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1. 发明申请

WO2007093305A2 LOW-FRIABILITY, PATIENT-FRIENDLY ORALLY DISINTEGRATING FORMULATIONS 审中-公开
标题翻译：低适应性，患者友好的ORALLY DISINC制剂
公开(公告)号：WO2007093305A2
公开(公告)日：2007-08-23
申请号：PCT/EP2007/001011
申请日：2007-02-06
申请人： ANTARES PHARMA IPL AG , GRENIER, Arnaud , DECAUDIN, Celine , CARRARA, Dario, Norberto , CONTE, Ubaldo , MAGGI, Lauretta
发明人： GRENIER, Arnaud , DECAUDIN, Celine , CARRARA, Dario, Norberto , CONTE, Ubaldo , MAGGI, Lauretta
CPC分类号： A61K9/0056 , A61K9/2018 , A61K9/2027 , A61K9/2095 , A61K31/78
摘要： The present invention relates to a rapidly disintegrating orally administratable solid dosage formulation that includes at least one active ingredient, at least one first disintegration agent that is at least one type-C methacrylic acid copolymer according to the U.S. Pharmacopoeia National Formulary US/NF, a second disintegration agent of crospovidone or a cross-linked povidone polymer derivative thereof, and a non-cariogenic diluent that does not increase glucose blood levels. The at least one first disintegration agent does not function as an enteric coating, insulation coating intended to protect active ingredient(s), or coating intended to mask taste or smell. The solid dosage form has a mass of about 50 to about 1000 mg, and the at least one first disintegration agent is present in the dosage form in an amount not exceeding 15%, with respect to the total weight of the dosage form. The second disintegration agent is present in the dosage form in an amount not exceeding 15% with respect to the total weight of the dosage form. The first and the second disintegration agent are present in total amounts that provide a weight ratio of about 1 : 1 to about 1:3, wherein the dosage form provides at least one of the in vitro or in vivo disintegration time that is less than 30 seconds, and has a friability of 1% or less according to the U.S. Pharmacopoeia test.
摘要翻译：本发明涉及快速崩解的可口服给药的固体剂型制剂，其包含至少一种活性成分，至少一种第一崩解剂，其是根据US Pharmacopoeia National Formulary US / NF至少一种C型甲基丙烯酸共聚物，交联聚维酮的第二崩解剂或其交联聚维酮聚合物衍生物和不增加葡萄糖血液水平的非致龋剂稀释剂。至少一种第一崩解剂不用作肠溶衣，旨在保护活性成分的绝缘涂层或旨在掩盖味道或气味的涂层。相对于剂型的总重量，固体剂型具有约50至约1000mg的质量，并且至少一种第一崩解剂以不超过15％的量存在于剂型中。相对于剂型的总重量，第二崩解剂以不超过15％的量存在于剂型中。第一和第二崩解剂以提供重量比为约1:1至约1:3的总量存在，其中该剂型提供至少一种体外或体内崩解时间小于30 秒，根据美国药典测试，其脆度为1％以下。

2. 发明申请

WO2011084668A1 NESTORONE®/ESTRADIOL TRANSDERMAL GEL 审中-公开
标题翻译： NESTORONE®/ ESTRADIOL TRANSDERMAL GEL
公开(公告)号：WO2011084668A1
公开(公告)日：2011-07-14
申请号：PCT/US2010/060941
申请日：2010-12-17
申请人： THE POPULATION COUNCIL, INC. , ANTARES PHARMA IPL AG , SITRUK-WARE, Regine , CARRARA, Dario Norberto, Ramon , GRENIER, Arnaud
发明人： SITRUK-WARE, Regine , CARRARA, Dario Norberto, Ramon , GRENIER, Arnaud
IPC分类号： A61K31/565 , A61K31/57 , A61K9/00 , A61P15/18
CPC分类号： A61K31/565 , A61K9/0014 , A61K31/57 , A61K2300/00
摘要： The invention discloses compositions and methods for ensuring in both women of fertile age where it ensures also a contraception with additional health benefits and in postmenopausal women where it offers a hormonal therapy with additional medical benefits such as the potential for lower risk of thrombosis. The aforementioned compositions comprising NES as a potent progestational and antiovulatory agent with no androgenic nor estrogenic nor glucocorticoid effect, and combined with estradiol formulated for non-oral transdermal administration as specific daily doses.
摘要翻译：本发明公开了用于确保两性生育年龄的妇女的组合物和方法，其确保具有额外的健康益处的避孕措施以及绝经后妇女，其中提供具有额外医疗益处的激素疗法，例如血栓形成风险降低的潜力。上述组合物包含NES作为无雄激素和雌激素而不是糖皮质激素作用的有效的孕激素和抗iov药，并与配制用于非口服透皮给药的雌二醇组合作为特定的日剂量。

