蒂莫金的自化固体分散,具有增强的生物制药和脏保护作用
Shimul Halder1, Sanjida Afrose1, Manik Chandra Shill2
1Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Dhaka, Dhaka, Bangladesh.
Drug delivery
|April 9, 2024
概括
这项研究开发了一种自化固体分散 (SMSD) 的Thymoquinone (TQM) 从Nigella sativa种子. 在SMSD显著提高了TQM的SMSD显著提高了TQM.
科学领域:
- 药理学和制药学 药理学和制药学
- 自然产品化学 自然产品化学
- 腎臟病學 (nephrology) 是一種醫學.
背景情况:
- 提摩 (TQM) 是来自尼格拉三草的关键植物营养素,具有潜在的脏保护性质,但具有较差的生物制药特性.
- 提高TQM的溶解度和生物可用性对于其治疗疗效至关重要.
- 自化固体分散剂 (SMSD) 是一种有前途的方法,可以提高难溶性化合物的输送.
研究的目的:
- 开发和优化Thymoquinone (TQM) 的自化固体分散 (SMSD),以改善其生物制药性质和脏保护功能.
- 评估开发的SMSD-TQM的物理化学特征,溶解特征,药理动力学行为和体内神经保护疗效.
- 调查SMSD-TQM在克服TQM生物制药局限性的潜力.
主要方法:
- 根据TQM表面溶解度选择合适的两性聚合物 (Soluplus®).
- 使用溶剂蒸发和冷干燥技术制备SMSD-TQM配方,具有不同的TQM负载 (5-15%).
- 优化和全面评估SMSD-TQM,包括颗粒大小,形态,溶解,大鼠的药理动力学,以及在西斯普拉丁诱导的急性损伤小鼠模型中的脏保护作用.
主要成果:
- 通过SMSD-TQM,TQM在水中的溶解得到了显著改善,在60分钟内释放了97.8%.
- 在老鼠中,口服SMSD-TQM导致系统性暴露增加4.9倍,与晶体TQM相比.
- 通过改善脏生物标志物和减少组织学损伤,SMSD-TQM显著增强了TQM在西斯普拉丁诱导的急性损伤小鼠模型中的脏保护作用.
结论:
- 开发的自化固体分散剂 (SMSD) 有效地提高了thymoquinone (TQM) 的溶解和口服生物可用性.
- SMSD-TQM表现出显著的脏保护作用,表明其作为改善脏保护的治疗剂的潜力.
- 这种配方策略成功克服了TQM固有的生物制药局限性,为其增强的临床应用铺平了道路.
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