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1. 发明申请

WO2005102283A1 DRY POWDER PHARMACEUTICAL COMPOSITION, ITS PREPARATION PROCESS AND STABLE AQUEOUS SUSPENSION OBTAINED FROM SUCH COMPOSITION 审中-公开
标题翻译：干粉药物组合物，其制备方法和由这些组合物获得的稳定的水性悬浮液
公开(公告)号：WO2005102283A1
公开(公告)日：2005-11-03
申请号：PCT/EP2005/004277
申请日：2005-04-21
申请人： ERATECH S.R.L. , CAPONETTI, Giovanni , ARTUSI, Mariella , MAGGI, Loretta , CORVI MORA, Paolo
发明人： CAPONETTI, Giovanni , ARTUSI, Mariella , MAGGI, Loretta , CORVI MORA, Paolo
IPC分类号： A61K9/16
CPC分类号： A61K9/145 , A61K9/0075 , A61K9/0078 , A61K9/14 , A61K9/143 , A61K31/192 , A61K31/573 , A61K31/58
摘要： Pharmaceutical composition in a dry powder form comprising at least one hydrophobic active principle, at least one water-soluble excipient and at least one surfactant, wherein the particles in said dry powder state have a Volume Mean Diameter VMD d greater than the Volume Mean Diameter VMD w of particles in a suspension obtained from said pharmaceutical composition at standard conditions of dispersion in a water-medium. It is also disclosed a process to prepare such dry composition and an extemporaneous suspension for inhalation therapy obtainable from said dry composition.
摘要翻译：包含至少一种疏水活性成分，至少一种水溶性赋形剂和至少一种表面活性剂的干粉形式的药物组合物，其中所述干粉状态的颗粒具有大于体积平均直径VMDwof颗粒的体积平均直径VMDd 在由水介质中分散的标准条件下由所述药物组合物获得的悬浮液中。还公开了制备这种干组合物和可从所述干组合物获得的用于吸入治疗的临时悬浮液的方法。

2. 发明申请

WO2007045689A2 INHALATORY PHARMACEUTICAL COMPOSITIONS IN FORM OF DRY POWDERS, SOLUTIONS OR SUSPENSIONS OBTAINED FROM THE SAME AND PROCESS FOR THEIR PREPARATION 审中-公开
标题翻译：干燥粉末形式的吸收性药物组合物，从其获得的溶液或悬浮液及其制备方法
公开(公告)号：WO2007045689A2
公开(公告)日：2007-04-26
申请号：PCT/EP2006/067619
申请日：2006-10-20
申请人： ERATECH S.r.l. , VENEZIANI, Cristina , CAPONETTI, Giovanni , MAGGI, Loretta , ZANELLOTTI, Laura
发明人： VENEZIANI, Cristina , CAPONETTI, Giovanni , MAGGI, Loretta , ZANELLOTTI, Laura
IPC分类号： A61K9/72 , A61K45/06
CPC分类号： A61K9/0078 , A61K9/0075 , A61K45/06
摘要： Inhalatory pharmaceutical composition comprising a drug, a soluble excipient and a surfactant, characterized by: - said soluble excipient is present in an amount between 10% and less than 100% by weight; - the weight ratio between said surfactant and said drug is between 0.01 and 10; - the particle size of at least 50% of the particles of said powder is below 5 µm; - the bulk density d b of said powder is between 0.1 and 0.3 g/cc; - the tapped density dt o f said powder is between 0.15 and 0.7 g/cc; - the ratio d b /d t is between 0.2 and 0.65.
摘要翻译：包含药物，可溶性赋形剂和表面活性剂的吸入性药物组合物，其特征在于： - 所述可溶性赋形剂的存在量为10重量％至小于100重量％; - 所述表面活性剂与所述药物之间的重量比为0.01至10; - 所述粉末的至少50％的颗粒的粒径小于5μm; - 所述粉末的堆积密度d b b为0.1至0.3g / cc; - 所述粉末的抽头密度dt在0.15和0.7g / cc之间; - 比率d / d 在0.2和0.65之间。

