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1. 发明申请

WO2011032108A3 FORMULATION FOR ROOM TEMPERATURE STABILIZATION OF A LIVE ATTENUATED BACTERIAL VACCINE 审中-公开
标题翻译：一种减毒活疫苗的室温稳定配方
公开(公告)号：WO2011032108A3
公开(公告)日：2011-03-17
申请号：PCT/US2010/048674
申请日：2010-09-13
申请人： TRUONG-LE, Vu , OHTAKE, Satoshi , CHIUEH, Gary , MARTIN, Russell , SAXENA, Atul , PHAM, Binh , LECHUGA-BALLESTEROS, David
发明人： TRUONG-LE, Vu , OHTAKE, Satoshi , CHIUEH, Gary , MARTIN, Russell , SAXENA, Atul , PHAM, Binh , LECHUGA-BALLESTEROS, David
IPC分类号： A61K39/02
摘要： This invention provides methods and compositions for stabilizing proteins and vaccines in dried formulations. In particular, a cavitation method and compositions of preparing a dried vaccine are provided that stabilize the viability of live bacteria and live virus vaccines at room temperature.
摘要翻译：本发明提供了用于稳定干燥制剂中的蛋白质和疫苗的方法和组合物。具体而言，提供了制备干疫苗的空化方法和组合物，其在室温下稳定活细菌和活病毒疫苗的存活力。

2. 发明申请

WO2011005354A9 GALLIUM FORMULATION FOR THE TREATMENT AND PREVENTION OF INFECTIOUS DISEASES 审中-公开
公开(公告)号：WO2011005354A9
公开(公告)日：2011-01-13
申请号：PCT/US2010/033599
申请日：2010-05-04
申请人： ARIDIS PHARMACEUTICALS , OHTAKE, Satoshi , TRUONG-LE, Vu , LECHUGA-BALLESTEROS, David , YEE, Luisa , PHAM, Binh V. , MARTIN, Russell , SAXENA, Atul
发明人： OHTAKE, Satoshi , TRUONG-LE, Vu , LECHUGA-BALLESTEROS, David , YEE, Luisa , PHAM, Binh V. , MARTIN, Russell , SAXENA, Atul
IPC分类号： A61K31/28
摘要： A method and composition for treatment of bacterial infections caused by gram negative or gram positive bacteria such as Staphylococcus aureus, Rhodococcus equi, Mycobacterium tuberculosis, Escherichia coli, Klebsiella pneumoniae, Klebsiella oxytoca, Pseudomonas aeruginosa, Haemophilus influenzae, Proteus mirabilis, Enterobacter species, Serratia marcescens as well as those caused by Burkholderia cepacia, Stenotrophomonas maltophilia, Alcaligenes xylosoxidans , and multidrug resistant Pseudomonas aeruginosa , using a formulation containing gallium (III), in a pharmaceutically acceptable salt or complex thereof.

3. 发明申请

WO2009042202A2 FORMULATIONS FOR PRESERVATION OF ROTA VIRUS 审中-公开
标题翻译：保存ROTA病毒的配方
公开(公告)号：WO2009042202A2
公开(公告)日：2009-04-02
申请号：PCT/US2008/011169
申请日：2008-09-24
申请人： ARIDIS PHARMACEUTICALS , TRUONG-LE, Vu , YEE, Luisa , LECHUGA-BALLESTEROS, David , OHTAKE, Satoshi
发明人： TRUONG-LE, Vu , YEE, Luisa , LECHUGA-BALLESTEROS, David , OHTAKE, Satoshi
IPC分类号： A01N63/00 , A61K39/15 , C12N7/01
CPC分类号： A61K39/15 , A61K39/12 , A61K2039/542 , C12N2720/12334
摘要： This invention provides formulations and methods for stabilizing viruses in liquid and dried formulations. In particular, formulations are provided including Zn 2 + cations that stabilize the viability of Rotaviruses . Methods of vaccination include neutralization of gastric contents and administration of the vaccine formulations of the invention.
摘要翻译：本发明提供了用于稳定液体和干燥制剂中的病毒的制剂和方法。具体而言，提供了包含稳定轮状病毒存活力的Zn 2 +阳离子的制剂。接种方法包括中和胃内容物并给予本发明的疫苗制剂。

