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1. 发明授权

US5665331A Co-microprecipitation of nanoparticulate pharmaceutical agents with crystal growth modifiers 失效
标题翻译：纳米颗粒药剂与晶体生长改性剂的共沉淀
公开(公告)号：US5665331A
公开(公告)日：1997-09-09
申请号：US370998
申请日：1995-01-10
申请人： Pranab Bagchi , Raymond P. Scaringe , H. William Bosch
发明人： Pranab Bagchi , Raymond P. Scaringe , H. William Bosch
IPC分类号： A61K9/14 , A61K49/04
CPC分类号： B82Y5/00 , A61K49/0485 , A61K9/145 , Y10S977/745 , Y10S977/881 , Y10S977/915 , Y10S977/927 , Y10S977/928
摘要： This invention describes the coprecipitation of nanoparticulate pharmaceutical agent dispersion via a process that comprises the dissolution of the said pharmaceutical agent in combination with a crystal growth modifier (CGM) in an alkaline solution and then neutralizing the said solution with an acid in the presence of suitable surface-modifying surface-active agent or agents to form a fine particle dispersion of the said pharmaceutical agent, followed by steps of diafiltration clean-up of the dispersion and then concentration of it to a desired level. This process of dispersion preparation leads to microcrystalline particles of Z-average diameters smaller than 400 nm as measured by photon correlation spectroscopy. Various modification of precipitation schemes are described, many of which are suitable for large-scale manufacture of these agent dispersions. It has been discovered that coprecipitation with CGM leads to smaller particle size compared to a case where precipitation is carried out using the pharmaceutical agent alone. Thus, this dispersion of instant invention is expected to have greater bioavailability. The CGM compound is a compound that has at least about 75% of its chemical structure identical to that of the pharmaceutical agent.
摘要翻译：本发明描述了纳米颗粒药剂分散体的共沉淀，该方法包括在碱性溶液中将所述药剂与晶体生长调节剂（CGM）组合溶解，然后在适当的存在下用酸中和所述溶液表面改性表面活性剂或试剂以形成所述药剂的细颗粒分散体，然后将分散体进行渗滤清洗，然后将其浓缩至期望水平。这种分散制备过程导致通过光子相关光谱测量的Z平均直径小于400nm的微晶颗粒。描述了各种改性的沉淀方案，其中许多适用于这些试剂分散体的大规模制造。已经发现，与仅使用药剂进行沉淀的情况相比，CGM的共沉淀导致较小的粒度。因此，本发明的这种分散体预期具有更大的生物利用度。 CGM化合物是其化学结构的至少约75％与药剂相同的化合物。

2. 发明申请

US20100329976A1 NANOPARTICULATE COMPOSITIONS OF ANGIOGENESIS INHIBITORS 审中-公开
标题翻译：血管生成抑制剂的纳米颗粒组成
公开(公告)号：US20100329976A1
公开(公告)日：2010-12-30
申请号：US12870749
申请日：2010-08-27
申请人： Elaine Merisko-Liversidge , H. William Bosch , Greta G. Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
发明人： Elaine Merisko-Liversidge , H. William Bosch , Greta G. Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
IPC分类号： A61K31/565 , A61K9/00 , A61K9/20 , A61K9/48 , A61K38/16 , A61K31/7052 , A61K49/00 , A61K36/00 , A61K36/886 , A61K36/82 , A61K36/55 , A61K35/60 , A61K35/00 , A61K39/00 , A61P9/00 , A61P35/00
CPC分类号： A61K31/00 , A61K9/145 , A61K9/146 , A61K9/148 , A61K31/565
摘要： Nanoparticulate compositions comprising at least one poorly soluble angiogenesis inhibitor and at least one surface stabilizer are described. The nanoparticulate compositions have an average particle size of less than about 2000 nm. The invention also describes methods of making and using such compositions.
摘要翻译：描述包含至少一种难溶性血管发生抑制剂和至少一种表面稳定剂的纳米颗粒组合物。纳米颗粒组合物具有小于约2000nm的平均粒度。本发明还描述了制备和使用这些组合物的方法。

3. 发明申请

US20100322852A1 NANOPARTICULATE COMPOSITIONS OF ANGIOGENESIS INHIBITORS 审中-公开
公开(公告)号：US20100322852A1
公开(公告)日：2010-12-23
申请号：US12870722
申请日：2010-08-27
申请人： Elaine Merisko-Liversidge , H. William Bosch , Greta G. Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
发明人： Elaine Merisko-Liversidge , H. William Bosch , Greta G. Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
IPC分类号： A61K31/565 , A61K9/00 , A61K38/16 , A61K31/7052 , A61K49/00 , A61K36/00 , A61K36/886 , A61K36/82 , A61K36/55 , A61K35/60 , A61K35/00 , A61K39/00 , A61P9/00 , A61P35/00
CPC分类号： A61K31/00 , A61K9/145 , A61K9/146 , A61K9/148 , A61K31/565
摘要： Nanoparticulate compositions comprising at least one poorly soluble angiogenesis inhibitor and at least one surface stabilizer are described. The nanoparticulate compositions have an average particle size of less than about 2000 nm. The invention also describes methods of making and using such compositions.

