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1. 发明公开

EP2124898A4 ENHANCED DELIVERY OF IMMUNOSUPPRESSIVE DRUG COMPOSITIONS FOR PULMONARY DELIVERY 有权转让
标题翻译：释放出更多的免疫抑制药物组合物肺部给药
公开(公告)号：EP2124898A4
公开(公告)日：2012-10-10
申请号：EP08780367
申请日：2008-01-10
申请人： UNIV TEXAS , DOW CHEMICAL CO
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 , A61K9/00 , A61K9/16 , 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.

2. 发明专利

CA2678455A1 ENHANCED DELIVERY OF IMMUNOSUPPRESSIVE DRUG COMPOSITIONS FORPULMONARY DELIVERY 未知
公开(公告)号：CA2678455A1
公开(公告)日：2008-10-23
申请号：CA2678455
申请日：2008-01-10
申请人： DOW CHEMICAL CO , UNIV TEXAS
发明人： ROGERS TRUE L , WATTS ALAN B , PETERS JAY , TALBERT ROBERT , SINWAT PRAPASRI , MCCONVILLE JASON T , JOHNSTON KEITH P , WILLIAMS ROBERT O III
IPC分类号： A61K9/14
摘要： The present invention includes compositions and methods for making and us ing a rapid dissolving, high potency, substantially amorphous nanostructured aggregate for pulmonary delivery of tacrolimus and a stabilizer matrix comp rising, 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 supersa turation for at least 0.5 hours when 11-15-times the aqueous crystalline sol ubility of tacrolimus is added to simulated lung fluid.

3. 发明公开

EP2187968A4 THERMO-KINETIC MIXING FOR PHARMACEUTICAL APPLICATIONS 无效转让
标题翻译： THERMOKINETISCHES MISCHENFÜRPHARMAZEUTISCHE ANWENDUNGEN
公开(公告)号：EP2187968A4
公开(公告)日：2013-02-20
申请号：EP08798412
申请日：2008-08-21
申请人： UNIV TEXAS , INTERGRICO COMPOSITES INC
发明人： BROUGH CHRIS , MCGINITY JAMES W , MILLER DAVE A , DINUNZIO JAMES C , WILLIAMS ROBERT O III
IPC分类号： A61K47/00 , A61K9/20 , A61K9/24
CPC分类号： A61K31/573 , A61J3/00 , A61J3/07 , A61J3/10 , A61K9/146 , A61K9/1694 , A61K9/2077 , A61K31/343 , A61K31/496 , A61K47/32 , A61K47/38
摘要： Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.
摘要翻译：用于制备药物剂型的组合物和方法包括制备药物组合物，其包含一种或多种活性药物成分（API）与一种或多种药学上可接受的赋形剂，通过热动力学复合成复合材料。将包含一种或多种API的复合材料与一种或多种赋形剂预处理的组合物和方法包括热动力学复合，其包括使API与赋形剂的热机械加工成复合材料，其中该复合材料可以通过本领域已知的常规方法进一步加工，例如热熔挤出，熔融造粒，压缩成型，片剂压缩，胶囊填充，薄膜包衣或注射成型。

4. 发明公开

EP3065705A4 COMPOSITIONS AND METHODS FOR ADMINISTRATION OF AN ENZYME TO A SUBJECT'S AIRWAY 审中-公开
公开(公告)号：EP3065705A4
公开(公告)日：2017-10-18
申请号：EP14857307
申请日：2014-11-04
申请人： UNIV TEXAS
发明人： WILLIAMS ROBERT O III , IDELL STEVEN
IPC分类号： A61K38/49 , A61K9/12 , A61P11/00 , A61P11/06
CPC分类号： A61K38/49 , A61K9/0078 , A61K9/008 , C12Y304/21073