3. 发明申请

WO2002067902A2 MODULATION OF RELEASE FROM DRY POWDER FORMULATIONS 审中-公开
标题翻译：干粉制剂的释放调节
公开(公告)号：WO2002067902A2
公开(公告)日：2002-09-06
申请号：PCT/US2002/005629
申请日：2002-02-22
申请人： ADVANCED INHALATION RESEARCH, INC. , BASU, Sujit, K. , CAPONETTI, Giovanni , DEAVER, Daniel, R. , ELBERT, Katharina, J. , HRKACH, Jeffrey, S. , LIPP, Michael, M.
发明人： BASU, Sujit, K. , CAPONETTI, Giovanni , DEAVER, Daniel, R. , ELBERT, Katharina, J. , HRKACH, Jeffrey, S. , LIPP, Michael, M.
IPC分类号： A61K9/16
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/1617 , A61K31/135 , A61K31/137 , A61K2300/00
摘要： Particles which include a bioactive agent are prepared to have a desired matrix transition temperature. Delivery of the particles via the pulmonary system results in modulation of drug release from the particles. Sustained release and/or sustained phamacologic action of the drug can be obtained by formin particles which include a combination of phospholipids that are miscible in one another and have a high matrix transition temperature.
摘要翻译：制备包含生物活性剂的颗粒具有所需的基质转变温度。通过肺系统递送颗粒导致药物从颗粒释放的调节。药物的持续释放和/或持续的药物作用可以通过包含彼此混溶并具有高基质转变温度的磷脂组合的形式蛋白颗粒获得。

4. 发明申请

WO2004002551A2 INHALABLE EPINEPHRINE 审中-公开
标题翻译：不可吸收的EPINEPHRINE
公开(公告)号：WO2004002551A2
公开(公告)日：2004-01-08
申请号：PCT/US2003/020166
申请日：2003-06-26
申请人： ADVANCED INHALATION RESEARCH, INC. , BATYCKY, Richard, P. , CAPONETTI, Giovanni , CHILDS, Mariko , EHRICH, Elliot , FU, Karen , HRKACH, Jeffery, S. , LI, Wen-I , LIPP, Michael, M. , PAN, Mei-Ling , SUMMA, Jason
发明人： BATYCKY, Richard, P. , CAPONETTI, Giovanni , CHILDS, Mariko , EHRICH, Elliot , FU, Karen , HRKACH, Jeffery, S. , LI, Wen-I , LIPP, Michael, M. , PAN, Mei-Ling , SUMMA, Jason
IPC分类号： A61M
CPC分类号： A61K31/137 , A61K9/0073 , A61K9/0075 , A61K9/1617 , A61K31/135 , A61M15/0091 , A61M2202/06
摘要： The present invention is directed toward particles for delivery of epinephrine to the respiratory system and methods for treating a patient in need of epinephrine. The particles and respirable compositions comprising the particles of the present invention described herein comprise the bioactive agent epinephrine, or a salt thereof, as a therapeutic agent. The particles are preferably formed by spray drying. Preferably, the particles and the respirable compositions are substantially dry and are substantially free of propellents. In a preferred embodiment, the particles have aerodynamic characteristics that permit targeted delivery of epinephrine to the site(s) of action.
摘要翻译：本发明涉及用于将肾上腺素递送至呼吸系统的颗粒以及用于治疗需要肾上腺素的患者的方法。包含本文所述的本发明颗粒的颗粒和可呼吸组合物包含生物活性剂肾上腺素或其盐作为治疗剂。颗粒优选通过喷雾干燥形成。优选地，颗粒和可呼吸组合物基本上是干的并且基本上不含促进剂。在一个优选的实施方案中，颗粒具有允许将肾上腺素靶向递送至作用部位的空气动力学特征。