4. 发明授权

US07521068B2 Dry powder aerosols of nanoparticulate drugs 有权
标题翻译：纳米颗粒药物的干粉气溶胶
公开(公告)号：US07521068B2
公开(公告)日：2009-04-21
申请号：US09190138
申请日：1998-11-12
申请人： H. William Bosch , Kevin D. Ostrander , Eugene R. Cooper
发明人： H. William Bosch , Kevin D. Ostrander , Eugene R. Cooper
IPC分类号： A61K8/00 , A61K9/14 , A61K9/16 , A61K31/12 , A61K31/04 , A61K31/28 , A61K31/33 , A61K31/56 , A61K31/70 , A61K38/00 , A61K38/02
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/008 , A61K9/146 , A61K9/1694 , A61K9/19 , Y10S514/826 , Y10S514/851 , Y10S514/872
摘要： There invention discloses aqueous dispersions of nanoparticulate aerosol formulations, dry powder nanoparticulate aerosol formulation, propellant-based aerosol formulations, methods of using the formulations in aerosol delivery devices, and methods of making such formulations. The nanoparticles of the aqueous dispersions or dry powder formulations comprise insoluble drug particles having a surface modifier on the surface thereof.
摘要翻译：本发明公开了纳米颗粒气雾剂配方的水性分散体，干燥粉末纳米颗粒气溶胶配制剂，基于推进剂的气溶胶制剂，在气溶胶递送装置中使用制剂的方法，以及制备这些制剂的方法。含水分散体或干粉配方的纳米颗粒包含在其表面上具有表面改性剂的不溶性药物颗粒。

5. 发明申请

US20080220075A1 Nanoparticulate compositions of angiogenesis inhibitors 审中-公开
标题翻译：血管生成抑制剂的纳米颗粒组成
公开(公告)号：US20080220075A1
公开(公告)日：2008-09-11
申请号：US12076247
申请日：2008-03-14
申请人： Elaine Merisko-Liversidge , H. William Bosch , Greta G. Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
发明人： Elaine Merisko-Liversidge , H. William Bosch , Greta G. Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
IPC分类号： A61K9/14 , A61P19/02 , A61K31/56
CPC分类号： A61K31/565 , A61K9/145 , A61K9/146 , A61K31/00
摘要： Nanoparticulate compositions comprising at least one poorly soluble angiogenesis inhibitor and at least one surface stabilizer are described. The nanoparticulate compositions have an average particle size of less than about 2000 nm. The invention also describes methods of making and using such compositions.
摘要翻译：描述包含至少一种难溶性血管发生抑制剂和至少一种表面稳定剂的纳米颗粒组合物。纳米颗粒组合物具有小于约2000nm的平均粒度。本发明还描述了制备和使用这些组合物的方法。

6. 发明申请

US20080050461A1 NANOPARTICULATE COMPOSITIONS OF ANGIOGENESIS INHIBITORS 审中-公开
公开(公告)号：US20080050461A1
公开(公告)日：2008-02-28
申请号：US11928250
申请日：2007-10-30
申请人： Elaine Merisko-Liversidge , H. William Bosch , Greta Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
发明人： Elaine Merisko-Liversidge , H. William Bosch , Greta Cary , John Pruitt , Tuula Ryde , Rajeev Jain , Amy Walters
IPC分类号： A61K31/565 , A61K36/00 , A61K38/02 , A61K9/14
CPC分类号： A61K31/00 , A61K9/145 , A61K9/146 , A61K9/148 , A61K31/565
摘要： Nanoparticulate compositions comprising at least one poorly soluble angiogenesis inhibitor and at least one surface stabilizer are described. The nanoparticulate compositions have an average particle size of less than about 2000 nm. The invention also describes methods of making and using such compositions.

