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1. 发明授权

US6423345B2 Matrices formed of polymer and hydrophobic compounds for use in drug delivery 有权
标题翻译：由聚合物和疏水化合物形成的矩阵用于药物递送
公开(公告)号：US6423345B2
公开(公告)日：2002-07-23
申请号：US25517999
申请日：1999-02-22
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , KHATTAK SARWAT , STRAUB JULIE
IPC分类号： A61K9/16 , A61K9/22 , A61K9/52 , A61K47/24 , A61K47/30 , A61K9/10
CPC分类号： A61K9/1617 , A61K9/1647 , Y10S514/951 , Y10S514/952
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.
摘要翻译：将脂质或其它疏水性或两亲性化合物（本文统称为“疏水化合物”）整合到用于药物递送的聚合物基质中以改变药物释放动力学。在药物是水溶性的实施方案中，与不将疏水性化合物掺入聚合物材料的聚合物基质的释放相比，药物在更长的时间内释放。与其中加入表面活性剂或脂质作为赋形剂的方法相反，疏水化合物实际上整合到聚合物基质中，从而改变水进入微粒的扩散并将溶解的药物扩散出基质。整合的疏水化合物还延长了形成基质的水解不稳定聚合物的降解，进一步延缓了包封药物的释放。

2. 发明专利

NZ516083A Porous drug matrices and methods of manufacture thereof 未知
公开(公告)号：NZ516083A
公开(公告)日：2003-08-29
申请号：NZ51608300
申请日：2000-05-25
申请人： ACUSPHERE INC
发明人： STRAUB JULIE , BERNSTEIN HOWARD , CHICKERING DONALD E , KHATTAK SARWAT , RANDALL GREG
IPC分类号： A61K9/14 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/16 , A61K9/20 , A61K9/48 , A61K47/02 , A61K47/12 , A61K47/26 , A61K47/34
摘要： Drugs, especially low aqueous solubility drugs, are provided in a porous matrix form, preferably microparticles, which enhances dissolution of the drug in aqueous media. These porous drug matrices are made using a process that includes: (i) dissolving a drug in an organic volatile solvent to form a drug solution, (ii) combining at least one pore forming agent with the drug solution to form an emulsion, suspension, or second solution containing the pore forming agent, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. The pore-forming agent can be either a volatile liquid that is immiscible with the drug solvent or a volatile solid compound, preferably a volatile salt. In a preferred embodiment, spray drying is used to remove the solvents and the pore-forming agent. The resulting porous matrix has a faster rate of dissolution following administration to a patient, as compared to non-porous matrix forms of the drug. In a preferred embodiment, microparticles of the porous drug matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral admisnistration. Paclitaxel or docetaxel can be provided in a porous matrix form, which allows the drug to be formulated without solubilizing agents and administered as a bolus.

3. 发明专利

CA2329875A1 MATRICES FORMED OF POLYMER AND HYDROPHOBIC COMPOUNDS FOR USE IN DRUG DELIVERY 未知
公开(公告)号：CA2329875A1
公开(公告)日：1999-11-11
申请号：CA2329875
申请日：1999-03-08
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , STRAUB JULIE , KHATTAK SARWAT , CHICKERING DONALD
IPC分类号： A61K9/16 , A61K9/22 , A61K9/52 , A61K47/24 , A61K47/30
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

4. 发明专利

DE69930240T2 未知
公开(公告)号：DE69930240T2
公开(公告)日：2006-11-23
申请号：DE69930240
申请日：1999-03-08
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , KHATTAK SARWAT , STRAUB JULIE
IPC分类号： A61K9/22 , A61K9/16 , A61K9/52 , A61K47/24 , A61K47/30
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

5. 发明专利

ES2259472T3 MATRICES FORMADAS DE POLIMERO Y COMPUESTOS HIDROFOBOS PARA USO EN LA ADMINISTRACION DE FARMACOS. 未知
公开(公告)号：ES2259472T3
公开(公告)日：2006-10-01
申请号：ES99911269
申请日：1999-03-08
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , KHATTAK SARWAT , STRAUB JULIE
IPC分类号： A61K9/16 , A61K9/22 , A61K9/52 , A61K47/24 , A61K47/30
摘要： Una matriz polimérica porosa para administrar un agente terapéutico o profiláctico, en la que la matriz se forma a partir de un polímero biocompatible que ha incorporado en su interior: un agente terapéutico o profiláctico una cantidad efectiva de un compuesto hidrófobo en el interior de la matriz para modificar la difusión de agua al interior de la matriz y la administración del agente terapéutico o profiláctico desde la matriz, en el que la matriz se obtiene emulsificando un agente formador de poros con un polímero disuelto en un solvente y a continuación eliminando el agente formador de poros y el solvente.

6. 发明专利

CA2329875C MATRICES FORMED OF POLYMER AND HYDROPHOBIC COMPOUNDS FOR USEIN DRUG DELIVERY 未知
公开(公告)号：CA2329875C
公开(公告)日：2003-09-16
申请号：CA2329875
申请日：1999-03-08
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , STRAUB JULIE , KHATTAK SARWAT
IPC分类号： A61K9/16 , A61K9/22 , A61K9/52 , A61K47/24 , A61K47/30
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of wat er into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying releas e of encapsulated drug.

7. 发明专利

AU746696B2 Matrices formed of polymer and hydrophobic compounds for use in drug delivery 未知
公开(公告)号：AU746696B2
公开(公告)日：2002-05-02
申请号：AU2995499
申请日：1999-03-08
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , KHATTAK SARWAT , STRAUB JULIE
IPC分类号： A61K9/16 , A61K9/22 , A61K9/52 , A61K47/24 , A61K47/30
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

8. 发明专利

NO20005452L 未知
公开(公告)号：NO20005452L
公开(公告)日：2000-12-29
申请号：NO20005452
申请日：2000-10-27
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , KHATTAK SARWAT , STRAUB JULIE ANN
IPC分类号： A61K9/16 , A61K9/22 , A61K9/52 , A61K47/24 , A61K47/30
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

9. 发明专利

NO20005452A 未知
公开(公告)号：NO20005452A
公开(公告)日：2000-12-29
申请号：NO20005452
申请日：2000-10-27
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , KHATTAK SARWAT , STRAUB JULIE ANN
IPC分类号： A61K9/16 , A61K9/22 , A61K9/52 , A61K47/24 , A61K47/30
CPC分类号： A61K9/1617 , A61K9/1647 , Y10S514/951 , Y10S514/952

10. 发明专利

DK1073422T3 未知
公开(公告)号：DK1073422T3
公开(公告)日：2006-07-03
申请号：DK99911269
申请日：1999-03-08
申请人： ACUSPHERE INC
发明人： BERNSTEIN HOWARD , CHICKERING DONALD , KHATTAK SARWAT , STRAUB JULIE
IPC分类号： A61K9/22 , A61K9/16 , A61K9/52 , A61K47/24 , A61K47/30
摘要： A lipid or other hydrophobic or amphiphilic compound (collectively referred to herein as "hydrophobic compounds") is integrated into a polymeric matrix for drug delivery to alter drug release kinetics. In embodiments where the drug is water soluble, the drug is released over longer periods of time as compared to release from the polymeric matrix not incorporating the hydrophobic compound into the polymeric material. In contrast to methods in which a surfactant or lipid is added as an excipient, the hydrophobic compound is actually integrated into the polymeric matrix, thereby modifying the diffusion of water into the microparticle and diffusion of solubilized drug out of the matrix. The integrated hydrophobic compound also prolongs degradation of hydrolytically unstable polymers forming the matrix, further delaying release of encapsulated drug.

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