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1. 发明申请

US20070275072A1 BUTYL LACTATE EMULSIONS FOR THE PRECIPITATION OF WATER-INSOLUBLE DRUG NANOPARTICLES 有权
标题翻译：用于降低水不溶性药物纳米颗粒的乳液乳液
公开(公告)号：US20070275072A1
公开(公告)日：2007-11-29
申请号：US11420035
申请日：2006-05-24
申请人： PRATIBHASH CHATTOPADHYAY , BORIS Y. SHEKUNOV , ADAM K. GIBSON
发明人： PRATIBHASH CHATTOPADHYAY , BORIS Y. SHEKUNOV , ADAM K. GIBSON
IPC分类号： A61K9/14 , B01J13/04
CPC分类号： A61K9/14 , A61K9/10 , A61K9/145
摘要： Emulsions for use in precipitating water-insoluble drug nanoparticles. The continuous phase of the emulsions include water and an external surfactant. The discontinuous phase of the emulsions include butyl lactate, a co-solvent, an internal surfactant and a water-insoluble drug that is solubilized in the discontinuous phase. The emulsions allow for the precipitation of nanoparticles of water-insoluble drugs that are otherwise difficult or impossible to precipitate using conventional emulsion techniques.
摘要翻译：用于沉淀水不溶性药物纳米粒子的乳液。乳液的连续相包括水和外部表面活性剂。乳液的不连续相包括乳酸丁酯，共溶剂，内表面活性剂和溶解在不连续相中的水不溶性药物。乳液允许使用常规乳液技术难于或不可能沉淀的水不溶性药物的纳米颗粒的沉淀。

2. 发明申请

US20080269449A1 METHODS FOR THE PURIFICATION OF POLYMERS 有权
标题翻译：聚合物的纯化方法
公开(公告)号：US20080269449A1
公开(公告)日：2008-10-30
申请号：US12017399
申请日：2008-01-22
申请人： Pratibhash Chattopadhyay , Boris Y. Shekunov , K. Adam Gibson
发明人： Pratibhash Chattopadhyay , Boris Y. Shekunov , K. Adam Gibson
IPC分类号： C08F120/18 , C08G63/08 , C08G65/04
CPC分类号： C08G63/90 , C08G63/08 , C08G65/30 , Y02P20/544
摘要： The present invention provides methods for purifying polymers. In each embodiment of the invention disclosed herein, a supercritical fluid is contacted with an organic solution that includes a polymer to be purified dissolved in an organic solvent. The supercritical fluid extracts the organic solvent from the organic solution. Impurities such as residual monomers and process solvents are removed with the organic solvent and supercritical fluid, thereby purifying the polymer. The methods of the invention are particularly suitable for use in the purification of biodegradable polymers for use in pharmaceutical applications.
摘要翻译：本发明提供了纯化聚合物的方法。在本文公开的本发明的每个实施方案中，将超临界流体与包含要溶解在有机溶剂中的待纯化聚合物的有机溶液接触。超临界流体从有机溶液中萃取有机溶剂。用有机溶剂和超临界流体除去残留单体和工艺溶剂等杂质，从而纯化聚合物。本发明的方法特别适用于纯化用于制药应用的可生物降解的聚合物。

3. 发明授权

US07449136B2 Method and apparatus for producing composite particles using supercritical fluid as plasticizing and extracting agent 有权
标题翻译：使用超临界流体作为增塑剂和提取剂生产复合颗粒的方法和装置
公开(公告)号：US07449136B2
公开(公告)日：2008-11-11
申请号：US10531008
申请日：2004-02-18
申请人： Boris Y. Shekunov , Pratibhash Chattopadhyay , Jeffrey S. Seitzinger
发明人： Boris Y. Shekunov , Pratibhash Chattopadhyay , Jeffrey S. Seitzinger
IPC分类号： B29B9/00 , A61K9/14
CPC分类号： B01D11/0411 , B01D11/0203 , B01D11/0403
摘要： The present invention provides methods for producing composite particles using supercritical fluid as a plasticizing and extracting agent, composite particles formed in accordance with the methods and an apparatus for carrying out the methods. In accordance with the methods of the invention, a polymer, a wax and/or a lipid that is a solid at standard temperature and pressure is contacted with a supercritical fluid to form a melt, either before or after the polymer, wax and/or lipid has been contacted with a solution comprising a solute dissolved in a solvent. The supercritical fluid plasticizes the polymer, wax and/or lip and extracts the solvent from the solution, resulting in the formation of a two-fraction system including a first melt-rich fraction that includes the plasticized melt and fine particles of precipitated solute that are dispersed in the melt, and a second fraction that includes the supercritical fluid and the solvent. Expansion of the first fraction across a pressure drop results in the formation of composite particles that include the polymer, wax and/or lipid and the solute.
摘要翻译：本发明提供了使用超临界流体作为增塑萃取剂，根据所述方法形成的复合颗粒和用于实施所述方法的装置来生产复合颗粒的方法。根据本发明的方法，在标准温度和压力下作为固体的聚合物，蜡和/或脂质与超临界流体接触以形成熔体，在聚合物之前或之后，蜡和/或脂质已经与包含溶解在溶剂中的溶质的溶液接触。超临界流体使聚合物，蜡和/或脂肪增塑，并从溶液中提取溶剂，从而形成包括第一富熔体部分的双组分体系，其包括增塑的熔体和沉淀的溶质的细颗粒，分散在熔体中，第二部分包括超临界流体和溶剂。通过压降的第一级分的膨胀导致形成包括聚合物，蜡和/或脂质和溶质的复合颗粒。

