使用瑞特维尔德方法通过粉末X射线衍射对梅本达A型和C型悬浮的固态稳定性的定量分析和评估
Julian Ticona Chambi1, Livia Deris Prado2, Beatriz Ferreira de Carvalho Patricio3
1Instituto de Ciência e Tecnologia (ICT), Universidade Federal de São Paulo (UNIFESP), Brazil.
International journal of pharmaceutics
|December 18, 2023
概括
梅本达 (MBZ) 悬浮剂从C型转化为A型,从而影响治疗效果. 一种新的定量方法准确地追踪了这种转变,这对于制药稳定性研究至关重要.
科学领域:
- 制药科学 制药科学
- 固态化学 固态化学
- 材料科学 材料科学 材料科学
背景情况:
- 梅本达 (MBZ) 是一种重要的抗寄生虫药物,有三种已知的固态形式 (A,B,C).
- 这些形式表现出明显的溶解率,显著影响治疗结果.
- 形式A的存在率超过30%,使得该配方无效,类似于安慰剂.
研究的目的:
- 开发一种可靠的定量方法来分析悬浮中的梅本达 (A和C形式).
- 在制药工业条件下研究MBZ悬浮物的固态稳定性和转化动力学.
主要方法:
- 开发和验证MBZ悬浮剂的干燥过程和定量方法.
- 用于数据收集的粉末X射线衍射 (PXRD).
- 瑞特维尔德方法 (RM) 和托帕斯软件用于固体形式量化; 动力分析的阿弗拉米方程.
主要成果:
- 结合干燥和量化方法在MBZ悬浮稳定性研究中被证明是非常准确的.
- 在加速和长期条件下,即使是1%的A表在1-2个月内启动了超过30%的转换 (C表到A表).
- 完整的转化发生在6-9个月内,远远短于产品的保质期.
结论:
- 成功建立了一种可靠的方法来量化悬浮中的MBZ形式A和C.
- 这项研究强调了MBZ悬挂中的快速固态转化,需要仔细控制.
- 该方法可用于监测和防止梅本达和其他活性药物成分 (API) 中不良的固态转化.
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