使用L-氨酸和热挤出方法制备和评估可吸入的微粒,以提高空气动力学性能和分散性
Jin-Hyuk Jeong1, Ji-Su Kim1, Yu-Rim Choi1
1Department of Pharmacy, Chungbuk National University, Cheongju 28644, Republic of Korea.
Pharmaceutics
|June 27, 2024
概括
氨酸改善了干粉吸入器的热挤出配方,提高了药物的分散性和空气动力学性能,以有效地传递深肺.
科学领域:
- 制药技术 制药技术 制药技术
- 材料科学 材料科学 材料科学
背景情况:
- 干粉吸入器 (DPI) 面临着由于粉末聚合和流动性差,影响药物输送的配方挑战.
- 在DPI中实现均和稳定的药物分散对于有效的肺部注射至关重要.
研究的目的:
- 研究L-氨酸 (LEU) 纳入热挤出 (HME) 的协同效应,以提高可吸入微粒的分散性和空气动力学性能.
- 评估不同LEU比率对伊特拉科纳 (ITZ) 溶解度,配方均性和颗粒特性的影响.
主要方法:
- 采用联合喷气削和HME然后喷气削来创建ITZ和LEU配方.
- 纳入了不同的LEU比率,以评估它们对关键配方参数的影响.
- 测量了溶解度,结晶度,接触角度,质量中介气动直径 (MMAD) 和超细粒子分数 (eFPF).
主要成果:
- HME加工增加了ITZ的溶解度,并降低了其结晶度.
- 较高的LEU比率显著降低了配方的接触角度.
- 通过增加LEU含量,观察到MMAD和空气动力学性能的协同增强,达到33.68±1.31%的最大eFPF.
结论:
- 热挤出与L-氨酸相结合是一种有效的策略,用于生产具有更好的分散性和空气动力学特性的可吸入微粒.
- 这种方法有望克服DPI的配方挑战,并确保稳定的深肺药物输送.
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