公开(公告)号：WO2012116238A1

公开(公告)日：2012-08-30

申请号：PCT/US2012/026407

申请日：2012-02-23

Applicant: DISPERSOL TECHNOLOGIES, LLC ,  BOARD OF REGENTS ,  BROUGH, Chris ,  WILLIAMS, Robert, O., III ,  MCGINITY, James, W. ,  MILLER, Dave, A.

Inventor： BROUGH, Chris ,  WILLIAMS, Robert, O., III ,  MCGINITY, James, W. ,  MILLER, Dave, A.

IPC: C07C61/28 ,  A61K31/404 ,  A61K31/05

CPC classification number: A61K31/19 ,  A61K31/05 ,  A61K31/12 ,  A61K31/404

Abstract: The present disclosure is directed to compositions and methods for formulating a pharmaceutical dosage form by forming a composition comprising acetyl-11-keto-β- boswellic acid, diindolylmethane, or curcumin with one or more pharmaceutically acceptable excipients for enhanced solubility to increase bioavailability and improve therapeutic efficacy. The composition can be processed by thermo-kinetic compounding along with conventional methods known in the art, such as hot melt extrusion, melt granulation, compression molding, tablet compression, capsule filling, film-coating, or injection molding.

Abstract translation: 本公开涉及通过形成包含乙酰基-11-酮基-β-乳糖酸，二吲哚基甲烷或姜黄素与一种或多种药学上可接受的赋形剂的组合物来配制药物剂型的组合物和方法，以提高溶解度以增加生物利用度并改善 治疗功效。 组合物可以通过本领域已知的常规方法，例如热熔融挤出，熔融造粒，压塑，压片，胶囊填充，薄膜包衣或注塑成型，通过热动力学复合加工。

公开(公告)号：WO2006026502A1

公开(公告)日：2006-03-09

申请号：PCT/US2005/030543

申请日：2005-08-26

Applicant: THE DOW CHEMICAL COMPANY ,  BOARD OF REGENTS, UNIVERSITY OF TEXAS SYSTEM ,  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

Inventor： 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: A61K9/12 ,  A61K31/496

CPC classification number: A61K31/496 ,  A61K9/0073 ,  A61K9/008 ,  A61K9/19

Abstract: 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 (C max ) 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.

Abstract translation: 描述了可吸入组合物。 可吸入组合物包含一种或多种可呼吸聚集体，可呼吸聚集体包含一种或多种难溶于水的活性剂，其中至少一种活性剂达到最大肺浓度（C

公开(公告)号：WO0074736A9

公开(公告)日：2002-08-08

申请号：PCT/US0040093

申请日：2000-06-02

Applicant: DELRX PHARMACEUTICAL CORP ,  MCCOY RANDALL E ,  LIBBEY MILES AUGUSTUS III ,  LIU JIE ,  WILLIAMS ROBERT O III

Inventor： MCCOY RANDALL E ,  LIBBEY MILES AUGUSTUS III ,  LIU JIE ,  WILLIAMS ROBERT O III

IPC: A61K9/12 ,  A61K9/00 ,  A61K9/10 ,  A61K9/14 ,  A61K9/19 ,  A61K38/00 ,  A61K38/28 ,  A61K47/10 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K47/26 ,  A61K47/32 ,  A61K47/34 ,  A61L9/04 ,  A61P3/10 ,  A61P5/48

CPC classification number: A61K9/006 ,  A61K9/19 ,  A61K38/28 ,  A61K47/20 ,  A61K47/26

Abstract: A formulation for non-invasive delivery of pharmaceutical agents, particularly proteins and peptides, by absorption through a membrane at a targeted site is provided, along with a process of making the formulation. The formulation comprises a suspension of solid-phase dehydrated particles in a delivery medium. The particles comprise the dehydration product of the pharmaceutical agent and at least one of a surfactant and permeation enhancer, and the delivery medium preferably comprises a propellant for pressurized aerosol delivery of the formulation. The formulation can be conveniently delivered to the patient's targeted site where the pharmaceutical agent is absorbed through the mucosa to achieve a desired bioavailability.

Abstract translation: 提供了通过在目标部位通过膜吸收而非侵入性递送药剂，特别是蛋白质和肽的制剂，以及制备该制剂的方法。 该制剂包含固相脱水颗粒在递送介质中的悬浮液。 颗粒包括药剂的脱水产物和表面活性剂和渗透增强剂中的至少一种，并且递送介质优选包含用于制剂的加压气溶胶递送的推进剂。 该制剂可以方便地递送到患者的靶点，其中药剂通过粘膜被吸收以获得所需的生物利用度。

公开(公告)号：WO2008127746A1

公开(公告)日：2008-10-23

申请号：PCT/US2008/050795

申请日：2008-01-10

Applicant: BOARD OF REGENTS THE UNIVERSITY OF TEXAS SYSTEM ,  THE DOW CHEMICAL COMPANY ,  WILLIAMS, Robert, O., III ,  JOHNSTON, Keith, P. ,  SINWAT, Prapasri ,  MCCONVILLE, Jason, T. ,  TALBERT, Robert ,  PETERS, Jay ,  WATTS, Alan, B. ,  ROGERS, True, L.

