公开(公告)号：US06964946B1

公开(公告)日：2005-11-15

申请号：US09055818

申请日：1998-04-06

申请人： Jose C. Gutierrez-Rocca ,  Janice L. Cacace ,  Sami Selim ,  Robert Testman ,  J. Michael Rutledge

发明人： Jose C. Gutierrez-Rocca ,  Janice L. Cacace ,  Sami Selim ,  Robert Testman ,  J. Michael Rutledge

IPC分类号： A61K9/10 ,  A61F2/02 ,  A61K9/107 ,  A61K9/20 ,  A61K9/48 ,  A61K9/64 ,  A61K31/335 ,  A61K31/337 ,  A61K38/13 ,  A61K45/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/40 ,  A61K47/44 ,  A61P1/16 ,  A61P1/18 ,  A61P13/08 ,  A61P13/12 ,  A61P33/06 ,  A61P35/00

CPC分类号： A61K9/4858 ,  A61K9/1075 ,  A61K9/4866 ,  A61K31/335 ,  A61K31/337 ,  A61K38/13 ,  A61K45/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/40 ,  Y02A50/411 ,  A61K2300/00

摘要： Pharmaceutical compositions for oral administration to mammalian subjects comprise a taxane or taxane derivative (e.g., paclitaxel or docetaxel) as active ingredient and a vehicle comprising at least 30% by weight of a carrier for the taxane, said carrier having an HLB value of at least about 10. The compositions may also comprise 0–70% of a viscosity-reducing co-solubilizer. The compositions may be incorporated into conventional oral pharmaceutical dosage forms, or can be in the form of a two-part medicament wherein the first part includes the taxane in a solubilizing vehicle and the second part comprises a carrier for the taxane to promote oral absorption. Methods of treatment of taxane-responsive disease conditions employing the novel compositions are also disclosed, whereby the compositions can be administered alone or in association with an oral bioavailability enhancing agent.

摘要翻译： 用于哺乳动物受试者的口服给药的药物组合物包含作为活性成分的紫杉烷或紫杉烷衍生物（例如紫杉醇或多西紫杉醇）和包含至少30重量％的紫杉烷的载体的载体，所述载体的HLB值至少为 约10份。组合物还可以包含0-70％的减粘剂共增溶剂。 组合物可以掺入常规的口服药物剂型中，或者可以是两部分药物的形式，其中第一部分在增溶载体中包含紫杉烷，第二部分包含用于紫杉烷促进口服吸收的载体。 还公开了使用该新型组合物治疗紫杉类反应性疾病状况的方法，其中组合物可以单独施用或与口服生物利用度增强剂联合施用。

公开(公告)号：US6056966A

公开(公告)日：2000-05-02

申请号：US81108

申请日：1998-05-18

申请人： Sami Selim ,  Robert Testman ,  Ho-Leung Fung ,  John A. Bauer

发明人： Sami Selim ,  Robert Testman ,  Ho-Leung Fung ,  John A. Bauer

IPC分类号： A61K9/06 ,  A61K9/00 ,  A61K9/08 ,  A61K9/10 ,  A61K9/12 ,  A61K9/70 ,  A61K31/04 ,  A61K31/21 ,  A61K47/10 ,  A61P15/10 ,  A61K6/00 ,  A61F13/00 ,  A01N13/02 ,  A01N13/24

CPC分类号： A61K9/0034 ,  A61K31/04 ,  Y10S514/968 ,  Y10S514/969

摘要： Pharmaceutical compositions in topical or parenteral form containing specific organic mono- or dinitrates, some of them novel compounds, are effective in treating male impotence and erectile dysfunction through topical or intracavernosal administration to the penis. Methods of treatment utilizing the mono- or dinitrate-containing compositions are also disclosed.

摘要翻译： 含有特定有机单硝酸盐或二硝酸盐的药物组合物，其中一些是新型化合物，通过局部或海绵体内阴茎给药可有效治疗男性阳ence和勃起功能障碍。 还公开了使用含单硝酸盐或含硝酸盐的组合物的处理方法。

公开(公告)号：US20050267201A1

公开(公告)日：2005-12-01

申请号：US11165896

申请日：2005-06-24

申请人： Jose Gutierrez-Rocca ,  Janice Cacace ,  Sami Selim ,  Robert Testman ,  J. Rutledge

发明人： Jose Gutierrez-Rocca ,  Janice Cacace ,  Sami Selim ,  Robert Testman ,  J. Rutledge

