公开(公告)号：US06730698B2

公开(公告)日：2004-05-04

申请号：US10072398

申请日：2002-02-06

申请人： Samuel Broder ,  Kenneth L. Duchin ,  Sami Selim

发明人： Samuel Broder ,  Kenneth L. Duchin ,  Sami Selim

IPC分类号： A61K31335

CPC分类号： A61K31/337 ,  A61K38/13 ,  A61K45/06 ,  Y02A50/411 ,  A61K2300/00

摘要： Taxane antineoplastic agents which have heretofore exhibited poor or non-existent oral bioavailability are administered orally to human patients suffering from taxane-responsive disease conditions and made sufficiently bioavailable to achieve therapeutic blood levels. In a preferred embodiment, the taxane, preferably paclitaxel, is co-administered to the patient with an oral cyclosporin enhancing agent, preferably cyclosporin A. By one preferred method, a dose of oral enhancer is administered about 0.5-72 hours before the taxane and a second dose of the enhancer and administered immediately before, together with or immediately after the taxane. A method of treating human patients suffering from taxane-responsive disease conditions is also provided, as well as a method for providing such treatment while preventing or reducing hypersensitivity and allergic reactions without the need for pre-medication.

公开(公告)号：US5968972A

公开(公告)日：1999-10-19

申请号：US608776

申请日：1996-02-29

申请人： Samuel Broder ,  Kenneth L. Duchin ,  Sami Selim

发明人： Samuel Broder ,  Kenneth L. Duchin ,  Sami Selim

IPC分类号： A61K31/135 ,  A61J20060101 ,  A61K20060101 ,  A61K31/337 ,  A61K38/08 ,  A61K38/13 ,  A61K45/06 ,  A61P35/00 ,  A61K31/335

CPC分类号： A61K38/13 ,  A61K31/337 ,  A61K45/06

摘要： A method of increasing the bioavailability upon oral administration of a pharmacologically active target agent, particularly an antitumor or antineoplastic agent which exhibits poor or inconsistent oral bioavailability (e.g., paclitaxel or etoposide), comprises the oral co-administration to a mammalian patient of the target agent and an oral bioavailability-enhancing agent, (e.g., cyclosporin A, cyclosporin D, ketoconazole or captopril). The enhancing agent may be administered orally from 0.5-24 hrs. prior to the oral administration of one or more doses of the target agent, substantially simultaneously with the target agent or both prior to and substantially simultaneously with the target agent. A method of treating mammalian patients suffering from diseases responsive to target agents with poor oral bioavailability, as well as oral dosage forms containing such target agents, combination oral dosage forms containing bioavailability-enhancing agents and target agents and kits containing enhancing and target agent dosage forms and dosing information for the co-administration of the same are also disclosed.

摘要翻译： 在口服给药药物活性的靶剂，特别是表现出差的或不一致的口服生物利用度的抗肿瘤剂（例如，紫杉醇或依托泊苷）时，提高生物利用度的方法包括向目标哺乳动物患者口服共同施用 药剂和口服生物利用度增强剂（例如环孢菌素A，环孢菌素D，酮康唑或卡托普利）。 增强剂可以在0.5-24小时口服给药。 在一次或多次剂量的目标试剂口服给药之前，基本上同时与目标试剂或两者在目标试剂之前和基本上同时进行。 治疗患有对具有差的口服生物利用度的靶因子起反应的疾病的哺乳动物患者的方法以及含有这些靶因子的口服剂型，含有生物利用度增强剂和靶剂的组合口服剂型和含有增强剂和靶剂剂型的试剂盒 并且还公开了其共同给药的给药信息。

公开(公告)号：US20050238634A1

公开(公告)日：2005-10-27

申请号：US11105081

申请日：2005-04-13

申请人： Samuel Broder ,  Kenneth Duchin ,  Sami Selim

发明人： Samuel Broder ,  Kenneth Duchin ,  Sami Selim

IPC分类号： A61K47/06 ,  A61K9/00 ,  A61K31/00 ,  A61K31/135 ,  A61K31/337 ,  A61K38/04 ,  A61K38/08 ,  A61K38/13 ,  A61K38/54 ,  A61K45/06 ,  A61K47/22 ,  A61P13/12 ,  A61P31/12 ,  A61P35/00

CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/337 ,  A61K38/13 ,  Y02A50/411 ,  A61K2300/00

摘要： A method of increasing the bioavailability upon oral administration of a pharmacologically active target agent, particularly an antitumor or antineoplastic agent which exhibits poor or inconsistent oral bioavailability (e.g., paclitaxel, docetaxel or etoposide), comprises the oral co-administration to a mammalian patient of the target agent and an oral bioavailability-enhancing agent (e.g., cyclosporin A, cyclosporin D, cyclosporin F or ketoconazole). The enhancing agent may be administered orally from 0.5-24 hrs. prior to the oral administration of one or more doses of the target agent, substantially simultaneously with the target agent or both prior to and substantially simultaneously with the target agent. A method of treating mammalian patients suffering from diseases responsive to target agents with poor oral bioavailability, as well as oral dosage forms containing such target agents, combination oral dosage forms containing bioavailability-enhancing agents and target agents and kits containing enhancing and target agent dosage forms and dosing information for the co-administration of the same are also disclosed.

