普里马昆酸盐的口味掩饰:对三种口味掩饰剂的比较评估
Galande Ankit1, Gagare Tejashree1, Sahu Surbhi1
1Shree Chanakya Education Society, Indira College of Pharmacy, Tathawade, Pune, Maharashtra, 411033, India.
AAPS PharmSciTech
|June 11, 2025
概括
通过使用离子交换树脂和Eudragit E 100实现了原酸 (PMQ) 的味道掩饰. 由此产生的口服分解片 (ODT) 为疟疾治疗提供了可口的选择,特别是对于儿科和老年患者.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 药用化学 医学化学
背景情况:
- 普里马基因酸盐 (PMQ) 对于治疗复发性疟疾至关重要,但具有强烈的苦味,限制了患者的遵守.
- 开发可口的剂量形式对于有效的疟疾治疗至关重要,特别是在脆弱人群中.
研究的目的:
- 开发原酸 (PMQ) 的口味掩饰配方,以提高口感.
- 评估不同口味掩饰技术的有效性及其对药物释放的影响.
- 为患者接受,制定和评估口服分解片 (ODT).
主要方法:
- 使用各种方法 (摇动瓶,共同研磨,,共同蒸发,喷雾干燥) 将PMQ与阴离子交换树脂 (AmberLiteTM IRP 64,69,88) 和基贝塔环氧 (HPBCD) 复合.
- 用Eudragit E 100 (E 100) 制备PMQ的固体分散物,通过喷雾干燥.
- 在酸性和中性pH条件下的体外药物释放研究,以及模拟的唾液液 (SSF).
- 选定的复合材料的配制成ODT和随后的人类面板味道评估.
主要成果:
- 喷雾干燥的PMQ-HPBCD复合物,PMQ-IER 69 (1:2) 复合物和PMQ-E100 (1:4) 分散物在SSF和酸性介质中显示出不同的药物释放特征.
- 用PMQ-E100分散剂配制的ODT显示最可接受的味道,其次是PMQ-IER 69 (2) 复合物和PMQ HPBCD复合物.
- 在酸性条件下,以分散为基础的PMQ-E100ODT在1小时内释放了超过85%的药物,确保了治疗疗效.
结论:
- 味道掩盖的普里马基因酸盐配方,特别是使用Eudragit E 100分散剂,显著提高了口感.
- 基于分散的PMQ-E100 ODT是一种有前途的方法,可以提高患者对疟疾治疗的遵从性.
- 这些ODT特别适用于对苦味敏感的儿科和老年人群.
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