在无形固体分散中,酸纤维素甲酸盐和基基甲基纤维素甲酸盐的水解
Jinghan Li1, Dongyue Yu2, Chaowang Zeng1
1Department of Pharmaceutics, College of Pharmacy, University of Minnesota, Minneapolis, MN 55455, USA.
Journal of pharmaceutical sciences
|April 12, 2024
概括
使用像CAP和HPMCP这样的酸性聚合物的无形固体分散 (ASD) 可以降解,形成酸. 这种副产品加速了药物的降解,影响了含有基托可纳 (KTZ) 的配方的稳定性.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 聚合物化学 聚合物化学
背景情况:
- 无形固体分散 (ASDs) 增强了难溶性药物的口服吸收.
- 酸性聚合物,包括纤维素甲酸 (CAP) 和基甲基纤维素甲酸 (HPMCP),是ASD的有效载体.
- 这些聚合物的水解降解已知,但其对ASD稳定性的影响尚未得到充分研究.
研究的目的:
- 为了研究在ASD中CAP和HPMCP的水解.
- 为了确定聚合物水解对装有可纳 (KTZ) 的ASD稳定性的影响.
- 评估药物负载 (10%和50%) 对ASD稳定性的影响.
主要方法:
- 制备含有基托可纳 (KTZ) 的无形固体分散剂 (ASD).
- 在各种温度和湿度条件下进行了60天的稳定性研究.
- 分析技术包括热分析,红外光谱和物理/化学稳定性评估.
主要成果:
- 凯托可纳 (KTZ) 在所有ASD配方中保持物理稳定.
- 晶体酸 (PA) 是水解的副产品,在高温和湿度下在ASD中形成.
- 由PA释放所造成的酸性环境加速了KTZ的化学降解.
结论:
- 纤维素甲酸 (CAP) 和基甲基纤维素甲酸 (HPMCP) 在ASD中容易发生水解降解.
- 甲基酸 (PA) 的形成对药物降解构成风险,特别是对于酸性化合物.
- 了解聚合物水解对于开发稳定的制药配方和改善药物的生物可用性和安全性至关重要.
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