有机酸对piracetam固态多态相变的作用
Fanfan Fan1, Shuyuan Xu1, Minshan Guo1
1State Key Laboratory of Natural Medicines, Department of Pharmaceutics, College of Pharmacy, China Pharmaceutical University, Nanjing 211198, China.
International journal of pharmaceutics
|October 23, 2023
概括
含量低的有机酸可以抑制皮拉 (PCM) 的相转换,这是一种诺托普药物. 酸和三碳酸有效地阻止了在PCM中的转基因稳定形式I到稳定形式II的转化.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 物理化学 物理化学
背景情况:
- 转移性多态体对于改善口服药物吸收至关重要,特别是对于水溶性较差的化合物.
- 固体相从变态稳定转变为稳定的多态体,在制药开发和质量控制方面带来了重大挑战.
研究的目的:
- 为了研究低含量的有机酸对piracetam (PCM) 固态多态相变化的影响.
- 了解特定有机酸在控制转移稳定的药物形式稳定性的作用.
主要方法:
- 对piracetam (PCM) 多态相转换的实验分析.
- 添加各种有机酸的低度 (1 mol%):酸 (CA),三碳酸 (TA),谷氨酸 (GA) 和酸 (AA).
- 分子模拟以阐明有机酸和PCM晶体之间的相互作用机制.
主要成果:
- 酸 (CA) 和三碳酸 (TA) 显著抑制了piracetam的I形式到II形式的相变.
- 谷氨酸 (GA) 和酸 (AA) 在多态转化过程中表现出较小的影响.
- 分子模拟显示有机酸分子吸附到PCM形式I晶体表面,阻碍分子运动.
结论:
- 含量低的有机酸,特别是CA和TA,可以有效地控制piracetam的固态多态稳定性.
- 有机酸在晶体表面的吸附是抑制相变的关键机制.
- 这项研究提供了有价值的见解,用于制定策略,以提高转移稳定的制药配方的稳定性.
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