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

IPC: A61K9/14

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

Abstract: 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 m 2 /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.

Abstract translation: 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 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，并且当他克莫司的水溶液结晶溶解度为11-15倍时，表现出过饱和至少0.5小时 添加到模拟肺液。

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

Applicant: UNIV TEXAS ,  BROUGH CHRIS ,  MCGINITY JAMES W ,  MILLER DAVE A ,  DINUNZIO JAMES C ,  WILLIAMS ROBERT O III

Inventor： BROUGH CHRIS ,  MCGINITY JAMES W ,  MILLER DAVE A ,  DINUNZIO JAMES C ,  WILLIAMS ROBERT O III

IPC: A61K47/00 ,  A61K9/20 ,  A61K9/24

CPC classification number: A61K31/573 ,  A61J3/00 ,  A61J3/07 ,  A61J3/10 ,  A61K9/146 ,  A61K9/1694 ,  A61K9/2077 ,  A61K31/343 ,  A61K31/496 ,  A61K47/32 ,  A61K47/38

Abstract: 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.

Abstract translation: 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。

公开(公告)号：WO2009026461A2

公开(公告)日：2009-02-26

申请号：PCT/US2008/073913

申请日：2008-08-21

Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM ,  BROUGH, Chris ,  MCGINITY, James, W. ,  MILLER, Dave, A. ,  DINUNZIO, James, C. ,  WILLIAMS, Robert, O., III

Inventor： BROUGH, Chris ,  MCGINITY, James, W. ,  MILLER, Dave, A. ,  DINUNZIO, James, C. ,  WILLIAMS, Robert, O., III

IPC: A61K9/00 ,  A61K9/20

CPC classification number: A61K31/573 ,  A61J3/00 ,  A61J3/07 ,  A61J3/10 ,  A61K9/146 ,  A61K9/1694 ,  A61K9/2077 ,  A61K31/343 ,  A61K31/496 ,  A61K47/32 ,  A61K47/38

Abstract: 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.

Abstract translation: 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，通过热动力学复合制成复合材料。 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，其包括将所述API与所述赋形剂的热动力学加工成复合材料，其中所述复合材料可以通过本领域已知的常规方法进一步加工， 热熔挤出，熔融造粒，压缩成型，片剂压缩，胶囊填充，薄膜包衣或注塑成型。

公开(公告)号：WO0047203A9

公开(公告)日：2001-09-07

申请号：PCT/US0003555

申请日：2000-02-11

Applicant: MQS INC ,  MCCOY RANDALL ,  WILLIAMS ROBERT O III ,  LIBBEY MILES A III

Inventor： MCCOY RANDALL ,  WILLIAMS ROBERT O III ,  LIBBEY MILES A III

IPC: A61K9/00 ,  A61K9/12 ,  A61K9/50 ,  A61K31/28 ,  A61K31/4468 ,  A61K38/25 ,  A61K31/44 ,  A61L9/04 ,  A61L9/14

CPC classification number: A61K9/006 ,  A61K31/4468 ,  A61K38/25

Abstract: A stable formulation is disclosed that enables the effective intra-oral delivery to a patient of a pharmaceutical agent. The formulation comprises the pharmaceutical agent mixed with an orally-acceptable oral-absorption enhancer in an orally-acceptable carrier-solvent, wherein the oral-absorption enhancer is adapted to modify the surface membrane such that absorption through the surface membrane is initiated or increased. The oral-absorption enhancer may comprise hydroxypropyl-beta-cyclodextrin and surfactants including benzalkonium chloride, benzethonium chloride, polysorbate 80, sodium lauryl sulfate, Brij surfactants, Tween and Pluronic surfactants. Also disclosed is a system for delivering the formulation including a mechanism for dispensing predetermined doses of the inventive formulation intra-orally as with an aerosol or spray pump or propellant device.

Abstract translation: 公开了稳定的制剂，其能够有效地口服给药剂的患者。 该制剂包含在口服可接受的载体 - 溶剂中与口服可接受的口服吸收增强剂混合的药剂，其中口服吸收增强剂适于改性表面膜，使得通过表面膜的吸收开始或增加。 口服吸收增强剂可以包含羟丙基-β-环糊精和表面活性剂，包括苯扎氯铵，苄索氯铵，聚山梨醇酯80，月桂基硫酸钠，Brij表面活性剂，吐温和Pluronic表面活性剂。 还公开了一种用于递送制剂的系统，其包括用气雾剂或喷雾泵或推进剂装置口腔内分配预定剂量的本发明制剂的机构。

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

Applicant: UNIV TEXAS ,  JOHNSTON KEITH P ,  WILLIAMS ROBERT O III ,  MATTEUCCI MICHAL E

Inventor： JOHNSTON KEITH P ,  WILLIAMS ROBERT O III ,  MATTEUCCI MICHAL E

IPC: A61K9/16 ,  A61K9/20 ,  A61K9/50 ,  A61K31/496 ,  A61K47/34 ,  C01B13/14

CPC classification number: A61K9/1635 ,  A61K9/5138 ,  A61K9/5146 ,  A61K9/5161 ,  A61K9/5192 ,  A61K31/496

Abstract: 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.

Abstract translation: 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。