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    • 1. 发明申请
      WO0072827A9 POROUS DRUG MATRICES AND METHODS OF MANUFACTURE THEREOF 审中-公开
    • POROUS DRUG MATRICES AND METHODS OF MANUFACTURE THEREOF
    • 多糖药物及其制造方法
    • WO0072827A9
    • 2002-01-31
    • PCT/US0014578
    • 2000-05-25
    • ACUSPHERE INC
    • STRAUB JULIE , BERNSTEIN HOWARD , CHICKERING DONALD E III , KHATAK SARWAT , RANDALL GREG
    • A61K9/14 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/16 , A61K9/20 , A61K9/48 , A61K47/02 , A61K47/12 , A61K47/26 , A61K47/34
    • A61K9/1635 , A61K9/1623 , A61K9/1688 , A61K9/1694
    • 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 solutions, 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. rocessed using standard techniques into tablets or capsules for oral administration. 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.
    • 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药物的多孔基质。 成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药物的片剂或胶囊。 紫杉醇或多西紫杉醇可以以多孔基质形式提供，其允许药物配制而不含增溶剂并作为大剂量给药。 使用标准技术加工成用于口服给药的片剂或胶囊。 紫杉醇或多西紫杉醇可以以多孔基质形式提供，其允许药物配制而不含增溶剂并作为大剂量给药。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 2. 发明申请
      WO0072827A2 POROUS DRUG MATRICES AND METHODS OF MANUFACTURE THEREOF 审中-公开
    • POROUS DRUG MATRICES AND METHODS OF MANUFACTURE THEREOF
    • 多糖药物及其制造方法
    • WO0072827A2
    • 2000-12-07
    • PCT/US0014578
    • 2000-05-25
    • ACUSPHERE INC
    • STRAUB JULIE , BERNSTEIN HOWARD , CHICKERING DONALD E III , KHATAK SARWAT , RANDALL GREG
    • A61K9/14 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/16 , A61K9/20 , A61K9/48 , A61K47/02 , A61K47/12 , A61K47/26 , A61K47/34
    • A61K9/1635 , A61K9/1623 , A61K9/1688 , A61K9/1694
    • 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 solutions, 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. rocessed using standard techniques into tablets or capsules for oral administration. 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.
    • 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药物的多孔基质。 成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药物的片剂或胶囊。 紫杉醇或多西紫杉醇可以以多孔基质形式提供，其允许药物配制而不含增溶剂并作为大剂量给药。 使用标准技术加工成用于口服给药的片剂或胶囊。 紫杉醇或多西紫杉醇可以以多孔基质形式提供，其允许药物配制而不含增溶剂并作为大剂量给药。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 3. 发明申请
      WO0195877A3 POROUS CELECOXIB MATRICES AND METHODS OF MANUFACTURE THEREOF 审中-公开
    • POROUS CELECOXIB MATRICES AND METHODS OF MANUFACTURE THEREOF
    • 多孔CELECOXIB MATRICES及其制造方法
    • WO0195877A3
    • 2002-05-02
    • PCT/US0119294
    • 2001-06-15
    • ACUSPHERE INC
    • STRAUB JULIE , BERNSTEIN HOWARD , CHICKERING DONALD E III , RANDALL GREG
    • A61K9/10 , A61K9/00 , A61K9/14 , A61K9/20 , A61K9/48 , A61K31/635 , A61K47/00 , A61K47/02 , A61P29/00 , A61K31/415
    • A61K47/02 , A61K9/0019 , A61K9/2095
    • Celecoxib is 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 celecoxib having a mean diameter between about 0.01 and 5 mu m and a total surface area greater than about 0.5 m /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 celecoxib matrices preferably are made using a process that includes: (i) dissolving celecoxib 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 celecoxib. 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.
