用于溶解增强的爱莫丁载体固体分散物的配方,表征和评估
L I Xiuyan1, Luo Yuting1, Wang Jinhui2
1Key Laboratory of Basic and Application Research of Beiyao, Heilongjiang University of Chinese Medicine, Ministry of Education, Harbin 150040, China.
概括
准备-埃莫丁固体分散剂 (AE-SD) 可以提高药物的吸收和生物可用性. AE-SD显示了改善的体内药理动力学和无毒性,为AE药物开发提供了一种新的方法.
科学领域:
- 药理学和制药学 药理学和制药学
- 药物输送系统 药物输送系统
- 自然产品化学 自然产品化学
背景情况:
- -埃莫丁 (AE) 是一种具有治疗潜力的天然化合物.
- 提高AE的可溶性和生物利用性对于其临床应用至关重要.
- 固体分散技术为提高药物输送提供了一个有前途的战略.
研究的目的:
- 使用各种载体制备-埃莫丁固体分散剂 (AE-SD).
- 描述AE-SD的物理状态和溶解特性.
- 与AE悬浮剂相比,评估AE-SD的体内药理动力学和毒理学概况.
主要方法:
- 通过使用PEG-6000,PVP-K30和poloxamer进行溶剂蒸发/化来制备AE-SD.
- 使用TGA,XRD,DSC,FTIR和SEM进行表征.
- 通过溶解研究优化AE-SD配方.
- 在体内进行的药理动力学分析和小鼠的急性毒性评估.
主要成果:
- 聚乙烯罗利 (PVP) 有效抑制了AE结晶,在AE-SD中促进了无形状态.
- 最佳的AE-PVP-POL比率 (1:2:2) 产生了优异的溶解.
- 与AE悬浮剂相比,AE-SD显示了更快的吸收,更高的Cmax,并减少了t1/2和平均停留时间.
- 无论是AE还是AE-SD都没有显著的毒性.
结论:
- 固体分散显著提高了-埃莫丁的溶解性和体外溶解.
- AE-SD 改善了-埃莫丁的体内生物可用性.
- 这项研究提供了一种新的策略,用于开发有效的-埃莫丁配方.
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