3. 发明申请

WO2005107812A1 PERMEATION ENHANCING COMPOSITIONS FOR ANTICHOLINERGIC AGENTS 审中-公开
标题翻译：渗透剂增强抗化学药剂组合物
公开(公告)号：WO2005107812A1
公开(公告)日：2005-11-17
申请号：PCT/EP2005/004799
申请日：2005-05-03
申请人： ANTARES PHARMA IPL AG , GRENIER, Arnaud , CARRARA, Dario, Norberto, R. , BESSE, Celine
发明人： GRENIER, Arnaud , CARRARA, Dario, Norberto, R. , BESSE, Celine
IPC分类号： A61K47/18
CPC分类号： A61K47/18 , A61K9/0014 , A61K9/06 , A61K9/7023 , A61K31/17 , A61K31/195 , A61K47/10 , Y10S514/818 , Y10S514/821 , A61K2300/00
摘要： A transdermal or topical composition including anticholinergic agents, such as oxybutynin, a urea-containing compound and a carrier system. A method is disclosed for treating a subject for urinary incontinence while reducing the incidences of peak concentrations of drug and undesirable side effects.
摘要翻译：一种透皮或局部组合物，包括抗胆碱剂，例如奥昔布宁，含尿素化合物和载体系统。公开了一种用于治疗受试者尿失禁同时减少药物峰值浓度和不良副作用的发生率的方法。

4. 发明申请

WO2005039531A1 TRANSDERMAL PHARMACEUTICAL FORMULATION FOR MINIMIZING SKIN RESIDUES 审中-公开
标题翻译：用于最小化皮肤残留物的透皮药物制剂
公开(公告)号：WO2005039531A1
公开(公告)日：2005-05-06
申请号：PCT/EP2004/011175
申请日：2004-10-06
申请人： ANTARES PHARMA IPL AG , R. CARRARA, Dario, Norberto , GRENIER, Arnaud , BESSE, Celine
发明人： R. CARRARA, Dario, Norberto , GRENIER, Arnaud , BESSE, Celine
IPC分类号： A61K9/06
CPC分类号： A61K9/7007 , A61K9/0014 , A61K9/006 , A61K9/06 , A61K31/025 , A61K31/435 , A61K47/08 , A61K47/10 , A61K47/12 , A61K47/32 , A61K47/38 , Y10S514/946 , Y10S514/947
摘要： This invention relates to novel transdermal or transmucosal pharmaceutical formulation which reduces the occurrences of contamination of other individuals and the transference to clothing of the user. The novel formulation includes at least one pharmacologically active ingredient, and a solvent system having a monoalkylether of diethylene gycol and a gycol present in specified ratios, and a mixture of water and alcohol. The invention also relates to a method for inhibiting or delaying crystallization of an active agent in a pharmaceutical formulation.
摘要翻译：本发明涉及新型透皮或透粘膜药物制剂，其减少其他个体的污染的发生以及对使用者衣服的转移。该新型制剂包含至少一种药理学活性成分，以及具有二乙二醇和一定比例存在的gycol的单烷基醚和水与醇的混合物的溶剂体系。本发明还涉及抑制或延迟药物制剂中活性剂结晶的方法。

5. 发明申请

WO2008012071A2 PHARMACEUTICAL COMPOSITIONS OF NICOTINE AND METHODS OF USE THEREOF 审中-公开
标题翻译：烟碱的药物组合物及其使用方法
公开(公告)号：WO2008012071A2
公开(公告)日：2008-01-31
申请号：PCT/EP2007/006579
申请日：2007-07-24
申请人： ANTARES PHARMA IPL AG , R. CARRARA, Dario, Norberto , GRENIER, Arnaud , BESSE, Celine
发明人： R. CARRARA, Dario, Norberto , GRENIER, Arnaud , BESSE, Celine
IPC分类号： A61K9/06 , A61P25/34
CPC分类号： A61K9/0014 , A61K9/7015 , A61K47/10
摘要： The present invention comprises non occlusive compositions for transdermal delivery of nicotine, and more particularly pharmaceutically acceptable salts thereof, and methods of making same. The composition may, for example, be a gel suitable for transdermal or transmucosal applications. The compositions of the present invention typically comprise a mixture of water and alcohol, and a solvent system having a mono alkyl ether of diethylene glycol and a glycol present in specified ratios and in specific amounts, wherein the pH of the gel is usually between about pH 5.5 and about pH 6.5. The compositions may include further components, for example, the hydroalcoholic vehicle may further comprise additional penetration enhancer(s), buffering agent(s), antioxidant(s), stabilizer(s) and/or gelling agent(s). The invention also relates to a method for the sustained delivery of nicotine pharmaceutically acceptable salts to treat a variety of conditions and disorders.
摘要翻译：本发明包括用于透皮递送尼古丁的非闭合性组合物，更特别是其药学上可接受的盐及其制备方法。例如，该组合物可以是适用于透皮或透粘膜应用的凝胶。本发明的组合物通常包含水和醇的混合物以及具有以特定比例和特定量存在的二甘醇和二醇的单烷基醚的溶剂体系，其中凝胶的pH通常在约pH 5.5和约pH 6.5。组合物可以包含其他组分，例如，水醇载体可以进一步包含另外的渗透增强剂，缓冲剂，抗氧化剂，稳定剂和/或胶凝剂。本发明还涉及持续输送尼古丁药学上可接受的盐以治疗多种病症和病症的方法。

