选择体内相关溶解试验参数,用于开发具有增强口服生物可用性的大麻素配方
Nathan Koch1, Quentin Bourcy1, Olivier Jennotte1
1Laboratory of Pharmaceutical Technology and Biopharmacy, Center for Interdisciplinary Research on Medicines (CIRM), University of Liège, 4000 Liège, Belgium.
Pharmaceutics
|January 25, 2025
概括
开发更好的体外溶解试验对于预测体内药物性能至关重要. FeSSIF和FaSSIF媒体显示出准确预测大麻二醇 (CBD) 吸收率和程度的前景.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物输送系统 药物输送系统
- 生物制药生物制药公司
背景情况:
- 大麻 (CBD) 具有治疗潜力,但由于溶解性差,在临床试验中面临挑战.
- 优化的无形和基于脂质的CBD配方在临床前模型中提高了生物可用性.
- 开发预测性体外溶解试验至关重要,以减少对昂贵和耗时的体内研究的依赖.
研究的目的:
- 确定最佳的体外溶解试验条件,以预测体内大麻素 (CBD) 的性能.
- 评估不同介质成分和条件对CBD溶解的影响,并预测吸收.
- 为了将体外溶解结果与体内生物利用率数据相关联.
主要方法:
- 使用各种介质 (FaSSGF,FaSSIF,FeSSIF,HCl,酸盐缓冲体) 进行CBD配方的溶解测试,使用和不使用表面活性剂 (SLS).
- 在水槽和非水槽条件下溶解的比较.
- 在体外溶解资料与来自小猪研究的体内生物可用性数据的相关性.
主要成果:
- 表面活性剂对于在体外实现适当的大麻 (CBD) 溶解至关重要.
- 中性介质为体内吸收的程度提供了良好的预测.
- 预测体内吸收率更具挑战性,FeSSIF和FaSSIF (水槽) 显示出最好的相关性.
结论:
- FeSSIF和FaSSIF (下沉) 介质最适合预测体内大麻 (CBD) 吸收的程度和速度.
- 乳化似乎是影响CBD体内可用性的关键因素.
- 这些发现支持开发用于药物开发的先进体外溶解方法.
相关概念视频
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