4. 发明申请

WO2006004646A1 AEROSOL FORMULATION COMPRISING NICOTINE SALT 审中-公开
标题翻译：包含NICOTINE盐的气溶胶制剂
公开(公告)号：WO2006004646A1
公开(公告)日：2006-01-12
申请号：PCT/US2005/022703
申请日：2005-06-28
申请人： NEKTAR THERAPEUTICS , LECHUGA-BALLESTEROS, David , KUO, Mei-Chang , SONG, Yuan , BUECHE, Blaine
发明人： LECHUGA-BALLESTEROS, David , KUO, Mei-Chang , SONG, Yuan , BUECHE, Blaine
IPC分类号： A61K9/72
CPC分类号： A61K9/008 , A01N43/40 , A61K31/4439 , A61K31/465 , A01N37/36 , A01N37/02 , A01N25/06 , A01N25/02 , A01N2300/00
摘要： An aerosolizable formulation comprises free-base nicotine, an organic acid, and a hydrofluoroalkane propellant. The organic acid is present in a mole ratio with said nicotine in a range of about 0.25:1 (organic acid:nicotine) to about 4:1 (organic acid:nicotine). The organic acid and said free-base nicotine form a nicotine salt. An equivalent mixture of free-base nicotine and organic acid in water has a pH between about pH 3.0 and about pH 9.0. The aerosolizable formulation is aerosolizable, for example, by a metered dose inhaler for administration to a user.
摘要翻译：可雾化的制剂包含游离碱尼古丁，有机酸和氢氟烷烃推进剂。有机酸以约0.25:1（有机酸：尼古丁）至约4:1（有机酸：尼古丁）的范围内与所述尼古丁的摩尔比存在。有机酸和游离碱尼古丁形成尼古丁盐。游离碱尼古丁和有机酸在水中的等效混合物的pH在约pH3.0和约pH9.0之间。可雾化制剂可雾化，例如通过用于给用户施用的计量吸入器。

5. 发明申请

WO2003094890A1 CAPSULES FOR DRY POWDER INHALERS AND METHODS OF MAKING AND USING SAME 审中-公开
标题翻译：干粉粉末吸收剂的制备方法及其制备方法和使用方法
公开(公告)号：WO2003094890A1
公开(公告)日：2003-11-20
申请号：PCT/US2003/014309
申请日：2003-05-07
申请人： NEKTAR THERAPEUTICS , MILLER, Danforth , LECHUGA-BALLESTEROS, David
发明人： MILLER, Danforth , LECHUGA-BALLESTEROS, David
IPC分类号： A61K9/12
CPC分类号： A61K9/0075 , A61K9/4816
摘要： Pulmonary delivery of dry powder formulations by aerosol inhalation has received much attention as an attractive alternative to intravenous, intramuscular, and subcutaneous injection, since this approach eliminates the necessity for injection syringes and needles. The present invention provides dry powder filled cellulose-based capsules having particular utility for use with dry powder inhalers. Such capsules not only readily coordinate with conventional DPIs but also coordinate with conventional powder filling technologies, thereby saving time, labor and cost. The invention further provides a novel procedure for determining, ab initio , appropriate and optimal conditions for preparing such powder filled capsules. Specifically, when packaging dry powder formulations for long-term storage, it is important to ensure that the water content of the powder does not exceed the critical moisture point, that point at which the powder loses physical and chemical stability. The present invention describes means for predicting equilibrium moisture contents, which in turn can be used to establish suitable capsule preparation and filling protocols.
摘要翻译：通过气溶胶吸入的干粉制剂的肺部输送作为静脉内，肌内和皮下注射的有吸引力的替代物已经受到很多关注，因为该方法消除了注射针管和针头的必要性。本发明提供了干粉填充的纤维素基胶囊，其特别适用于干粉吸入器。这种胶囊不仅可以容易地与传统的DPI协调，而且还可以配合传统的粉末填充技术，从而节省时间，人力和成本。本发明还提供了一种用于确定制备这种填充粉末的胶囊的从头，适当和最佳条件的新方法。具体来说，当包装干粉配方用于长期储存时，重要的是确保粉末的含水量不超过临界水分点，即粉末失去物理和化学稳定性的点。本发明描述了用于预测平衡水分含量的方法，其依次可用于建立合适的胶囊制备和填充方案。

