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    Parenteral and oral formulations of benzimidazoles
    1.
    发明申请
    Parenteral and oral formulations of benzimidazoles 审中-公开
    苯并咪唑的肠胃外和口服制剂

    公开(公告)号：US20080293796A1

    公开(公告)日：2008-11-27

    申请号：US12220364

    申请日：2008-07-24

    申请人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Jaymin Shah ,  Peter Wisniecki

    发明人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Jaymin Shah ,  Peter Wisniecki

    IPC分类号： A61K31/4184 ,  A61P35/00

    CPC分类号： A61K9/0019 ,  A61K9/0095 ,  A61K9/1075 ,  A61K31/4184

    摘要： Provided herein are drug delivery systems comprising nanosuspension formulations suitable for parenteral delivery to a subject. The nanosuspension formulations may comprise a benzimidazole derivative, e.g., mebendazole, and surface stabilizers, such as block copolymer(s), e.g., Pluronic F108, and surfactant(s), e.g., Tween 80, and, optionally, water. Provided are methods for defining nanosuspensions of a benzimidazole derivative as having maximum therapeutic efficacy for a treatment regimen by adjusting and/or selecting particles size(s) based on pharmacokinetic parameters of the derivative in the tissue. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition and for treating a cancer by using formulation(s) combining particle diameters whereby the retention of the benzimidazole derivative within the particles increases as the diameter increases such that, upon administration, release of the benzimidazole derivative from the particles into tissue is continuous over a range of time as determined by the particle diameters.

    摘要翻译： 本文提供的药物递送系统包括适于肠胃外递送给个体的纳米悬浮制剂。 纳米悬浮液制剂可以包含苯并咪唑衍生物，例如甲苯咪唑和表面稳定剂，例如嵌段共聚物，例如Pluronic F108和表面活性剂，例如吐温80和任选的水。 提供了通过基于组织中衍生物的药代动力学参数调节和/或选择颗粒大小来定义苯并咪唑衍生物的纳米悬浮液对于治疗方案具有最大治疗功效的方法。 还提供了用于在治疗病理生理状况期间改善苯并咪唑衍生物的生物利用度和通过使用结合粒径的配方治疗癌症的方法，由此直径增加时，颗粒内苯并咪唑衍生物的保留增加， 在施用时，将苯并咪唑衍生物从颗粒中释放到组织中在由颗粒直径确定的时间范围内是连续的。

    Parenteral and oral formulations of benzimidazoles
    2.
    发明授权
    Parenteral and oral formulations of benzimidazoles 有权

    公开(公告)号：US09259391B2

    公开(公告)日：2016-02-16

    申请号：US12802621

    申请日：2010-06-10

    申请人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    发明人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    IPC分类号： A61K31/4184 ,  A61K9/107 ,  A61P33/10 ,  A61P33/12 ,  A61K9/00

    CPC分类号： A61K9/1075 ,  A61K9/0019 ,  A61K9/0095 ,  A61K31/4184

    摘要： Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.

    Parenteral and oral formulations of benzimidazoles
    3.
    发明授权
    Parenteral and oral formulations of benzimidazoles 有权

    公开(公告)号：US09259390B2

    公开(公告)日：2016-02-16

    申请号：US12220374

    申请日：2008-07-24

    申请人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    发明人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    IPC分类号： A61K31/4184 ,  A61K9/107 ,  A61K9/00

    CPC分类号： A61K9/1075 ,  A61K9/0019 ,  A61K9/0095 ,  A61K31/4184

    摘要： Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.

    Parenteral and oral formulations of benzimidazoles
    4.
    发明申请
    Parenteral and oral formulations of benzimidazoles 审中-公开
    苯并咪唑的肠胃外和口服制剂

    公开(公告)号：US20100310611A1

    公开(公告)日：2010-12-09

    申请号：US12802621

    申请日：2010-06-10

    申请人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    发明人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    IPC分类号： A61K31/4184 ,  A61K9/107 ,  A61P33/10 ,  A61P33/12

    CPC分类号： A61K9/1075 ,  A61K9/0019 ,  A61K9/0095 ,  A61K31/4184

    摘要： Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.

