通过包括复杂和固体分散技术来提高BCSII类拉洛西芬化的生物可用性
Jimishaben D Kher1,2, Kishorkumar Sorathia3
1Research Scholar, Faculty of Pharmacy, Dharmsinh Desai University, Nadiad, Gujarat, India.
概括
这项研究使用β-环氧德 (β-CD) 复合增强了拉洛西芬化 (RLX) 的溶解性,达到9倍的增加. 在改善RLX生物可用性方面,β-CD方法比固体分散更有效.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
背景情况:
- 拉洛西芬化 (RLX) 由于广泛的第一通代谢和较低的水溶性 (BCS II类) 而表现出较差的口服生物利用率 (2%).
- 有效的骨质疏松症治疗需要提高RLX溶解度和生物可用性.
研究的目的:
- 为了提高拉洛西芬化 (RLX) 的溶解性和生物可用性.
- 使用β-cyclodextrin (β-CD) 和使用Poloxamer 407.7的固体分散物来制备一个包含复合物.
主要方法:
- 通过,共同沉和物理混合来制备RLX纳入复合物和固体分散物.
- 药物与载体比率的优化 (1:1, 1:2, 1:3).
- 使用X射线衍射 (XRD),微分扫描热度计 (DSC) 和里埃变换红外光谱法 (FTIR) 的表征.
主要成果:
- 共同沉方法产生了一个包含复合物,RLX水溶性增加了9倍.
- XRD和DSC分析证实RLX从结晶状态转变为无形状态.
- 与固体分散相比,Beta-cyclodextrin复合表现出优异的可溶性增强.
结论:
- 贝塔-环氧德克斯复合是一种高效的策略,可以提高拉洛西芬化的可溶性.
- 在优化复合体 (IC-6) 中实现的无形状态有助于增强溶解度.
- 这种方法为改善RLX在骨质疏松症治疗中的生物利用性提供了一个有希望的方法.
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