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拉洛西芬HCl - 纳林因共形系统:制备,表征和药理动力学研究

Navya Sree Kola Srinivas¹, Dani Lakshman Yarlagadda¹, Brahmam Bheemishetty²

¹Department of Pharmaceutical Quality Assurance, Manipal College of Pharmaceutical Sciences, Manipal Academy of Higher Education, Manipal, Karnataka 576104, India.

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

|February 17, 2025

概括

共同形态系统 (CAMs) 增强了像Raloxifene HCl (RLX) 这样的难以溶解药物的可溶性和生物利用性. 这项研究表明RLX与Naringin (NRG) 结合,显著提高了药物的性能.

科学领域:

制药科学制药科学
药物输送系统药物输送系统
物理化学物理化学

背景情况:

低水溶性影响约90%的NCE和40%的批准药物,限制了口服生物可用性.
拉洛西芬HCl (RLX) 是一种BCSII类药物,由于溶解性差 (0.5μg/mL) 和通过CYP3A4和P-glycoprotein (P-gp) 进行广泛的系统前代谢,其口服生物利用率低 (2%) .
纳林 (NRG) 是一种天然化合物,作为CYP3A4和P-gp的抑制剂,为药物配方提供了潜在的协同方法.

研究的目的:

探索拉洛西芬HCl (RLX) 与纳林因 (NRG) 的共同形态化,以提高RLX的溶解性和生物可用性.
研究由此产生的共同形态系统 (CAM) 的分子相互作用和固态特性.
评估RLX-NRG CAMs的增强溶解性,药物释放和体内药理动力学特征.

主要方法:

使用溶剂蒸发技术制备RLX和NRG的同形系统 (CAM).
进行了固态表征,以分析分子水平的变化.
进行了溶解性,药物释放性,ex vivo透性和体内药理动学的研究.

主要成果:

与单独使用RLX相比,RLX-NRG CAM显示可溶性增加了3.5倍.
活体透研究显示增强了10倍,而体内研究显示Cmax增加了8.1倍,AUC增加了2.8倍.
这些改善表明RLX的口服生物可用性在配制为CAM与NRG时显著提高.

结论:

使用Naringin的同形化是一种可行的策略,可以克服Raloxifene HCl.的可溶性和生物可用性不佳的挑战.
开发的RLX-NRGCAM表现出卓越的药理动力学特性,这表明它有可能成为改善分子水平药物性能的平台技术.

关键词:

同形态系统是同形态系统.玻璃过渡温度是玻璃过渡温度.液体液相分离器液体液相分离器纳林丁 (Naringin) 是一个名为"纳林丁"的东西.拉洛西芬 HCl 的含量固体分散的分散方式

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