5. 发明公开

EP1817008A4 STABILIZED HME COMPOSITION WITH SMALL DRUG PARTICLES 有权转让
标题翻译： STABILISIERTE HME-ZUSAMMENSETZUNG MIT KLEINEN WIRKSTOFFPARTIKELN
公开(公告)号：EP1817008A4
公开(公告)日：2016-10-12
申请号：EP05858310
申请日：2005-11-09
申请人： UNIV TEXAS
发明人： MILLER DAVE A , MCCONVILLE JASON T , MCGINITY JAMES W , WILLIAMS ROBERT O III
IPC分类号： A61F2/06 , A61K9/14 , A61K9/16 , A61K9/51
CPC分类号： A61K9/146 , A61K9/1635 , A61K9/1641 , A61K9/5138 , A61K31/496 , A61K31/55 , A61K31/58 , A61K38/13
摘要： A hot-melt extruded composition having finely divided drug-containing particles dispersed within a polymeric and/or lipophyllic carrier matrix is provided. The carrier softens or melts during hot-melt extrusion but it does not dissolve the drug-containing particles during extrusion. As a result, a majority or at least 90% wt. of the drug-containing particles in the extrudate are deaggregated during extrusion into essentially primary crystalline and/or amorphous particles. PEO is a suitable carrier material for drugs insoluble in the solid state in this carrier. Various functional excipients can be included in the carrier system to stabilize the particle size and physical state of the drug substance in either a crystalline and/or amorphous state. The carrier system is comprised of at least one thermal binder, and may also contain various functional excipients, such as: super-disintegrants, antioxidants, surfactants, wetting agents, stabilizing agents, retardants, or similar functional excipients. A hydrophilic polymer, such as hydroxypropyl methylcellulose (HPMC E15), polyvinyl alcohol (PVA), or poloxamer, and/or a surfactant, such as sodium lauryl sulfate (SLS), can be included in the composition. A process for preparing the extrudate is conducted at a temperature approximating or above the softening or melting temperature of the matrix and below the point of solubilization of drug-containing particles in the carrier system, and below the recrystallization point in the case of amorphous fine drug particles.
摘要翻译：提供了具有分散在聚合物和/或脂肪载体基质内的细分散的含药颗粒的热熔挤出组合物。载体在热熔挤出过程中软化或熔化，但在挤出过程中不溶解含药颗粒。结果，大多数或至少90重量％的挤出物中的含药颗粒在挤出过程中被解聚为基本上为初级结晶和/或无定形颗粒。 PEO是适用于载体中不溶于固体的药物的载体材料。载体体系中可以包括各种功能赋形剂，以稳定药物物质在晶体和/或非晶状态下的粒度和物理状态。载体系统由至少一种热粘合剂组成，并且还可以含有各种功能性赋形剂，例如：超级崩解剂，抗氧化剂，表面活性剂，润湿剂，稳定剂，阻滞剂或类似的功能赋形剂。亲水性聚合物如羟丙基甲基纤维素（HPMC E15），聚乙烯醇（PVA）或泊洛沙姆，和/或表面活性剂如十二烷基硫酸钠（SLS）可以包括在组合物中。制备挤出物的方法在接近或高于基质的软化或熔融温度的温度下进行，并且低于载体体系中药物含量的溶解点，并且在无定形精细药物的情况下在重结晶点以下粒子。

6. 发明申请

WO02060411A3 PROCESS FOR PRODUCTION OF NANOPARTICLES AND MICROPARTICLES BY SPRAY FREEZING INTO LIQUID 审中-公开
标题翻译：通过喷雾冷冻成液体生产纳米颗粒和微生物的方法
公开(公告)号：WO02060411A3
公开(公告)日：2003-02-27
申请号：PCT/US0202894
申请日：2002-01-30
申请人： UNIV TEXAS
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： A61J3/02 , A61K9/14 , A61K9/16 , A61K31/55 , A61K31/58 , A61K38/23 , A61K38/28 , A61P3/10 , A61P3/14 , A61P5/44 , A61P13/00 , A61P25/08 , A61P35/00 , B01J19/00 , F25B19/00 , F25C1/00 , F26B3/08 , F26B5/06 , A61K9/19
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.
摘要翻译：本发明提供了可以溶解的材料的微粒和纳米粒子的制造系统和方法。本发明的系统和方法提供更快的冷冻时间，其又产生更均匀的粒度分布，较小的颗粒，具有增加的孔隙率的颗粒和颗粒组分的更加紧密的混合。本发明的系统和方法还产生比常规方法具有更大表面积的颗粒。本发明的一种形式提供了制备颗粒的方法。将有效成分与水，一种或多种溶剂或其组合混合，并将所得混合物通过位于或低于低温液体水平的绝缘喷嘴喷雾。喷雾产生冷冻颗粒。

7. 发明申请

WO2009117410A8 FORMATION OF NANOSTRUCTURED PARTICLES OF POORLY WATER SOLUBLE DRUGS AND RECOVERY BY MECHANICAL TECHNIQUES 审中-公开
标题翻译：形成非水溶性药物的纳米颗粒和机械技术回收
公开(公告)号：WO2009117410A8
公开(公告)日：2010-08-12
申请号：PCT/US2009037391
申请日：2009-03-17
申请人： UNIV TEXAS , JOHNSTON KEITH P , WILLIAMS ROBERT O III , MATTEUCCI MICHAL E
发明人： JOHNSTON KEITH P , WILLIAMS ROBERT O III , MATTEUCCI MICHAL E
IPC分类号： A61K9/16 , A61K9/20 , A61K9/50 , A61K31/496 , A61K47/34 , C01B13/14
CPC分类号： A61K9/1635 , A61K9/5138 , A61K9/5146 , A61K9/5161 , A61K9/5192 , A61K31/496
摘要： The present invention provides a composition and method of forming an amorphous drug-loaded particle by forming one or more amorphous drug-loaded nanoparticles comprising one or more active agents stabilized by one or more polymers, desolvating the one or more amorphous drug-loaded nanoparticles to form one or more flocculated amorphous drug-loaded nanoparticles, filtering the one or more flocculated amorphous drug-loaded nanoparticles and drying the one or more flocculated amorphous drug-loaded nanoparticles to form amorphous drug-loaded particles.
摘要翻译：本发明提供了一种通过形成一种或多种无定形药物负载纳米颗粒来形成无定形药物负载颗粒的组合物和方法，所述纳米颗粒包含一种或多种由一种或多种聚合物稳定的活性剂，将一种或多种无定形药物负载的纳米颗粒脱溶剂形成一种或多种絮凝的无定形药物负载的纳米颗粒，过滤一种或多种絮凝的无定形药物负载纳米颗粒并干燥一种或多种絮凝的无定形药物负载纳米颗粒以形成无定形药物负载的颗粒。

