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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

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。

3. 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。

4. 发明申请

WO02067902A3 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：WO02067902A3
公开(公告)日：2003-03-13
申请号：PCT/US0205629
申请日：2002-02-22
申请人： ADVANCED INHALATION RES 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 , A61K9/00 , A61K9/26 , A61K9/72 , A61K31/135 , A61K31/137 , A61K31/566 , A61K38/00 , A61K45/00 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/24 , A61K47/26 , A61K47/28 , A61K47/30 , A61K47/36 , A61K47/42 , A61P11/06
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。

5. 发明申请

WO1997044013A1 AERODYNAMICALLY LIGHT PARTICLES FOR PULMONARY DRUG DELIVERY 审中-公开
标题翻译：用于脉冲药物递送的空气微粒
公开(公告)号：WO1997044013A1
公开(公告)日：1997-11-27
申请号：PCT/US1997008895
申请日：1997-05-23
申请人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY , THE PENN STATE RESEARCH FOUNDATION , EDWARDS, David, A. , CAPONETTI, Giovanni , HRKACH, Jeffrey, S. , LOTAN, Noah , HANES, Justin , BEN-JEBRIA, Abdell, Aziz , LANGER, Robert, S.
发明人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY , THE PENN STATE RESEARCH FOUNDATION
IPC分类号： A61K09/00
CPC分类号： A61K9/0075 , A61K9/1647 , A61K31/137
摘要： Improved aerodynamically light particles for delivery to the pulmonary system, and methods for their preparation and administration are provided. In a preferred embodiment, the aerodynamically light particles are made of a biodegradable material and have a tap density less than 0.4 g/cm and a mass mean diameter between 5 mu m and 30 mu m. The particles may be formed of biodegradable materials such as biodegradable polymers. For example, the particles may be formed of a functionalized polyester graft copolymer consisting of a linear alpha -hydroxy-acid polyester backbone having at least one amino acid group incorporated therein and at least one poly(amino acid) side chain extending from an amino acid group in the polyester backbone. In one embodiment, aerodynamically light particles having a large mean diameter, for example greater than 5 mu m, can be used for enhanced delivery of a therapeutic or diagnostic agent to the alveolar region of the lung. The aerodynamically light particles optionally can incorporate a therapeutic or diagnostic agent, and may be effectively aerosolized for administration to the respiratory tract to permit systemic or local delivery of wide variety of incrorporated agents.
摘要翻译：提供了用于递送至肺系统的改善的空气动力学轻微颗粒，以及其制备和给药方法。在优选实施方案中，空气动力学轻微颗粒由可生物降解材料制成，并且振实密度小于0.4g / cm 3，质量平均直径在5μm至30μm之间。颗粒可以由可生物降解的材料如可生物降解的聚合物形成。例如，颗粒可以由官能化的聚酯接枝共聚物形成，该聚酯接枝共聚物由具有至少一个氨基酸基团的直链α-羟基酸聚酯主链和至少一个从氨基酸延伸的聚（氨基酸）侧链组成集团在聚酯骨干。在一个实施方案中，具有大平均直径（例如大于5μm）的空气动力学轻微颗粒可用于增强治疗剂或诊断剂递送至肺泡区域。空气动力学轻微颗粒任选地可以掺入治疗剂或诊断剂，并且可以有效地雾化以用于向呼吸道施用以允许全身或局部递送各种各样的掺入剂。

6. 发明申请

WO2004002551A3 INHALABLE EPINEPHRINE 审中-公开
标题翻译：可吸入的EPINEPHRINE
公开(公告)号：WO2004002551A3
公开(公告)日：2004-08-12
申请号：PCT/US0320166
申请日：2003-06-26
申请人： ADVANCED INHALATION RES 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： A61K9/00 , A61K9/12 , A61K9/14 , A61K9/16 , A61K31/137 , A61K31/19 , A61K31/195 , A61L9/04 , A61M20060101
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：本发明涉及将肾上腺素递送至呼吸系统的颗粒和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的颗粒的颗粒和可呼吸组合物包含作为治疗剂的生物活性剂肾上腺素或其盐。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燥的并且基本上不含推进剂。在优选的实施方案中，颗粒具有空气动力学特性，其允许将肾上腺素靶向递送至作用部位。

