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一种集成的节约材料的方法,用于确定直接压缩片填充剂的稀释潜力
Weeraya Tharanon1, Yiwang Guo2, Jomjai Peerapattana1
1Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Journal of pharmaceutical sciences
|December 25, 2025
概括
这项研究引入了一种新的,节约材料的方法,以评估联合加工的粘性大米粉 (CP-GRS) 作为直接压缩填充剂的"稀释潜力". 该方法成功地确定了乙氨基和布洛芬的最佳药物负载,确保了药片的质量和可制造性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 化学工程是化学工程的重要组成部分.
背景情况:
- 直接压缩 (DC) 药片配方需要具有最佳流动性和紧缩性的填充剂.
- 了解这个问题的理解
- 稀释潜力的稀释潜力
- 填充剂的使用对于在不同的API和装载中保持一致的平板电脑质量和可制造性至关重要.
研究的目的:
- 开发和验证一种综合的,节约材料的实验室规模的方法,用于评估共同加工的粘性大米粉 (CP-GRS) 的稀释潜力.
- 评估CP-GRS作为使用乙氨基 (APAP) 和布洛芬 (IBN) 作为模型药物的DC平板电脑填充剂.
主要方法:
- 开发了一种综合实验室规模的方法来评估填充剂稀释潜力.
- 基于易碎性 (<1%的体重损失),分解时间 (DT <15分钟) 和相对于微晶纤维素 (Avicel® PH102) 的流动性来评估药片的性能.
- 在临界压力 (Pc) 时确定最大的API负载,以定义稀释潜力.
主要成果:
- 颗粒型APAP (gAPAP) 在CP-GRS中在240MPa时负载高达34%.
- 精细的APAP负载在143-288MPa范围内达到20%.
- 布洛芬 (IBN) 在115-150MPa之间实现了40%的负载.
结论:
- 综合方法有效地评估了CP-GRS稀释潜力,证实了其作为DC填充剂的适用性.
- 这种节约材料的方法通过快速优化DC配方,促进了早期药物开发.
- 该方法在APAP和IBN的成功表明该方法对各种API具有广泛的适用性.
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