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1. 发明专利

JP2011140527A Dosage formulation of ultrasound contrast agent 审中-公开
标题翻译：超声对比剂的剂量配方
公开(公告)号：JP2011140527A
公开(公告)日：2011-07-21
申请号：JP2011094529
申请日：2011-04-20
申请人： Acusphere Inc , アキュスフィア, インコーポレイテッド
发明人： WALOVITCH RICHARD , BERNSTEIN HOWARD , CHICKERING DONALD E III , STRAUB JULIE
IPC分类号： A61K49/00 , A61K9/10 , A61K9/14 , A61K47/06 , A61K47/24 , A61K47/26 , A61K47/34
摘要： PROBLEM TO BE SOLVED: To provide dosage formulations including microparticles which provide enhanced images of long duration, and to provide a kit for administering the dosage formulations including the microparticles for use in the ultrasound imaging technology.
SOLUTION: Clinical studies have been conducted and specific dosage formulations have been developed which provides significantly enhanced images of long duration by using polymeric microparticles. The polymeric microparticles have incorporated therein perfluorocarbon gases. The dosage formulation includes microparticles formed of a biocompatible polymer, preferably including a lipid incorporated therein, and containing a perfluorocarbon that is a gas at body temperature. The microparticles are provided to a patient in an amount effective to enhance ultrasound imaging in the cardiac ventricle for more than 5 minutes or in the myocardium for more than a minute, (in a dose ranging from 0.025 to 8.0 mg microparticles/kg body weight).
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供包括提供长时间增强图像的微粒的剂型，并提供用于施用包含用于超声成像技术的微粒的剂型。解决方案：已经进行了临床研究，并且开发了具体的剂型，其通过使用聚合物微粒提供了显着增强的持续时间的图像。聚合物微粒中已加入全氟化碳气体。剂量制剂包括由生物相容性聚合物形成的微粒，其优选包括掺入其中的脂质，并且含有在体温下作为气体的全氟化碳。将微粒以有效增强心室超声波成像超过5分钟或心肌超过一分钟（剂量范围为0.025至8.0mg微粒/ kg体重）的量提供给患者，。版权所有（C）2011，JPO＆INPIT

2. 发明申请

US20040121005A1 Porous COX-2 inhibitor matrices and methods of manufacture thereof 失效
标题翻译：多孔COX-2抑制剂基质及其制备方法
公开(公告)号：US20040121005A1
公开(公告)日：2004-06-24
申请号：US10441440
申请日：2003-05-19
申请人： Acusphere, Inc.
发明人： David Altreuter , Julie Straub , Howard Bernstein , Donald E. Chickering III , Paul Kopesky , Greg Randall
IPC分类号： A61K031/415 , A61K009/20
CPC分类号： A61K9/0019 , A61K9/2095 , A61K47/02
摘要： One or more COX-2 inhibitors are provided in a porous matrix form wherein the dissolution rate of the drug is enhanced when the matrix is contacted with an aqueous medium. The porous matrix yields upon contact with an aqueous medium nanoparticles and microparticles of COX-2 inhibitors having a mean diameter between about 0.01 and 5 nullm and a total surface area greater than about 0.5 m2/mL. The dry porous matrix preferably is in a dry powder form having a TAP density less than or equal to 1.0 g/mL. The porous COX-2 inhibitor matrices preferably are made using a process that includes (i) dissolving one or more COX-2 inhibitors in a 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, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the dry porous matrix of COX-2 inhibitors. 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.
摘要翻译：以多孔基质形式提供一种或多种COX-2抑制剂，其中当基质与水性介质接触时药物的溶解速度增强。当与水性介质纳米颗粒和平均直径在约0.01至5μm之间且总表面积大于约0.5m 2 / mL的COX-2抑制剂的微粒接触时，多孔基质产生。干多孔基质优选为TAP密度小于或等于1.0g / mL的干粉形式。多孔COX-2抑制剂基质优选使用包括（i）将一种或多种COX-2抑制剂溶解在挥发性溶剂中以形成药物溶液的方法制备，（ii）将至少一种成孔剂与药物溶液以形成乳液，悬浮液或第二溶液，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂，得到COX-2抑制剂的干燥多孔基质。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。