7. 发明申请

US20120183476A1 METHODS OF ADMINISTERING LIQUID DROPLET AEROSOLS OF NANOPARTICULATE DRUGS 审中-公开
标题翻译：管理液体药物喷雾剂的方法
公开(公告)号：US20120183476A1
公开(公告)日：2012-07-19
申请号：US13348351
申请日：2012-01-11
申请人： Ray W. WOOD , Lan DeCastro , H. William Bosch
发明人： Ray W. WOOD , Lan DeCastro , H. William Bosch
IPC分类号： A61K49/00 , A61P11/00 , A61P11/08 , A61K9/12 , A61P11/06 , B82Y15/00 , B82Y5/00
CPC分类号： A61K9/0078 , A61K9/145 , A61K9/146 , A61K49/00 , A61K49/049 , B82Y5/00
摘要： There is disclosed an aerosol comprising droplets of an aqueous dispersion of nanoparticles, said nanoparticles comprising insoluble therapeutic or diagnostic agent particles having a surface modifier on the surface thereof. There is also disclosed a method for making the aerosol and methods for treatment and diagnosis using the aerosol.
摘要翻译：公开了一种包含纳米颗粒的水分散体的液滴的气溶胶，所述纳米颗粒包含在其表面上具有表面改性剂的不溶性治疗剂或诊断剂颗粒。还公开了一种制造气溶胶的方法以及使用该气溶胶的治疗和诊断方法。

8. 发明授权

US08124057B2 Propellant-based nanoparticulate dry powder aerosols and method of making 有权
标题翻译：基于推进剂的纳米颗粒干粉气溶胶及其制备方法
公开(公告)号：US08124057B2
公开(公告)日：2012-02-28
申请号：US12320431
申请日：2009-01-26
申请人： H. William Bosch , Kevin D. Ostrander , Eugene R. Cooper
发明人： H. William Bosch , Kevin D. Ostrander , Eugene R. Cooper
IPC分类号： A61K9/00 , A61K9/10 , A61K9/12
CPC分类号： A61K9/0078 , A61K9/0075 , A61K9/008 , A61K9/146 , A61K9/1694 , A61K9/19 , Y10S514/826 , Y10S514/851 , Y10S514/872
摘要： There invention discloses aqueous dispersions of nanoparticulate aerosol formulations, dry powder nanoparticulate aerosol formulation, propellant-based aerosol formulations, methods of using the formulations in aerosol delivery devices, and methods of making such formulations. The nanoparticles of the aqueous dispersions or dry powder formulations comprise insoluble drug particles having a surface modifier on the surface thereof.
摘要翻译：本发明公开了纳米颗粒气雾剂配方的水性分散体，干燥粉末纳米颗粒气溶胶配制剂，基于推进剂的气溶胶制剂，在气溶胶递送装置中使用制剂的方法，以及制备这些制剂的方法。含水分散体或干粉配方的纳米颗粒包含在其表面上具有表面改性剂的不溶性药物颗粒。

9. 发明申请

US20100255102A1 STERILIZATION OF DISPERSIONS OF NANOPARTICULATE ACTIVE AGENTS WITH GAMMA RADIATION 有权
标题翻译：纳米粒子活性剂与伽马辐射的分散剂灭菌
公开(公告)号：US20100255102A1
公开(公告)日：2010-10-07
申请号：US10851661
申请日：2004-05-24
申请人： H. William Bosch , Janine Keller
发明人： H. William Bosch , Janine Keller
IPC分类号： A61K9/14 , A61K31/192 , A61K31/58 , A61P29/00 , A61P31/00 , A61P25/04 , A61P25/24 , A61P35/00 , A61P37/06 , A61P25/20 , A61P11/00 , A61L2/08
CPC分类号： A61L2/0035 , A61K9/146 , A61L2202/21
摘要： The present invention relates to methods for sterilization of dispersions of one or more nanoparticulate active agents via gamma irradiation.
摘要翻译：本发明涉及通过γ照射灭菌一种或多种纳米颗粒活性剂的分散体的方法。

10. 发明申请

US20080171091A1 NANOPARTICULATE COMPOSITIONS OF IMMUNOSUPPRESSIVE AGENTS 审中-公开
标题翻译：免疫抑制剂的纳米颗粒组合物
公开(公告)号：US20080171091A1
公开(公告)日：2008-07-17
申请号：US12051448
申请日：2008-03-19
申请人： Ray W. Wood , Ian DeCastro , H. William Bosch
发明人： Ray W. Wood , Ian DeCastro , H. William Bosch
IPC分类号： A61K9/50 , A61K31/56
CPC分类号： A61K9/0078 , A61K9/145 , A61K9/146 , A61K49/00 , A61K49/049 , B82Y5/00
摘要： There is disclosed an aerosol comprising droplets of an aqueous dispersion of nanoparticles, said nanoparticles comprising insoluble therapeutic or diagnostic agent particles having a surface modifier on the surface thereof. There is also disclosed a method for making the aerosol and methods for treatment and diagnosis using the aerosol.
摘要翻译：公开了一种包含纳米颗粒的水分散体的液滴的气溶胶，所述纳米颗粒包含在其表面上具有表面改性剂的不溶性治疗剂或诊断剂颗粒。还公开了一种制造气溶胶的方法以及使用该气溶胶的治疗和诊断方法。

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