7. 发明申请

WO03079885A2 INHALABLE SUSTAINED THERAPEUTIC FORMULATIONS 审中-公开
标题翻译：可持续的持续治疗方案
公开(公告)号：WO03079885A2
公开(公告)日：2003-10-02
申请号：PCT/US0308537
申请日：2003-03-19
申请人： ADVANCED INHALATION RES 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： A61M31/00 , A61K9/00 , A61K9/14 , A61K9/16 , A61K9/72 , A61K31/137 , A61K31/566 , A61K38/00 , A61K38/28 , A61K45/00 , A61K47/02 , A61K47/10 , A61K47/12 , A61K47/14 , A61K47/18 , A61K47/24 , A61K47/26 , A61K47/36 , A61K47/42 , A61K47/44 , A61P3/10 , A61P5/30 , A61P11/08 , A61B
CPC分类号： A61K9/0075 , A61K9/1617 , A61K31/198 , A61K31/66 , A61K45/06 , A61K2300/00
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.
摘要翻译：本发明部分地基于意想不到的发现，即用于肺部递送包含磷脂和足够量的亮氨酸的治疗性，预防性或诊断剂的颗粒可以产生药剂的持久作用。具体地，用于肺部递送包含磷脂或磷脂组合的治疗性预防或诊断剂的颗粒，其中磷脂或磷脂组合以约1至46重量％的量存在于颗粒中; 和亮氨酸，其中亮氨酸以至少46重量％的量存在于颗粒中，可有助于药剂的持续作用。包含至少46重量百分比的亮氨酸但不含磷脂的颗粒不具有这些相同的持续作用特性。

8. 发明申请

WO0113892A3 LARGE POROUS PARTICLES BY SPRAY-DRYING 审中-公开
标题翻译：大量的多孔颗粒通过喷雾干燥
公开(公告)号：WO0113892A3
公开(公告)日：2001-06-21
申请号：PCT/US0023118
申请日：2000-08-23
申请人： ADVANCED INHALATION RES INC , LIPP MICHAEL M , BATYCKY RICHARD P , CAPONETTI GIOVANNI
发明人： LIPP MICHAEL M , BATYCKY RICHARD P , CAPONETTI GIOVANNI
IPC分类号： A61K9/14 , A61K9/00 , A61K9/16 , A61K31/137 , A61K45/00 , A61K47/04 , A61K47/12 , A61K47/24 , A61K49/00 , A61P11/00 , A61K9/72
CPC分类号： A61K9/0075 , A61K9/1611 , A61K9/1617
摘要： Particles having a tap density less than about 0.4 g/cm are formed by spray drying from a colloidal solution including a carboxylic acid or salt thereof, a phospholipid, a divalent salt and a solvent such as an aqueous-organic solvent. The colloidal solution can also include a therapeutic, prophylactic or diagnostic agent. Preferred carboxylic acids include at least two carboxyl groups. Preferred phospholipids include phosphatidylcholines, phosphatidylethanolamines, phosphatidylglycerols, phophAtidylserines, phosphatidylinositols and combinations thereof. The particles are suitable for pulmonary delivery.
摘要翻译：振实密度小于约0.4g / cm 3的颗粒通过从包含羧酸或其盐，磷脂，二价盐和溶剂如水有机溶剂的胶体溶液喷雾干燥形成。胶体溶液还可以包括治疗剂，预防剂或诊断剂。优选的羧酸包括至少两个羧基。优选的磷脂包括磷脂酰胆碱，磷脂酰乙醇胺，磷脂酰甘油，磷酰丝氨酸，磷脂酰肌醇及其组合。这些颗粒适用于肺部输送。

9. 发明申请

WO2007045689A3 INHALATORY PHARMACEUTICAL COMPOSITIONS IN FORM OF DRY POWDERS, SOLUTIONS OR SUSPENSIONS 审中-公开
标题翻译：干粉，溶液或悬浮液形式的吸入性药物组合物
公开(公告)号：WO2007045689A3
公开(公告)日：2007-09-07
申请号：PCT/EP2006067619
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。

10. 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。

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