开发一种基于Hydroxypropyl-β-Cyclodextrin的液体配方,用于在儿科治疗中口服Propranolol
Marzia Cirri1, Paola Mura1, Simona Benedetti2
1Department of Chemistry Ugo Schiff (DICUS), University of Florence, 50019 Sesto Fiorentino, Italy.
Pharmaceutics
|September 28, 2023
概括
这项研究开发了一种稳定且可口味的口服普拉诺醇 (PPN) 溶液,用于使用环氧德克斯特林复合剂的儿童. 基基β-环极 (HPβCD) 增强了PPN对光的稳定性和改善了味道,解决了关键的配方挑战.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 儿科配方 儿科配方 儿科配方
背景情况:
- 醇 (PPN) 对儿科心血管疾病至关重要,但现有的制剂面临稳定性和食感性问题.
- 临时的PNP制剂缺乏稳定性和质量控制,需要改进的配方.
- 目前的挑战包括PPN的光敏感性,pH不稳定性,苦味,以及避免有毒辅助剂的必要性.
研究的目的:
- 开发一种安全,稳定和可口的口服儿科普拉诺洛尔溶液.
- 为了利用循环德克斯特林复合来克服PPN配方障碍.
- 为了提高PPN的稳定性,味道和整体适合儿科使用.
主要方法:
- 选各种环极素 (CDs) 以确定最佳的复合剂.
- 根据复杂化效率和安全性选择基基β-环氧化 (HPβCD).
- 制备PPN-HPβCD物理混合物和共同接地系统 (1:1或 1:2 mol:mol) 用于0.2% w/v 溶液.
- 使用电子舌头测试评估光稳定性,储存稳定性 (6个月和加快条件) 和口感.
主要成果:
- HPβCD显示出显著的光保护作用,在紫外线照射下降低PPN降解率高达75%.
- PPN-HPβCD溶液在室温和加速条件下 (40°C) 在6个月内保持了物理化学性质和药物度.
- 电子舌头测试证实HPβCD的口味掩饰能力,减少30%的感知苦味.
结论:
- 循环德克斯林复合,特别是HPβCD,提供了一个可行的策略,用于创建稳定和可口的儿科普拉诺洛尔口服溶液.
- 开发的配方解决了关键的稳定性 (光,pH) 和食感问题,可能取代不稳定的临时制剂.
- 这种方法提高了在儿科患者中使用普拉诺洛尔的安全性和疗效.
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