IPC分类号： A61K9/10 ,  A61F2/02 ,  A61K9/107 ,  A61K9/20 ,  A61K9/48 ,  A61K9/64 ,  A61K31/335 ,  A61K31/337 ,  A61K38/13 ,  A61K45/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/40 ,  A61K47/44 ,  A61P1/16 ,  A61P1/18 ,  A61P13/08 ,  A61P13/12 ,  A61P33/06 ,  A61P35/00

CPC分类号： A61K9/4858 ,  A61K9/1075 ,  A61K9/4866 ,  A61K31/335 ,  A61K31/337 ,  A61K38/13 ,  A61K45/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/22 ,  A61K47/40 ,  Y02A50/411 ,  A61K2300/00

摘要： Pharmaceutical compositions for oral administration to mammalian subjects comprise a taxane or taxane derivative (e.g., paclitaxel or docetaxel) as active ingredient and a vehicle comprising at least 30% by weight of a carrier for the taxane, said carrier having an HLB value of at least about 10. The compositions may also comprise 0-70% of a viscosity-reducing co-solubilizer. The compositions may be incorporated into conventional oral pharmaceutical dosage forms, or can be in the form of a two-part medicament wherein the first part includes the taxane in a solubilizing vehicle and the second part comprises a carrier for the taxane to promote oral absorption. Methods of treatment of taxane-responsive disease conditions employing the novel compositions are also disclosed, whereby the compositions can be administered alone or in association with an oral bioavailability enhancing agent.

公开(公告)号：US07041640B2

公开(公告)日：2006-05-09

申请号：US10800990

申请日：2004-03-15

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

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

IPC分类号： A61K31/337

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.

公开(公告)号：US06245805B1

公开(公告)日：2001-06-12

申请号：US08733142

申请日：1996-10-16

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

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

IPC分类号： A01N4302

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：US20070060635A1

公开(公告)日：2007-03-15

申请号：US11503607

申请日：2006-08-14

申请人： Samuel Broder ,  Kenneth Duchin ,  Sami Selim

发明人： Samuel Broder ,  Kenneth Duchin ,  Sami Selim

IPC分类号： A61K31/337

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：US06610735B2

公开(公告)日：2003-08-26

申请号：US09829846

申请日：2001-04-10

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

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

IPC分类号： A61K31337

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.

公开(公告)号：US06936583B2

公开(公告)日：2005-08-30

申请号：US10794383

申请日：2004-03-05

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

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

IPC分类号： A61K31/337 ,  A61K38/13 ,  A61K45/06 ,  A61K38/00 ,  A61K31/335

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.

摘要翻译： 迄今为止表现出差或不存在的口服生物利用度的紫杉烷抗肿瘤药物经口给患有紫杉烷反应性疾病病症的人类患者，并且具有足够的生物利用度以达到治疗血液水平。 在一个优选的实施方案中，使用口服环孢菌素增强剂（优选环孢菌素A）将紫杉烷，优选紫杉醇共同施用于患者。通过一种优选的方法，口服增强剂的剂量在紫杉烷和紫杉烷之前约0.5-72小时 第二剂量的增强剂，并在紫杉烷之前，之前或之后施用。 还提供了治疗患有紫杉烷反应性疾病病症的人类患者的方法，以及一种在不需要预先给药的情况下预防或减少过敏反应和过敏反应的方法。

公开(公告)号：US06395770B1

公开(公告)日：2002-05-28

申请号：US09385246

申请日：1999-08-28

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 taxaneresponsive 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.

摘要翻译： 迄今为止表现出差或不存在的口服生物利用度的紫杉烷抗肿瘤药物经口给患有紫杉烷反应性疾病病症的人类患者，并且具有足够的生物利用度以达到治疗血液水平。 在一个优选的实施方案中，使用口服环孢菌素增强剂（优选环孢菌素A）将紫杉烷，优选紫杉醇共同施用于患者。通过一种优选的方法，口服增强剂的剂量在紫杉烷和紫杉烷之前约0.5-72小时 第二剂量的增强剂，并在紫杉烷之前，之前或之后施用。 还提供了治疗患有紫杉烷应答疾病病症的人类患者的方法，以及一种在不需要预先给药的情况下预防或减少过敏反应和过敏反应的方法。

公开(公告)号：US06818615B2

公开(公告)日：2004-11-16

申请号：US10242050

申请日：2002-09-12

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

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

IPC分类号： A61K31337

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。