6. 发明申请

WO2005000267A2 PHARMACEUTICAL FORMULATION COMPRISING A WATER-INSOLUBLE ACTIVE AGENT 审中-公开
标题翻译：包含水不溶性活性剂的药物制剂
公开(公告)号：WO2005000267A2
公开(公告)日：2005-01-06
申请号：PCT/US2004/016696
申请日：2004-05-27
申请人： NEKTAR THERAPEUTICS , VEHRING, Reinhard , LECHUGA-BALLESTEROS, David , MILLER, Danforth, P.
发明人： VEHRING, Reinhard , LECHUGA-BALLESTEROS, David , MILLER, Danforth, P.
IPC分类号： A61K9/00
CPC分类号： A61K9/0075 , A61K9/1617 , A61K9/167 , A61K9/1694 , A61K9/5015 , A61K9/5089 , A61K31/00
摘要： A method of preparing a pharmaceutical formulation comprises providing a solution comprising a first solvent, a second solvent, an active agent, and an excipient. The second solvent is less polar than the first solvent and the excipient is more soluble in water than the active agent. The first and second solvents are removed from the solution to produce particles comprising the active agent and the excipient. In one version, the excipient comprises an amino acid and/or a phospholipid. A pharmaceutical formulation made by a version of the invention comprises particles comprising an active agent and an excipient which at least partially encapsulates the active agent, wherein the excipient is more soluble in water than the active agent.
摘要翻译：制备药物制剂的方法包括提供包含第一溶剂，第二溶剂，活性剂和赋形剂的溶液。第二溶剂的极性比第一溶剂少，赋形剂比活性剂更易溶于水。从溶液中除去第一和第二溶剂以产生包含活性剂和赋形剂的颗粒。在一个版本中，赋形剂包含氨基酸和/或磷脂。由本发明版本制成的药物制剂包含包含至少部分包封活性剂的活性剂和赋形剂的颗粒，其中赋形剂比活性剂更易溶于水。

7. 发明申请

WO2009064469A1 PULMONARY DELIVERY OF A MACROLIDE ANTIBIOTIC 审中-公开
标题翻译：脉冲递送抗大鼠抗生素
公开(公告)号：WO2009064469A1
公开(公告)日：2009-05-22
申请号：PCT/US2008/012796
申请日：2008-11-14
申请人： NEKTAR THERAPEUTICS , LALONDE, Guy , LECHUGA-BALLESTEROS, David , LIANG, Yi , DAILEY, Lea Ann
发明人： LALONDE, Guy , LECHUGA-BALLESTEROS, David , LIANG, Yi , DAILEY, Lea Ann
IPC分类号： A61K31/7052 , A61K9/72
CPC分类号： A61K9/0073 , A61K31/7052
摘要： The present invention provides macrolide antibiotic containing compositions for oral inhalation to the lung. The macrolide antibiotic compositions are useful in the treatment and prophylaxis of both pulmonary and systemic bacterial infections.
摘要翻译：本发明提供了用于口服吸入肺的含大环内酯类抗生素的组合物。大环内酯抗生素组合物可用于治疗和预防肺部和全身性细菌感染。

8. 发明申请

WO2006055950A1 PHARMACEUTICAL DRY POWDER FORMULATION ON THE BASIS PARTICLES COMPRISING MULTIPLE ACTIVE AGENTS 审中-公开
标题翻译：基于包含多种活性剂的基础颗粒的药物干粉
公开(公告)号：WO2006055950A1
公开(公告)日：2006-05-26
申请号：PCT/US2005/042277
申请日：2005-11-18
申请人： NEKTAR THERAPEUTICS , MILLER, Danforth , LECHUGA-BALLESTEROS, David
发明人： MILLER, Danforth , LECHUGA-BALLESTEROS, David
IPC分类号： A61K9/12 , A61K9/00 , A61K9/14 , A61P31/04 , A61P31/06
CPC分类号： A61K9/0075 , A61K9/14 , A61K9/1688
摘要： One or more embodiments of the present invention relate to a pharmaceutical formulation on the basis of particles comprising multiple active agents.
摘要翻译：本发明的一个或多个实施方案涉及基于包含多种活性剂的颗粒的药物制剂。

