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11. 发明申请

US20050069580A1 Compositions containing both sedative and non-sedative antihistamines and sleep aids 有权
标题翻译：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：US20050069580A1
公开(公告)日：2005-03-31
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： A61K47/14 , A61K9/22 , A61K9/24 , A61K9/50 , A61K31/00 , A61K31/135 , A61K31/137 , A61K31/4402 , A61K31/445 , A61K31/4545 , A61K31/495 , A61K45/06 , A61K47/32 , A61K47/36 , A61K47/38 , A61K47/42 , A61K47/44 , A61K47/46 , A61P11/00 , A61P11/02 , A61P37/08 , A61P43/00 , A61K9/48
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。

12. 发明申请

US20050281748A1 Abuse-deterrent drug formulations 有权
标题翻译：滥用威慑药物制剂
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
IPC分类号： A61K9/14 , A61K9/20 , A61K9/48 , A61K9/50 , A61K49/00
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。

13. 发明申请

US20070036843A1 Non-ionic non-aqueous vehicles for topical and oral administration of carrier-complexed active agents 审中-公开
标题翻译：用于局部和口服载体复合活性剂的非离子非水性载体
公开(公告)号：US20070036843A1
公开(公告)日：2007-02-15
申请号：US11341016
申请日：2006-01-27
申请人： Jane Hirsh , Roman Rariy , Mark Trumbore , Alison Fleming , Mark Hirsh
发明人： Jane Hirsh , Roman Rariy , Mark Trumbore , Alison Fleming , Mark Hirsh
IPC分类号： A61K9/70 , A61K9/22
CPC分类号： A61K31/4402 , A61K9/006 , A61K9/5026 , A61K31/137 , A61K47/585
摘要： An improved controlled release composition for non-parenteral administration of active agents and other therapeutics, particularly for oral or topical administration, has been developed. The composition is made by dispersing a complex formed of an active agent bound to an ion-exchange resin or to another form of resin or carrier, in a non-ionic non-aqueous (“NINA”) vehicle. The complexes are optionally coated with one or more layers of coating material to provide a controlled pattern of release of active agent from the carrier. Replacing the usual aqueous vehicle with a NINA vehicle, such as an oil or an ointment, allows the active agent-carrier complexes, with or without coatings, to be both orally and topically administered. The compositions can be formulated as powders, liquids, liquid suspensions, gels, capsules, soft gelatin capsules, tablets, chewable tablets, topical ointments, lotions, pourable or pumpable fluids, semisolid, crushable tablets, and unit-of-use sachets or capsules for reconstitution or direct application. The combination of multiple active agents is possible with this system, in which one or more active agents are bound to particles and one or more active agents are dissolved or dispersed in the NINA vehicle. This allows the combination of two or more active agents, which are otherwise incompatible, into a single dosage form.
摘要翻译：已经开发了用于非肠胃外给药活性剂和其它治疗剂，特别是用于口服或局部给药的改进的控释组合物。该组合物通过在非离子非水（“NINA”）载体中分散由与离子交换树脂结合的活性剂形成的络合物或另一种形式的树脂或载体。复合物任选地涂覆有一层或多层涂层材料，以提供活性剂从载体中释放的受控模式。用诸如油或软膏的NINA载体代替普通的水性载体，允许具有或不具有涂层的活性剂 - 载体复合物均经口和局部施用。组合物可以配制成粉末，液体，液体悬浮液，凝胶，胶囊，软明胶胶囊，片剂，咀嚼片，局部软膏，洗剂，可倾倒或可泵送的液体，半固体，可压碎片剂和单位使用的小袋或胶囊用于重组或直接应用。该系统可以使用多种活性剂的组合，其中一种或多种活性剂与颗粒结合，一种或多种活性剂溶解或分散在NINA载体中。这允许将两种或更多种否则不相容的活性剂组合成单一剂型。

14. 发明授权

US08449909B2 Abuse-deterrent drug formulations 有权
标题翻译：滥用威慑药物制剂
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
IPC分类号： A61K9/54 , A61K9/42 , A61K31/44
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。

15. 发明申请

US20050181050A1 Dosage forms using drug-loaded ion exchange resins 审中-公开
标题翻译：使用药物负载离子交换树脂的剂型
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

