罗拉塔丁的语言下快速溶解薄膜:表征,体外和活体评估
Yahya Alhamhoom1, Ashitha Kakarlapudi Said2, Avichal Kumar2
1Department of Pharmaceutics, College of Pharmacy, King Khalid University, Al Faraa, Abha 62223, Saudi Arabia.
Polymers
|October 26, 2024
概括
开发了洛拉塔丁 (LOR) 和酸共同形态系统的新型语言下膜. 这些快速溶解的薄膜旨在改善洛拉塔丁的生物利用性,并通过绕过第一通代谢来加快其治疗效果.
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:
- 洛拉塔丁 (LOR) 是第二代抗胰岛素,其口服生物利用率较低 (10-40%),并且由于溶解性差和广泛的第一通代谢,发病时间延迟.
- 临床需要改善洛拉塔丁配方,以提供更快的治疗效果和更好的生物可用性.
- 同形态系统和新型传递路线是克服这些局限性的潜在策略.
研究的目的:
- 为了开发loratadine-酸共同形态系统 (LOR-CA) 的语言下快速溶解的薄膜.
- 为了提高洛拉塔丁的生物可用性,并实现更快的起作用.
- 优化配方参数,以有效地进行语言下药物输送.
主要方法:
- 语言下快速溶解的LOR薄膜是使用电影造技术来制定的.
- 使用了性聚合物 (HPMC E15,PVP K30,HPC-EF),酸 (pH调节器) 和糖 (可塑剂).
- 描述包括FTIR,SEM,DSC,XRD,体外溶解和体外粘膜粘附研究.
主要成果:
- 优化的配方 (F1) 使用HPMC E15,甘油和酸,表现出理想的物理特性 (光滑,透明,灵活) 和良好的粘粘度 (11.27 ± 0.418 gm/cm2).
- 配方F1显示显著缩短了30.30±0.6秒的分解时间 (DT).
- 观察到LOR的快速释放,在60分钟内释放了92.10 ± 2.3%,明显优于其他配方 (ANOVA,p < 0.001).
结论:
- 开发的LOR-CA系统的语言下快速溶解膜显示了更快的治疗效果的潜力.
- 这种配方策略可以有效地绕过第一通代谢,从而改善洛拉塔丁的生物可用性.
- 舌下输送提供了一个有希望的替代方案,可以提高像洛拉塔丁这样生物可用性较差的药物的疗效.
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