    摘要翻译： 本文提供了药物递送系统，例如适合于向对象的肠胃外或口服递送的自 - 纳米乳化药物递送系统，自乳化药物递送系统和胃肠外微乳剂制剂。 药物递送系统可以在微乳液制剂中包含苯并咪唑衍生物，例如甲苯达唑，油，表面活性剂，辅助表面活性剂和偶极非质子溶剂。 还提供了通过使用组合特定乳剂液滴直径的组合物和其中表面活性剂：助表面活性剂的比例来改善治疗病理生理状况期间苯并咪唑衍生物的生物利用度的方法，用于增加苯并咪唑衍生物在肺中的浓度和保留通过 具有约35nm至小于100nm的液滴尺寸的肠胃外可施用的微乳液，并且在通过具有表面活性剂的肠胃外可施用的微乳液的治疗性治疗期间限定苯并咪唑衍生物的溶血安全微乳液：辅助表面活性剂含量为约6％至48％ 。

    Parenteral and oral formulations of benzimidazoles
    5.
    发明申请
    Parenteral and oral formulations of benzimidazoles 有权
    苯并咪唑的肠胃外和口服制剂

    公开(公告)号：US20090048322A1

    公开(公告)日：2009-02-19

    申请号：US12220374

    申请日：2008-07-24

    申请人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    发明人： Diana Shu-Lian Chow ,  Pranav Gupta ,  Yulan Qi ,  Dong Liang

    IPC分类号： A61K31/4184

    CPC分类号： A61K9/1075 ,  A61K9/0019 ,  A61K9/0095 ,  A61K31/4184

    摘要： Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.

    摘要翻译： 本文提供了药物递送系统，例如适合于向对象的肠胃外或口服递送的自 - 纳米乳化药物递送系统，自乳化药物递送系统和胃肠外微乳剂制剂。 药物递送系统可以在微乳液制剂中包含苯并咪唑衍生物，例如甲苯达唑，油，表面活性剂，辅助表面活性剂和偶极非质子溶剂。 还提供了通过使用组合特定乳剂液滴直径的组合物和其中表面活性剂：助表面活性剂的比例来改善治疗病理生理状况期间苯并咪唑衍生物的生物利用度的方法，用于增加苯并咪唑衍生物在肺中的浓度和保留通过 具有约35nm至小于100nm的液滴尺寸的肠胃外可施用的微乳液，并且在通过具有表面活性剂的肠胃外可施用的微乳液的治疗性治疗期间限定苯并咪唑衍生物的溶血安全微乳液：辅助表面活性剂含量为约6％至48％ 。

    Parenteral and oral formulations of benzimidazoles
    7.
    发明授权
    Parenteral and oral formulations of benzimidazoles 有权
    苯并咪唑的肠胃外和口服制剂

    公开(公告)号：US07419996B2

    公开(公告)日：2008-09-02

    申请号：US10640467

    申请日：2003-08-13

    申请人： Diana Shu-Lian Chow ,  Dong Liang

    发明人： Diana Shu-Lian Chow ,  Dong Liang

    IPC分类号： A61K31/4439 ,  A61K31/418

    CPC分类号： A61K9/0019 ,  A61K9/0095 ,  A61K9/1075 ,  A61K31/4184

    摘要： Pharmaceutical compositions of a benzimidazole or a benzimidazole derivative are disclosed. For example, in certain embodiments the pharmaceutical compositions include a benzimidazole, PEG 400, and a dipolar aprotic solvent. In other embodiments, pharmaceutical compositions include a benzimidazole, an oil, a dipolar aproptic solvent, and a surfactant. In certain embodiments, the benzimidazole is mebendezole. The pharmaceutical compositions are formulated for delivery to a subject by any means, and include formulations for oral and parenteral delivery.

    摘要翻译： 公开了苯并咪唑或苯并咪唑衍生物的药物组合物。 例如，在某些实施方案中，药物组合物包括苯并咪唑，PEG400和偶极非质子溶剂。 在其它实施方案中，药物组合物包括苯并咪唑，油，偶极亲和溶剂和表面活性剂。 在某些实施方案中，苯并咪唑是mebendezole。 将药物组合物配制成通过任何方式递送到受试者，并且包括用于口服和胃肠外递送的制剂。