16. 发明申请

US20070154402A1 Topical Pharmaceutical Foam Composition 审中-公开
标题翻译：局部药物泡沫组合物
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
IPC分类号： A61K38/46 , A61K9/12 , A61K31/19 , A61K31/203 , A61K36/18 , A61K31/17
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。

17. 发明申请

US20050255048A1 Sprayable formulations for the treatment of acute inflammatory skin conditions 审中-公开
标题翻译：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。

18. 发明申请

US20070232695A1 Gelled Periodontal Anesthetic Preparation 审中-公开
标题翻译：凝胶牙周麻醉制剂
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。

19. 发明申请

US20060003004A1 Pulsatile release compositions of milnacipran 审中-公开
标题翻译：米那普仑的脉冲释放组合物
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。

20. 发明申请

US20050123484A1 Non-flammable topical anesthetic liquid aerosols 审中-公开
标题翻译：不易燃的局部麻醉液体气溶胶
公开(公告)号：US20050123484A1
公开(公告)日：2005-06-09
申请号：US10956819
申请日：2004-10-01
申请人： Jane Hirsh , Donald Tibbetts , Mark Hirsh
发明人： Jane Hirsh , Donald Tibbetts , Mark Hirsh
IPC分类号： A61K9/12 , A61K31/00 , A61K31/24 , A61K31/245 , A61K45/06 , A61P23/02 , A61L9/04
CPC分类号： A61K31/245 , A61K9/12 , A61K31/00 , A61K31/24 , A61K45/06 , A61K2300/00
摘要： A topical liquid aerosol formulation for accurate metered dose delivery has been developed which includes a concentrate comprising a local anesthetic in a non-alcohol solvent and a hydrofluorocarbon (HFC) propellant. In the preferred embodiment, the concentration of the non-alcohol solvent in the concentrate is between about 75% and 85% by weight of the formulation. In the most preferred embodiment, the non-alcohol solvent is a water-soluble polyol such as ethylene glycol, propylene glycol, glycerol, diethylene glycol, dipropylene glycol, oligoalkylene glycols, liquid polyalkylene glycols, or combinations thereof. In one embodiment, the concentration of the local anesthetic in the concentrate is between about 15% and 25% by weight. In the preferred embodiment, the hydrofluorocarbon propellant is 1,1,1,2-tetrafluoroethane 1,1,1,2,3,3,3-heptafluoropropane or combinations thereof, in a concentration between about 35% and 65% by weight of the final formulation, more preferably between about 45% and 55% by weight of the final formulation. A particularly preferred formulation includes benzocaine, tetracaine, and butylaminobenzoate, wherein the concentration of benzocaine in the concentrate is 14% by weight, the concentration of tetracaine in the concentrate is 2% by weight, and the concentration of butylaminobenzoate in the concentrate is 2% by weight. It has been found that the formulation is more stable in the substantial absence of oxygen. The formulation is preferably administered using a metered dose device for release of a controlled amount of the local anesthetic.
摘要翻译：已经开发了用于精确计量剂量递送的局部液体气溶胶制剂，其包括在非醇溶剂中的局部麻醉剂和氢氟烃（HFC）推进剂的浓缩物。在优选的实施方案中，浓缩物中非醇溶剂的浓度为制剂重量的约75％至85％。在最优选的实施方案中，非醇溶剂是水溶性多元醇，例如乙二醇，丙二醇，甘油，二甘醇，二丙二醇，低聚亚烷基二醇，液体聚亚烷基二醇或其组合。在一个实施方案中，浓缩物中局部麻醉剂的浓度为约15重量％至25重量％。在优选的实施方案中，氢氟烃推进剂是1,1,1,2-四氟乙烷1,1,1,2,3,3,3-七氟丙烷或其组合，其浓度为约35-65重量％最终制剂，更优选为最终制剂重量的约45％至55％。特别优选的制剂包括苯佐卡因，丁卡因和丁基氨基苯甲酸酯，其中浓缩物中苯佐卡因的浓度为14重量％，浓缩物中丁卡因的浓度为2重量％，浓缩物中丁基氨基苯甲酸酯的浓度为2重量％重量。已经发现，在基本不存在氧的情况下，制剂更加稳定。制剂优选使用计量剂量装置施用以释放受控量的局部麻醉剂。

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