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公开(公告)号：US20070154402A1
公开(公告)日：2007-07-05
申请号：US11552457
申请日：2006-10-24
申请人： Mark Trumbore , Ronald Gurge , Jane Hirsh
发明人： Mark Trumbore , Ronald Gurge , Jane Hirsh
CPC分类号： A61K9/122 , A61K9/0014 , A61K9/06 , A61K9/12 , A61K9/124 , A61K31/17 , A61K31/19 , A61K31/203 , A61K38/4873 , A61K45/06 , A61K47/18 , C12Y304/22002 , A61K2300/00
摘要： A stable topical alcohol-free aerosol foam containing one or more keratolytic agents is provided. The foam-forming formulation is an emulsion which contains an HFA propellant and one or more keratolytic agents. The emulsion has an oil phase and an aqueous, i.e. water-containing, phase. The active agent(s) may be present in either phase of the emulsion 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/or other excipients. The foam is stable on the skin, for example, for at least 5 minutes at body temperature, preferably at least 20 minutes at body temperature, and disappears into the skin upon rubbing or after prolonged standing. In one embodiment, the formulation contains an HFA propellant which does not contain additional co-solvents or co-propellants. The formulations demonstrate reduced intensity of the odor and/or color associated with the keratolytic agent(s) as compared to conventional formulations containing keratolytic agents.
摘要翻译： 提供了含有一种或多种角质分解剂的稳定的局部无酒精气溶胶泡沫体。 泡沫形成制剂是含有HFA推进剂和一种或多种角质分解剂的乳液。 乳液具有油相和含水相，即含水相。 活性剂可以存在于乳液的任一相中或分散在乳液中。 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/或其它赋形剂。 泡沫在皮肤上是稳定的，例如在体温下至少5分钟，优选在体温至少20分钟，并且在摩擦或长时间放置后消失在皮肤中。 在一个实施方案中，制剂含有不含额外的共溶剂或共推进剂的HFA推进剂。 与含有角质分解剂的常规制剂相比，该配方表现出与角质分解剂相关的气味和/或颜色的强度降低。
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2.发明申请Sprayable formulations for the treatment of acute inflammatory skin conditions 审中-公开用于治疗急性炎症皮肤病症的可喷雾制剂公开(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。
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公开(公告)号：US09044398B2
公开(公告)日：2015-06-02
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
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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公开(公告)号：US08449909B2
公开(公告)日：2013-05-28
申请号：US12823628
申请日：2010-06-25
申请人： Jane Hirsh , Alison Fleming , Roman Rariy , Alexander Kilbanov
发明人： Jane Hirsh , Alison Fleming , Roman Rariy , Alexander Kilbanov
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。
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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
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。
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公开(公告)号：US20080260819A1
公开(公告)日：2008-10-23
申请号：US12112937
申请日：2008-04-30
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 。
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公开(公告)号：US20070116757A1
公开(公告)日：2007-05-24
申请号：US11557889
申请日：2006-11-08
申请人： Roman Rariy , Jane Hirsh
发明人： Roman Rariy , Jane Hirsh
IPC分类号： A61K31/5415 , C07D279/24 , A61K9/64 , A61K9/20
CPC分类号： C07D279/18 , A61K9/1617 , A61K31/5415 , C07D265/38 , C07D279/20
摘要： Pharmaceutical compositions comprising a fatty acid salt, a dicarboxylic acid salt, an alkyl sulfate salt, an aryl sulfate salt or an alkyl aryl sulfonate salt of methylene blue or a derivative of methylene blue are described herein. The compositions are preferably administered orally and can be administered as tablets, soft or hard shell capsules (e.g. soft gelatin capsules), suspensions or solutions. The composition can also be formulated as a suppository or enema or rectal administration. The compositions further comprise a pharmaceutically acceptable carrier and optionally one or more pharmaceutically acceptable excipients. Suitable excipients include diluents, binders, plasticizers, lubricants, disintegrants, colorants, stabilizers, surfactants, and combinations thereof. The fatty acid salts, alkyl sulate salts, aryl sulfate salts or alkyl aryl sulfonate salts can be co-mixed or co-melted with one or more fatty acids to make more hydrophobic compositions, which may result in less staining formulations. The compositions can be formulated for immediate release, controlled release such as extended release, delayed release, and pulsatile release, or combinations thereof. In one embodiment, the derivative of methylene blue is methylene dodecylsulfate.