    • 提供塞来昔布以多孔基质形式提供，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塞来昔布的微粒接触时，多孔基质产生的平均直径为约0.01至5μm，总表面积大于约0.5m 2 / mL。 干多孔基质优选为TAP密度小于或等于1.0g / mL的干粉形式。 多孔塞来昔布基质优选使用以下方法制备，所述方法包括：（i）将塞来昔布溶解在挥发性溶剂中以形成药物溶液; （ii）将至少一种成孔剂与药物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，得到塞来考昔的干多孔基质。 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。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 6. 发明专利
      DE60008720T2  未知
    • DE60008720T2
    • 2005-03-24
    • DE60008720
    • 2000-04-26
    • ACUSPHERE INC
    • CHICKERING E , KEEGAN J , RANDALL GREG , BERNSTEIN HOWARD , STRAUB JULIE
    • F26B3/06 , A61K9/16 , B01D1/18 , B01J2/04 , F26B17/10 , F26B17/16 , F26B23/10
    • 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 The ratio of the length of tubing to the length of the primary drying chamber is at least 2:1. The tubing diameter is substantially smaller than the diameter of the primary drying chamber, such that the particles move at higher velocity through the tubing to minimize product losses. The ratio of the cross-sectional area of the primary drying chamber to the cross-sectional area of the tubing most preferably is about 16:1. The tubing preferably is in a compact coil design, which can more easily be transported and which has minimum space requirements, and may optionally include a jacket to control the temperature of the secondary drying process. A preferred application for the spray drying process and equipment is in the production of polymeric microparticles, between about 1 and 200 mum in diameter, which can be used to deliver therapeutic and diagnostic agents.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 7. 发明专利
      AU768022B2 Porous drug matrices and methods of manufacture thereof 未知
    • Porous drug matrices and methods of manufacture thereof
    • AU768022B2
    • 2003-11-27
    • AU5445900
    • 2000-05-25
    • ACUSPHERE INC
    • STRAUB JULIE , BERNSTEIN HOWARD , CHICKERING DONALD E III , KHATAK SARWAT , RANDALL GREG
    • A61K9/14 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/16 , A61K9/20 , A61K9/48 , A61K47/02 , A61K47/12 , A61K47/26 , A61K47/34
    • 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 solutions, 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. rocessed using standard techniques into tablets or capsules for oral administration. 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 8. 发明专利
      BR0011226A  未知
    • BR0011226A
    • 2002-05-07
    • BR0011226
    • 2000-04-26
    • ACUSPHERE INC
    • CHICKERING DONALD E , KEEGAN MARK J , RANDALL GREG , BERNSTEIN HOWARD , STRAUB JULIE
    • F26B3/06 , A61K9/16 , B01D1/18 , B01J2/04 , F26B17/10 , F26B17/16 , F26B23/10
    • 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 The ratio of the length of tubing to the length of the primary drying chamber is at least 2:1. The tubing diameter is substantially smaller than the diameter of the primary drying chamber, such that the particles move at higher velocity through the tubing to minimize product losses. The ratio of the cross-sectional area of the primary drying chamber to the cross-sectional area of the tubing most preferably is about 16:1. The tubing preferably is in a compact coil design, which can more easily be transported and which has minimum space requirements, and may optionally include a jacket to control the temperature of the secondary drying process. A preferred application for the spray drying process and equipment is in the production of polymeric microparticles, between about 1 and 200 mum in diameter, which can be used to deliver therapeutic and diagnostic agents.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明专利
      BR0010984A  未知
    • BR0010984A
    • 2002-04-30
    • BR0010984
    • 2000-05-25
    • ACUSPHERE INC
    • STRAUB JULIE , BERNSTEIN HOWARD , CHICKERING DONALD E III , KHATAK SARWAT , RANDALL GREG
    • A61K9/14 , A61K9/02 , A61K9/08 , A61K9/10 , A61K9/16 , A61K9/20 , A61K9/48 , A61K47/02 , A61K47/12 , A61K47/26 , A61K47/34
    • 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 solutions, 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. rocessed using standard techniques into tablets or capsules for oral administration. 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.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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