公开(公告)号：EP1789018A1

公开(公告)日：2007-05-30

申请号：EP05804416.5

申请日：2005-08-26

申请人： THE DOW CHEMICAL COMPANY ,  Board of Regents, The University of Texas System

发明人： HITT, James, E. ,  ROGERS, True, L. ,  GILLESPIE, Ian, B. ,  SCHERZER, Brian, D. ,  GARCIA, Paula, C. ,  BECK, Nicholas, S. ,  TUCKER, Christopher, J. ,  YOUNG, Timothy, J. ,  HAYES, David, A. ,  WILLIAMS, Robert, O., III ,  JOHNSTON, Keith, P. ,  MCCONVILLE, Jason, T. ,  PETERS, Jay, I. ,  TALBERT, Robert ,  BURGESS, David

IPC分类号： A61K9/12 ,  A61K31/496

CPC分类号： A61K31/496 ,  A61K9/0073 ,  A61K9/008 ,  A61K9/19

摘要： Inhalable compositions are described. The inhalable compositions comprise one or more respirable aggregates, the respirable aggregates comprising one or more poorly water soluble active agents, wherein at least one of the active agents reaches a maximum lung concentration (Cmax) of at least about 0.25 μg/gram of lung tissue and remains at such concentration for a period of at least one hour after being delivered to the lung. Methods for making such compositions and methods for using such compositions are also disclosed.

公开(公告)号：EP2124898B1

公开(公告)日：2013-08-14

申请号：EP08780367.2

申请日：2008-01-10

申请人： Board of Regents, The University of Texas System ,  The Dow Chemical Company

发明人： WILLIAMS, Robert, O., III ,  JOHNSTON, Keith, P. ,  SINWAT, Prapasri ,  MCCONVILLE, Jason, T. ,  TALBERT, Robert ,  PETERS, Jay ,  WATTS, Alan, B. ,  ROGERS, True, L.

IPC分类号： A61K9/14 ,  A61K9/16 ,  A61K9/00 ,  A61K9/19

CPC分类号： A61K31/436 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/1623 ,  A61K9/1694 ,  A61K9/19 ,  A61K9/5161 ,  A61K9/5192 ,  A61K38/13

摘要： The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

公开(公告)号：EP2124898A1

公开(公告)日：2009-12-02

申请号：EP08780367.2

申请日：2008-01-10

申请人： Board of Regents, The University of Texas System ,  The Dow Chemical Company

发明人： WILLIAMS, Robert, O., III ,  JOHNSTON, Keith, P. ,  SINWAT, Prapasri ,  MCCONVILLE, Jason, T. ,  TALBERT, Robert ,  PETERS, Jay ,  WATTS, Alan, B. ,  ROGERS, True, L.

IPC分类号： A61K9/14

CPC分类号： A61K31/436 ,  A61K9/0075 ,  A61K9/0078 ,  A61K9/1623 ,  A61K9/1694 ,  A61K9/19 ,  A61K9/5161 ,  A61K9/5192 ,  A61K38/13

摘要： The present invention includes compositions and methods for making and using a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comprising, optionally, a polymeric or non-polymeric surfactant, a polymeric or non-polymeric saccharide or both, wherein the aggregate comprises a surface area greater than 5 m2/g as measured by BET analysis and exhibiting supersaturation for at least 0.5 hours when 11-15-times the aqueous crystalline solubility of tacrolimus is added to simulated lung fluid.

摘要翻译： 本发明包括用于制备和使用快速溶解，高效力，基本上无定形纳米结构化聚集体用于肺移植他克莫司的组合物和方法，以及包含任选的聚合物或非聚合物表面活性剂，聚合物或非聚合物糖的稳定剂基质 或两者，其中所述骨料包含通过BET分析测量的大于5m 2 / g的表面积，并且当将他克莫司的水溶液结晶溶解度加入到模拟肺液中时，表现出过饱和至少0.5小时。

公开(公告)号：EP2170283B1

公开(公告)日：2019-01-09

申请号：EP08771657.7

申请日：2008-06-20

申请人： Board of Regents, The University of Texas System

发明人： JOHNSTON, Keith, P. ,  ENGSTROM, Joshua ,  WILLIAMS III, Robert O.

IPC分类号： A61K9/14 ,  A61K9/16

公开(公告)号：EP0855906B1

公开(公告)日：2008-02-20

申请号：EP96936782.0

申请日：1996-10-17

申请人： Jagotec AG ,  THE BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM

发明人： HENRIKSEN, Inge, B. ,  MISHRA, Awadesh, K. ,  PACE, Gary, W. ,  JOHNSTON, Keith, P. ,  MAWSON, Simon

IPC分类号： A61K9/14

CPC分类号： B01J3/008 ,  A61K9/14 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1688 ,  B01F1/00 ,  B01F3/1214 ,  B01F3/1271 ,  B01F5/02 ,  B01F5/0287 ,  B01F2003/0064 ,  B01F2003/125 ,  B01F2215/0032 ,  Y02P20/544 ,  Y10S977/896 ,  Y10S977/906

摘要： Particles of water insoluble biologically active compounds, particularly water-insoluble drugs, with an average size of 100 nm to about 300 nm, are prepared by dissolving the compound in a solution then spraying the solution into compressed gaz, liquid or supercritical fluid in the presence of appropriate surface modifiers.