摘要翻译： 本文描述了包含脂肪酸盐，二羧酸盐，烷基硫酸盐，芳基硫酸盐或亚甲基蓝或亚甲基衍生物的烷基芳基磺酸盐的药物组合物。 组合物优选口服施用，并且可以片剂，软或硬壳胶囊（例如软明胶胶囊），悬浮液或溶液给药。 组合物也可以配制成栓剂或灌肠剂或直肠给药。 组合物还包含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。 合适的赋形剂包括稀释剂，粘合剂，增塑剂，润滑剂，崩解剂，着色剂，稳定剂，表面活性剂及其组合。 脂肪酸盐，烷基磺酸盐，芳基硫酸盐或烷基芳基磺酸盐可以与一种或多种脂肪酸共混或共熔，以制备更疏水的组合物，这可能导致较少的染色制剂。 组合物可以配制成立即释放，控制释放，例如延长释放，延迟释放和脉动释放，或其组合。 在一个实施方案中，亚甲基蓝的衍生物是十二烷基硫酸亚甲酯。
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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。
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公开(公告)号：US20060024366A1
公开(公告)日：2006-02-02
申请号：US11192885
申请日：2005-07-29
申请人： Jane Hirsh , Roman Rariy , Shubha Chungi , Srinivas Rao , Michael Heffernan
发明人： Jane Hirsh , Roman Rariy , Shubha Chungi , Srinivas Rao , Michael Heffernan
IPC分类号： A61K9/22
CPC分类号： A61K9/2054 , A61K9/2846
摘要： A once-a-day oral milnacipran modified release formulation has been developed. The formulation comprises an extended release dosage unit (optionally containing the immediate release portion) coated with delayed release coating. The milnacipran composition, when administered orally, first passes through the stomach releasing from zero to less than 10% of the total milnacipran dose and then enters the intestines where drug is released slowly over an extended period of time. The release profile is characterized by a 0.05-4 hours lag time period during which less than 10% of the total milnacipran dose is released followed by a slow or extended release of the remaining drug over a defined period of time. The composition provides in vivo drug plasma levels characterized by Tmax at 4-10 hours and an approximately linear drop-off thereafter and Cmax below 3000 ng/ml, preferably below 2000 ng/ml, and most preferably below 1000 ng/ml. The composition provides 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： 已经开发了一天一次的口服米那普仑改性释放制剂。 该制剂包含用延迟释放包衣涂覆的延长释放剂量单位（任选地含有速释部分）。 当口服给药时，米那普仑组合物首先通过胃从零释放至总的米那普仑剂量的10％，然后进入肠道，药物在较长时间内缓慢释放。 释放曲线的特征在于0.05-4小时的滞后时间，在此期间，释放总的米那普仑总量的不到10％，然后在规定的时间段内缓慢或延长释放剩余的药物。 该组合物在4-10小时时提供特征为T max max的体内药物血浆水平，此后大约线性下降，低于3000ng / ml，优选低于 2000ng / ml，最优选低于1000ng / ml。 当给予需要的患者时，该组合物在约24小时内提供治疗效果，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，尿频，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，呕吐，紧张，口干，腹痛， 烦躁不安和失眠。
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公开(公告)号：US20050181050A1
公开(公告)日：2005-08-18
申请号：US11046608
申请日：2005-01-28
申请人： Jane Hirsh , Alison Fleming , Roman Rariy
发明人： Jane Hirsh , Alison Fleming , Roman Rariy
IPC分类号： A61K9/50 , A61K31/785 , A61K47/48 , A61K9/20 , A61K9/26
CPC分类号： A61K31/785 , A61K9/5026 , A61K47/585
摘要： A multiparticulate, modified release composition for oral administration has been developed. The formulation is made by complexing a drug with an ion-exchange resin in the form of small particles, typically less than 150 microns. The present invention provides novel extended release coated ion exchange particles comprising drug-resin complexes, produced by binding the salt form of the drug, that do not require impregnating agents to insure the integrity of the extended release coat. To prepare a modified release formulation, one or more of the following types of particles are formulated into a final dosage form: (a) Immediate release particles, (b) Enteric coated particles, (c) Extended release particles, (d) Enteric coated-extended release particles; and (e) Delayed release particles. The various drug-containing particles described above can be further formulated into a number of different easy-to-swallow final dosage forms including, but not limited to, a liquid suspension, gel, chewable tablet, crushable tablet, rapidly dissolving tablet, or unit of use sachet or capsule for reconstitution
摘要翻译： 已经开发了用于口服给药的多微粒，改性释放组合物。 通过将药物与通常小于150微米的小颗粒形式的离子交换树脂络合来制备该制剂。 本发明提供了新颖的延长释放包被的离子交换颗粒，其包含通过结合药物的盐形式产生的药物 - 树脂复合物，其不需要浸渍剂以确保延长释放包衣的完整性。 为了制备改性释放制剂，将下列类型的一种或多种颗粒配制成最终剂型：（a）即时释放颗粒，（b）肠溶包衣颗粒，（c）延长释放颗粒，（d）肠溶衣 - 释放颗粒; 和（e）延迟释放颗粒。 上述各种含药颗粒可以进一步配制成许多不同的易吞咽最终剂型，包括但不限于液体悬浮液，凝胶，咀嚼片，可压碎片剂，快速溶解片剂或单元 的小袋或胶囊用于重建
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