在自乳化药物输送系统中验证的稳定性指示RP-HPLC方法为nirmatrelvir:配方特性和透性增强
Ravi Patel1, Ritu Sharma1, Dignesh Khunt1
1School of Pharmacy, Gujarat Technological University, Gandhinagar, India.
Archiv der Pharmazie
|September 23, 2025
概括
这项研究开发了一种新型的自我乳化药物输送系统 (SEDDS),以改善尼尔马特里尔维尔的口服输送. 经过验证的HPLC方法确保了这种基于脂质的配方中的抗病毒剂的质量评估.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 分析化学 分析化学
背景情况:
- 尼尔马特里尔维尔是一种水溶性较差的抗病毒药物,需要加强口服输送策略.
- 在先进配方中难以溶解的药物的质量评估提出了分析挑战.
研究的目的:
- 开发和描述一种自我乳化药物输送系统 (SEDDS),以改善尼尔马特里尔维尔的口服输送.
- 建立和验证一种稳定性指示HPLC方法,用于在SEDDS中评估Nirmatrelvir的质量.
主要方法:
- 使用Labrafac MC 60,乙醇和Transcutol HP.使用Nirmatrelvir装载的SEDDS的配方.
- 纳米乳液性质的表征,包括滴滴大小,多分散性和传导性.
- 根据ICH指南,开发和验证反相HPLC方法.
- 强制降解研究 (氧化,热,光解,酸性,性) 和降解剂的LC-TQ/MS分析.
主要成果:
- 优化的SEDDS产生了145.23nm的液滴大小和高透射率 (98.97%) 的纳米乳液.
- 与平板电脑相比,SEDDS配方显示Caco-2细胞透率增加了五倍.
- 经过验证的HPLC方法表现出极好的线性 (R2=0.9999),准确性 (98.6%-100.2%) 和精度 (%RSD<0.3%).
- 在氧化,热和光解条件下,涅马特里尔维尔表现出良好的稳定性,在性压力下降解最大.
结论:
- 开发的SEDDS有效地提高了Nirmatrelvir的口服透性,并提供了一个可行的输送策略.
- 经过验证的稳定性指示HPLC方法为基于脂质的配方中Nirmatrelvir的常规质量控制提供了可靠的工具.
- 该研究提供了一个全面的方法来制定配方开发和分析方法验证难溶性药物.
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