6. 发明申请

WO2004080413A2 USES AND FORMULATIONS FOR TRANSDERMAL OR TRANSMUCOSAL APPLICATION OF ACTIVE AGENTS 审中-公开
标题翻译：用于活性剂的透皮或透射应用的用途和制剂
公开(公告)号：WO2004080413A2
公开(公告)日：2004-09-23
申请号：PCT/US2004/007291
申请日：2004-03-11
申请人： ANTARES PHARMA IPL AG , CARRARA, Dario, Norberto, R. , GRENIER, Arnaud , BESSE, Céline , SIMES, Stephen, M. , LEHMAN, Leah, M.
发明人： CARRARA, Dario, Norberto, R. , GRENIER, Arnaud , BESSE, Céline , SIMES, Stephen, M. , LEHMAN, Leah, M.
IPC分类号： A61K
CPC分类号： A61K31/56 , A61K9/0014 , A61K9/06 , A61K47/10 , A61K47/32 , A61K47/38
摘要： Uses and formulations for providing transdermal or transmucosal delivery of active agents to subjects in need thereof. The formulations and methods treat symptoms of hormonal disorders including hypogonadism, female sexual desire disorder, female menopausal disorder, and adrenal insufficiency.
摘要翻译：用于将活性剂透皮或经粘膜递送至有需要的受试者的用途和制剂。制剂和方法治疗激素失调症状，包括性腺机能减退，女性性欲障碍，女性绝经障碍和肾上腺功能不全。

7. 发明申请

WO2008001204A2 TRANSDERMAL COMPOSITIONS OF PRAMIPEXOLE HAVING ENHANCED PERMEATION PROPERTIES 审中-公开
标题翻译：具有增强渗透性能的透明质酸酯组合物
公开(公告)号：WO2008001204A2
公开(公告)日：2008-01-03
申请号：PCT/IB2007/001760
申请日：2007-06-27
申请人： ANTARES PHARMA IPL AG , GRENIER, Arnaud , CARRARA, Dario Norberto
发明人： GRENIER, Arnaud , CARRARA, Dario Norberto
CPC分类号： A61K31/428 , A61K9/0014
摘要： A pharmaceutical composition for transdermal or transmucosal delivery of an active agent to treat a movement disorder such as Parkinson's disease. The composition provides enhanced transdermal or transmucosal delivery of the active agent by including an alkanolamine as a permeation enhancer with a carrier of water and at least one short-chain alcohol and with the composition having a neutral pH. The composition provides controlled and sustained release of the active agent suitable for daily administration.
摘要翻译：用于透皮或经粘膜递送活性剂以治疗运动障碍如帕金森病的药物组合物。该组合物通过将含有水和至少一种短链醇的载体作为渗透促进剂的链烷醇胺和具有中性pH的组合物来提供增强的透皮或经粘膜递送活性剂。组合物提供适于日常给药的活性剂的受控和持续释放。

8. 发明申请

WO2008001200A3 TRANSDERMAL COMPOSITION HAVING ENHANCED COLOR STABILITY 审中-公开
公开(公告)号：WO2008001200A3
公开(公告)日：2008-01-03
申请号：PCT/IB2007/001752
申请日：2007-06-27
申请人： ANTARES PHARMA IPL AG , GRENIER, Arnaud , CARRARA, Dario, Norberto
发明人： GRENIER, Arnaud , CARRARA, Dario, Norberto
IPC分类号： A61K9/08 , A61K47/02 , A61K31/428
摘要： A pharmaceutical composition for transdermal or transmucosal delivery of a pharmaceutical agent effective to treat a neurological disorder such as Parkinson's disease is disclosed. The composition contains an antioxidant, which provides color and chemical stability of the pharmaceutical agent. The antioxidant may also provide enhanced skin permeability of the agent.

