由胃肠道模拟器alpha生成的BCSII类药物的溶解概况比综合USPII方法具有优势
Marvin D Naing1, Yasuhiro Tsume1
1Biopharmaceutics-Sterile Speciality Products, Merck & Co., Inc., Rahway, NJ, USA.
概括
与传统方法相比,胃肠道模拟器alpha (GIS-α) 提供了优越的体外药物溶解配置文件. 这种生物相关物转移方法提高了口服药物的生物可用性预测的准确性,有助于配方开发.
科学领域:
- 制药科学 制药科学
- 药物运输 药物运输 药物运输
- 生物制药生物制药公司
背景情况:
- 口服药物的水溶性差限制了胃肠道溶解和口服生物可用性.
- 传统的体外溶解测试 (USP装置I和II) 缺乏预测体内药物行为的预测能力.
- 准确的体外模型对于预测药物性能和优化配方至关重要.
研究的目的:
- 评估胃肠道模拟器alpha (GIS-α) 的性能,以评估药物溶解.
- 为了将GIS-α溶解谱与BCSII类药物的综合方法进行比较.
- 评估GIS-α数据在in silico药理动力学建模中的有用性.
主要方法:
- 使用了胃肠道模拟器alpha (GIS-α),这是一个带有环静脉的多隔间生物相关传输系统.
- 研究了达纳,费诺纤维酸盐,切莱科西布和里托纳维尔 (BCS II类药物) 的溶解概况.
- 将GIS-α结果与USP装置II溶解数据进行比较,并使用GastroPlusTM进行in silico建模.
主要成果:
- 使用生物相关缓冲器,GIS-α始终为使用生物相关缓冲器测试的所有BCSII类药物提供了优异的溶解配置.
- 使用GastroPlusTM的in silico建模显示,当使用GIS-α数据作为输入数据时,与USP II数据相比,预测准确度有所提高.
- GIS-α表现出增强生成与体内条件相关的药物溶解配置文件的能力.
结论:
- GIS-α是一种有价值的工具,可以产生比综合方法更具预测性的体外溶解概况.
- 在早期药物和配方开发中,GIS-α特别有用,以优化溶解性和生物可用性.
- 这种生物相关的方法有助于了解药物溶解行为和潜在的吸收模式,这对于配方设计至关重要.
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