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量化粉糖酸的交叉结合强度及其对药片分解和溶解的影响
Pauline H M Janssen1, Willem Rijpkema2, Kathleen Stout2
1Department of Pharmaceutical Technology and Biopharmacy, University of Groningen, Antonius Deusinglaan 1, 9713 AV Groningen, the Netherlands; DFE Pharma, Klever Strasse 187, 47568 Goch, Germany.
了解基于粉的品种 (SSG) 的交叉链强度是强大的口服药物配方的关键. 与交叉连接相比,交叉连接提供了更高的稳定性和更快的药物溶解.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
背景情况:
- 开发强大的口服固体剂型需要了解影响性能和稳定性的变化,并与设计质量 (QbD) 保持一致.
- 这需要深入了解原材料特性,工艺参数和最终产品质量之间的相互作用.
研究的目的:
- 提出一种方法来量化基于粉的品种 (SSG) 中的交叉连接 (SXL) 的强度.
- 评估不同类型的交叉链 (与) 对SSG稳定性和药物溶解的影响.
主要方法:
- 通过比较性暴露前后的降水沉积物体积来量化SXL.
- 评估使用SSG与和交叉链接的配方的药片分解和阿提诺洛尔溶解.
主要成果:
- 具有交叉连接的SSG表现出较高的SXL (≈1) 和比具有交叉连接 (SXL 0.4-0.7) 的SSG更强的抗水解能力.
- 含交联SSG的配方在25分钟内实现了80%的阿提诺洛溶解,而交联SSG需要超过45分钟.
- 在SXL和药物溶解时间之间发现了强烈的相关性.
结论:
- 在SSG中交叉链的类型是影响药物溶解成功的关键属性.
- 量化SXL支持制剂商开发符合QbD原则的强大的配方.
- 使用含交叉链的SSG可提高配方的抗压强度,降低产品故障风险.
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