波萨可纳的水中介相变:一个复杂的林的晶体形式
Matteo Guidetti1, Rolf Hilfiker2, Martin Kuentz3
1Solvias AG, Solid-State Development Department, Römerpark 2, Kaiseraugst CH- 4303, Switzerland; Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Campusvej 55, Odense 5230, Denmark.
概括
波萨可纳 (Posaconazole) 是一种可靠的药物.
科学领域:
- 固态化学 固态化学
- 制药科学 制药科学
- 药物的配方 药物的配方
背景情况:
- 波萨可纳具有广泛的多态性,有14种已报告的晶体形式.
- 了解固态特性和稳定性对于药物开发和防止相变是至关重要的.
- 关于波萨可纳多态的稳定性关系的知识有限.
研究的目的:
- 描述波萨可纳的多态,水合物和溶解物.
- 为了研究水性悬浮中的固体相变化.
- 在各种条件下确定最稳定的固体形式.
主要方法:
- 粉末X射线衍射 (PXRD) 是一种方法.
- 动态蒸汽吸附 (DVS) 是一种
- 光谱和热技术的使用.
- 拉曼显微镜用于水性悬浮液.
主要成果:
- 在市场上销售的口服悬浮液中存在的S形式并不是水中最稳定的形式.
- 在水中,S型在两周内转化为更稳定的水合物 (A型).
- 商业配方中的80聚酸盐阻止了这种转化.
结论:
- 市场上市的口服悬浮液的稳定性依赖于聚酸盐 80,以防止从S型转换为A型.
- 辅助剂对固态稳定性的作用对于制药配方至关重要.
- 这项研究为Posaconazole配方开发提供了重要的见解.
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