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热"溶解"挤出卢拉西与天然液体小分子为无形固体分散的基于自组装的亚微米乳液
Peiya Shen1, Enshi Hu1, Chunfeng Zhang2
1School of Pharmacy, China Pharmaceutical University, Nanjing, 211198, P. R. China.
Advanced healthcare materials
|December 5, 2023
概括
一种新型的无形固体分散 (ASD) 使用跨乙醇 (TA) 显著提高了卢拉西 (LUS) 的生物可用性. 这种药物输送系统提高了溶解度,并保持了长时间的超和.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 材料科学 材料科学 材料科学
背景情况:
- 低生物可用性是大约90%的新药候选药物面临的主要挑战.
- 低溶解度和透性显著限制了许多药物的治疗疗效.
- 开发先进的药物输送系统对于克服生物可用性障碍至关重要.
研究的目的:
- 为了研究转乙醇 (TA) 作为无形固体分散 (ASD) 中的一个成分,以改善卢拉西 (LUS) 的生物可用性,其潜力.
- 从LUS-TA-VA64 ASD评估自乳化药物递送系统 (SEDDS) 的形成.
- 评估与商业盐形式相比,开发的LUS-TA-VA64 ASD的体内药理动力学性能.
主要方法:
- 无形固体分散 (ASD) 的制备,其中包括卢拉西 (LUS),跨乙醇 (TA) 和聚1-维尼尔皮罗立-协同乙 (VA64).
- 描述ASD兼容性和自我乳化特性.
- 在体外超和研究以评估药物释放和维持.
- 在口服后对子进行体内药理动力学研究.
主要成果:
- LUS-TA-VA64 ASD显示了更好的组件兼容性,并促进了SEDDS的形成.
- 随着药物水平持续超过24小时,观察到LUS的增强超和.
- 该ASD至少在10小时内表现出稳定的亚微米乳液形成.
- 在子中,ASD显示Cmax和AUC增加了两倍,Tmax增加了1.5倍,与LUS盐相比,AUC的CV显著减少 (59%至26%).
结论:
- 超乙醇 (TA) 有效地提高了在无形固体分散 (ASD) 系统中与VA64.4的卢拉西 (LUS) 的兼容性.
- 开发的LUS-TA-VA64 ASD促进超和,形成稳定的自我乳化药物递送系统 (SEDDS),从而改善了口服生物可用性.
- 这种新的ASD配方代表了一种有前途的策略,用于增强像卢拉西这样的溶解不良药物的治疗效果.
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