Trumbore

IPC分类号： A61K9/12 ,  B65B1/04 ,  A61Q19/00 ,  A61P17/00 ,  A61K8/02

CPC分类号： A61K47/34 ,  A61K9/0014 ,  A61K9/12 ,  A61K31/4178 ,  A61K31/4196 ,  A61K31/496 ,  A61K31/7034 ,  A61K47/02

摘要： Aerosol spray formulations capable of delivering high concentrations of active agent-containing materials and/or excipient are described herein. The formulation contains a carrier fluid, a propellant and a therapeutic, prophylactic, cosmeticeutical and/or inert solid suspended, dissolved, or dispersed in the formulation. The active ingredient may be an antibiotic, an antihistamine, an anesthetic, an anti-inflammatory, and/or an astringent. In one embodiment, the active agent is an antifungal agent. In another embodiment, the active agent is a cosmeticeutical. The active agent can optionally be dispersed on, or associated with, a carrier powder. The carrier fluid is a highly volatile silicone liquid, which evaporates in less than 10 minutes after application of the formulation to the patient's skin. The formulation may also contain one or more pharmaceutically acceptable excipients The formulation can be packaged in a conventional aerosol spray can.

摘要翻译： 本文描述了能够递送高浓度的含活性剂的物质和/或赋形剂的气溶胶喷雾制剂。 制剂含有悬浮，溶解或分散在制剂中的载体流体，推进剂和治疗性，预防性，美容化妆品和/或惰性固体。 活性成分可以是抗生素，抗组胺剂，麻醉剂，抗炎剂和/或收敛剂。 在一个实施方案中，活性剂是抗真菌剂。 在另一个实施方案中，活性剂是cosmeticutical。 活性剂可以任选地分散在载体粉末上或与载体粉末相关联。 载体流体是高挥发性有机硅液体，其在将制剂施用于患者皮肤后不到10分钟就蒸发。 制剂还可以含有一种或多种药学上可接受的赋形剂。该制剂可以包装在常规的气溶胶喷雾罐中。

公开(公告)号：US20090010869A9

公开(公告)日：2009-01-08

申请号：US11843158

申请日：2007-08-22

申请人： Mark Trumbore ,  Roman Rariy ,  Mark Hirsh ,  Jane Hirsh ,  Julie Saunders

发明人： Mark Trumbore ,  Roman Rariy ,  Mark Hirsh ,  Jane Hirsh ,  Julie Saunders

IPC分类号： A61K31/74 ,  A61K33/38 ,  A61K35/00 ,  A61K38/43 ,  A61P17/00

CPC分类号： A61K9/0014 ,  A61K9/12 ,  A61K33/18 ,  A61K33/38 ,  A61K36/48 ,  A61K38/482 ,  A61K38/4826 ,  A61K38/4873 ,  A61K38/4886 ,  A61K47/44 ,  A61L15/34 ,  A61L15/38 ,  A61L15/48 ,  A61K2300/00

摘要： Formulations are described for the treatment by enzymatic debridement of wounds and ulcers. The formulations have a clear, transparent composition that allows for easy visualization of the wound, and are non-staining for easy clean up. These formulations can also exhibit increased enzymatic debridement activity, improved post-treatment lubricity and coating occlusivity, and stability. The formulations, optionally containing non-animal source biologics, may be in the form of lotions, aerosols to provide a spray, or a foam. A non-reactive substrate may be used as a composition carrier. A non-aqueous lotion formulation having improved enzymatic activity is provided. The non-aqueous lotion viscosity is adjusted to achieve high enzymatic activity while maintaining the application benefits of high viscosity non-aqueous lotions. The lotion formulation may be delivered in a patch.

摘要翻译： 描述了用于通过创伤和溃疡的酶清除治疗的制剂。 制剂具有清晰，透明的组合物，其允许容易地观察伤口，并且是无污染的以便于清洁。 这些制剂还可以表现出增加的酶清除活性，改善的后处理润滑性和涂层封闭性以及稳定性。 任选地含有非动物源生物制剂的制剂可以是洗剂，提供喷雾剂或泡沫剂的气溶胶的形式。 非反应性底物可以用作组合物载体。 提供了具有改善的酶活性的非水性乳液制剂。 调节非水性乳液粘度以达到高酶活性，同时保持高粘度非水性乳液的应用益处。 洗剂制剂可以在贴剂中递送。

公开(公告)号：US20060188449A1

公开(公告)日：2006-08-24

申请号：US10565346

申请日：2004-10-04

申请人： Jane Hirsh ,  John Willis ,  Mark Hirsh

发明人： Jane Hirsh ,  John Willis ,  Mark Hirsh

IPC分类号： A61K31/573 ,  A61L9/04 ,  A61K31/56 ,  A61K31/24

CPC分类号： A61K31/24 ,  A61K9/0014 ,  A61K9/122 ,  A61K9/124 ,  A61K31/56 ,  A61K31/573

摘要： A stable topical aerosol foam is provided. The foam-forming formulation includes a HFA propellant and an active agent in an emulsion. The emulsion has an oil phase and an aqueous, i.e. water-containing, phase. The active agent may be present in either phase or dispersed in the emulsion. The oil phase may consist at least in part of the HFA propellant. Either or both of the oil phase and the aqueous phase may contain one or more surfactants, emulsifiers, emulsion stabilizers, buffers, and other excipients. In an alternative embodiment, the aqueous phase contains a water-soluble active agent, for example, a local anesthetic, and the oil phase contains a water-insoluble second active agent. The foam is stable on the skin, for example for at least 10 minutes at body temperature, and will disappear into the skin upon rubbing or after prolonged standing. The formulation has the advantage of an inert non-flammable hydrofluorocarbon propellant without requiring the use of additional co-solvents or co-propellants. The composition is administered to the skin or mucous membranes.

摘要翻译： 提供稳定的局部气溶胶泡沫。 泡沫形成制剂包括HFA推进剂和乳液中的活性剂。 乳液具有油相和含水相，即含水相。 活性剂可以以任一相存在或分散在乳液中。 油相可以至少部分地由HFA推进剂组成。 油相和水相中的任一种或两者可以含有一种或多种表面活性剂，乳化剂，乳液稳定剂，缓冲剂和其它赋形剂。 在另一个实施方案中，水相含有水溶性活性剂，例如局部麻醉剂，油相含有水不溶性第二活性剂。 泡沫在皮肤上是稳定的，例如在体温下至少10分钟，并且在摩擦或长时间放置后将消失在皮肤中。 该配方具有惰性不易燃氢氟烃推进剂的优点，而不需要使用额外的共溶剂或共推进剂。 将组合物施用于皮肤或粘膜。

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：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。