3. 发明申请

US20040121003A1 Methods for making pharmaceutical formulations comprising deagglomerated microparticles 审中-公开
标题翻译：制备包含解聚微粒的药物制剂的方法
公开(公告)号：US20040121003A1
公开(公告)日：2004-06-24
申请号：US10324558
申请日：2002-12-19
申请人： ACUSPHERE, INC.
发明人： Donald E. Chickering III , Shaina Reese , Sridhar Narasimhan , Julie A. Straub , Howard Bernstein , David Altreuter , Eric K. Huang
IPC分类号： A61K009/14 , A61K009/20
CPC分类号： B01D1/18 , A61K9/0075 , A61K9/145 , A61K9/1647 , A61K9/1694 , B01J2/04
摘要： Methods are provided for making a dry powder blend pharmaceutical formulation comprising (i) forming microparticles which comprise a pharmaceutical agent; (ii) providing at least one excipient in the form of particles having a volume average diameter that is greater than the volume average diameter of the microparticles; (iii) blending the microparticles with the excipient to form a powder blend; and (iv) jet milling the powder blend to deagglomerate at least a portion of any of the microparticles which have agglomerated, while substantially maintaining the size and morphology of the individual microparticles. Jet milling advantageously can eliminate the need for more complicated wet deagglomeration processes, can lower residual moisture and solvent levels in the microparticles (which leads to better stability and handling properties for dry powder formulations), and can improve wettability, suspendability, and content uniformity of dry powder blend formulations.
摘要翻译：提供用于制备干粉混合物药物制剂的方法，其包含（i）形成包含药剂的微粒; （ii）提供至少一种具有体积平均直径大于微粒的体积平均直径的颗粒形式的赋形剂; （iii）将微粒与赋形剂混合以形成粉末混合物; 和（iv）喷射研磨粉末共混物以使至少一部分具有附聚的任何微粒分解，同时基本保持各个微粒的尺寸和形态。喷射铣削有利地可以消除对更复杂的湿解聚过程的需要，可以降低微粒中的残留水分和溶剂水平（这导致干粉配方的更好的稳定性和处理性能），并且可以改善润湿性，悬浮性和含量均匀性干粉混合配方。

4. 发明申请

US20030147962A1 Matrices formed of polymer and hydrophobic compounds for use in drug delivery 失效
公开(公告)号：US20030147962A1
公开(公告)日：2003-08-07
申请号：US10383264
申请日：2003-03-05
申请人： Acusphere, Inc.
发明人： Howard Bernstein , Donald Chickering , Sarwat Khattak , Julie Straub
IPC分类号： A61K031/685 , A61K009/14
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 nullhydrophobic compoundsnull) 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. 发明申请

US20020142050A1 Porous drug matrices and methods of manufacture thereof 有权
标题翻译：多孔药物基质及其制造方法
公开(公告)号：US20020142050A1
公开(公告)日：2002-10-03
申请号：US10053929
申请日：2002-01-22
申请人： Acusphere Inc.
发明人： Julie Straub , David Altreuter , Howard Bernstein , Donald E. Chickering III , Sarwat Khattak , Greg Randall
IPC分类号： A61K009/14 , A61K009/50
CPC分类号： A61K9/1635 , A61K9/1611 , A61K9/1623 , A61K9/1688 , A61K9/1694
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. The drug matrices preferably are made using a process that includes (i) dissolving a drug, preferably a drug having low aqueous solubility, in a 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 and hydrophilic or hydrophobic excipients that stabilize the drug and inhibit crystallization, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of drug. Hydrophobic or hydrophilic excipients may be selected to stabilize the drug in crystalline form by inhibiting crystal growth or to stabilize the drug in amorphous form by preventing crystallization. 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 administration.
摘要翻译：药物，特别是低含水溶性药物以多孔基质形式提供，优选微粒，其增强药物在水性介质中的溶解。药物基质优选使用以下方法制备，所述方法包括（i）将挥发性溶剂中的药物（优选为低溶解度的药物）溶解以形成药物溶液，（ii）将至少一种成孔剂与药物溶液以形成稳定药物并抑制结晶的乳液，悬浮液或第二溶液和亲水或疏水赋形剂，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生多孔基质药物。可以选择疏水性或亲水性赋形剂，以通过抑制晶体生长来稳定药物的结晶形式，或者通过防止结晶来稳定药物的无定形形式。造孔剂可以是与药物溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。与药物的无孔基质形式相比，得到的多孔基质在给予患者后具有更快的溶解速率。在优选的实施方案中，多孔药物基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