5. 发明申请

WO2003079885A3 INHALABLE SUSTAINED THERAPEUTIC FORMULATIONS 审中-公开
公开(公告)号：WO2003079885A3
公开(公告)日：2003-10-02
申请号：PCT/US2003/008537
申请日：2003-03-19
申请人： ADVANCED INHALATION RESEARCH, INC. , BASU, Sujit, K. , CAPONETTI, Giovanni , CLARK, Robert , ELBERT, Katharina, J.
发明人： BASU, Sujit, K. , CAPONETTI, Giovanni , CLARK, Robert , ELBERT, Katharina, J.
IPC分类号： A61K9/12
摘要： The present invention is based, in part, on the unexpected discovery that particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that comprise a phospholipid and a sufficient amount of leucine can produce sustained effect of the agent. Specifically, particles for pulmonary delivery of a therapeutic, prophylactic or diagnostic agent that contain a phospholipid or combination of phospholipids, wherein the phospholipid or combination of phospholipids is present in the particles in an amount of about 1 to 46 weight percent; and leucine, wherein leucine is present in the particles in an amount of at least 46 weight percent, can contribute to sustained effect of the agent. Particles that comprise at least 46 weight percent leucine but that do not contain phospholipids do not exhibit these same sustained effect properties.

6. 发明申请

WO2016055544A1 COMPOSITION COMPRISING AT LEAST ONE DRY POWDER OBTAINED BY SPRAY DRYING TO INCREASE THE STABILITY OF THE FORMULATION 审中-公开
标题翻译：组合物包含由喷雾干燥获得的至少一种干粉，以增加配方的稳定性
公开(公告)号：WO2016055544A1
公开(公告)日：2016-04-14
申请号：PCT/EP2015/073188
申请日：2015-10-07
申请人： ERATECH S.R.L.
发明人： MAGGI, Loretta , CAPONETTI, Giovanni , BUTTI, Heike , VENEZIANI, Cristina , ZANELLOTTI, Laura
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K31/167 , A61K31/439 , A61K31/58
CPC分类号： A61K9/1623 , A61K9/0075 , A61K9/1617 , A61K31/167 , A61K31/439 , A61K31/58
摘要： The present invention relates to inhalation formulations of drugs in the form of dry powder for inhalation administration deliverable as such with an inhaler and provided with high deliverability, respirability and stability. In particular, the invention relates to a pharmaceutical composition for inhalation use in powder form comprising a first powder comprising at least a powder (a1) comprising an active agent or a pharmaceutically acceptable salt thereof, in an amount greater than 1% by weight of the powder, leucine in an amount from 5 to 70% by weight of said powder, a sugar in an amount from 20 to 90%> by weight of the powder; and a second powder comprising a mixture of a first lactose which has an X50 from 35 to 75 μm, with a second lactose which has an X50 from 1.5 to 10 μm, the content of the first and second lactose in the mixture are respectively from 85% to 96% and from 4% to 15%. The ratio by weight between the first powder and the second powder is from 1/5 to 1/100, and the composition has a fine particle fraction (FPF) greater than 60% and a delivered fraction (DF) greater than 85%.
摘要翻译：本发明涉及用于吸入管理形式的干粉形式的药物吸入制剂，其可与吸入器一起递送并具有高递送性，呼吸性和稳定性。特别地，本发明涉及一种粉末形式的吸入用药物组合物，其包含至少包含含有活性剂或其药学上可接受的盐的粉末（a1）的第一粉末，其量大于粉末，亮氨酸的量为所述粉末的5至70重量％，糖为粉末的20至90重量％; 和第二粉末，其包含具有35至75μm的X50的第一乳糖和1.5至10微米的X50的第二乳糖的混合物，混合物中第一和第二乳糖的含量分别为85 至96％及4％至15％。第一粉末和第二粉末之间的重量比为1/5至1/100，并且组合物具有大于60％的细颗粒分数（FPF）和大于85％的递送部分（DF）。