4. 发明授权

US07073349B2 Lyophilization method and apparatus for producing particles 有权
标题翻译：冻干方法和生产颗粒的装置
公开(公告)号：US07073349B2
公开(公告)日：2006-07-11
申请号：US11078554
申请日：2005-03-11
申请人： Boris Y. Shekunov , Pratibhash Chattopadhyay , Jeffrey S. Seitzinger
发明人： Boris Y. Shekunov , Pratibhash Chattopadhyay , Jeffrey S. Seitzinger
IPC分类号： B01D9/04 , C02F1/22
CPC分类号： F25D3/102 , A61K9/1623 , A61K9/1694 , A61K9/19 , F25B9/02 , F26B5/065
摘要： A method and apparatus for producing particles, the apparatus includes a solution source that supplies a solution, and a fluid source that supplies a fluid. The solution includes a solvent and a solute. A mixer receives the solution and the fluid from the sources, and mixes the solution and the fluid together to form a mixture. The mixture is supplied from the mixer to an expansion assembly at first pressure. The expansion assembly sprays and expands the mixture substantially simultaneously to form frozen droplets, and preferably to form a low-density powder of frozen droplets. A freeze-dry apparatus sublimes the solvent from the particles. A high mass-transfer rate and a uniform open-structure of the powder bed enhances the freeze-drying process. Solid particles having a controlled size distribution are obtained. The particles preferably have a hollow or porous morphology suitable for differing drug delivery applications to include aerosol formulations.
摘要翻译：一种用于生产颗粒的方法和装置，该装置包括提供溶液的溶液源和供应流体的流体源。溶液包括溶剂和溶质。混合器接收来自源的溶液和流体，并将溶液和流体混合在一起形成混合物。混合物在第一压力下从混合器供应到膨胀组件。膨胀组件基本上同时喷雾和膨胀混合物以形成冷冻液滴，并且优选地形成冷冻液滴的低密度粉末。冷冻干燥装置使颗粒中的溶剂升华。粉末床的高质量转移率和均匀的开放结构提高了冷冻干燥过程。获得具有受控尺寸分布的固体颗粒。颗粒优选具有适于不同药物递送应用的中空或多孔形态以包括气溶胶制剂。

5. 发明申请

US20080260852A1 SUPERCRITICAL FLUID EXTRACTION PRODUCED BY IN-LINE HOMOGENIZATION 审中-公开
标题翻译：通过在线均相生产的超临界流体萃取
公开(公告)号：US20080260852A1
公开(公告)日：2008-10-23
申请号：US12017414
申请日：2008-01-22
申请人： Pratibhash Chattopadhyay , Boris Y. Shekunov , K. Adam Gibson
发明人： Pratibhash Chattopadhyay , Boris Y. Shekunov , K. Adam Gibson
IPC分类号： A61K9/14
CPC分类号： A61K9/1647 , A61K9/1694
摘要： A method for producing micro and/or nanoparticles by contacting an emulsion with a supercritical fluid. The method can be used to produce an aqueous suspension of particles that include a drug encapsulated in a polymer. The drug and polymer are dissolved in an organic solvent to form an organic solution. The organic solution is pumped into contact with an aqueous solution in an in-line homogenization device to form an emulsion. Immediately after the emulsion in the in-line homogenization device, the emulsion contacts the supercritical fluid. The supercritical fluid extracts the organic solvent from the oil droplets of the emulsion, causing the drug and polymer to precipitate into the aqueous phase of the emulsion and thereby form an aqueous suspension of particles that include a drug encapsulated in a polymer.
摘要翻译：一种通过使乳液与超临界流体接触来生产微米和/或纳米颗粒的方法。该方法可用于产生包含封装在聚合物中的药物的颗粒水性悬浮液。将药物和聚合物溶解在有机溶剂中以形成有机溶液。将有机溶液泵入与在线均化装置中的水溶液接触以形成乳液。在在线均化装置中的乳液立即之后，乳液接触超临界流体。超临界流体从乳液的油滴中提取有机溶剂，导致药物和聚合物沉淀到乳液的水相中，从而形成包含封装在聚合物中的药物的颗粒水悬浮液。

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