9. 发明申请

WO2007022924A2 PHARMACEUTICAL COMPOSITIONS WITH MELTING POINT DEPRESSANT AGENTS AND METHOD OF MAKING SAME 审中-公开
标题翻译：具有熔点不良剂的药物组合物及其制备方法
公开(公告)号：WO2007022924A2
公开(公告)日：2007-03-01
申请号：PCT/EP2006/008170
申请日：2006-08-18
申请人： ANTARES PHARMA IPL AG , CARRARA, Dario, Norberto , GRENIER, Arnaud , ALBERTI, Ingo , ROGUE, Christelle , BESSE, Celine , LAETITIA, Henry
发明人： CARRARA, Dario, Norberto , GRENIER, Arnaud , ALBERTI, Ingo , ROGUE, Christelle , BESSE, Celine , LAETITIA, Henry
IPC分类号： A61K9/00 , A61K9/06 , A61K31/00 , A61K47/14 , A61K47/34 , A61K47/32
CPC分类号： A61K9/0014 , A61K9/06 , A61K31/00 , A61K47/10 , A61K47/24 , A61K47/32 , A61K47/44
摘要： The invention relates to the use of chemical fragrance ingredient to lower the melting point of active agents, thereby changing crystalline active agents into an amorphous state. The invention also relates to methods of enhancing the transdermal or transmucosal skin permeation or skin penetration of pharmacologically active agents to patients in need thereof. The compositions of the present invention present the additional benefits of being substantially alcohol-free and having a pleasant olfactory profile.
摘要翻译：本发明涉及使用化学香料成分来降低活性剂的熔点，从而将结晶活性剂改变成无定形状态。本发明还涉及增强药理学活性剂对有需要的患者的透皮或经粘膜皮肤渗透或皮肤渗透的方法。本发明的组合物具有基本上无醇且具有令人愉悦的嗅觉特征的额外益处。

10. 发明申请

WO2005105059A1 PERMEATION ENHANCER COMPRISING GENUS CURCUMA OR GERMACRONE FOR TRANSDERMAL AND TOPICAL ADMINISTRATION OF ACTIVE AGENTS 审中-公开
标题翻译：渗透性增强剂包括基因曲霉或灭活剂用于活性代谢物的超导和局部给药
公开(公告)号：WO2005105059A1
公开(公告)日：2005-11-10
申请号：PCT/EP2005/004594
申请日：2005-04-28
申请人： ANTARES PHARMA IPL AG , CARRARA, Dario, Norberto, R. , GRENIER, Arnaud , BESSE, Celine , ALBERTI, Ingo , HENRY, Laetitia
发明人： CARRARA, Dario, Norberto, R. , GRENIER, Arnaud , BESSE, Celine , ALBERTI, Ingo , HENRY, Laetitia
IPC分类号： A61K9/70
CPC分类号： A61K9/0014 , A61K31/121 , A61K36/9066 , A61K47/10 , A61K47/32 , A61K47/38 , A61K47/46 , A61K2300/00
摘要： A formulation, method and system for the topical, transdermal or transmucosal administration of a therapeutically effective active agent. Particularly, the invention provides a formulation, system and method for enhancing the permeation or penetration of active agents across the dermal or mucosal surfaces of a mammalian subject. The formulation includes a plant extract of the genus Curcuma of the family Zingiberaceae, a germacrone, or a natural or synthetic constituent thereof, which has been found to increase penetration of the active agent across the dermal or mucosal surface. If desired, a secondary permeation enhancer of a polyalcohol, a monoalkyl ether of diethylene glycol, a tetraglycol, or a mixture thereof can be used for certain active agents for optimal permeation enhancement.
摘要翻译：用于局部，透皮或经粘膜给药治疗有效活性剂的制剂，方法和系统。特别地，本发明提供了用于增强活性剂穿过哺乳动物受试者的皮肤或粘膜表面的渗透或渗透的制剂，系统和方法。该制剂包括姜科科植物的姜黄属植物提取物，锗菌属或其天然或合成成分，其已被发现增加活性剂穿过皮肤或粘膜表面的渗透。如果需要，可以使用多元醇的二次渗透增强剂，二甘醇的单烷基醚，四甘醇或其混合物，用于某些活性剂以获得最佳的渗透增强作用。

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