7. 发明申请

WO2014167023A1 COMPOSITION COMPRISING AT LEAST TWO DRY POWDERS OBTAINED BY SPRAY DRYING TO INCREASE THE STABILITY OF THE FORMULATION 审中-公开
标题翻译：包含由喷雾干燥获得的至少两个干粉的组合物以增加制剂的稳定性
公开(公告)号：WO2014167023A1
公开(公告)日：2014-10-16
申请号：PCT/EP2014/057200
申请日：2014-04-09
申请人： ERATECH S.R.L.
发明人： CAPONETTI, Giovanni , MAGGI, Loretta , VENEZIANI, Cristina , VENTURA, Paolo , ZANELLOTTI, Laura
IPC分类号： A61K9/16
CPC分类号： A61K9/0073 , A61K9/0075 , A61K9/1617 , A61K9/1623 , A61K31/167 , A61K31/439 , A61K31/58 , A61K47/183 , A61K47/26
摘要： The present invention relates to inhalation formulations of drugs in the form of dry powder for inhalation administration deliverable as such with an inhaler and provided with high deliverability, respirability and stability. In particular, the invention relates to a pharmaceutical composition for inhalation in the form of powder comprising at least a first and a second powder, in which at least said first powder contains an active agent in an amount greater than 1% by weight with respect to the weight of said first powder. Both the powders comprise leucine in an amount ranging from 5 to 70% by weight with respect to the weight of each powder and a sugar in an amount ranging from 20 to 90% by weight with respect to the weight of each powder. The composition has a fine particle fraction (FPF) greater than 60% and a delivered fraction (DF) greater than 80.
摘要翻译：本发明涉及用于吸入给药的干粉形式的药物的吸入制剂，其可与吸入器一起递送并具有高递送性，呼吸性和稳定性。特别地，本发明涉及以粉末形式吸入的药物组合物，其包含至少第一和第二粉末，其中至少所述第一粉末含有相对于第一粉末的量大于1重量％的活性剂所述第一粉末的重量。两种粉末相对于每种粉末的重量相对于每种粉末的重量和相对于每种粉末重量的20至90重量％的量的糖，其含量为5-70重量％的亮氨酸。该组合物具有大于60％的细颗粒级分（FPF）和大于80的递送级分（DF）。

8. 发明申请

WO2013068565A2 MELATONIN-BASED SOLUTIONS AND POWDERS FOR THEIR PREPARATION 审中-公开
标题翻译：基于MELATONIN的解决方案和粉末制备
公开(公告)号：WO2013068565A2
公开(公告)日：2013-05-16
申请号：PCT/EP2012/072327
申请日：2012-11-09
申请人： ERATECH S.R.L.
发明人： MAGGI, Loretta , CAPONETTI, Giovanni
IPC分类号： A61K9/14 , A61K9/16 , A61K31/4045 , A61K9/00
CPC分类号： A61K47/26 , A23C9/206 , A61K9/0019 , A61K9/0031 , A61K9/08 , A61K9/14 , A61K9/1617 , A61K9/1623 , A61K9/1641 , A61K31/4045 , A61K47/10 , A61K47/183 , A61K47/34 , A61K47/38
摘要： The present invention relates to a powder for reconstitution before use for preparations for injection containing melatonin, at least one soluble excipient and at least one surfactant for the treatment of neonatal cerebral infarction. The present invention also relates to a preparation for injection in the form of a solution obtained by dissolving a powder to be reconstituted comprising melatonin, at least one soluble excipient and at least one surfactant, in a mixture of water and polyalkylene glycol, in which the melatonin is present in quantities of from 3 to 30 mg/ml and the polyalkylene glycol is present in quantities from 5 to 40% of the total volume of the liquid used.
摘要翻译：本发明涉及在使用前用于重组的粉末，其含有褪黑激素，至少一种可溶性赋形剂和至少一种用于治疗新生儿脑梗塞的表面活性剂。本发明还涉及通过将包含褪黑素，至少一种可溶性赋形剂和至少一种表面活性剂的重构粉末溶解在水和聚亚烷基二醇的混合物中而获得的溶液形式的注射剂型，其中褪黑激素的存在量为3至30mg / ml，聚亚烷基二醇的存在量为所用液体总体积的5至40％。