9. 发明申请

WO2006002140A2 COMPOSITION COMPRISING AMPHOTERICINB METHODS AND SYSTEMS 审中-公开
标题翻译：包含两性霉素方法和系统的组合物
公开(公告)号：WO2006002140A2
公开(公告)日：2006-01-05
申请号：PCT/US2005/021886
申请日：2005-06-21
申请人： NEKTAR THERAPEUTICS , DUDDU, Sarma , PALAKODATY, Srinivas , LECHUGA-BALLESTEROS, David , MILLER, Danforth , KUGLER, Alan, R. , FRANTZ, Christopher , TAN, Trixie , MALCOLMSON, Richard , WASHCO, Keith , SWEENEY, Theresa , TARARA, Thomas, E. , DWIVEDI, Sarvajna , ELDON, Michael, A.
发明人： DUDDU, Sarma , PALAKODATY, Srinivas , LECHUGA-BALLESTEROS, David , MILLER, Danforth , KUGLER, Alan, R. , FRANTZ, Christopher , TAN, Trixie , MALCOLMSON, Richard , WASHCO, Keith , SWEENEY, Theresa , TARARA, Thomas, E. , DWIVEDI, Sarvajna , ELDON, Michael, A.
IPC分类号： A61K9/72
CPC分类号： A61K9/0075 , A61K9/1611 , A61K9/1617 , A61K9/1694 , A61K31/7048 , A61M15/0028 , A61M15/0041 , A61M2202/064
摘要： A composition includes particles including at least about 95 wt% of amphotericin B, wherein the particles have a mass median diameter ranging from about 1.1 µm to about 1.9 µm. Another composition also includes particles including at least about 95 wt% of amphotericin B, wherein at least about 80 wt% of the particles have a geometric diameter ranging from about 1.1 µm to about 1.9 gm. Yet another composition includes particles including amphotericin B, wherein the particles have a mass median diameter less than about 1.9 µm, and wherein the amphotericin B has a crystallinity level of at least about 20%. Unit dosage forms, delivery systems, and methods may involve similar compositions.
摘要翻译：组合物包括含有至少约95重量％的两性霉素B的颗粒，其中所述颗粒的质量中值直径范围为约1.1微米至约1.9微米。另一种组合物还包括包含至少约95重量％的两性霉素B的颗粒，其中至少约80重量％的颗粒具有约1.1微米至约1.9微米的几何直径。又一种组合物包括包含两性霉素B的颗粒，其中颗粒的质量中值直径小于约1.9μm，并且其中两性霉素B的结晶度水平为至少约20％。单位剂型，输送系统和方法可能涉及相似的组合物。

10. 发明申请

WO2003035051A3 THE USE OF PROTON SEQUESTERING AGENTS IN DRUG FORMULATIONS 审中-公开
公开(公告)号：WO2003035051A3
公开(公告)日：2003-05-01
申请号：PCT/US2002/033017
申请日：2002-10-16
申请人： INHALE THERAPEUTIC SYSTEMS, INC. , LEHRMAN, S. Russ , CHIANG, Hi-Shi , KUO, Mei-Chang , ZHANG, Jiang , LECHUGA-BALLESTEROS, David
发明人： LEHRMAN, S. Russ , CHIANG, Hi-Shi , KUO, Mei-Chang , ZHANG, Jiang , LECHUGA-BALLESTEROS, David
IPC分类号： A61K9/16
摘要： Methods are provided for preparing spray-dried, drug-containing particles comprising the steps of: (a) selecting a drug, an aqueous solution, and a proton-sequestering agent; (b) adding the drug and the proton-sequestering agent to the solution to form a feed solution; and(c) spray drying the feed solution to form the spray- dried, drug-containing particles, wherein at least a portion of the proton-sequestering agent remains mixed with the drug in the spray-dried, drug containing particles. particles and pharmaceutical formulations comprising the prepared particles as well as methods of use are also provided.

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