会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 7. 发明申请
    • Solid dosage formulation containing a Factor Xa inhibitor and method
    • 含有因子Xa抑制剂和方法的固体剂量制剂
    • US20050059719A1
    • 2005-03-17
    • US10924043
    • 2004-08-23
    • Sherif BadawyMunir HussainDuxin Sun
    • Sherif BadawyMunir HussainDuxin Sun
    • A61K9/20A61K31/42
    • A61K9/2054A61K31/42
    • An oral solid dosage formulation is provided which contains a Factor Xa inhibitor for which oral bioavailability is not reduced by co-administration of antacids, H2 antagonists and proton pump inhibitors. Such solid dosage formulation includes the Factor Xa inhibitor of the structure, a pharmaceutically acceptable carrier, and an acid component, such as tartaric acid, whereby upon ingestion of the oral solid dosage formulation, the acid component increases solubility of the Factor Xa inhibitor in the local environment of the dissolving solid dosage formulation resulting in an otherwise lower degree of supersaturation of the Factor Xa inhibitor in such environment, than if the acid were not present. The result is that precipitation of the Factor Xa inhibitor in the form of its insoluble free base is minimized during dissolution of the Factor Xa inhibitor thereby increasing its oral bioavailability. A method for enhancing bioavailability of the Factor Xa inhibitor is also provided wherein an acid such as tartaric acid is incorporated with the solid dosage pharmaceutical carrier for the Factor Xa inhibitor.
    • 提供口服固体剂量制剂,其含有通过共同给予抗酸剂,H 2拮抗剂和质子泵抑制剂而不降低口服生物利用度的因子Xa抑制剂。 这种固体剂量制剂包括结构的因子Xa抑制剂,药学上可接受的载体和酸组分,例如酒石酸,由此,在摄取口服固体剂量制剂后,酸组分增加因子Xa抑制剂在 溶解固体剂量制剂的局部环境导致因素Xa抑制剂在这种环境中的过饱和程度低于不存在酸的情况。 结果是在因子Xa抑制剂的溶解过程中,其不溶性游离碱形式的因子Xa抑制剂的沉淀被最小化,从而增加其口服生物利用度。 还提供了用于提高因子Xa抑制剂的生物利用度的方法,其中将诸如酒石酸的酸与用于因子Xa抑制剂的固体剂量药物载体结合。