开发一种即时释放配方,在各种饮食中可靠地吸收里瓦罗克萨班
Jan Bosák1, Martin Šíma2, Tereza Krejčí1
1Zentiva, k.s., Prague, Czech Republic.
Clinical and translational science
|May 13, 2024
概括
新的里瓦洛克萨班配方消除了食物效应,确保了可靠的药物吸收. 这项创新旨在改善患者对抗凝血剂治疗的坚持和治疗结果.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
- 临床药房 临床药房
背景情况:
- 利瓦洛克萨班的生物可用性,特别是在较高剂量 (15-20毫克) 中,在空腹服用时显著降低,可能会损害抗凝剂的有效性.
- 目前的建议建议与食物一起服用更高剂量的里瓦罗克萨班,但这种剂量要求可能会成为患者遵守药物的障碍.
- 开发减轻食物影响的配方对于药物持续吸收和改善治疗结果至关重要.
研究的目的:
- 评估旨在消除食物对药物的生物可用性影响的创新利瓦洛克萨班配方.
- 为了确保可靠的药物吸收,并提高患者对抗凝血剂治疗的坚持.
- 为了比较新型里瓦洛克萨班原型与参考产品的生物可用性和食品效应.
主要方法:
- 开发了三种含有里瓦罗克萨班的原型:Cocrystal,HPMCP和Kollidon.
- 在人类受试者中进行开放标签,随机,单剂口服,交叉研究.
- 在禁食和食条件下给药试验产品,在食条件下给药参考产品,以评估生物可用性和食物效应.
主要成果:
- 所有测试的里瓦洛克萨班原型在食和禁食条件下都显示出可比的生物利用性.
- 度-时间曲线下的面积的几何平均比率的90%置信区间处于标准可接受范围 (80.00%-125.00%).
- 开发的配方有效地消除了食物对利瓦洛克萨班吸收的影响.
结论:
- 成功开发了一种创新的即时释放的里瓦罗克萨班配方,它对生物可用性没有食物影响.
- 这一进步是改善患者对利瓦洛克萨班治疗的坚持性的重要一步.
- 新配方有可能提高治疗结果并降低整体医疗保健成本.
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