通过高压均质化,设计微型和纳米型制药盐晶体
Md Sadeque Hossein Mithu1, Saumil Bhatt1, Vivek Garg2
1Cubic Pharmaceuticals Ltd., Unit 3, Neptune Close, Medway City Estate, Rochester, Kent ME2 4LU, UK.
International journal of pharmaceutics
|February 5, 2026
概括
高压均质化 (HPH) 为制造制药盐提供了一种可持续的方法. 这种技术可以显著减少颗粒大小和增强药物溶解,改善药物配方.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 化学工程是化学工程的重要组成部分.
背景情况:
- 制药盐的传统结晶方法可能是低效和环境负担.
- 开发可扩展和可持续的合成路径以改善药物输送至关重要.
研究的目的:
- 研究高压均质化 (HPH) 作为一种新的,绿色的制造技术,用于制药盐合成.
- 描述所产生的盐,并评估它们的溶解性能.
主要方法:
- 利用高压均质化 (HPH) 形成盐,使用可纳 (KTZ) 和酸 (OA) 与各种稳定剂.
- 采用X射线粉碎衍射 (XRPD),FT-IR光谱和扫描电子显微镜 (SEM) 进行结构和形态分析.
- 在pH值4.4进行溶解研究,以评估药物释放概况.
主要成果:
- 通过HPH成功合成了新的KTZ:OA制药盐,通过XRPD和FT-IR证实了这一点,表明了质子转移和结合.
- 通过控制晶体形态,通过稳定剂度和温度可调节,实现了显著的颗粒大小减小到次微米范围.
- 与散装KTZ相比,HPH加工的盐在15分钟内释放高达80%的药物,证明了大幅改善的溶解率.
结论:
- 高压均质化 (HPH) 是一种多功能,无溶剂和连续制造平台,用于生产高纯度的制药盐.
- 在HPH加工过程中,可以获得卓越的溶解性能,为固态药物配方提供了改造性的方法.
- 该方法为制药开发中的传统结晶技术提供了一个可扩展和环境可持续的替代方案.
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