固体形式的相对生物可用性评估通过人工胃和十二指肠装置
Yiwang Guo1, Alexander Byer-Alcorace2, Cody Thomas2
1Pharmaceutical Materials Science and Engineering Laboratory, Department of Pharmaceutics, College of Pharmacy, University of Minnesota, 308 Harvard St. S.E. Minneapolis, MN 55455, United States.
Journal of pharmaceutical sciences
|May 20, 2024
概括
人工胃和十二指肠 (ASD) 模型准确地预测了BI-639667.7在老鼠中的药物生物可用性. 这种溶解测试有助于选择最佳的固体形式来开发平板电脑.
科学领域:
- 药理动力学和药物新陈代谢
- 材料科学与工程 材料科学与工程
- 制药科学 制药科学
背景情况:
- 预测口服药物的生物可用性对于药物开发至关重要.
- 固态特性显著影响难溶性化合物的生物可用性.
- 人工胃和十二指肠 (ASD) 模型为评估药物性能提供了一个潜在的体外方法.
研究的目的:
- 评估人工胃和十二指肠 (ASD) 模型对体内生物可用性的预测能力.
- 为了研究一种难以溶解的化合物 (BI-639667) 的不同固体形式对其生物可用性的影响.
- 评估体外溶解概况与体内结果之间的相关性.
主要方法:
- 测试了一种难以溶解的化合物,BI-639667,溶液和四种不同的固体形式 (悬浮).
- 使用人工胃和十二指肠 (ASD) 装置评估溶解性能.
- 在大鼠体内确定BI-639667的生物可用性以进行比较.
- 相关联的体外溶解数据与体内生物可用性结果.
主要成果:
- 由ASD模型预测的生物可用性排名顺序与老鼠体内结果非常接近.
- 观察到的生物可用性顺序是:溶液 > 酸晶 > 酸盐 > 酸盐 > 单.
- 固体形式保持超和的能力与生物可用性相关,突显了溶解性能的重要性.
结论:
- 人工胃和十二指肠 (ASD) 模型展示了强大的预测能力,体内药物生物可用性.
- ASD测试是描述不同固体形式的溶解性能的一个有价值的工具.
- 使用ASD模型可以帮助在药片配方开发过程中合理选择固体形式.
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