6. 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。

7. 发明申请

US20040118007A1 Methods and apparatus for making particles using spray dryer and in-line jet mill 失效
标题翻译：使用喷雾干燥器和直列式喷射磨机制造颗粒的方法和设备
公开(公告)号：US20040118007A1
公开(公告)日：2004-06-24
申请号：US10324943
申请日：2002-12-19
申请人： ACUSPHERE, INC.
发明人： Donald E. Chickering III , Sridhar Narasimhan , David Altreuter , Paul Kopesky , Mark Keegan , Julie A. Straub , Howard Bernstein
IPC分类号： F26B017/12 , F26B003/08 , F26B007/00 , F26B017/00
CPC分类号： F26B17/102 , A61K9/1647 , A61K9/1688 , B01D1/18 , B01J2/04 , F26B3/12
摘要： Methods and apparatus are provided for making particles comprising: (a) spraying an emulsion, solution, or suspension, which comprises a solvent and a bulk material (e.g., a pharmaceutical agent), through an atomizer and into a primary drying chamber, having a drying gas flowing therethrough, to form droplets comprising the solvent and bulk material dispersed in the drying gas; (b) evaporating, in the primary drying chamber, at least a portion of the solvent into the drying gas to solidify the droplets and form particles dispersed in drying gas; and (c) flowing the particles and at least a portion of the drying gas through a jet mill to deagglomerate or grind the particles. By coupling spray drying with nullin-linenull jet milling, a single step process is created from two separate unit operations, and an additional collection step is advantageously eliminated. The one-step, in-line process has further advantages in time and cost of processing.
摘要翻译：提供了用于制备颗粒的方法和装置，包括：（a）通过雾化器喷雾包含溶剂和散装材料（例如药剂）的乳液，溶液或悬浮液，并进入初级干燥室，其具有干燥气体流过其中以形成包含分散在干燥气体中的溶剂和散装材料的液滴; （b）在初级干燥室中将至少一部分溶剂蒸发到干燥气体中以固化液滴并形成分散在干燥气体中的颗粒; 和（c）使颗粒和至少一部分干燥气体流过喷射磨机以使颗粒解聚或研磨。通过将喷雾干燥与“直列式”喷射式研磨相结合，由两个单独的单元操作产生单步骤，有利地消除了另外的收集步骤。一步一步的在线过程在处理时间和成本方面具有进一步的优势。

8. 发明申请

US20030037459A1 Spray drying apparatus and methods of use 有权
标题翻译：喷雾干燥装置及使用方法
公开(公告)号：US20030037459A1
公开(公告)日：2003-02-27
申请号：US10045419
申请日：2001-10-26
申请人： Acusphere, Inc.
发明人： Donald E. Chickering III , Mark J. Keegan , Greg Randall , Howard Bernstein , Julie Straub
IPC分类号： F26B017/00
CPC分类号： B01J2/04 , B01D1/18
摘要： Improved spray drying apparati, and methods of use thereof, have been developed. The spray drying equipment includes a primary drying chamber and a secondary drying apparatus which includes tubing having a length sufficient to increase the contact time between the drying gas and the droplets/particles to dry the particles to the extent desired, at a drying rate and temperature which would be too low to provide adequate drying without the secondary drying apparatus. The secondary drying apparatus increases the drying efficiency of the spray dryer system without increasing the drying rate, while minimizing loss in yield. Te secondary drying apparatus can include multiple secondary apparati, which are independently controlled for temperature and/or have different dimensions (cross-sectional areas and/or lengths), to allow for optimization of drying conditions. For example, in one embodiment, the temperatures of the secondary appararatiare set to gradually increase, or decrease, enabling the particles to be dried at multiple temperatures and drying conditions. In another embodiment, the apparatihave different dimensions to alter the velocity at which the particles are dried, to accommodate changes in particle aggregation or other properties affecting product yield. A preferred application for the spray drying process and equipment is in the production of microparticles, between about 1 and 200 nullm in diameter, which can be used to deliver therapeutic and diagnostic agents.
摘要翻译：已经开发了改进的喷雾干燥装置及其使用方法。喷雾干燥设备包括初级干燥室和次级干燥设备，其包括具有足以增加干燥气体和液滴/颗粒之间的接触时间的长度的管道，以将干燥颗粒以期望的程度以干燥速率和温度这不足以在没有二次干燥装置的情况下提供足够的干燥。二次干燥装置提高喷雾干燥器系统的干燥效率，而不增加干燥速率，同时最小化产率损失。 Te二次干燥装置可以包括多个二次装置，其独立地控制温度和/或具有不同的尺寸（横截面积和/或长度），以允许优化干燥条件。例如，在一个实施方案中，二次装置的温度设定为逐渐增加或降低，使颗粒能够在多个温度和干燥条件下干燥。在另一个实施方案中，提供不同的尺寸以改变颗粒干燥速度，以适应颗粒聚集的变化或影响产品产率的其它性质。用于喷雾干燥方法和设备的优选应用是生产直径约1-200μm的微粒，其可用于递送治疗和诊断剂。