8. 发明公开

EP3193842A4 METHODS OF PREPARING EXTRUDATES 审中-公开
公开(公告)号：EP3193842A4
公开(公告)日：2018-05-16
申请号：EP15842831
申请日：2015-09-18
申请人： UNIV TEXAS
发明人： ZHANG FENG , MILLER ABBE , HUANG SIYUAN , WILLIAMS ROBERT O III
IPC分类号： A61K9/16 , A61K9/20 , B29C47/10
CPC分类号： A61K31/4184 , A61J3/10 , A61K9/1635 , A61K9/2027 , A61K9/2054 , A61K9/2095 , A61K31/192 , B29C47/0007 , B29K2105/0035 , B29K2995/0059 , C08L1/02 , C08L1/284
摘要： Compositions and methods of preparing amorphous drug formulations through hot melt extrusion which result in decreased decomposition of the desired drug are provided herein. Also provided are methods and compositions which further comprise a pharmaceutically acceptable thermoplastic polymer. In some embodiments, these compositions comprise a therapeutically active agent which is only sparingly soluble in water.

9. 发明申请

WO2015066664A3 COMPOSITIONS AND METHODS FOR ADMINISTRATION OF AN ENZYME TO A SUBJECT'S AIRWAY 审中-公开
标题翻译：组合物和方法用于将主体管理给主体的航空
公开(公告)号：WO2015066664A3
公开(公告)日：2015-09-17
申请号：PCT/US2014063784
申请日：2014-11-04
申请人： UNIV TEXAS
发明人： WILLIAMS ROBERT O III , IDELL STEVEN
IPC分类号： A61K9/12
CPC分类号： A61K38/49 , A61K9/0078 , A61K9/008 , C12Y304/21073
摘要： Methods and composition for delivery of enzymes to a subject's airway. In some aspects, nebulized composition of enzymes, such as plasminogen activators are provided. In further aspects perfluorocarbon compositions comprising enzymes, such as plasminogen activators are provided. Compositions may, in some aspects, be used for the treatment of lung infections or acute lung injury, such as inhalational smoke induced acute lung injury (ISALI).
摘要翻译：将酶递送至受检者气道的方法和组成。在一些方面，提供酶的雾化组合物，例如纤溶酶原激活剂。在另外的方面，提供了包含酶的全氟化碳组合物，例如纤溶酶原激活剂。在某些方面，组合物可用于治疗肺部感染或急性肺损伤，例如吸入性烟雾引起的急性肺损伤（ISALI）。

10. 发明申请

WO2009026461A3 THERMO-KINETIC MIXING FOR PHARMACEUTICAL APPLICATIONS 审中-公开
标题翻译：用于药物应用的热 - 力学混合
公开(公告)号：WO2009026461A3
公开(公告)日：2009-04-30
申请号：PCT/US2008073913
申请日：2008-08-21
申请人： UNIV TEXAS , BROUGH CHRIS , MCGINITY JAMES W , MILLER DAVE A , DINUNZIO JAMES C , WILLIAMS ROBERT O III
发明人： BROUGH CHRIS , MCGINITY JAMES W , MILLER DAVE A , DINUNZIO JAMES C , WILLIAMS ROBERT O III
IPC分类号： A61K47/00 , A61K9/20 , A61K9/24
CPC分类号： A61K31/573 , A61J3/00 , A61J3/07 , A61J3/10 , A61K9/146 , A61K9/1694 , A61K9/2077 , A61K31/343 , A61K31/496 , A61K47/32 , A61K47/38
摘要： Compositions and methods for making a pharmaceutical dosage form include making a pharmaceutical composition that includes one or more active pharmaceutical ingredients (API) with one or more pharmaceutically acceptable excipients by thermokinetic compounding into a composite. Compositions and methods of preprocessing a composite comprising one or more APIs with one or more excipients include thermokinetic compounding, comprising thermokinetic processing the APIs with the excipients into a composite, wherein the composite can be further processed by conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.
摘要翻译：用于制备药物剂型的组合物和方法包括通过热动力学混合将复合物制成包含一种或多种活性药物成分（API）与一种或多种药学上可接受的赋形剂的药物组合物。预处理包含一种或多种API与一种或多种赋形剂的复合材料的组合物和方法包括热动力学复合，包括将API与赋形剂热动力学加工成复合材料，其中复合材料可以通过本领域已知的常规方法进一步加工，例如热熔挤出，熔体造粒，压缩成型，压片，胶囊填充，薄膜包衣或注射成型。

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