热挤出无形固体分散的溶解-透,包括HPMCAS的实验等级
Hironori Tanaka1, Tetsuya Miyano2, Hiroshi Ueda3
1Formulation R&D Laboratory, Shionogi & Co., Ltd., Hyogo 660-0813, Japan.
ADMET & DMPK
|October 13, 2023
概括
基甲基纤维素酸糖酸盐 (HPMCAS-MX) 促进了无形固体分散的低温热挤出. 这增强了印梅他辛的溶解和透性,改善了药物输送性能.
科学领域:
- 材料科学 材料科学 材料科学
- 制药技术 制药技术 制药技术
- 药物运输 药物运输 药物运输
背景情况:
- 使用基甲基纤维素酸 (HPMCAS-MX) 调查无形固体分散的物理化学特性.
- 专注于一种具有较低玻璃过渡温度的HPMCAS-MX实验等级.
研究的目的:
- 评估HPMCAS-MX在热挤出 (HME) 中的适用性.
- 评估使用HPMCAS-MX制备的ASD的溶解和透性能.
- 将HPMCAS-MX与商业级的HPMCAS-MG进行比较.
主要方法:
- 通过热挤出,用HPMCAS-MX和HPMCAS-MG制备的印梅他辛 (IMC) 的ASDs.
- 在HME期间测量扭矩,以确定加工温度.
- 使用拉曼映射来确认无形状态.
- 评估ASD的溶解-透性能和稳定性.
主要成果:
- 与HPMCAS-MG (170°C) 相比,HPMCAS-MX使HME在较低的温度 (120°C) 中能够使用.
- 准备好的ASDs (IMC-MX和IMC-MG) 在40°C下在三个月内保持无形.
- 自闭症患者的初始溶解率和溶解度高于晶体印梅他素.
- 印美因自闭症的明显透性大约是晶体印美的两倍.
结论:
- HPMCAS-MX适用于在降低温度下进行HME处理.
- HPMCAS-MX增强了印莫他辛ASD的溶解和透性能.
- 这项研究表明,使用HPMCAS-MX在HME中改善了药物输送潜力.
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