9. 发明申请

US20020041896A1 Porous paclitaxel matrices and methods of manufacture thereof 有权
标题翻译：多孔紫杉醇基质及其制备方法
公开(公告)号：US20020041896A1
公开(公告)日：2002-04-11
申请号：US09798824
申请日：2001-03-02
申请人： Acusphere, Inc.
发明人： Julie Straub , Howard Bernstein , Donald E. Chickering III , Sarwat Khattak , Greg Randall
IPC分类号： A61K009/48 , A61K009/20 , A61K009/14
CPC分类号： A61K9/1623 , A61K9/1611 , A61K9/1635 , A61K9/1694 , Y10S977/906
摘要： Paclitaxel is provided in a porous matrix form, which allows the drug to be formulated without Cremophor and administered as a bolus. The paclitaxel matrices preferably are made using a process that includes (i) dissolving paclitaxel in a volatile solvent to form a paclitaxel solution, (ii) combining at least one pore forming agent with the paclitaxel solution to form an emulsion, suspension, or second solution, and (iii) removing the volatile solvent and pore forming agent from the emulsion, suspension, or second solution to yield the porous matrix of paclitaxel. The pore forming agent can be either a volatile liquid that is immiscible with the paclitaxel 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. In a preferred embodiment, microparticles of the porous paclitaxel matrix are reconstituted with an aqueous medium and administered parenterally, or processed using standard techniques into tablets or capsules for oral administration.
摘要翻译：紫杉醇以多孔基质形式提供，其允许药物在没有Cremophor的情况下配制并作为大剂量给药。紫杉醇基质优选使用包括（i）将紫杉醇溶解在挥发性溶剂中以形成紫杉醇溶液的方法制备，（ii）将至少一种成孔剂与紫杉醇溶液组合以形成乳液，悬浮液或第二溶液，和（iii）从乳液，悬浮液或第二溶液中除去挥发性溶剂和成孔剂以产生紫杉醇的多孔基质。成孔剂可以是与紫杉醇溶剂或挥发性固体化合物，优选挥发性盐不混溶的挥发性液体。在优选的实施方案中，使用喷雾干燥来除去溶剂和成孔剂。在优选的实施方案中，多孔紫杉醇基质的微粒用水性介质重新配制，并肠胃外给药，或使用标准技术加工成用于口服给药的片剂或胶囊。

10. 发明申请

WO2007070843A3 PROCESSES FOR MAKING PARTICLE-BASED PHARMACEUTICAL FORMULATIONS FOR ORAL ADMINISTRATION 审中-公开
标题翻译：制造基于粒子的药物制剂进行口腔管理的方法
公开(公告)号：WO2007070843A3
公开(公告)日：2007-10-25
申请号：PCT/US2006062073
申请日：2006-12-14
申请人： ACUSPHERE INC , ALTREUTER DAVID , BERNSTEIN HOWARD , BRITO LUIS A , BRITO SHAINA , CHICKERING DONALD E III , HUANG ERIC K , JAIN RAJEEV , NARASIMHAN SRIDHAR , STRAUB JULIE A
发明人： ALTREUTER DAVID , BERNSTEIN HOWARD , BRITO LUIS A , BRITO SHAINA , CHICKERING DONALD E III , HUANG ERIC K , JAIN RAJEEV , NARASIMHAN SRIDHAR , STRAUB JULIE A
IPC分类号： A61K9/14 , A61K9/16 , A61K9/20
CPC分类号： A61K9/145 , A61K9/0056 , A61K9/0095 , A61K9/2072 , A61K9/2077 , A61K9/2095
摘要： A method is provided for making an oral dosage form of a pharmaceutical agent which includes the steps of (a) providing particles which include a pharmaceutical agent; (b) blending the particles with particles of a pre-processed excipient to form a primary blend, wherein the pre-processed excipient is prepared by (i) dissolving a bulking agent (e.g., a sugar) and at least one non-friable excipient (e.g., a waxy or liquid surfactant) in a solvent to form an excipient solution, and (ii) removing the solvent from the excipient solution to form the pre-processed excipient in dry powder form; (c) milling the primary blend to form a milled pharmaceutical formulation blend that includes microparticles or nanoparticles of the pharmaceutical agent; and (d) processing the milled pharmaceutical formulation blend into a solid oral dosage form or liquid suspension for oral administration. The process yields formulations having improved wettability or dispersibility.
摘要翻译：提供了制备药剂口服剂型的方法，其包括以下步骤：（a）提供包含药剂的颗粒; （b）将颗粒与预处理的赋形剂的颗粒混合以形成初级共混物，其中预处理的赋形剂通过以下步骤制备：（i）将填充剂（例如糖）和至少一种不易碎的赋形剂（例如，蜡状或液体表面活性剂）在溶剂中形成赋形剂溶液，和（ii）从赋形剂溶液中除去溶剂以形成干粉末形式的预处理赋形剂; （c）研磨初级共混物以形成研磨的药物配方混合物，其包括药剂的微粒或纳米颗粒; 和（d）将经研磨的药物制剂混合物加工成固体口服剂型或用于口服给药的液体悬浮液。该方法产生具有改善的润湿性或分散性的制剂。

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