公开(公告)号：EP1357900A2

公开(公告)日：2003-11-05

申请号：EP02709265.9

申请日：2002-01-30

申请人： Board of Regents,The University of Texas System

发明人： WILLIAMS, Robert, O., III ,  JOHNSTON, Keith, P. ,  YOUNG, Timothy, J. ,  ROGERS, True, L. ,  BARRON, Melisa, K. ,  YU, Zhongshui ,  HU, Jiahui

IPC分类号： A61K9/16

CPC分类号： F26B5/065 ,  A61K9/1617 ,  A61K9/1623 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1647 ,  A61K9/1652 ,  A61K9/1688 ,  A61K9/1694 ,  F25B19/005 ,  F25C1/00 ,  F25D2400/30 ,  F26B3/08

摘要： The present invention provides a system and a method for the production of microparticles and nanoparticles of materials that can be dissolved. The system and method of the present invention provide quicker freezing times, which in turn produces a more uniform distribution of particle sizes, smaller particles, particles with increased porosity and a more intimate mixing of the particle components. The system and method of the present invention also produce particles with greater surface area than conventional methods. One form of the present invention provides a method for the preparation of particles. An effective ingredient is mixed with water, one or more solvents, or a combination thereof, and the resulting mixture is sprayed through an insulating nozzle located at or below the level of a cryogenic liquid. The spray generates frozen particles.

公开(公告)号：EP2683362A2

公开(公告)日：2014-01-15

申请号：EP12755064.8

申请日：2012-03-09

申请人： Board of Regents, The University of Texas System

发明人： JOHNSTON, Keith, P. ,  MAYNARD, Jennifer, A. ,  MILLER, Andrea ,  WILSON, Brian ,  TRUSKETT, Thomas, M. ,  DININ, Aileen ,  BORWANKAR, Ameya

IPC分类号： A61K9/12 ,  A61K9/10 ,  A61K9/16 ,  A61K9/14 ,  A61K47/48

CPC分类号： C07K16/00 ,  A61K9/0019 ,  A61K9/19 ,  A61K47/10 ,  A61K47/16 ,  A61K47/183 ,  A61K47/26 ,  A61K47/6881

摘要： Provided herein, inter alia, are protein dispersions comprising dense protein nanoclusters and methods of making the. Upon dilution, the clusters may reversibly dissociate into native protein molecules with high biological activity. The viscosities of the nanocluster dispersions may be sufficiently low to allow small-volume subcutaneous injections.

公开(公告)号：EP2170283A1

公开(公告)日：2010-04-07

申请号：EP08771657.7

申请日：2008-06-20

申请人： Board of Regents, The University of Texas System

发明人： JOHNSTON, Keith, P. ,  ENGSTROM, Joshua

IPC分类号： A61K9/14

CPC分类号： A61K9/1682 ,  A61K9/1658 ,  B01D9/005 ,  Y10T428/2982

摘要： The present invention includes compositions and methods for preparing micron-sized or submicron-sized particles by dissolving a water soluble effective ingredient in one or more solvents; spraying or dripping droplets solvent such that the effective ingredient is exposed to a vapor-liquid interface of less than 50, 100, 150, 200, 250, 200, 400 or 500 cm−1 area/volume to, e.g., increase protein stability; and contacting the droplet with a freezing surface that has a temperature differential of at least 30° C. between the droplet and the surface, wherein the surface freezes the droplet into a thin film with a thickness of less than 500 micrometers and a surface area to volume between 25 to 500 cm−1.

公开(公告)号：EP2376522A2

公开(公告)日：2011-10-19

申请号：EP09826617.4

申请日：2009-11-10

申请人： Board of Regents, The University of Texas System

发明人： JOHNSTON, Keith, P. ,  MAZUSKI, Maria, Andrea ,  ENGSTROM, Joshua ,  RODRIGUES, Miguel, Angelo

IPC分类号： C07K1/14 ,  C07K1/02 ,  A61K38/00

CPC分类号： A61K9/0019 ,  A61K38/385 ,  C07K1/113

摘要： The present invention also provides a high concentration low viscosity suspension of an pharmaceutically acceptable solvent with one or more sub-micron or micron-sized non-crystalline particles comprising one or more proteins or peptides. Optionally one or more additives in the pharmaceutically acceptable solvent to form a high concentration low viscosity suspension with a concentration of at least 20 mg/ml and a solution viscosity of between 2 and 100 centipoise that is suspendable upon shaking or agitation, wherein upon delivery the one or more sub-micron or micron-sized peptides dissolves and do not form peptide aggregates syringeable through a 21 to 27-gauge needle.

公开(公告)号：EP1335705B1

公开(公告)日：2004-12-15

申请号：EP01989339.5

申请日：2001-10-22

申请人： Board of Regents, The University of Texas System

发明人： JOHNSTON, Keith, P. ,  WILLIAMS, Robert, O. ,  YOUNG, Timothy, J. ,  CHEN, Xiaoxia

IPC分类号： A61K9/14

CPC分类号： B82Y5/00 ,  A61K9/1694

摘要： A method for preparing poorly water soluble drug particles is disclosed. The method comprises dissolving a drug in at least one organic solvent to form a drug/organic mixture, spraying the drug/organic mixture into an aqueous solution and concurrently evaporating the organic solvent in the presence of the aqueous solution to form an aqueous dispersion of the drug particles. The resulting drug particles are in the nanometer to micrometer size range and show enhanced dissolution rates and reduced crystallinity when compared to the unprocessed drug.