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

    IPC分类号: A61K31/4184 A61P35/00

    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。

    TRANSORAL DOSAGE FORMS COMPRISING SUFENTANIL AND NALOXONE
    2.
    发明申请
    TRANSORAL DOSAGE FORMS COMPRISING SUFENTANIL AND NALOXONE 审中-公开
    包含SUFENTANIL和NALOXONE的转运剂型

    公开(公告)号:US20100010031A1

    公开(公告)日:2010-01-14

    申请号:US12449292

    申请日:2008-02-08

    IPC分类号: A61K31/4535 A61K31/485

    摘要: The invention pertains to methods that include administering to a subject a transoral dosage form comprising a pharmaceutical carrier and sufentanil, and maintaining a mean pH ranging from about 3.5 to about 5.5 during a dosing period after administration of the transoral dosage form as determined using an in vitro donor media test. Related dosage forms are also disclosed. Also disclosed are transoral dosage forms and related methods, wherein a transoral dosage form may comprise: (1) about 5 to about 1000 micrograms of sufentanil; (2) about 50 micrograms to about 100 milligrams of naloxone; and (3) acidifying material in an amount sufficient to provide a mean pH ranging from about 3.5 to about 5.5 during a dosing period after administration of the transoral dosage form as determined using an in vitro donor media test; wherein the dosing period begins no earlier than about 1 minute after administration of the transoral dosage form, and ends no later than about 120 minutes after administration of the transoral dosage form.

    摘要翻译: 本发明涉及包括向受试者施用包含药物载体和舒芬太尼的经口给药形式的方法,并且在给予经口给药后的给药期间保持约3.5至约5.5的平均pH,所述给药期间使用 体外供体介质试验。 还公开了相关的剂型。 还公开了经口给药剂型和相关方法,其中经口剂型可包含:(1)约5至约1000微克的舒芬太尼; (2)约50微克至约100毫克的纳洛酮; 和(3)足量的酸化材料,其在施用经口给药形式后的给药期间提供约3.5至约5.5的平均pH,使用体外供体培养基测试确定; 其中给药期在给予经口给药后不早于约1分钟开始,并且在给予经口给药后不迟于约120分钟结束。

    In vitro predictive method
    3.
    发明申请
    In vitro predictive method 审中-公开
    体外预测方法

    公开(公告)号:US20060031021A1

    公开(公告)日:2006-02-09

    申请号:US11195894

    申请日:2005-10-24

    IPC分类号: G01N33/48

    CPC分类号: A61K49/0004 G01N33/15

    摘要: An in vitro method for predicting in vivo pharmacokinetic parameters such as Cmax for poorly soluble drug compounds in formulations.

    摘要翻译: 用于预测制剂中难溶性药物化合物的体内药代动力学参数例如C max max的体外方法。

    Method for increasing the bioavailability of metaxalone
    5.
    发明授权
    Method for increasing the bioavailability of metaxalone 有权
    增加metaxalone生物利用度的方法

    公开(公告)号:US06407128B1

    公开(公告)日:2002-06-18

    申请号:US09998206

    申请日:2001-12-03

    IPC分类号: A61K3142

    CPC分类号: A61K31/421

    摘要: A method of increasing the bioavailability of metaxalone by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of metaxalone in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food.

    摘要翻译: 提供了一种通过给予口服剂型与食物来提高美他沙酮的生物利用度的方法,以及包含口服剂型的美他沙酮在合适的容器中并与印刷标签相关联的制品,其描述了增加的生物利用度 用食物在容器中服药。

    Methods of using metaxalone in the treatment of musculoskeletal conditions
    6.
    发明授权
    Methods of using metaxalone in the treatment of musculoskeletal conditions 有权
    使用美沙酮治疗肌肉骨骼病症的方法

    公开(公告)号:US06683102B2

    公开(公告)日:2004-01-27

    申请号:US10104044

    申请日:2002-03-25

    IPC分类号: A61K3142

    CPC分类号: A61K31/421

    摘要: A method of increasing the bioavailability of metaxalone by administration of an oral dosage form with food is provided, as well as an article of manufacture comprising an oral dosage form of metaxalone in a suitable container and associated with printed labeling which describes the increased bioavailability of the medication in the container when taken with food.

    摘要翻译: 提供了一种通过给予口服剂型与食物来提高美他沙酮的生物利用度的方法,以及包含口服剂型的美他沙酮在合适的容器中并与印刷标签相关联的制品,其描述了增加的生物利用度 用食物在容器中服药。