摘要翻译： 在口服给药药物活性的靶剂，特别是表现出差的或不一致的口服生物利用度（例如紫杉醇，多西紫杉醇或依托泊苷）的抗肿瘤剂或抗肿瘤药物时，增加生物利用度的方法包括向哺乳动物患者口服共同施用 目标剂和口服生物利用度增加剂（例如环孢菌素A，环孢菌素D，环孢菌素F或酮康唑）。 增强剂可以在0.5-24小时口服给药。 在一次或多次剂量的目标试剂口服给药之前，基本上同时与目标试剂或两者在目标试剂之前和基本上同时进行。 治疗患有对具有差的口服生物利用度的靶因子起反应的疾病的哺乳动物患者的方法以及含有这些靶因子的口服剂型，含有生物利用度增强剂和靶剂的组合口服剂型和含有增强剂和靶剂剂型的试剂盒 并且还公开了其共同给药的给药信息。

公开(公告)号：US5695901A

公开(公告)日：1997-12-09

申请号：US576812

申请日：1995-12-21

申请人： Sami Selim

发明人： Sami Selim

IPC分类号： C01G49/06 ,  C01G49/08 ,  G03G9/083

CPC分类号： B82Y30/00 ,  C01G49/06 ,  C01G49/08 ,  G03G9/0831 ,  G03G9/0833 ,  G03G9/0839 ,  C01P2004/64 ,  C01P2006/42 ,  Y10T428/2991

摘要： Provided is a method for producing nano-size magnetic particles, and particularly magnetite and maghemite particles, that are useful in preparing toner products for reprographic processes. The magnetic particles are made of a controlled size through the use of a microemulsion. Precursor particles are precipitated in droplets of a disperse aqueous phase of the microemulsion. The precursor particles are oxidized in a carefully controlled environment to form the desired magnetic particles and to avoid overoxidation to produce undesirable nonmagnetic particles, such as hematite. In one embodiment, the nano-size magnetic particles are treated to improve their hydrophobicity. The treated particles have a reduced tendency to agglomerate and are easier to disperse in the preparation of toner products. The hydrophobic treatment may include connecting hydrophobic chemical groups to the magnetic particles through the use of silane coupling agents. In addition to improving the flowability characteristics of the magnetic particles, hydrophobic treatment may also be used to at least partially mask the inherent color of the nano-size magnetic particles that could otherwise interfere with preparation of color toners for use in developing sharp color images.

摘要翻译： 提供用于制备用于制备用于再现工艺的调色剂产品的纳米尺寸磁性颗粒，特别是磁铁矿和磁赤铁矿颗粒的方法。 磁性颗粒通过使用微乳液由受控的尺寸制成。 前体颗粒在微乳液的分散水相的液滴中沉淀。 前体颗粒在仔细控制的环境中被氧化以形成所需的磁性颗粒，并避免过氧化以产生不需要的非磁性颗粒，例如赤铁矿。 在一个实施方案中，处理纳米尺寸磁性颗粒以改善其疏水性。 经处理的颗粒具有减少聚集的倾向并且在调色剂产物的制备中更容易分散。 疏水处理可以包括通过使用硅烷偶联剂将疏水化学基团连接到磁性颗粒上。 除了改善磁性颗粒的流动性特征之外，还可以使用疏水处理来至少部分掩蔽纳米尺寸磁性颗粒的固有颜色，否则可能干扰制备彩色调色剂以用于显影尖锐彩色图像。

公开(公告)号：US5695900A

公开(公告)日：1997-12-09

申请号：US576811

申请日：1995-12-21

申请人： Sami Selim

发明人： Sami Selim

IPC分类号： C01G49/06 ,  C01G49/08 ,  G03G9/083

CPC分类号： B82Y30/00 ,  C01G49/06 ,  C01G49/08 ,  G03G9/0838 ,  G03G9/0839 ,  C01P2004/64 ,  C01P2006/42 ,  Y10T428/31678

摘要： Provided is a method for producing nano-size magnetic particles, and particularly magnetite and maghemite particles, that are useful in preparing toner products for reprographic processes. The magnetic particles are made of a controlled size through the use of a microemulsion. Precursor particles are precipitated in droplets of a disperse aqueous phase of the microemulsion. The precursor particles are oxidized in a carefully controlled environment to form the desired magnetic particles and to avoid overoxidation to produce undesirable nonmagnetic particles, such as hematite. In one embodiment, the nano-size magnetic particles are treated to improve their hydrophobicity. The treated particles have a reduced tendency to agglomerate and are easier to disperse in the preparation of toner products. The hydrophobic treatment may include connecting hydrophobic chemical groups to the magnetic particles through the use of silane coupling agents. In addition to improving the flowability characteristics of the magnetic particles, hydrophobic treatment may also be used to at least partially mask the inherent color of the nano-size magnetic particles that could otherwise interfere with preparation of color toners for use in developing sharp color images.

摘要翻译： 提供用于制备用于制备用于再现工艺的调色剂产品的纳米尺寸磁性颗粒，特别是磁铁矿和磁赤铁矿颗粒的方法。 磁性颗粒通过使用微乳液由受控的尺寸制成。 前体颗粒在微乳液的分散水相的液滴中沉淀。 前体颗粒在仔细控制的环境中被氧化以形成所需的磁性颗粒，并避免过氧化以产生不需要的非磁性颗粒，例如赤铁矿。 在一个实施方案中，处理纳米尺寸磁性颗粒以改善其疏水性。 经处理的颗粒具有减少聚集的倾向并且在调色剂产物的制备中更容易分散。 疏水处理可以包括通过使用硅烷偶联剂将疏水化学基团连接到磁性颗粒上。 除了改善磁性颗粒的流动性特征之外，还可以使用疏水处理来至少部分掩蔽纳米尺寸磁性颗粒的固有颜色，否则可能干扰制备彩色调色剂以用于显影尖锐彩色图像。