同时喷雾干燥的马西坦-塔达拉菲尔与氨酸微粒用于肺动脉高血压中可吸入的输送
Chang-Soo Han1, Jin-Hyuk Jeong1, Hyeon Woo Moon1,2
1Department of Pharmacy, Chungbuk National University, Cheongju 28644, Republic of Korea.
这项研究开发了一种吸入的macitentan-tadalafil粉末用于肺动脉高血压,改善药物输送到肺部并减少全身暴露. 优化的配方增强了PAH患者的治疗结果.
科学领域:
- 制药技术 制药技术 制药技术
- 药物运输 药物运输 药物运输
- 呼吸系统医学 呼吸系统医学
背景情况:
- 肺动脉高血压 (PAH) 需要联合治疗.
- 口服组合疗法可能导致全身副作用.
- 肺部药物输送提供了一个有针对性的方法.
研究的目的:
- 为了开发一个macitentan (MAC) -tadalafil (TAD) 干粉吸入制剂.
- 为了增强肺部输送和减少全身暴露.
- 为了研究PAH治疗的悬浮式喷雾干燥.
主要方法:
- 对MAC-TAD复合粉末的联合喷雾干燥.
- 优化MAC:TAD比率和L-氨酸含量的优化.
- 颗粒大小分析,气溶性能和结晶性评估.
主要成果:
- 喷雾干燥配方显示出更好的颗粒均性和更高的排放剂量.
- 含25%L-氨酸的M2-T8配方显著增加了两种药物的细颗粒剂量.
- 在干燥后,MAC和TAD的结晶性保持不变.
结论:
- 基于悬浮的喷雾干燥对于创建统一的MAC-TAD吸入式配方是有效的.
- 优化的2:8配方与25%的L-氨酸显示出优异的肺沉积.
- 这种吸入疗法对PAH治疗具有前景.
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