9. 发明公开

EP3203983A1 COMPOSITION COMPRISING AT LEAST ONE DRY POWDER OBTAINED BY SPRAY DRYING TO INCREASE THE STABILITY OF THE FORMULATION 审中-实审转让
标题翻译：通过喷雾干燥获得的至少一种干粉的组合物，以增加配方的稳定性
公开(公告)号：EP3203983A1
公开(公告)日：2017-08-16
申请号：EP15784293.1
申请日：2015-10-07
申请人： Eratech S.r.l.
发明人： MAGGI, Loretta , CAPONETTI, Giovanni , BUTTI, Heike , VENEZIANI, Cristina , ZANELLOTTI, Laura
IPC分类号： A61K9/00 , A61K9/14 , A61K9/16 , A61K31/167 , A61K31/439 , A61K31/58
CPC分类号： A61K9/1623 , A61K9/0075 , A61K9/1617 , A61K31/167 , A61K31/439 , A61K31/58
摘要： The present invention relates to inhalation formulations of drugs in the form of dry powder for inhalation administration deliverable as such with an inhaler and provided with high deliverability, respirability and stability. In particular, the invention relates to a pharmaceutical composition for inhalation use in powder form comprising a first powder comprising at least a powder (a1) comprising an active agent or a pharmaceutically acceptable salt thereof, in an amount greater than 1% by weight of the powder, leucine in an amount from 5 to 70% by weight of said powder, a sugar in an amount from 20 to 90%> by weight of the powder; and a second powder comprising a mixture of a first lactose which has an X50 from 35 to 75 μm, with a second lactose which has an X50 from 1.5 to 10 μm, the content of the first and second lactose in the mixture are respectively from 85% to 96% and from 4% to 15%. The ratio by weight between the first powder and the second powder is from 1/5 to 1/100, and the composition has a fine particle fraction (FPF) greater than 60% and a delivered fraction (DF) greater than 85%.
摘要翻译：本发明涉及用于吸入给药的干粉形式的药物吸入制剂，其可以用吸入器本身递送，并且具有高生产能力，可呼吸性和稳定性。具体而言，本发明涉及用于粉末吸入用途的药物组合物，其包含第一粉末和第二粉末，所述第一粉末包含至少一种包含活性剂或其药学上可接受的盐的粉末（a1），其量大于粉末，占所述粉末重量的5-70％的亮氨酸，占粉末重量的20-90％的糖; 以及第二粉末，其包含具有35至75μm的X50的第一乳糖与具有1.5至10μm的X50的第二乳糖的混合物，混合物中第一和第二乳糖的含量分别为85 ％至96％和4％至15％。第一粉末与第二粉末之间的重量比为1/5至1/100，并且组合物具有大于60％的细颗粒部分（FPF）和大于85％的递送部分（DF）。

10. 发明授权

EP1937229B1 INHALATORY PHARMACEUTICAL COMPOSITIONS IN FORM OF DRY POWDERS, SOLUTIONS OR SUSPENSIONS 有权转让
标题翻译：对于吸入药物组合物的干粉，溶液或混悬液形式
公开(公告)号：EP1937229B1
公开(公告)日：2015-03-11
申请号：EP06807435.0
申请日：2006-10-20
申请人： Eratech S.r.l.
发明人： VENEZIANI, Cristina , CAPONETTI, Giovanni , MAGGI, Loretta , ZANELLOTTI, Laura
IPC分类号： A61K9/72 , A61K45/06
CPC分类号： A61K9/0078 , A61K9/0075 , A61K45/06

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